NMR and molecular dynamics study of the size, shape, and composition of reverse micelles in a cetyltrimethylammonium bromide (CTAB)/n-hexane/pentanol/water microemulsion.

PubMed

Mills, Amanda J; Wilkie, John; Britton, Melanie M

2014-09-11

The size, shape, and composition of reverse micelles (RMs) in a cetyltrimethylammonium bromide (CTAB)/pentanol/n-hexane/water microemulsion were investigated using pulsed gradient stimulated echo (PGSTE) nuclear magnetic resonance (NMR) measurements and molecular modeling. PGSTE data were collected at observation times (Δ) of 10, 40, and 450 ms. At long observation times, CTAB and pentanol exhibited single diffusion coefficients. However, at short (Δ ≤ 40 ms) observation times both CTAB and pentanol exhibited slow and fast diffusion coefficients. These NMR data indicate that both CTAB and pentanol molecules reside in different environments within the microemulsion and that there is exchange between regions on the millisecond time scale. Molecular dynamic simulations of the CTAB RM, in a solvent box containing n-hexane and pentanol, produced an ellipsoid shaped RM. Using structural parameters from these simulations and the Stokes-Einstein relation, the structure factor and dimensions of the reverse micelle were determined. Analysis of the composition of the interphase also showed that there was a variation in the ratio of surfactant to cosurfactant molecules depending on the curvature of the interphase.

Electrochemical capacitance of nanostructured ruthenium-doped tin oxide Sn1- x Ru x O2 by the microemulsion method

NASA Astrophysics Data System (ADS)

Saraswathy, Ramanathan

2017-12-01

Synthesis of nanostructured Ru-doped SnO2 was successfully carried out using the reverse microemulsion method. The phase purity and the crystallite size were analyzed by XRD. The surface morphology and the microstructure of synthesized nanoparticles were analyzed by SEM and TEM. The vibration mode of nanoparticles was investigated using FTIR and Raman studies. The electrochemical behavior of the Ru-doped SnO2 electrode was evaluated in a 0.1 mol/L Na2SO4 solution using cyclic voltammetry. The 5% Ru-doped SnO2 electrode exhibited a high specific capacitance of 535.6 F/g at a scan rate 20 mV/s, possessing good conductivity as well as the electrocycling stability. The Ru-doped SnO2 composite shows excellent electrochemical properties, suggesting that this composite is a promising material for supercapacitors.

Anisotropic reversed micelles with fluorocarbon-hydrocarbon hybrid surfactants in supercritical CO2.

PubMed

Sagisaka, Masanobu; Ono, Shinji; James, Craig; Yoshizawa, Atsushi; Mohamed, Azmi; Guittard, Frédéric; Enick, Robert M; Rogers, Sarah E; Czajka, Adam; Hill, Christopher; Eastoe, Julian

2018-08-01

Previous work (M. Sagisaka, et al. Langmuir 31 (2015) 7479-7487), showed the most effective fluorocarbon (FC) and hydrocarbon (HC) chain lengths in the hybrid surfactants FCm-HCn (sodium 1-oxo-1-[4-(perfluoroalkyl)phenyl]alkane-2-sulfonates, where m = FC length and n = HC length) were m and n = 6 and 4 for water solubilization, whereas m 6 and n 6, or m 6 and n 5, were optimal chain lengths for reversed micelle elongation in supercritical CO 2 . To clarify why this difference of only a few methylene chain units is so effective at tuning the solubilizing power and reversed micelle morphology, nanostructures of water-in-CO 2 (W/CO 2 ) microemulsions were investigated by high-pressure small-angle neutron scattering (SANS) measurements at different water-to-surfactant molar ratios (W 0 ) and surfactant concentrations. By modelling SANS profiles with cylindrical and ellipsoidal form factors, the FC6-HCn/W/CO 2 microemulsions were found to increase in size with increasing W 0 and surfactant concentration. Ellipsoidal cross-sectional radii of the FC6-HC4/W/CO 2 microemulsion droplets increased linearly with W 0 , and finally reached ∼39 Å and ∼78 Å at W 0  = 85 (close to the upper limit of solubilizing power). These systems appear to be the largest W/CO 2 microemulsion droplets ever reported. The aqueous domains of FC6-HC6 rod-like reversed micelles increased in size by 3.5 times on increasing surfactant concentration from 35 mM to 50 mM: at 35 mM, FC6-HC5 formed rod-like reversed micelles 5.3 times larger than FC6-HC6. Interestingly, these results suggest that hybrid HC-chains partition into the microemulsion aqueous cores with the sulfonate headgroups, or at the W/CO 2 interfaces, and so play important roles for tuning the W/CO 2 interfacial curvature. The super-efficient W/CO 2 -type solubilizer FC6-HC4, and the rod-like reversed micelle forming surfactant FC6-HC5, represent the most successful cases of low fluorine content additives. These surfactants facilitate VOC-free, effective and energy-saving CO 2 solvent systems for applications such as extraction, dyeing, dry cleaning, metal-plating, enhanced oil recovery and organic/inorganic or nanomaterial synthesis. Copyright © 2017 Elsevier B.V. All rights reserved.

Innovative formulations for the delivery of levothyroxine to the skin.

PubMed

Padula, Cristina; Nicoli, Sara; Santi, Patrizia

2009-05-08

The aim of this work was to realize innovative transdermal formulations containing sodium levothyroxine in view of topical administration. Permeation experiments were performed in vitro, using rabbit ear skin as barrier. At the end of the permeation experiments levothyroxine retained in the skin was extracted and quantified by HPLC. Formulations tested were microemulsions and transdermal films. Microemulsions containing isopropyl myristate and isobutanol were shown to be able to increase levothyroxine solubility by the inclusion in reverse micelles. However, the inclusion in reversed micelles reduced the drug release to a significant extent, and consequently skin retention, compared to aqueous solutions. When the microemulsion was included in the transdermal film, drug retention was increased, probably for the enhancer effect of its excipients. The transdermal film proposed in this work could be an interesting alternative to semisolid formulations for the ease of use and the control in the amount of active applied. Additional benefit can be obtained if the film is used in occlusive conditions.

Microemulsion impregnated catalyst composite and use thereof in a synthesis gas conversion process

DOEpatents

Abrevaya, H.; Targos, W.M.

1987-12-22

A catalyst composition is described for synthesis gas conversion comprising a ruthenium metal component deposited on a support carrier wherein the average metal particle size is less than about 100 A. The method of manufacture of the composition via a reverse micelle impregnation technique and the use of the composition in a Fischer-Tropsch conversion process is also disclosed.

Reverse micelle synthesis of oxide nanopowders: mechanisms of precipitate formation and agglomeration effects.

PubMed

Graeve, Olivia A; Fathi, Hoorshad; Kelly, James P; Saterlie, Michael S; Sinha, Kaustav; Rojas-George, Gabriel; Kanakala, Raghunath; Brown, David R; Lopez, Enrique A

2013-10-01

We present an analysis of reverse micelle stability in four model systems. The first two systems, composed of unstable microemulsions of isooctane, water, and Na-AOT with additions of either iron sulfate or yttrium nitrate, were used for the synthesis of iron oxide or yttrium oxide powders. These oxide powders were of nanocrystalline character, but with some level of agglomeration that was dependent on calcination temperature and cleaning procedures. Results show that even though the reverse micellar solutions were unstable, nanocrystalline powders with very low levels of agglomeration could be obtained. This effect can be attributed to the protective action of the surfactant on the surfaces of the powders that prevents neck formation until after all the surfactant has volatilized. A striking feature of the IR spectra collected on the iron oxide powders is the absence of peaks in the ~1715 cm(-1) to 1750 cm(-1) region, where absorption due to the symmetric C=O (carbonyl) stretching occurs. The lack of such peaks strongly suggests the carbonyl group is no longer free, but is actively participating in the surfactant-precipitate interaction. The final two microemulsion systems, containing CTAB as the surfactant, showed that loss of control of the reverse micelle synthesis process can easily occur when the amount of salt in the water domains exceeds a critical concentration. Both model systems eventually resulted in agglomerated powders of broad size distributions or particles that were large compared to the sizes of the reverse micelles, consistent with the notion that the microemulsions were not stable and the powders were precipitated in an uncontrolled fashion. This has implications for the synthesis of nanopowders by reverse micelle synthesis and provides a benchmark for process control if powders of the highest quality are desired. Copyright © 2013 Elsevier Inc. All rights reserved.

Acoustic activation of water-in-oil microemulsions for controlled salt dissolution.

PubMed

Baxamusa, Salmaan; Ehrmann, Paul; Ong, Jemi

2018-06-18

The dynamic nature of the oil-water interface allows for sequestration of material within the dispersed domains of a microemulsion. Microstructural changes should therefore change the dissolution rate of a solid surface in a microemulsion. We hypothesize that microstructural changes due to formulation and cavitation in an acoustic field will enable control over solid dissolution rates. Water-in-oil microemulsions were formulated using cyclohexane, water, Triton X-100, and hexanol. The microstructure and solvation properties of Winsor Type IV formulations were characterized. Dissolution rates of KH 2 PO 4 (KDP), were measured. A kinetic analysis isolated the effect of the microstructure, and rate enhancements due to cavitation effects on the microstructure were characterized by measuring dissolution rates in an ultrasonic field. Dispersed aqueous domains of 2-6 nm radius dissolve a solid block of KDP at 0-10 nm/min. Dissolution rate is governed not by the domain-surface collision frequency but rather by a dissolution probability per domain-surface encounter. Higher probabilities are correlated with larger domains. Rapid and reversible dissolution rate increases of up to 270× were observed under ultrasonic conditions, with <20% of the increase due to bulk heating effects. The rest is attributed to cavitation-induced changes to the domain microstructure, providing a simple method for remotely activating and de-activating dissolution. Copyright © 2018 Elsevier Inc. All rights reserved.

Investigation of the micropolarity of reverse micelles using quinolinium betaine compounds as probes

DOE Office of Scientific and Technical Information (OSTI.GOV)

Ueda, Mitsuo; Kimura, Akimune; Wakida, Tomoji

1994-03-15

There is considerable interest in the utilization of reverse micelle and microemulsion systems in a variety of applications such as reactivity control, tertiary oil recovery, solar energy conversion, enzyme mediated synthesis, etc. Fundamental to understanding improved applications of such systems are questions concerning solubilization; thus substantial efforts have been focused on the investigation of the solubilizing state of the assemblies. N-octyl-quinolinium betaine is introduced as an absorption probe for the micropolarity of the interior of reverse micelles. its solubilization by reverse micelles and water/oil microemulsions of Aerosol-OT in isooctane is compared with that of N-methyl-quinolinium betaine at various water contentsmore » of the solution. Analysis of the excitation energies in the visible range of the spectrum indicates that the methyl derivative probes the polarity of the aqueous pool of the micelle, whereas the octyl derivative behaves as a cosurfactant probe that reports on the polarity of the water/oil interfacial region.« less

Influence of polyethylene glycol on percolation dynamics of reverse microemulsions

NASA Astrophysics Data System (ADS)

Geethu, P. M.; Yadav, Indresh; Aswal, V. K.; Satapathy, D. K.

2018-04-01

We explore the influence of a hydrophilic polymer, polyethylene glycol (PEG), on the structure and the percolation dynamics of reverse microemulsions (ME) stabilized by an anionic surfactant AOT (sodium bis(2-ethylhexyl) sulfosuccinate). The percolation transition of MEs is probed using dielectric relaxation spectroscopy (DRS). Notably, an increase in percolation temperature is observed by the incorporation of PEG-polymer into larger ME droplets which is explained by considering the model of polymer adsorption at surfactant-water interface. The stability of the droplet phase of microemulsion after the incorporation of PEG is confirmed by small-angle neutron scattering (SANS) experiment. Further, a net decrease in percolation transition temperature is observed with the addition of PEG polymer for smaller ME droplets and is discussed in relation with the destabilization of droplets owing to the polymer induced bridging and the associated clustering of droplets. We conjecture that the adsorption of PEG polymer chains at the surfactant-water interface as well as the PEG-induced bridging of droplets are due to the strong ion-dipole interaction between anionic head group of AOT surfactant and dipoles present in PEG polymer chains.

Anionic microemulsion to solvent stacking for on-line sample concentration of cationic analytes in capillary electrophoresis.

PubMed

Kukusamude, Chunyapuk; Srijaranai, Supalax; Quirino, Joselito P

2014-05-01

The common SDS microemulsion (i.e. 3.3% SDS, 0.8% octane, and 6.6% butanol) and organic solvents were investigated for the stacking of cationic drugs in capillary zone electrophoresis using a low pH separation electrolyte. The sample was prepared in the acidic microemulsion and a high percentage of organic solvent was included in the electrolyte at anodic end of capillary. The stacking mechanism was similar to micelle to solvent stacking where the micelles were replaced by the microemulsion for the transport of analytes to the organic solvent rich boundary. This boundary is found between the microemulsion and anodic electrolyte. The effective electrophoretic mobility of the cations reversed from the direction of the anode in the microemulsion to the cathode in the boundary. Microemulsion to solvent stacking was successfully achieved with 40% ACN in the anodic electrolyte and hydrodynamic sample injection of 21 s at 1000 mbar (equivalent to 30% of the effective length). The sensitivity enhancement factors in terms of peak height and corrected peak area were 15 to 35 and 21 to 47, respectively. The linearity R(2) in terms of corrected peak area were >0.999. Interday precisions (%RSD, n = 6) were 3.3-4.0% for corrected peak area and 2.0-3.0% for migration time. Application to spiked real sample is also presented. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Characterization of nanoparticles of lidocaine in w/o microemulsions using small-angle neutron scattering and dynamic light scattering

NASA Astrophysics Data System (ADS)

Shukla, A.; Kiselev, M. A.; Hoell, A.; Neubert, R. H. H.

2004-08-01

Microemulsions (MEs) are of special interest because a variety of Reactants can be introduced into the nanometer-sized aqueous domains, leading to materials with controlled size and shape [1,2]. In the past few years, significant research has been conducted in the reverse ME-mediated synthesis of organic nanoparticles [3,4]. In this study, a w/o ME medium was employed for the synthesis of lidocaine by direct precipitation in w/o microemulsion systems: water/isopropylpalmitat/Tween80/Span80. The particle size as well as the location of nanoparticles in the ME droplet were characterized by means of dynamic light scattering (DLS) and small angle neutron scattering (SANS). It is observed that lidocaine precipitated in the aqueous cores because of its insolubility in water. Hydrodynamic radius and gyration radius of microemulsion droplets were estimated as ~15 nm and ~4.50 nm from DLS and SANS respectively. Furthermore, different size parameters obtained by DLS and SANS experiments were compared

Microstructure characterization of a food-grade U-type microemulsion system by differential scanning calorimetry and electrical conductivity techniques.

PubMed

Zhang, Hui; Taxipalati, Maierhaba; Que, Fei; Feng, Fengqin

2013-12-01

The microstructure transitions of a food-grade U-type microemulsion system containing glycerol monolaurate and propionic acid at a 1:1 mass ratio as oil phase and Tween 80 as surfactant were investigated along a water dilution line at a ratio of 80:20 mass% surfactant/oil phase, based on a previously studied phase diagram. From the water thermal behaviours detected by differential scanning calorimetry, three structural regions are identified along the dilution line. In the first region, all water molecules are confined to the water core of the reverse micelles, leading to the formation of w/o microemulsion. As the water content increases, the water gains mobility, transforms into bicontinuous in the second region, and finally the microemulsion become o/w in the third region. The thermal transition points coincide with the structural phase transitions by electrical conductivity measurements, indicating that the structural transitions occur at 35 and 65 mass% of water along the dilution line. Copyright © 2013 Elsevier Ltd. All rights reserved.

Formulation and In-vivo Pharmacokinetic Consideration of Intranasal Microemulsion and Mucoadhesive Microemulsion of Rivastigmine for Brain Targeting.

PubMed

Shah, Brijesh; Khunt, Dignesh; Misra, Manju; Padh, Harish

2018-01-02

Presence of tight junctions in blood brain barrier (BBB) pose a major hurdle for delivery of drug and severely affects adequate therapeutic concentration to reach the brain. In present work, we have selected Rivastigmine hydrogen tartrate (RHT), a reversible cholinesterase inhibitor, which exhibits extensive first-pass metabolism, resulting in limited absolute bioavailability (36%). RHT shows extremely low aqueous solubility and poor penetration, resulting in inadequate concentration reaching the brain, thus necessitating frequent oral dosing. To overcome these problems of RHT, microemulsion (ME) and mucoadhesive microemulsion (MME) of RHT were formulated for brain targeting via intranasal delivery route and compared on the basis of in vivo pharmacokinetics. ME and MME formulations containing RHT were developed by water titration method. Characterization of ME and MME was done for various physicochemical parameters, nasal spray pattern, and in vivo pharmacokinetics quantitatively and qualitatively (gamma scintigraphy studies). The developed ME and MME were transparent having globule size approximately in the range of 53-55 nm. Pharmacokinetic studies showed higher values for C max and DTP for intranasal RHT: CH-ME over RHT-ME, thus indicating the effect of chitosan in modulating tight junctions, thereby enhanced paracellular transport of RHT. Gamma scintigraphy and in vivo pharmacokinetic study suggested enhanced RHT concentration, upon intranasal administration of RHT:CH-ME, compare with other groups administered formulations intranasally. These findings suggested the potential of non-invasive intranasal route for brain delivery, especially for therapeutics, facing challenges in oral administration.

In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion

PubMed Central

Zhang, Yong-Tai; Huang, Zhe-Bin; Zhang, Su-Juan; Zhao, Ji-Hui; Wang, Zhi; Liu, Ying; Feng, Nian-Ping

2012-01-01

Objective To investigate the cellular uptake of evodiamine and rutaecarpine in a microemulsion in comparison with aqueous suspensions and tinctures. Materials and methods A microemulsion was prepared using the dropwise addition method. Mouse skin fibroblasts were cultured in vitro to investigate the optimal conditions for evodiamine and rutaecarpine uptake with different drug concentrations and administration times. Under optimal conditions, the cellular uptake of microemulsified drugs was assayed and compared to tinctures and aqueous suspensions. Rhodamine B labeling and laser scanning confocal microscopy (LSCM) were used to explore the distribution of fluorochrome transferred with the microemulsion in fibroblasts. Cellular morphology was also investigated, using optical microscopy to evaluate microemulsion-induced cellular toxicity. Results The maximum cellular drug uptake amounts were obtained with a 20% concentration (v/v) of microemulsion and an 8 hour administration time. Drug uptake by mouse skin fibroblasts was lowest when the drugs were loaded in microemulsion. After incubation with rhodamine B-labeled microemulsion for 8 hours, the highest fluorescence intensity was achieved, and the fluorochrome was primarily distributed in the cytochylema. No obvious cellular morphologic changes were observed with the administration of either the microemulsion or the aqueous suspension; for the tincture group, however, massive cellular necrocytosis was observed. Conclusion The lower cellular uptake with microemulsion may be due to the fact that most of the drug loaded in the microemulsion vehicle was transported via the intercellular space, while a small quantity of free drug (released from the vehicle) was ingested through transmembrane transport. Mouse skin fibroblasts rarely endocytosed evodiamine and rutaecarpine with a microemulsion as the vehicle. The microemulsion had no obvious effect on cellular morphology, suggesting there is little or no cellular toxicity associated with the administration of microemulsion on mouse skin fibroblasts. PMID:22679361

Investigating the evolution of the phase behavior of AOT-based w/o microemulsions in dodecane as a function of droplet volume fraction.

PubMed

Ganguly, R; Choudhury, N

2012-04-15

AOT-based water in oil (w/o) microemulsions are one of the most extensively studied reverse micellar systems because of their rich phase behavior and their ability to form in the absence of any co-surfactant. The aggregation characteristics and interaction of the microemulsion droplets in these systems are known to be governed by AOT-oil compatibility and water to AOT molar ratio (w). In this manuscript by using Dynamic Light Scattering (DLS) and viscometry techniques, we show that droplet volume fraction too plays an important role in shaping the phase behavior of these microemulsions in dodecane. The phase separation characteristics and the evolution of the viscosity and the hydrodynamic radius of the microemulsion droplets on approaching the cloud points have thus been found to undergo complete transformation as one goes from low to high droplet volume fraction even at a fixed 'w'. Modeling of the DLS data attributes this to the weakening of inter droplet attractive interaction caused by the growing dominance of the excluded volume effect with increase in droplet volume fraction. In the literature, the inter droplet attractive interaction driven phase separation in these microemulsions is explained based on gas-liquid type phase transition, conceptualized in the framework of Baxter adhesive hard sphere theory. The modeling of our viscosity data, however, does not support such proposition as the characteristic stickiness parameter (τ(-1)) of the microemulsion droplets in this system remains much lower than the critical value (τ(c)(-1)≈10.25) required to enforce such phase transition. Copyright © 2012 Elsevier Inc. All rights reserved.

Surface engineered nanoparticles for improved surface enhanced Raman scattering applications and method for preparing same

DOEpatents

Simmons, Blake A [San Francisco, CA; Talin, Albert Alec [Livermore, CA

2009-11-27

A method for producing metal nanoparticles that when associated with an analyte material will generate an amplified SERS spectrum when the analyte material is illuminated by a light source and a spectrum is recorded. The method for preparing the metal nanoparticles comprises the steps of (i) forming a water-in-oil microemulsion comprising a bulk oil phase, a dilute water phase, and one or more surfactants, wherein the water phase comprises a transition metal ion; (ii) adding an aqueous solution comprising a mild reducing agent to the water-in-oil microemulsion; (iii) stirring the water-in-oil microemulsion and aqueous solution to initiate a reduction reaction resulting in the formation of a fine precipitate dispersed in the water-in-oil microemulsion; and (iv) separating the precipitate from the water-in-oil microemulsion.

Nanodevices from Nanocomponents: Memory Logic and Mechanical Nanodevices

DTIC Science & Technology

2009-05-11

microemulsion method at room temperature. The microemulsion system was made up of cyclohexane, NP-5, PbSe and dimethylamine. Typically, 10 ml...30 min after the microemulsion system was formed, 100 \\i\\ dimethylamine aqueous solution (40wt %) was introduced to initiate the polymerization...growth was completed after 24 h of stirring. The nanoparticles were destabilized from the microemulsion using acetone and precipitated by

Synthesis of tin monosulfide (SnS) nanoparticles using surfactant free microemulsion (SFME) with the single microemulsion scheme

NASA Astrophysics Data System (ADS)

Tarkas, Hemant S.; Marathe, Deepak M.; Mahajan, Mrunal S.; Muntaser, Faisal; Patil, Mahendra B.; Tak, Swapnil R.; Sali, Jaydeep V.

2017-02-01

Synthesis of monomorphic, SnS nanoparticles without using a capping agent is a difficult task with chemical route of synthesis. This paper reports on synthesis of tin monosulfide (SnS) nanopartilces with dimension in the quantum-dot regime using surfactant free microemulsion with single microemulsion scheme. This has been achieved by reaction in microreactors in the CME (C: chlorobenzene, M: methanol and E: ethylene glycol) microemulsion system. This is an easy and controllable chemical route for synthesis of SnS nanoparticles. Nanoparticle diameter showed prominent dependence on microemulsion concentration and marginal dependence on microemulsion temperature in the temperature range studied. The SnS nanoparticles formed with this method form stable dispersion in Tolune.

Enhanced effect and mechanism of water-in-oil microemulsion as an oral delivery system of hydroxysafflor yellow A

PubMed Central

Qi, Jianping; Zhuang, Jie; Wu, Wei; Lu, Yi; Song, Yunmei; Zhang, Zhetao; Jia, Jia; Ping, Qineng

2011-01-01

Background: A microemulsion is an effective formulation for improving the oral bioavailability of poorly soluble drugs. In this paper, a water-in-oil (w/o) microemulsion was investigated as a system for enhancing the oral bioavailability of Biopharmaceutic Classification System (BCS) III drugs. Methods: The microemulsion formulation was optimized using a pseudoternary phase diagram, comprising propylene glycol dicaprylocaprate (PG), Cremophor® RH40, and water (30/46/24 w/w). Results: The microemulsion increased the oral bioavailability of hydroxysafflor yellow A which was highly water-soluble but very poorly permeable. The relative bioavailability of hydroxysafflor yellow A microemulsion was about 1937% compared with a control solution in bile duct-nonligated rats. However, the microemulsion showed lower enhanced absorption ability in bile duct-ligated rats, and the relative bioavailability was only 181%. In vitro experiments were further employed to study the mechanism of the enhanced effect of the microemulsion. In vitro lipolysis showed that the microemulsion was digested very quickly by pancreatic lipase. About 60% of the microemulsion was digested within 1 hour. Furthermore, the particle size of the microemulsion after digestion was very small (53.3 nm) and the digested microemulsion had high physical stability. An everted gut sac model demonstrated that cumulative transport of the digested microemulsion was significantly higher than that of the diluted microemulsion. Conclusion: These results suggested that digestion of the microemulsion by pancreatic lipase plays an important role in enhancing oral bioavailability of water-soluble drugs. PMID:21720510

Micro-scale displacement of NAPL by surfactant and microemulsion in heterogeneous porous media

NASA Astrophysics Data System (ADS)

Javanbakht, Gina; Arshadi, Maziar; Qin, Tianzhu; Goual, Lamia

2017-07-01

Industrial processes such as remediation of oil-contaminated aquifers and enhanced oil recovery (EOR) often utilize chemical additives to increase the removal of non-aqueous phase liquids (NAPLs) from subsurface formations. Although the majority of crude oils are classified as LNAPLs, they often contain heavy molecules (DNAPLs) such as asphaltenes that tend to adsorb on minerals and alter their wettability. Effective additives are therefore those that can reduce the threshold capillary pressure, thus mobilizing LNAPL inside pore spaces and solubilizing DNAPL from rock surfaces. Nonionic surfactants in brine have often been injected to oil or contaminated aquifer formations in order to enhance NAPL displacement through IFT reduction. Recent studies revealed that surfactant-based microemulsions have a higher tendency to alter the wettability of surfaces, compared to surfactants alone, leading to more effective NAPL removal. However, the impact of these additives on pore-scale displacement mechanisms and multi-phase fluid occupancy in porous media is, to date, still unclear. In this study, x-ray microtomography experiments were performed to investigate the impact of surfactants and microemulsions on the mobilization and solubilization of NAPL in heterogeneous rocks. Saturation profiles indicated that an incremental NAPL removal was attained by addition of microemulsion to brine, compared with surfactant. Residual cluster size distributions revealed that microemulsions could break up large clusters into smaller disconnected ones, improving their mobilization in the rock. In-situ contact angle measurements showed that microemulsions could reverse the wettability of rough contaminated surfaces to a higher extent than surfactants. Unlike surfactant alone, the surfactant-solvent blend in the carrier fluid of microemulsions was able to penetrate rough grain surfaces, particularly those of dolomite cement, and desorb asphaltenes in the form of small-emulsified NAPL droplets, which were eventually washed away by the continuous flow process. The greater wettability alteration caused by microemulsions resulted in a lower threshold capillary pressure, which in turn promoted the mobilization of NAPL ganglia more than surfactant alone.

Novel isotretinoin microemulsion-based gel for targeted topical therapy of acne: formulation consideration, skin retention and skin irritation studies

NASA Astrophysics Data System (ADS)

Patel, Mrunali R.; Patel, Rashmin B.; Parikh, Jolly R.; Patel, Bharat G.

2016-04-01

Isotretinoin was formulated in novel microemulsion-based gel formulation with the aim of improving its solubility, skin tolerability, therapeutic efficacy, skin-targeting efficiency and patient compliance. Microemulsion was formulated by the spontaneous microemulsification method using 8 % isopropyl myristate, 24 % Labrasol, 8 % plurol oleique and 60 % water as an external phase. All plain and isotretinoin-loaded microemulsions were clear and showed physicochemical parameters for the desired topical delivery and stability. The permeation profiles of isotretinoin through rat skin from selected microemulsion formulation followed zero-order kinetics. Microemulsion-based gel was prepared by incorporating Carbopol®971 in optimized microemulsion formulation having suitable skin permeation rate and skin uptake. Microemulsion-based gel showed desired physicochemical parameters and demonstrated advantage over marketed formulation in improving the skin tolerability of isotretinoin, indicating its potential in improving topical delivery of isotretinoin. The developed microemulsion-based gel may be a potential drug delivery vehicle for targeted topical delivery of isotretinoin in the treatment of acne.

Assessment of Aprotinin Loaded Microemulsion Formulations for Parenteral Drug Delivery: Preparation, Characterization, in vitro Release and Cytotoxicity Studies.

PubMed

Okur, Neslihan Üstündağ; Özdemir, Derya İlem; Kahyaoğlu, Şennur Görgülü; Şenyiğit, Zeynep Ay; Aşıkoğlu, Makbule; Genç, Lütfi; Karasulu, H Yeşim

2015-01-01

The object of the current study was to prepare novel microemulsion formulations of aprotinin for parenteral delivery and to compare in vitro characteristics and release behaviour of different Technetium-99m ((99m)Tc)-Aprotinin loaded microemulsion formulations. In addition, cytotoxicity of microemulsion formulation was evaluated with cell culture studies on human immortalized pancreatic duct epithelial-like cells. For this aim, firstly, pseudo-ternary phase diagrams were plotted to detect the formulation region and optimal microemulsions were characterized for their thermodynamic stability, conductivity, particle size, zeta potential, viscosity, pH and in vitro release properties. For in vitro release studies aprotinin was labelled with (99m)Tc and labelling efficiency, radiochemical purity and stability of the radiolabeled complex were determined by several chromatography techniques. Radiolabeling efficiency of (99m)Tc-Aprotinin was found over than 90% without any significant changes up to 6 hours after labelling at room temperature. After that, in vitro release studies of (99m)Tc-Aprotinin loaded microemulsions were performed with two different methods; dissolution from diffusion cells and dialysis bags. Both methods showed that release rate of (99m)Tc- Aprotinin from microemulsion could be controlled by microemulsion formulations. Drug release from the optimized microemulsion formulations was found lower compared to drug solution at the end of six hours. According to stability studies, the optimized formulation was found to be stable over a period of 12 months. Also, human immortalized pancreatic duct epithelial-like cells were used to evaluate the cytotoxicity of optimum formulation. Developed microemulsion did not reveal cytotoxicity. In conclusion the present study indicated that the M1-APT microemulsion is appropriate for intravenous application of aprotinin.

Silver/poly(vinyl alcohol) nanocomposite film prepared using water in oil microemulsion for antibacterial applications.

PubMed

Fatema, Ummul K; Rahman, M Muhibur; Islam, M Rakibul; Mollah, M Yousuf A; Susan, Md Abu Bin Hasan

2018-03-15

Water in oil microemulsion (w/o) is a simple preparative route for nanoparticles where water droplets (dispersed in continuous oil medium and stabilized by surfactants and cosurfactants) act as nanoreactors to carry out chemical reactions. If polymeric matrix is incorporated inside the core of the microemulsions, it should prevent the agglomeration of nanoparticles after separation from microemulsions. Thus polymer nanocomposite films prepared from w/o microemulsions are expected to give narrow and homogeneous size distribution of nanoparticles throughout the polymer host. Silver/poly(vinyl alcohol) (Ag/PVA) nanocomposite film was successfully prepared, for the first time, using Triton X-100 (TX-100)/1-butanol/cyclohexane/water microemulsion. Reduction of the metal salt was carried out in the core of w/o microemulsion droplets containing PVA polymeric matrix. After separation from the microemulsion, Ag/PVA nanocomposite film was then prepared by solution casting method. The antibacterial activity of the nanocomposites was tested against Gram-negative, Escherichia coli and Gram-positive, Staphylococcus aureus by agar diffusion method. Ag nanoparticles with an average diameter of 105 nm could be synthesized using PVA, whereas in the absence of PVA the nanoparticles agglomerated. The distribution of Ag nanoparticles on PVA surface of the nanocomposite film prepared using microemulsion was uniform, whereas the film prepared through in situ generation of Ag nanoparticles by chemical reduction process on PVA host showed non-uniform, coagulated, bunches of Ag nanoparticles. The film synthesized using microemulsion exhibited enhanced antibacterial efficacy compared to that prepared through in situ synthesis under the same test condition. Copyright © 2017 Elsevier Inc. All rights reserved.

Novel self-assembled gels and materials synthesis in unconventional environments

NASA Astrophysics Data System (ADS)

Irvin, Glen Clifford, Jr.

This thesis deals specifically with the fabrication of novel nanophase and polymer materials using novel microstructured mediums. Enzymatic polymerization in a new microemulsion system using dense carbon dioxide and fluorinated surfactants was carried out. The morphology, molecular weight, and chemical structure of the polymer are characterized through electron microscopy, HPLC, FTIR, and 1HNMR. Structural characteristics indicate similarity to polymers formed in AOT-inverse micelles. Spectroscopic information of the polymerization system on a molecular level has been performed. The results indicate strong hydrogen bonding interactions between the monomer, water, and perfluorinated surfactant implying the partitioning of the monomer to the surfactant headgroup region. An extension of the microemulsion environment is found with novel microemulsion based gels. The gels contain both lecithin and AOT surfactants where roughly equal volumes of hydrocarbon and water forms a three-dimensional gel network. This microemulsion system is unique from a fundamental scientific and practical interest. Analysis of the system microstructures using 1HNMR, 13CNMR 31PNNM, Rheology, SAXS, SANS, and conductivity is presented. Nanomaterial templated syntheses were conducted and are discussed. A new technique was developed for the rapid production of clathrate hydrates either in aqueous or water-in-microemulsion environments. The systems devised for this technology have significantly greater interfacial contact between water and gas molecules (clathrate hydrate constituents). The rapid clathrate hydrate technique was utilized for synthesis of nanoclusters in aqueous and reverse micelle based systems using the remarkable phenomenon of clathrate hydrate formation. Conversion of water to crystalline ice-like (clathrate hydrate) form is exploited to arrest particle growth, thereby restricting particle size to the nanometer range. The technique is used to generate high synthesis rates of nanoclusters (specifically ferrites) in aqueous solution. By controlling process conditions, ferrite particles with spherical or high aspect ratio acicular morphologies are obtained. Characterization of magnetic materials produced using this new technique was detailed with XRD, SQUID, and TEM. An extension of the rapid hydrate technique to AOT/water/Isooctane microemulsions found that for the same [water]/[AOT] ratio, nanoclusters of smaller size could be formed simply by subjecting the reversed micelles to hydrate forming conditions. Analysis of a model semiconductor (PbS) is presented using UV-VIS, XRD, EDAX, TEM, and Electron Diffraction.

Synergistic cosolubilization of omega-3 fatty acid esters and CoQ10 in dilutable microemulsions.

PubMed

Deutch-Kolevzon, Rivka; Aserin, Abraham; Garti, Nissim

2011-10-01

Water-dilutable microemulsions were prepared and loaded with two types of omega-3 fatty acid esters (omega-3 ethyl esters, OEE; and omega-3 triacylglycerides, OTG), each separately and together with ubiquinone (CoQ(10)). The microemulsions showed high and synergistic loading capabilities. The linear fatty acid ester (OEE) solubilization capacity was greater than that of the bulky and robust OTG. The location of the guest molecules within the microemulsions at any dilution point were determined by electrical conductivity, viscosity, DSC, SAXS, cryo-TEM, SD-NMR, and DLS. We found that OEE molecules pack well within the surfactant tails to form reverse micelles that gradually, upon water dilution, invert into bicontinuous phase and finally into O/W droplets. The CoQ(10) increases the stabilization and solubilization of the omega-3 fatty acid esters because it functions as a kosmotropic agent in the micellar system. The hydrophobic and bulky OTG molecule strongly interferes with the tail packing and spaces them significantly - mainly in the low and medium range water dilutions. When added to the micellar system, CoQ(10) forms some reverse hexagonal mesophases. The inversion into direct micelles is more difficult in comparison to the OEE system and requires additional water dilution. The OTG with or without CoQ(10) destabilizes the structures and decreases the solubilization capacity since it acts as a chaotropic agent to the micellar system and as a kosmotropic agent to hexagonal packing. These results explain the differences in the behavior of these molecules with vehicles that solubilize them in aqueous phases. Temperature disorders the bicontinuous structures and reduces the supersaturation of the system containing OEE with CoQ(10); as a result CoQ(10) crystallization is retarded. Copyright © 2011. Published by Elsevier Ireland Ltd.

A step toward the development of high-temperature stable ionic liquid-in-oil microemulsions containing double-chain anionic surface active ionic liquid.

PubMed

Rao, Vishal Govind; Banerjee, Chiranjib; Ghosh, Surajit; Mandal, Sarthak; Kuchlyan, Jagannath; Sarkar, Nilmoni

2013-06-20

Owing to their fascinating properties and wide range of potential applications, interest in nonaqueous microemulsions has escalated in the past decade. In the recent past, nonaqueous microemulsions containing ionic liquids (ILs) have been utilized in performing chemical reactions, preparation of nanomaterials, synthesis of nanostructured polymers, and drug delivery systems. The most promising fact about IL-in-oil microemulsions is their high thermal stability compared to that of aqueous microemulsions. Recently, surfactant-like properties of surface active ionic liquids (SAILs) have been used for preparation of microemulsions with high-temperature stability and temperature insensitivity. However, previously described methods present a limited possibility of developing IL-in-oil microemulsions with a wide range of thermal stability. With our previous work, we introduced a novel method of creating a huge number of IL-in-oil microemulsions (Rao, V. G.; Ghosh, S.; Ghatak, C.; Mandal, S.; Brahmachari, U.; Sarkar, N. J. Phys. Chem. B2012, 116, 2850-2855), composed of a SAIL as a surfactant, room-temperature ionic liquids as a polar phase, and benzene as a nonpolar phase. The use of benzene as a nonpolar solvent limits the application of the microemulsions to temperatures below 353 K. To overcome this limitation, we have synthesized N,N-dimethylethanolammonium 1,4-bis(2-ethylhexyl) sulfosuccinate (DAAOT), which was used as a surfactant. DAAOT in combination with isopropyl myristate (IPM, as an oil phase) and ILs (as a polar phase) produces a huge number of high-temperature stable IL-in-oil microemulsions. By far, this is the first report of a huge number of high-temperature stable IL-in-oil microemulsions. In particular, we demonstrate the wide range of thermal stability of [C6mim][TF2N]/DAAOT/IPM microemulsions by performing a phase behavior study, dynamic light scattering measurements, and (1)H NMR measurements and by using coumarin-480 (C-480) as a fluorescent probe molecule.

Optimisation and validation of a rapid and efficient microemulsion liquid chromatographic (MELC) method for the determination of paracetamol (acetaminophen) content in a suppository formulation.

PubMed

McEvoy, Eamon; Donegan, Sheila; Power, Joe; Altria, Kevin

2007-05-09

A rapid and efficient oil-in-water microemulsion liquid chromatographic method has been optimised and validated for the analysis of paracetamol in a suppository formulation. Excellent linearity, accuracy, precision and assay results were obtained. Lengthy sample pre-treatment/extraction procedures were eliminated due to the solubilising power of the microemulsion and rapid analysis times were achieved. The method was optimised to achieve rapid analysis time and relatively high peak efficiencies. A standard microemulsion composition of 33 g SDS, 66 g butan-1-ol, 8 g n-octane in 1l of 0.05% TFA modified with acetonitrile has been shown to be suitable for the rapid analysis of paracetamol in highly hydrophobic preparations under isocratic conditions. Validated assay results and overall analysis time of the optimised method was compared to British Pharmacopoeia reference methods. Sample preparation and analysis times for the MELC analysis of paracetamol in a suppository were extremely rapid compared to the reference method and similar assay results were achieved. A gradient MELC method using the same microemulsion has been optimised for the resolution of paracetamol and five of its related substances in approximately 7 min.

Novel microemulsion-based gel formulation of tazarotene for therapy of acne.

PubMed

Patel, Mrunali Rashmin; Patel, Rashmin Bharatbhai; Parikh, Jolly R; Patel, Bharat G

2016-12-01

The objective of this study was to develop and evaluate a novel microemulsion based gel formulation containing tazarotene for targeted topical therapy of acne. Psudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant, and co-surfactant for microemulsion formation. The optimized microemulsion formulation containing 0.05% tazarotene was formulated by spontaneous microemulsification method consisting of 10% Labrafac CC, mixed emulsifiers 15% Labrasol-Cremophor-RH 40 (1:1), 15% Capmul MCM, and 60% distilled water (w/w) as an external phase. All plain and tazarotene-loaded microemulsions were clear and showed physicochemical parameters for desired topical delivery and stability. The permeation profiles of tazarotene through rat skin from optimized microemulsion formulation followed the Higuchi model for controlled permeation. Microemulsion-based gel was prepared by incorporating Carbopol®971P NF in optimized microemulsion formulation having suitable skin permeation rate and skin uptake. Microemulsion-based gel showed desired physicochemical parameters and demonstrated advantage over marketed formulation in improving the skin tolerability of tazarotene indicating its potential in improving its topical delivery. The developed microemulsion-based gel may be a potential drug delivery vehicle for targeted topical delivery of tazarotene in the treatment of acne.

Quantification of the level of fat-soluble vitamins in feed based on the novel microemulsion electrokinetic chromatography (MEEKC) method.

PubMed

Olędzka, Ilona; Kowalski, Piotr; Bałuch, Alicja; Bączek, Tomasz; Paradziej-Łukowicz, Jolanta; Taciak, Marcin; Pastuszewska, Barbara

2014-02-01

Simultaneous quantification of liposoluble vitamins is not a new area of interest, since these compounds co-determine the nutritional quality of food and feed, a field widely explored in the human and animal diet. However, the development of appropriate methods is still a matter of concern, especially when the vitamin composition is highly complex, as is the case with feed designated for laboratory animals, representing a higher health and microbiological status. A method combining microemulsion electrokinetic chromatography (MEEKC) with liquid-liquid extraction was developed for the determination of four fat-soluble vitamins in animal feed. A separation medium consisting of 25 mmol L⁻¹ phosphate buffer (pH 2.5), 2-propanol, 1-butanol, sodium dodecyl sulfate and octane allowed the simultaneous determination of vitamins A, D, E and K within a reasonable time of 25 min. The polarity of the separation voltage was reversed in view of the strongly suppressed electro-osmotic flow, and the applied voltage was set at 12 kV. The fat-soluble vitamins were separated in the order of decreasing hydrophobicity. It was proved that the proposed MEEKC method was sufficiently specific and sensitive for screening fat-soluble vitamins in animal feed samples after their sterilization. © 2013 Society of Chemical Industry.

[Study on extracting and separating curcuminoids from Curcuma longa rhizome using ultrasound strengthen by microemulsion].

PubMed

Yue, Chun-Hua; Zheng, Li-Tao; Guo, Qi-Ming; Li, Kun-Ping

2014-05-01

To establish a new method for the extraction and separation of curcuminoids from Curcuma longa rhizome by cloud-point preconcentration using microemulsions as solvent. The spectrophotometry was used to detect the solubility of curcumin in different oil phase, emulsifier and auxiliary emulsifier, and the microemulsion prescription was used for false three-phase figure optimization. The extraction process was optimized by uniform experiment design. The curcuminoids were separated from microemulsion extract by cloud-point preconcentration. Oil phase was oleic acid ethyl ester; Emulsifier was OP emulsifier; Auxiliary emulsifier was polyethylene glycol(peg) 400; The quantity of emulsifier to auxiliary emulsifier was the ratio of 5: 1; Microemulsion prescription was water-oleic acid ethyl ester-mixed emulsifier (0.45:0.1:0.45). The optimum extraction process was: time for 12.5 min, temperature of 52 degrees C, power of 360 W, frequency of 400 kHz, and the liquid-solid ratio of 40:1. The extraction rate of curcuminoids was 92.17% and 86.85% in microemulsion and oil phase, respectively. Curcuminoids is soluble in this microemulsion prescription with good extraction rate. This method is simple and suitable for curcuminoids extraction from Curcuma longa rhizome.

PREPARATION AND PROPERTIES OF COMPOUND ARNEBIAE RADIX MICROEMULSION GEL

PubMed Central

Chen, Jing; He, Yanping; Gao, Ting; Zhang, Licheng; Zhao, Yuna

2017-01-01

Background: Compound Arnebiae radix oil has been clinically applied to treat burns and scalds for a long time. However, it is unstable and inconvenient to use. The aim of this study was to prepare a compound Arnebiae radix microemulsion gel for transdermal delivery system and evaluate its characteristics. Materials and Methods: Based on the solubility of Shikonin, the active component of Arnebiae radix and the results of phase studies, adequate ratio of each component in microemulsion was determined. The optimized microemulsion gel was prepared using Carbomer 940. The gels were characterized in terms of appearance, preliminary stability test and the content of Shikonin in the compound Arnebiae radix microemulsion gel with HPLC analysis. Results: The optimized conditions for preparing microemulsion were Tween-80, glycerin, isopropyl myristate (IPM) with the ratio of 6:3:2. The optimal microemulsion gel was obtained with Carbomer 940 (1.0%). Conclusion: The prepared compound Arnebiae radix microemulsion gel showed good stability over time. It is more convenience in application than the previous used formulations. PMID:28480438

Heteropolytungstate nanoparticles: Microemulsion-mediated preparation and investigation of their catalytic activity in the epoxidation of olefins

DOE Office of Scientific and Technical Information (OSTI.GOV)

Masteri-Farahani, M., E-mail: mfarahany@yahoo.com; Ghorbani, M.

2016-04-15

Highlights: • Keggin type Q{sub 3}PW{sub 12}O{sub 40} nanoparticles were synthesized by using microemulsion system. • The nanoparticles have uniform size of about 25 nm and spherical morphologies. • The prepared nanoparticles act as reusable catalyst in the epoxidation of olefins with H{sub 2}O{sub 2}. - Abstract: Keggin type Q{sub 3}PW{sub 12}O{sub 40} nanoparticles (Q = cetyltrimethylammonium cation) were synthesized in water-in-oil (w/o) microemulsion consisted of water/cetyltrimethylammonium bromide/n-butanol/isooctane. Reaction of Na{sub 2}WO{sub 4}, Na{sub 2}HPO{sub 4} and hydrochloric acid within water containing nanoreactors of reverse micelles resulted in the preparation of Q{sub 3}PW{sub 12}O{sub 40} nanoparticles. The resultant nanoparticles weremore » analyzed by physicochemical methods such as FT-IR spectroscopy, X-ray diffraction, energy-dispersive X-ray analysis, thermogravimetric analyses (TGA-DTA), scanning and transmission electron microscopy and atomic force microscopy which show nearly uniform spherical nanoparticles with size of about 15 nm. Finally, catalytic activity of the Q{sub 3}PW{sub 12}O{sub 40} nanoparticles was examined in the epoxidation of olefins with H{sub 2}O{sub 2}. The prepared nanoparticles acted as recoverable and reusable catalyst in the epoxidation of olefins with H{sub 2}O{sub 2}.« less

Antioxidant and antimicrobial activities of clove bud essential oil and eugenol nanoparticles in alcohol-free microemulsion.

PubMed

Hamed, Said Fatouh; Sadek, Zainab; Edris, Amr

2012-01-01

Clove bud essential oil (CEO) and its major individual phenolic constituent eugenol were formulated as nanoparticles in water-based microemulsion systems. The oil titration method was used to incorporate different amounts of the oil and eugenol in the micellar solution of Tween-20. The Antioxidant and antimicrobial activities were evaluated using the DPPH* free radical scavenging assay and the agar disc dilution method, respectively. Results showed that microemulsion improved the evaluated activities of CEO and eugenol compared with the crude counterparts. Individual eugenol microemulsion was more effective than CEO microemulsion which contained only 61.7% eugenol among its constituents. The results of this study could have potential applications in water-based disinfectants, preservation and flavoring of food and in personal hygiene products. It may also have promising applications in the nutraceutical and functional beverage field.

The novel formulation design of self-emulsifying drug delivery systems (SEDDS) type O/W microemulsion III: the permeation mechanism of a poorly water soluble drug entrapped O/W microemulsion in rat isolated intestinal membrane by the Ussing chamber method.

PubMed

Araya, Hiroshi; Tomita, Mikio; Hayashi, Masahiro

2006-02-01

We used ibuprofen as a poorly water soluble model drug, to examine the influence of bile salts and mucin layers on the permeability of that entrapped in an O/W microemulsion, in a rat isolated intestinal membrane by the Ussing chamber method. Under the presence of 3 kinds of the primary bile salts such a sodium taurocholate, etc., or a secondary bile salt such a sodium taurochenodeoxycholate at 0.01 mmol/L concentration, a significant difference was not demonstrated in the permeation clearance of the ibuprofen entrapped O/W microemulsion, as compared with the case without the bile salts. Thus, the bile salts did not have a remarkable influence on the permeability of the drug entrapped in the O/W microemulsion, and it was verified that this O/W microemulsion was hardly influenced by the flow of the bile secretion. On the other hand, when N-acetyl-L-cysteine (NAC) with the removal ability of a mucin layer was combined with the ibuprofen entrapped O/W microemulsion at the concentration of 3 and 10 mmol/L, it was shown that the permeation clearance of free ibuprofen did not decrease, but that of ibuprofen entrapped in the O/W microemulsion decreased with the increase of the NAC concentration. Therefore, it is confirmed that the mucin layer participates in the permeability of the drug entrapped in the O/W microemulsion. From these results, the mechanism in which the drug entrapped in the O/W microemulsion is released in a mucin layer, without passing through the route of the mixed micelle formation by bile, thereafter the drug permeates an intestinal membrane, is supposed.

Effect of Fluorocarbon and Hydrocarbon Chain Lengths in Hybrid Surfactants for Supercritical CO2.

PubMed

Sagisaka, Masanobu; Ono, Shinji; James, Craig; Yoshizawa, Atsushi; Mohamed, Azmi; Guittard, Frédéric; Rogers, Sarah E; Heenan, Richard K; Yan, Ci; Eastoe, Julian

2015-07-14

Hybrid surfactants containing both fluorocarbon (FC) and hydrocarbon (HC) chains have recently been shown to solubilize water and form elongated reversed micelles in supercritical CO2. To clarify the most effective FC and HC chain lengths, the aggregation behavior and interfacial properties of hybrid surfactants FCm-HCn (FC length m/HC length n = 4/2, 4/4, 6/2, 6/4, 6/5, 6/6, and 6/8) were examined in W/CO2 mixtures as functions of pressure, temperature, and water-to-surfactant molar ratio (W0). The solubilizing power of hybrid surfactants for W/CO2 microemulsions was strongly affected by not only the FC length but also by that of the HC. Although the surfactants having short FC and/or HC tails (namely, m/n = 4/2, 4/4, and 6/2) did not dissolve in supercritical CO2 (even at ∼17 mM, ≤400 bar, temperature ≤ 75 °C, and W0 = 0-40), the other hybrid surfactants were able to yield transparent single-phase W/CO2 mixtures identified as microemulsions. The solubilizing power of FC6-HCm surfactants reached a maximum (W0 ∼ 80 at 45 °C and 350 bar) with a hydrocarbon length, m, of 4. The W0 value of 80 is the highest for a HC-FC hybrid surfactant, matching the highest value reported for a FC surfactant which contained more FC groups. High-pressure small-angle neutron scattering measurements from FCm-HCn/D2O/CO2 microemulsions were consistent with growth of the microemulsion droplets with increasing W0. In addition, not only spherical reversed micelles but also nonspherical assemblies (rodlike or ellipsoidal) were found for the systems with FC6-HCn (n = 4-6). At fixed surfactant concentration and W0 (17 mM and W0 = 20), the longest reversed micelles were obtained for FC6-HC6 where a mean aspect ratio of 6.3 was calculated for the aqueous cores.

Development and Evaluation of a Novel Microemulsion of Dexamethasone and Tobramycin for Topical Ocular Administration.

PubMed

Bachu, Rinda Devi; Stepanski, Marina; Alzhrani, Rami M; Jung, Rose; Boddu, Sai H S

2018-05-01

The purpose of this study was to develop and evaluate a novel dexamethasone- and tobramycin-loaded microemulsion for its potential for treating anterior segment eye infections. The microemulsion was evaluated for pH, particle size, zeta potential, light transmittance, morphology, and in vitro drug release. Sterility of the microemulsion was evaluated by direct as well as plate inoculation methods. Anti-inflammatory activity of dexamethasone, bactericidal activity of tobramycin, and cytotoxicity of the microemulsion were assessed and compared to that of the marketed eye drop suspension (Tobradex ® ). Histological evaluation was performed in bovine corneas to assess the safety of microemulsion in comparison to Tobradex suspension. In addition, the stability of the microemulsion was studied at 4°C, 25°C, and 40°C. The pH of the microemulsion was close to the pH of tear fluid. The microemulsion displayed an average globule size under 20 nm, with light transmittance around 95%-100%. The aseptically prepared microemulsion remained sterile for up to 14 days. The cytotoxicity of the microemulsion in bovine corneal endothelial cells was comparable to that of the Tobradex suspension. The anti-inflammatory activity of dexamethasone and the antibacterial activity of tobramycin from the microemulsion were significantly higher than those of the Tobradex suspension (P < 0.05). Histological evaluation showed an intact corneal epithelium without any signs of toxicity, and the developed microemulsion was found to be stable at 4°C and 25°C for 3 months. In conclusion, the developed microemulsion could be explored as a suitable alternative to the marketed suspension for treating anterior segment eye infections.

In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion.

PubMed

Zhang, Yong-Tai; Huang, Zhe-Bin; Zhang, Su-Juan; Zhao, Ji-Hui; Wang, Zhi; Liu, Ying; Feng, Nian-Ping

2012-01-01

To investigate the cellular uptake of evodiamine and rutaecarpine in a microemulsion in comparison with aqueous suspensions and tinctures. A microemulsion was prepared using the dropwise addition method. Mouse skin fibroblasts were cultured in vitro to investigate the optimal conditions for evodiamine and rutaecarpine uptake with different drug concentrations and administration times. Under optimal conditions, the cellular uptake of microemulsified drugs was assayed and compared to tinctures and aqueous suspensions. Rhodamine B labeling and laser scanning confocal microscopy (LSCM) were used to explore the distribution of fluorochrome transferred with the microemulsion in fibroblasts. Cellular morphology was also investigated, using optical microscopy to evaluate microemulsion-induced cellular toxicity. The maximum cellular drug uptake amounts were obtained with a 20% concentration (v/v) of microemulsion and an 8 hour administration time. Drug uptake by mouse skin fibroblasts was lowest when the drugs were loaded in microemulsion. After incubation with rhodamine B-labeled microemulsion for 8 hours, the highest fluorescence intensity was achieved, and the fluorochrome was primarily distributed in the cytochylema. No obvious cellular morphologic changes were observed with the administration of either the microemulsion or the aqueous suspension; for the tincture group, however, massive cellular necrocytosis was observed. The lower cellular uptake with microemulsion may be due to the fact that most of the drug loaded in the microemulsion vehicle was transported via the intercellular space, while a small quantity of free drug (released from the vehicle) was ingested through transmembrane transport. Mouse skin fibroblasts rarely endocytosed evodiamine and rutaecarpine with a microemulsion as the vehicle. The microemulsion had no obvious effect on cellular morphology, suggesting there is little or no cellular toxicity associated with the administration of microemulsion on mouse skin fibroblasts.

Microemulsion for simultaneous transdermal delivery of benzocaine and indomethacin: in vitro and in vivo evaluation.

PubMed

El Maghraby, Gamal M; Arafa, Mona F; Osman, Mohamed A

2014-12-01

This study investigated simultaneous transdermal delivery of indomethacin and benzocaine from microemulsion. Eucalyptus oil based microemulsion was used with Tween 80 and ethanol being employed as surfactant and cosurfactant, respectively. A microemulsion formulation comprising eucalyptus oil, polyoxyethylene sorbitan momooleate (Tween 80), ethanol and water (20:30:30:20) was selected. Indomethacin (1% w/w) and benzocaine (20% w/w) were incorporated separately or combined into this formulation before in vitro and in vivo evaluation. Application of indomethacin microemulsion enhanced the transdermal flux and reduced the lag time compared to saturated aqueous control. The same trend was evident for benzocaine microemulsion. Simultaneous application of the two drugs in microemulsion provided similar enhancement pattern. The in vivo evaluation employed the pinprick method and revealed rapid anesthesia after application of benzocaine microemulsion with the onset being 10 min and the action lasting for 50 min. For indomethacin microemulsion, the analgesic effect was recorded after 34.5 min and lasted for 70.5 min. Simultaneous application of benzocaine and indomethacin provided synergistic effect. The onset of action was achieved after 10 min and lasted for 95 min. The study highlighted the potential of microemulsion formulation in simultaneous transdermal delivery of two drugs.

Microemulsion utility in pharmaceuticals: Implications for multi-drug delivery.

PubMed

Callender, Shannon P; Mathews, Jessica A; Kobernyk, Katherine; Wettig, Shawn D

2017-06-30

Emulsion technology has been utilized extensively in the pharmaceutical industry. This article presents a comprehensive review of the literature on an important subcategory of emulsions, microemulsions. Microemulsions are optically transparent, thermodynamically stable colloidal systems, 10-100nm diameter, that form spontaneously upon mixing of oil, water and emulsifier. This review is the first to address advantages and disadvantages, as well as considerations and challenges in multi-drug delivery. For the period 1 January 2011-30 April 2016, 431 publications related to microemulsion drug delivery were identified and screened according to microemulsion, drug classification, and surfactant types. Results indicate the use of microemulsions predominantly in lipophilic drug delivery (79.4%) via oil-in-water microemulsions and non-ionic surfactants (90%) for oral or topical administration. Cancer is the disease state most targeted followed by inflammatory diseases, microbial infections and cardiovascular disease. Key generalizations from this analysis include: 1) microemulsion formulation is largely based on trial-and-error despite over 1200 publications related to microemulsion drug delivery since their discovery in 1943; 2) characterization using methods including interfacial tension, droplet size, electrical conductivity, turbidity and viscosity may provide additional information for greater predictability; 3) microemulsion drug delivery publications arise primarily from China (27%) and India (21%) suggesting additional research opportunities elsewhere. Copyright © 2017 Elsevier B.V. All rights reserved.

Phase boundaries, structural characteristics, and NMR spectra of ionic liquid-in-oil microemulsions containing double chain surface active ionic liquid: a comparative study.

PubMed

Rao, Vishal Govind; Mandal, Sarthak; Ghosh, Surajit; Banerjee, Chiranjib; Sarkar, Nilmoni

2013-02-07

A method developed for the first time, to create a huge number of ionic liquid (IL)-in-oil microemulsions has been discussed in our earlier publication (Rao, V. G.; Ghosh, S.; Ghatak, C.; Mandal, S.; Brahmachari, U.; Sarkar, N. J. Phys. Chem. B 2012, 116, 2850-2855). Here, we present facile methods to adjust the structural parameters of microemulsions using different ionic liquids (ILs) as additives (polar phase). We have characterized ILs/[C(4)mim][AOT]/benzene ternary system by performing a phase behavior study, dynamic light scattering (DLS) measurements, and (1)H NMR measurements. The IL loading capacity of microemulsions (area of single phase region) (i) increases with increase in alkyl chain length of cation of ILs and follows the trend [C(6)mim][TF(2)N] > [C(4)mim][TF(2)N] > [C(2)mim][TF(2)N], (ii) increases with decrease in cation anion interaction strength of added ILs and follows the trend [C(4)mim][TF(2)N] > [C(4)mim][PF(6)] > [C(4)mim][BF(4)]. So depending on the IL used, the amount of IL within the core of microemulsions can be easily manipulated to directly affect the size of aggregates in microemulsions. The size increase with increasing R value (R value is defined as the molar ratio of RTILs to [C(4)mim][AOT]) was found to be maximum in the case of [C(2)mim][TF(2)N]/[C(4)mim][AOT]/benzene microemulsions and follows the trend [C(2)mim][TF(2)N] > [C(4)mim][TF(2)N] > [C(6)mim][TF(2)N]. However, the size increase was almost the same with increase in R value in the case of ILs with different anions. The most promising fact about IL-in-oil microemulsions is their high thermal stability compared to that of aqueous microemulsions, so we investigated the effect of temperature on size of aggregates in microemulsions at R = 1.0. It is evident from dynamic light scattering measurements that the aggregates in microemulsions remain monodisperse in nature with increasing temperature, and in all the cases, the size of aggregates in microemulsions decreases with increasing temperature. The effect of water addition on IL-in-oil (IL/O) microemulsions was also studied in detail. By far, this is the first report where the effect of water addition on microemulsions containing hydrophobic ILs is being reported and compared with microemulsions containing hydrophilic ILs. We observed that the added water has a prominent effect on the microstructure of the microemulsions. In all the cases, (1)H NMR spectra provide more detailed information about intra/intermolecular interactions thus affording a clear picture of locations of (i) the RTILs in RTILs/[C(4)mim][AOT]/benzene microemulsions and (ii) the added water molecules in microemulsions.

Chiral separation of β-blockers by MEEKC using neutral microemulsion: Analysis of separation mechanism and further elucidation of resolution equation.

PubMed

Hu, Shao-Qiang; Lü, Wen-Juan; Ma, Yan-Hua; Hu, Qin; Dong, Li-Jun; Chen, Xing-Guo

2013-01-01

Based on the investigation of the effect of microemulsion charge on the chiral separation, a new chiral separation method with MEEKC employing neutral microemulsion was established. The method used a microemulsion containing 3.0% (w/v) neutral surfactant Tween 20 and 0.8% (w/v, 30 mM) dibutyl l-tartrate in 40 mM sodium tetraborate buffer to separate the enantiomers of β-blockers. The effect of major parameters on the chiral separation was investigated. The applied voltage had little effect on the resolution, but the chiral separation could be improved by suppressing the EOF. Nine racemic β-blockers obtained relatively good enantioseparation after appropriate concentrations of tetradecyl trimethyl ammonium bromide were added into the microemulsion to suppress the EOF. These results were explained based on the analysis of the separation mechanism of the method and deduced separation equations. The resolution equation of the method was further elucidated. It was found that the fourth term in the resolution equation, an additional term compared to the conventional resolution equation for column chromatography, represents the ratio of the relative movement distance between the analyte and microemulsion droplets relative to the effective capillary length. It can be regarded as a correction for the effective capillary length. These findings are significant for the development of the theory of MEEKC and the development of new chiral MEEKC method. © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Formulation and evaluation of microemulsion-based hydrogel for topical delivery

PubMed Central

Sabale, Vidya; Vora, Sejal

2012-01-01

Background: The purpose of this study was to develop microemulsion-based hydrogel formulation for topical delivery of bifonazole with an objective to increase the solubility and skin permeability of the drug. Materials and Methods: Oleic acid was screened as the oil phase of microemulsions, due to a good solubilizing capacity of the microemulison systems. The pseudo-ternary phase diagrams for microemulsion regions were constructed using oleic acid as the oil, Tween 80 as the surfactant and isopropyl alcohol (IPA) as the cosurfactant. Various microemulsion formulations were prepared and optimized by 32 factorial design on the basis of percentage (%) transmittance, globule size, zeta potential, drug release, and skin permeability. The abilities of various microemulsions to deliver bifonazole through the skin were evaluated ex vivo using Franz diffusion cells fitted with rat skins. The Hydroxy Propyl Methyl Cellulose (HPMC) K100 M as a gel matrix was used to construct the microemulsion-based hydrogel for improving the viscosity of microemulsion for topical administration. The optimized microemulsion-based hydrogel was evaluated for viscosity, spreadability, skin irritancy, skin permeability, stability, and antifungal activity by comparing it with marketed bifonazole cream. Results: The mechanism of drug release from microemulsion-based hydrogel was observed to follow zero order kinetics. The studied optimized microemulsion-based hydrogel showed a good stability over the period of 3 months. Average globule size of optimized microemulsion (F5) was found to be 18.98 nm, zeta potential was found to be -5.56 mv, and permeability of drug from microemulsion within 8 h was observed 84%. The antifungal activity of microemulsion-based hydrogel was found to be comparable with marketed cream. Conclusion: The results indicate that the studied microemulsion-based hydrogel (F5) has a potential for sustained action of drug release and it may act as promising vehicle for topical delivery of ibuprofen. PMID:23373005

Phase behavior and kinetics of phase separation of a nonionic microemulsion of C12E5/water/1-chlorotetradecane upon a temperature quench.

PubMed

Roshan Deen, G; Oliveira, Cristiano L P; Pedersen, Jan Skov

2009-05-21

The phase behavior and phase separation kinetics of a model ternary nonionic microemulsion system composed of pentaethylene glycol dodecyl ether (C12E5), water, and 1-chlorotetradecane were studied. With increasing temperature, the microemulsion exhibits the following rich phase behavior: oil-in-water phase (L1+O), droplet microemulsion phase (L1), lamellar liquid crystalline phase (Lproportional), and sponge-like (liquid) phase (L3). The microemulsion with a fixed surfactant-to-oil volume fraction ratio (Phis/Phio) of 0.81 and droplet volume fraction of 0.087 was perturbed from equilibrium by a temperature quench from the L1 region (24 degrees C) to an unstable region L1+O (13 degrees C), where the excess oil phase is in equilibrium with the microemulsion droplets. The process of phase separation in the unstable region was followed by time-resolved small-angle X-ray scattering (TR-SAXS) and time-resolved turbidity methods. Due to the large range of scattering vector (q=0.004-0.22 A(-1)) that is possible to access with the TR-SAXS method, the growth of the oil droplets and shrinking of the microemulsion droplets as a result of phase separation could be studied simultaneously. By using an advanced polydisperse ellipsoidal hard-sphere model, the experimental curves have been quantitatively analyzed. The microemulsion droplets were modeled as polydisperse core-shell ellipsoidal particles, using molecular constraints, and the oil droplets are modeled as polydisperse spheres. The radius of gyration (Rg) of the growing oil droplets, volume fraction of oil in the microemulsion droplets, and polydispersity were obtained from the fit parameters. The volume equivalent radius at the neutral plane between the surfactant head and tail of the microemulsion droplet decreased from 76 to 51 A, while the radius of oil drop increased to 217 A within the 160 min of the experiment. After about 48 min from the temperature quench, the system reaches a steady state and continues to coarsen at a constant fraction of the oil of 0.51 in the oil phase by Ostwald ripening with the power law dependence of Roil proportional, variant t1/3. The size of the oil droplets determined by the time-resolved turbidity method is in good agreement with that of the TR-SAXS, highlighting the usefulness of the method in the size determination of oil-in-water microemulsions on an absolute scale.

Lower irritation microemulsion-based rotigotine gel: formulation optimization and in vitro and in vivo studies

PubMed Central

Wang, Zheng; Mu, Hong-Jie; Zhang, Xue-Mei; Ma, Peng-Kai; Lian, Sheng-Nan; Zhang, Feng-Pu; Chu, Sheng-Ying; Zhang, Wen-Wen; Wang, Ai-Ping; Wang, Wen-Yan; Sun, Kao-Xiang

2015-01-01

Background Rotigotine is a potent and selective D1, D2, and D3 dopaminergic receptor agonist. Due to an extensive first-pass effect, it has a very low oral bioavailability (approximately 0.5% in rats). Purpose The present investigation aimed to develop a microemulsion-based hydrogel for transdermal rotigotine delivery with lower application site reactions. Methods Pseudoternary phase diagrams were constructed to determine the region of oil in water (o/w)-type microemulsion. Central composite design was used to support the pseudoternary phase diagrams and to select homogeneous and stable microemulsions with an optimal amount of rotigotine permeation within 24 hours. In vitro skin permeation experiments were performed, using Franz diffusion cells, to compare rotigotine-loaded microemulsions with rotigotine solutions in oil. The optimized formulation was used to prepare a microemulsion-based hydrogel, which was subjected to bioavailability and skin irritancy studies. Results The selected formulations of rotigotine-loaded microemulsions had enhanced flux and permeation coefficients compared with rotigotine in oil. The optimum microemulsion contained 68% water, 6.8% Labrafil®, 13.44% Cremophor® RH40, 6.72% Labrasol®, and 5.04% Transcutol® HP; the drug-loading rate was 2%. To form a microemulsion gel, 1% Carbomer 1342 was added to the microemulsion. The bioavailability of the rotigotine-loaded microemulsion gel was 105.76%±20.52% with respect to the marketed rotigotine patch (Neupro®). The microemulsion gel irritated the skin less than Neupro. Conclusion A rotigotine microemulsion-based hydrogel was successfully developed, and an optimal formulation for drug delivery was identified. This product could improve patient compliance and have broad marketability. PMID:25609965

Establishment of quantitative retention-activity model by optimized microemulsion liquid chromatography.

PubMed

Xu, Liyuan; Gao, Haoshi; Li, Liangxing; Li, Yinnong; Wang, Liuyun; Gao, Chongkai; Li, Ning

2016-12-23

The effective permeability coefficient is of theoretical and practical importance in evaluation of the bioavailability of drug candidates. However, most methods currently used to measure this coefficient are expensive and time-consuming. In this paper, we addressed these problems by proposing a new measurement method which is based on the microemulsion liquid chromatography. First, the parallel artificial membrane permeability assays model was used to determine the effective permeability of drug so that quantitative retention-activity relationships could be established, which were used to optimize the microemulsion liquid chromatography. The most effective microemulsion system used a mobile phase of 6.0% (w/w) Brij35, 6.6% (w/w) butanol, 0.8% (w/w) octanol, and 86.6% (w/w) phosphate buffer (pH 7.4). Next, support vector machine and back-propagation neural networks are employed to develop a quantitative retention-activity relationships model associated with the optimal microemulsion system, and used to improve the prediction ability. Finally, an adequate correlation between experimental value and predicted value is computed to verify the performance of the optimal model. The results indicate that the microemulsion liquid chromatography can serve as a possible alternative to the PAMPA method for determination of high-throughput permeability and simulation of biological processes. Copyright © 2016. Published by Elsevier B.V.

Optical study of xanthene-type dyes in nano-confined liquid

NASA Astrophysics Data System (ADS)

Mahdi Shavakandi, Seyyed; Alizadeh, Khalil; Sharifi, Soheil; Marti, Othmar; Amirkhani, Masoud

2017-04-01

The optical activity of dye molecules in different environments is of great interest for many applications such as laser system or biological imaging. We investigate the fluorescence and absorption spectrum of nano-confined xanthene dyes (RhB and fluorescein sodium salt) in a two-phase liquid. Each show very distinct optical behavior in the water phase of a reverse microemulsion. Their optical properties such as absorption and fluorescence for different concentrations of dye and nanodroplets are investigated. We show that for the same concentration of dye in the microemulsion the peak of fluorescence intensity is varied by altering the concentration of nanodroplets. However, the trend of the change is widely different depending on the hydrophobicity of dyes. Quantum-mechanical second order perturbation theory is used to calculate the ratio of dipole moments in the ground and excited states, which accounts for the Stokes shift in fluorescence peak. Photon correlation spectroscopy is employed to check the trace of the dye in the oil phase of the microemulsion.

[Analysis of phthalate esters in plastic-packaging bags on-line sample stacking-microemulsion electrokinetic chromatography].

PubMed

Xiao, Jia; Huang, Ying; Wang, Minyi; Chen, Guonan

2012-09-01

Two convenient, effective, and reproducible methods using microemulsion electrokinetic chromatography (MEEKC)-normal stacking mode (NSM) and reversed electrode polarity stacking mode (REPSM) were developed for the on-line sample stacking of phthalate esters (PAEs). REPSM coupled with MEEKC increased the sensitivity of 937.5 to 7,143 times for four PAEs compared to the conventional MEEKC. The separating conditions in the MEEKC method were studied, and many factors influencing the two sample stacking processes were investigated in detail. The optimum sample matrices for the two stacking methods were as follows: 30 mmol/L sodium cholate (SC) and 30.0 mmol/L borate (pH 8.5). Additionally, sample injections as large as 3.45 kPa x 40 s and 3.45 kPa x 90 s were applied for NSM-MEEKC and REPSM-MEEKC, respectively. The linear relationship and reproducibility were also examined. Under the optimum conditions, the detection limits (S/N = 3) of the PAEs were in the ranges of 0.021 - 0.33 mg/L and 0.7 - 4 microg/L for NSM-MEEKC and REPSM-MEEKC, respectively. The proposed REPSM-MEEKC has been successfully applied to determine PAEs in plastic-packaging bags, and the spiked recoveries were in the range of 89.1% - 105.6% with satisfactory results.

Analysis and antibacterial activity of Nigella sativa essential oil formulated in microemulsion system.

PubMed

Shaaban, Hamdy A; Sadek, Zainab; Edris, Amr E; Saad-Hussein, Amal

2015-01-01

The Essential oil (EO) of Nigella sativa (black cumin) was extracted from the crude oil and the volatile constituents were characterized using gas chromatographic analysis. The EO was formulated in water-based microemulsion system and its antibacterial activity against six pathogenic bacteria was evaluated using the agar well diffusion method. This activity was compared with two other well known biologically active natural and synthetic antimicrobials namely eugenol and Ceftriaxone(®). Results showed that N. sativa EO microemulsion was highly effective against S. aureus, B. cereus and S. typhimurium even at the lowest tested concentration of that EO in the microemulsion (100.0 μg/well). Interestingly, the EO microemulsion showed higher antibacterial activity than Ceftriaxone solution against S. typhimurium at 400.0 μg/well and almost comparable activity against E. coli at 500.0 μg/well. No activity was detected for the EO microemulsion against L. monocytogenes and P. aeruginosa. Eugenol which was also formulated in microemulsion was less effective than N. sativa EO microemulsion except against P. aeruginosa. The synthetic antibiotic (Ceftriaxone) was effective against most of the six tested bacterial strains. This work is the first report revealing the formulation of N. sativa EO in microemulsion system and investigating its antibacterial activity. The results may offer potential application of that water-based microemulsion in controlling the prevalence of some pathogenic bacteria.

A novel method to produce solid lipid nanoparticles using n-butanol as an additional co-surfactant according to the o/w microemulsion quenching technique.

PubMed

Mojahedian, Mohammad M; Daneshamouz, Saeid; Samani, Soliman Mohammadi; Zargaran, Arman

2013-09-01

Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC) are novel medicinal carriers for controlled drug release and drug targeting in different roots of administration such as parenteral, oral, ophthalmic and topical. These carriers have some benefits such as increased drug stability, high drug payload, the incorporation of lipophilic and hydrophilic drugs, and no biotoxicity. Therefore, due to the cost-efficient, proportionally increasable, and reproducible preparation of SLN/NLC and the avoidance of organic solvents used, the warm microemulsion quenching method was selected from among several preparation methods for development in this research. To prepare the warm O/W microemulsion, lipids (distearin, stearic acid, beeswax, triolein alone or in combination with others) were melted at a temperature of 65°C. After that, different ratios of Tween60 (10-22.5%) and glyceryl monostearate (surfactant and co-surfactant) and water were added, and the combination was stirred. Then, 1-butanol (co-surfactant) was added dropwise until a clear microemulsion was formed and titration continued to achieve cloudiness (to obtain the microemulsion zone). The warm o/w microemulsions were added dropwise into 4°C water (1:5 volume ratio) while being stirred at 400 or 600 rpm. Lipid nanosuspensions were created upon the addition of the warm o/w microemulsion to the cold water. The SLN were obtained over a range of concentrations of co-surfactants and lipids and observed for microemulsion stability (clearness). For selected preparations, characterization involved also determination of mean particle size, polydispersity and shape. According to the aim of this study, the optimum formulations requiring the minimum amounts of 1-butanol (1.2%) and lower temperatures for creation were selected. Mono-disperse lipid nanoparticles were prepared in the size range 77 ± 1 nm to 124 ± 21 nm according to a laser diffraction particle size analyzer and transmission electron microscopy. This method for preparing lipid nanoparticles by warm o/w microemulsion quenching was found to be more cost efficient and proportionally increasable in comparison with other preparation methods such as high pressure homogenization. These lipid nanoparticles, due to the combination of hard lipids with soft and/or liquid lipids, become good candidates for a wide range of medicaments as carriers for pharmaceutical and medicinal purposes. Crown Copyright © 2013. Published by Elsevier Ireland Ltd. All rights reserved.

Design and Development of Repaglinide Microemulsion Gel for Transdermal Delivery.

PubMed

Shinde, Ujwala A; Modani, Sheela H; Singh, Kavita H

2018-01-01

Microemulsion formulation of repaglinide, a BCS class II hypoglycemic agent with limited oral bioavailability, was developed considering its solubility in various oils, surfactants, and cosurfactants. The pseudo-ternary phase diagrams for microemulsion regions were constructed by water titration method at K m 1:1 and characterized for optical birefringence, percentage transmittance, pH, refractive index, globule size, zeta potential, viscosity, drug content, and thermodynamic stability. To enhance the drug permeation and residence time, the optimized microemulsions having mean globule size of 36.15 ± 9.89 nm was gelled with xanthan gum. The developed microemulsion-based gel was characterized for globule size, zeta potential, pH, and drug content. All evaluation parameters upon gelling were found to be satisfactory. Ex vivo permeability study across rat skin demonstrated higher steady-state flux (P < 0.05) for microemulsion of repaglinide in comparison to the repaglinide microemulsion gel. At the end of 24 h, the cumulative drug permeation from microemulsion and microemulsion gel was found to be 229.19 ± 24.34 and 180.84 ± 17.40 μg/cm 2 , respectively. The microemulsion formulation showed 12.30-fold increase in flux as compared to drug suspension with highest enhancement ratio (E r ) of 12.36. Whereas microemulsion gel exhibited 10.97-fold increase in flux (with highest E r , 11.78) as compared to repaglinide (RPG) suspension. In vivo efficacy study was performed in normal Sprague-Dawley rats by using oral glucose tolerance test. Results of RPG transdermal microemulsion gel demonstrated remarkable advantage over orally administered RPG by reducing the glucose level in controlled manner. Hence, it could be a new, alternative dosage form for effective therapy of type 2 diabetes mellitus.

Enhancement of transdermal delivery of ibuprofen using microemulsion vehicle

PubMed Central

Hu, Liandong; Hu, Qiaofeng; Yang, Jianxue

2014-01-01

Objective(s): The objective of this study was to find a stable microemulsion vehicle for transdermal delivery of ibuprofen to improve the skin permeability. Materials and Methods: Microemulsion was prepared using different sorts of oils, surfactants and co-surfactants. Pseudo-ternary phase diagrams were used to evaluate the microemulsion domain. The effects of oleic acid and surfactant mixture on skin permeation of ibuprofen were evaluated with excised skins. Results: The optimum formulation F3 consisting of 6% oleic acid, 30% Cremophor RH40/Transcutol P (2:1, w/w) and 59% water phase, showed a high permeation rate of 42.98 µg/cm2/hr. The mean droplet size of microemulsion was about 43 nm and no skin irritation signs were observed on the skin of rabbits. Conclusion: These results indicated that this novel microemulsion is a useful formulation for the transdermal delivery of ibuprofen. PMID:25729544

[Optimize preparation of compound licorice microemulsion with D-optimal design].

PubMed

Ma, Shu-Wei; Wang, Yong-Jie; Chen, Cheng; Qiu, Yue; Wu, Qing

2018-03-01

In order to increase the solubility of essential oil in compound licorice microemulsion and improve the efficacy of the decoction for treating chronic eczema, this experiment intends to prepare the decoction into microemulsion. The essential oil was used as the oil phase of the microemulsion and the extract was used as the water phase. Then the microemulsion area and maximum ratio of water capacity was obtained by plotting pseudo-ternary phase diagram, to determine the appropriate types of surfactant and cosurfactant, and Km value-the mass ratio between surfactant and cosurfactant. With particle size and skin retention of active ingredients as the index, microemulsion prescription was optimized by D-optimal design method, to investigate the in vitro release behavior of the optimized prescription. The results showed that the microemulsion was optimal with tween-80 as the surfactant and anhydrous ethanol as the cosurfactant. When the Km value was 1, the area of the microemulsion region was largest while when the concentration of extract was 0.5 g·mL⁻¹, it had lowest effect on the particle size distribution of microemulsion. The final optimized formulation was as follows: 9.4% tween-80, 9.4% anhydrous ethanol, 1.0% peppermint oil and 80.2% 0.5 g·mL⁻¹ extract. The microemulsion prepared under these conditions had a small viscosity, good stability and high skin retention of drug; in vitro release experiment showed that microemulsion had a sustained-release effect on glycyrrhizic acid and liquiritin, basically achieving the expected purpose of the project. Copyright© by the Chinese Pharmaceutical Association.

Development and Characterization of a Microemulsion System Containing Amphotericin B with Potential Ocular Applications.

PubMed

da Silveira, Walteçá Louis Lima; Damasceno, Bolivar P G L; Ferreira, Laura F; Ribeiro, Izabel L S; Silva, Karolyne S; Silva, André Leandro; Giannini, Maria José Mendes; da Silva-Júnior, Arnóbio Antônio; de Oliveira, Anselmo Gomes; do Egito, E Sócrates Tabosa

2016-01-01

Amphotericin B eye drops are widely used in the treatment of ocular infections. However, amphotericin's toxicity leads to low patient compliance and aggravation of symptoms. This work describes the development of a microemulsion system containing amphotericin B, aiming for its use in ocular applications. The microemulsion was developed by the titration technique. The physicochemical characteristics were determined with both loaded and unloaded amphotericin B-microemulsion. The nanostructures were analyzed by polarized light microscopy. The microdilution method was used to establish the minimum inhibitory concentration against fungal strains, and, therefore, evaluate the microemulsion activity. Additionally, in order to evaluate the microemulsion toxicity an in vitro toxicity assay against red blood cells was performed. The performed studies showed that the presence of amphotericin B loaded into the system did not induce serious changes in the physicochemical properties of the microemulsion when compared to the unloaded system. The spectrophotometric studies depicted amphotericin B-self-associated species, which allow predicting its behavior in vitro. The high pressure liquid chromatography results revealed high drug content entrapment in the microemulsion droplet. Finally, the amphotericin B-microemulsion in vitro susceptibility test showed high activity against Candida strains and a low toxicity profile against red blood cells when compared to Fungizone®. The physicochemical characterization of the microemulsion demonstrated that its characteristics are compatible with the topical ocular route, making it eligible for consideration as a new and interesting amphotericin B-deliverydosage form to be used as eye drop formulation.

Tuning Micellar Structures in Supercritical CO2 Using Surfactant and Amphiphile Mixtures.

PubMed

Peach, Jocelyn; Czajka, Adam; Hazell, Gavin; Hill, Christopher; Mohamed, Azmi; Pegg, Jonathan C; Rogers, Sarah E; Eastoe, Julian

2017-03-14

For equivalent micellar volume fraction (ϕ), systems containing anisotropic micelles are generally more viscous than those comprising spherical micelles. Many surfactants used in water-in-CO 2 (w/c) microemulsions are fluorinated analogues of sodium bis(2-ethylhexyl) sulfosuccinate (AOT): here it is proposed that mixtures of CO 2 -philic surfactants with hydrotropes and cosurfactants may generate elongated micelles in w/c systems at high-pressures (e.g., 100-400 bar). A range of novel w/c microemulsions, stabilized by new custom-synthesized CO 2 -phillic, partially fluorinated surfactants, were formulated with hydrotropes and cosurfactant. The effects of water content (w = [water]/[surfactant]), surfactant structure, and hydrotrope tail length were all investigated. Dispersed water domains were probed using high pressure small-angle neutron scattering (HP-SANS), which provided evidence for elongated reversed micelles in supercritical CO 2 . These new micelles have significantly lower fluorination levels than previously reported (6-29 wt % cf. 14-52 wt %), and furthermore, they support higher water dispersion levels than other related systems (w = 15 cf. w = 5). The intrinsic viscosities of these w/c microemulsions were estimated based on micelle aspect ratio; from this value a relative viscosity value can be estimated through combination with the micellar volume fraction (ϕ). Combining these new results with those for all other reported systems, it has been possible to "map" predicted viscosity increases in CO 2 arising from elongated reversed micelles, as a function of surfactant fluorination and micellar aspect ratio.

Heterogeneous enantioselective hydrogenation of beta-keto esters using chirally modified supported Ni nanoparticles

NASA Astrophysics Data System (ADS)

Acharya, Sushma

Enantioselective heterogeneous catalysis is an important and rapidly expanding research area. The two most heavily researched examples of this type of catalysis are the enantioselective hydrogenation of α-keto-esters over Pt-based catalysts and the enantioselective hydrogenation of β-keto-esters over Ni-based catalysts. These enantioselective surface reactions are controlled by the presence of adsorbed chiral molecules i.e. tartaric acid on the surface of the metal component of the catalyst. The work presented in this thesis focuses on two parts, the synthesis of pure nickel nanoparticles and enantioselective behavior of the modified nickel nanoparticles. The works on the synthesis of pure nickel nanoparticles were carried out using two methods, the reverse microemulsion and the reduction method. It was discovered that the reverse microemulsion method produced nickel oxide nanoparticles, whereas the reduction method produced pure nickel nanoparticles. Chiral modifications of Raney nickel (RNi) and C-supported catalysts were studied. The catalysts were employed in enantioselective hydrogenation of methyl acetoacetate (MAA) to (R) - and (S)-enantiomers of methyl 3-hydroxybutyrate (MHB). The effects of modification and hydrogenation parameters such as concentration of modifier temperature, pressure and solvent on the enantioselectivity of MAA hydrogenation were discussed. For RNi methanol was found to be the best solvent, with tartaric acid concentration 0.2 mol/L for achieving the highest enantiomeric excess under 8 bar at 70 oC. Characteristic features of the in-situ modification of Raney nickel and C-supported Ni were also evaluated and the results obtained were compared with the conventional (pre-modification) approach. Parameters for the conventional and in-situ methods were optimised in a series of experiments for both types of catalysts. The in-situ modified catalyst was found more active for both RNi and C-supported catalysts with 98 % and 42% enantiomeric excess, respectively.

Formulation, characterization, and in vitro/ex vivo evaluation of quercetin-loaded microemulsion for topical application.

PubMed

Kajbafvala, Azar; Salabat, Alireza; Salimi, Anayatollah

2016-12-09

The aim of this study was to develop a new microemulsion formulation for topical application of poorly soluble drug named quercetin. In order to design suitable microemulsion system, the pseudo-ternary phase diagrams of microemulsion systems were constructed at different surfactant/co-surfactant ratios using tween 80 as surfactant, transcutol ® P as a co-surfactant and oleic acid as an oil phase. Some physicochemical properties such as droplet size, density, refractive index, electrical conductivity, pH, surface tension, and viscosity of the microemulsion systems were measured at 298.15 K. The average hydrodynamic droplet size of the optimized microemulsions was obtained by dynamic light scattering method. Morphology assessment of the optimized quercetin-loaded microemulsion by transmission electron microscopy analysis indicated that the particles have the size of about 25 nm and spherical with narrow size distribution. Equilibrium solubility, in vitro drug release at a 24 h time period, release kinetic evaluation as well as ex vivo permeation and retention of quercetin-loaded microemulsions through rat skin has been investigated. The obtained results showed a slow release behavior without any transdermal delivery. Most of the formulations fitted best with zero-order kinetic model with a non-Fickian mechanisms. This study illustrated that the proposed QU-microemulsion has a good potential for use in sunscreen formulations. [Formula: see text].

Microstructure of microemulsion modified with ionic liquids in microemulsion electrokinetic chromatography and analysis of seven corticosteroids.

PubMed

Ni, Xinjiong; Yu, Meijuan; Cao, Yuhua; Cao, Guangqun

2013-09-01

In this work, the influences of ionic liquid (IL) as a modifier on microemulsion microstructure and separation performance in MEEKC were investigated. Experimental results showed that synergetic effect between IL 1-butyl-3-methylimidazolium tetrafluoro-borate (BmimBF4 ) and surfactant SDS gave a decreased CMC. With increment of IL in microemulsion, negative ζ potential of the microdroplets reduced gradually. The influence of IL on the dimensions of microdroplet was complicated. At BmimBF4 less than 8 mM, IL made microemulsion droplet smaller in size. While at BmimBF4 more than 10 mM, the size increased and reached to a maximum value at 12 mM, where the microdroplets were larger than that without IL. After that, the micreodroplet size decreased again. Relative fluorescence intensity of the first vibration band of pyrene to the third one (I1 /I3 ) enhanced as IL was added to microemulsion, which indicated that this addition increased environmental polarity in the inner core of microdroplets. Prednisone, hydrocortisone, prednisolone, hydrocortisone acetate, cortisone acetate, prednisolone acetate, and triamcinolone acetonide were analyzed with MEEKC modified with IL to evaluate the separation performance. Cortisone acetate and prednisolone acetate could not be separated at all in typical microemulsion. The seven analytes could be separated by the addition of 10 mM BmimBF4 into the microemulsion system. The method has been used for analysis of corticosteroids in cosmetic samples with simple extraction; the recoveries for seven analytes were between 86 and 114%. This method provides accuracy, reproducibility, pretreatment simplicity, and could be applied to the quality control of cosmetics. © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Analysis of phenolic acids by ionic liquid-in-water microemulsion liquid chromatography coupled with ultraviolet and electrochemical detector.

PubMed

Peng, Li-Qing; Cao, Jun; Du, Li-Jing; Zhang, Qi-Dong; Shi, Yu-Tin; Xu, Jing-Jing

2017-05-26

An environmentally friendly ionic liquid-in-water (IL/W) microemulsion was established and applied as mobile phase in microemulsion liquid chromatography (MELC) with ultraviolet (UV) detection or electrochemical detector (ECD) for analysis of phenolic compounds in real samples. The optimal condition of the method was using the best composition of microemulsion (0.2% w/v [HMIM]PF 6 , 1.0% w/v SDS, 3.0% w/v n-butanol, 95.8% v/v water, pH 2.5) with UV detection. The validation results indicated that the method provided high degree of sensitivity, precision and accuracy with the low limit of detections ranged from 17.9-238ng/mL, satisfactory mean recovery values in the range of 80.1-105% and good linearity (r 2 >0.9994). Additionally, this method exhibited high selectivity and resolution for the analytes and was more eco-friendly compared with traditional MELC method. Consequently, the established IL/W MELC method was successfully applied to simultaneously separate and determine target compounds in Danshen sample and its preparation. Copyright © 2017 Elsevier B.V. All rights reserved.

Preparation methods for monodispersed garlic oil microspheres in water using the microemulsion technique and their potential as antimicrobials.

PubMed

Zheng, Hua Ming; Li, Hou Bin; Wang, Da Wei; Liu, Dun

2013-08-01

Garlic oil is considered as a natural broad-spectrum antibiotic because of its well-known antimicrobial activity. However, the characteristics of easy volatility and poor aqueous solubility limit the application of garlic oil in industry. The purpose of the present work is to develop and evaluate an oil-free microemulsion by loading garlic oil in microemulsion system. Microemulsions were prepared with ethoxylated hydrogenated castor (Cremophor RH40) as surfactant, n-butanol (or ethanol) as cosurfactant, oleic acid-containing garlic oil as oil phase, and ultrapure water as water phase. The effects of the ratio of surfactant to cosurfactant and different oil concentration on the area of oil-in-water (O/W) microemulsion region in pseudoternary phase diagrams were investigated. The particle size and garlic oil encapsulation efficiency of the formed microemulsions with different formulations were also investigated. In addition, the antimicrobial activity in vitro against Escherichia coli and Staphylococcus aureus was assessed. The experimental results show that a stable microemulsion region can be obtained when the mass ratio of surfactant to cosurfactant is, respectively, 1:1, 2:1, and 3:1. Especially, when the mixture surfactants of RH40/n-butanol 2/1 (w/w) is used in the microemulsion formulation, the area of O/W microemulsion region is 0.089 with the particle size 13.29 to 13.85 nm and garlic oil encapsulation efficiency 99.5%. The prepared microemulsion solution exhibits remarkable antibacterial activity against S. aureus. © 2013 Institute of Food Technologists®

Effect of Synthesis Method of La1 - x Sr x MnO3 Manganite Nanoparticles on Their Properties

NASA Astrophysics Data System (ADS)

Shlapa, Yulia; Solopan, Sergii; Belous, Anatolii; Tovstolytkin, Alexandr

2018-01-01

Nanoparticles of lanthanum-strontium manganite were synthesized via different methods, namely, sol-gel method, precipitation from non-aqueous solution, and precipitation from reversal microemulsions. It was shown that the use of organic compounds and non-aqueous media allowed significantly decreasing of the crystallization temperature of nanoparticles, and the single-phased crystalline product was formed in one stage. Morphology and properties of nanoparticles depended on the method and conditions of the synthesis. The heating efficiency directly depended on the change in the magnetic parameters of nanoparticles, especially on the magnetization. Performed studies showed that each of these methods of synthesis can be used to obtain weakly agglomerated manganite nanoparticles; however, particles synthesized via sol-gel method are more promising for use as hyperthermia inducers. PACS: 61.46.Df 75.75.Cd 81.20. Fw

Crystallization using reverse micelles and water-in-oil microemulsion systems: the highly selective tool for the purification of organic compounds from complex mixtures.

PubMed

Kljajic, Alen; Bester-Rogac, Marija; Klobcar, Andrej; Zupet, Rok; Pejovnik, Stane

2013-02-01

The active pharmaceutical ingredient orlistat is usually manufactured using a semi-synthetic procedure, producing crude product and complex mixtures of highly related impurities with minimal side-chain structure variability. It is therefore crucial for the overall success of industrial/pharmaceutical application to develop an effective purification process. In this communication, we present the newly developed water-in-oil reversed micelles and microemulsion system-based crystallization process. Physiochemical properties of the presented crystallization media were varied through surfactants and water composition, and the impact on efficiency was measured through final variation of these two parameters. Using precisely defined properties of the dispersed water phase in crystallization media, a highly efficient separation process in terms of selectivity and yield was developed. Small-angle X-ray scattering, high-performance liquid chromatography, mass spectrometry, and scanning electron microscopy were used to monitor and analyze the separation processes and orlistat products obtained. Typical process characteristics, especially selectivity and yield in regard to reference examples, were compared and discussed. Copyright © 2012 Wiley Periodicals, Inc.

Transdermal delivery of paeonol using cubic gel and microemulsion gel

PubMed Central

Luo, Maofu; Shen, Qi; Chen, Jinjin

2011-01-01

Background The aim of this study was to develop new systems for transdermal delivery of paeonol, in particular microemulsion gel and cubic gel formulations. Methods Various microemulsion vehicles were prepared using isopropyl myristate as an oil phase, polyoxyethylated castor oil (Cremophor® EL) as a surfactant, and polyethylene glycol 400 as a cosurfactant. In the optimum microemulsion gel formulation, carbomer 940 was selected as the gel matrix, and consisted of 1% paeonol, 4% isopropyl myristate, 28% Cremophor EL/polyethylene glycol 400 (1:1), and 67% water. The cubic gel was prepared containing 3% paeonol, 30% water, and 67% glyceryl monooleate. Results A skin permeability test using excised rat skins indicated that both the cubic gel and microemulsion gel formulations had higher permeability than did the paeonol solution. An in vivo pharmacokinetic study done in rats showed that the relative bioavailability of the cubic gel and microemulsion gel was enhanced by about 1.51-fold and 1.28-fold, respectively, compared with orally administered paeonol suspension. Conclusion Both the cubic gel and microemulsion gel formulations are promising delivery systems to enhance the skin permeability of paeonol, in particular the cubic gel. PMID:21904450

Crocin loaded nano-emulsions: Factors affecting emulsion properties in spontaneous emulsification.

PubMed

Mehrnia, Mohammad-Amin; Jafari, Seid-Mahdi; Makhmal-Zadeh, Behzad S; Maghsoudlou, Yahya

2016-03-01

Spontaneous emulsification may be used for encapsulating bioactive compounds in food and pharmaceutical industry. It has several advantages over high energy and other low energy methods including, protecting sensitive compounds against severe conditions of high energy method and its ability to minimize surfactant, removal of cosurfactant and thermal stability compared with other low energy methods. In this study, we examined possibility of encapsulating highly soluble crocin in W/O micro-emulsions using spontaneous method which further could be used for making double emulsions. Nonionic surfactants of Span 80 and polyglycerol polyricinoleate (PGPR) were used for making micro-emulsions that showed the high potential of PGPR for spontaneous method. Surfactant to water ratio (SWR%) was evaluated to find the highest amount of aqueous phase which can be dispersed in organic phase. Droplet size decreased by increasing SWR toward the SWR=100% which had the smallest droplet size and then increased at higher levels of surfactant. By increasing SWR, shear viscosity increased which showed the high effect of PGPR on rheological properties. This study shows in addition to W/O micro-emulsions, spontaneous method could be used for preparing stable O/W micro-emulsions. Copyright © 2015 Elsevier B.V. All rights reserved.

Preparation, characterization and relative bioavailability of oral elemene o/w microemulsion.

PubMed

Zeng, Zhaowu; Zhou, Guanglin; Wang, Xiaoli; Huang, Eric Zhijian; Zhan, Xiaori; Liu, Jun; Wang, Shuling; Wang, Anming; Li, Haifeng; Pei, Xiaolin; Xie, Tian

2010-09-07

The objective was to develop an elemene oil/water (o/w) microemulsion and evaluate its characteristics and oral relative bioavailability in rats. Elemene was used as the oil phase and drug, polysorbate 80 as a surfactant along with ethanol, propylene glycol, and glycerol as the cosurfactants. The microemulsion was prepared by mixing method, or ultrasonication method in an ultrasonic bath. Its three-dimensional response surface diagram was drawn by Mathcad software. The microemulsion was characterized by visual observation, cross-polarized microscopy, size, zeta potential, acidity, viscosity, and surface tension measurement. The drug content and entrapment efficiency were determined by ultra fast liquid chromatography (UFLC) and liquid surface method. Blood was drawn from rats at different time points after oral administration of an elemene microemulsion or a commercial elemene emulsion for measurement of the drug in plasma by UFLC to establish the pharmacokinetic parameters and relative bioavailability. The elemene microemulsion as a clarified and isotropic system containing 1% elemene (w/v), 5% ethanol (v/v), 15% propylene glycol (v/v), 15% glycerol (v/v), and 5% polysorbate 80 (w/v), was characterized as (57.7 ± 2.8) nm in size, 0.485 ± 0.032 in polydispersity index, (3.2 ± 0.4) mv in zeta potential, (5.19 ± 0.08) in pH, 6 mpa·s in viscosity, (31.8 ± 0.3) mN·m(-1) in surface tension, (8.273 ± 0.018) mg·mL(-1) in content of β-elemene, and (99.81 ± 0.24)% in average entrapment efficiency. The area under the concentration-time curves from 0 h to 24 h (AUC(0→24h)) of the elemene microemulsion and commercial elemene emulsion were integrated to be 3.092 mg·h·L(-1) and 1.896 mg·h·L(-1) respectively, yielding a relative bioavailability of 163.1%. The present study demonstrates the elemene microemulsion as a new formulation with ease of preparation, high entrapment efficiency, excellent clarity, good stability, and improved bioavailability.

Preparation, characterization and relative bioavailability of oral elemene o/w microemulsion

PubMed Central

Zeng, Zhaowu; Zhou, Guanglin; Wang, Xiaoli; Huang, Eric Zhijian; Zhan, Xiaori; Liu, Jun; Wang, Shuling; Wang, Anming; Li, Haifeng; Pei, Xiaolin; Xie, Tian

2010-01-01

The objective was to develop an elemene oil/water (o/w) microemulsion and evaluate its characteristics and oral relative bioavailability in rats. Elemene was used as the oil phase and drug, polysorbate 80 as a surfactant along with ethanol, propylene glycol, and glycerol as the cosurfactants. The microemulsion was prepared by mixing method, or ultrasonication method in an ultrasonic bath. Its three-dimensional response surface diagram was drawn by Mathcad software. The microemulsion was characterized by visual observation, cross-polarized microscopy, size, zeta potential, acidity, viscosity, and surface tension measurement. The drug content and entrapment efficiency were determined by ultra fast liquid chromatography (UFLC) and liquid surface method. Blood was drawn from rats at different time points after oral administration of an elemene microemulsion or a commercial elemene emulsion for measurement of the drug in plasma by UFLC to establish the pharmacokinetic parameters and relative bioavailability. The elemene microemulsion as a clarified and isotropic system containing 1% elemene (w/v), 5% ethanol (v/v), 15% propylene glycol (v/v), 15% glycerol (v/v), and 5% polysorbate 80 (w/v), was characterized as (57.7 ± 2.8) nm in size, 0.485 ± 0.032 in polydispersity index, (3.2 ± 0.4) mv in zeta potential, (5.19 ± 0.08) in pH, 6 mpa·s in viscosity, (31.8 ± 0.3) mN·m−1 in surface tension, (8.273 ± 0.018) mg·mL−1 in content of β-elemene, and (99.81 ± 0.24)% in average entrapment efficiency. The area under the concentration-time curves from 0 h to 24 h (AUC0→24h) of the elemene microemulsion and commercial elemene emulsion were integrated to be 3.092 mg·h·L−1 and 1.896 mg·h·L−1 respectively, yielding a relative bioavailability of 163.1%. The present study demonstrates the elemene microemulsion as a new formulation with ease of preparation, high entrapment efficiency, excellent clarity, good stability, and improved bioavailability. PMID:20856831

Method for extracting metals from aqueous waste streams for long term storage

DOEpatents

Chaiko, D.J.

1995-03-07

A liquid-liquid extraction method for removing metals and hydrous metal colloids from waste streams is provided wherein said waste streams are contacted with a solvent system containing a water-in-oil microemulsion wherein the inverted micelles contain the extracted metal. A silicon alkoxide, either alone or in combination with other metal alkoxide compounds is added to the water-in-oil microemulsion, thereby allowing encapsulation of the extracted metal within a silicon oxide network. Lastly, the now-encapsulated metal is precipitated from the water-in-oil microemulsion phase to yield aggregates of metal-silicate particles having average individual particle sizes of approximately 40 nanometers. 2 figs.

Method for extracting metals from aqueous waste streams for long term storage

DOEpatents

Chaiko, D.J.

1993-01-01

A liquid-liquid extraction method for removing metals and hydrous metal colloids from waste streams is provided wherein said waste streams are contacted with a solvent system containing a water-in-oil microemulsion wherein the inverted micelles contain the extracted metal. A silicon alkoxide, either alone or in combination with other metal alkoxide compounds is added to the water-in-oil microemulsion, thereby allowing encapsulation of the extracted metal within a silicon oxide network. Lastly, the now-encapsulated metal is precipitated from the water-in-oil microemulsion phase to yield aggregates of metal-silicate particles having average. individual particle sizes of approximately 40 manometers.

Method for extracting metals from aqueous waste streams for long term storage

DOEpatents

Chaiko, David J.

1995-01-01

A liquid--liquid extraction method for removing metals and hydrous metal colloids from waste streams is provided wherein said waste streams are contacted with a solvent system containing a water-in-oil microemulsion wherein the inverted micelles contain the extracted metal. A silicon alkoxide, either alone or in combination with other metal alkoxide compounds is added to the water-in-oil microemulsion, thereby allowing encapsulation of the extracted metal within a silicon oxide network. Lastly, the now-encapsulated metal is precipitated from the water-in-oil microemulsion phase to yield aggregates of metal-silicate particles having average individual particle sizes of approximately 40 nanometers.

Biotinylated vanadium and chromium sulfide nanoparticles as probes for colocalization of membrane proteins.

PubMed

Loukanov, Alexandre; Emin, Saim

2016-09-01

We report the microemulsion synthesis of vanadium and chromium sulfide nanoparticles (NPs) and their biological application as nanoprobes for colocalization of membrane proteins. Spherical V2 S3 and Cr2 S3 NPs were prepared in reverse microemulsion droplets, as nanoreactors, obtained by the surfactant sodium bis(2-ethylhexyl) sulfosuccinate (AOT) in nonpolar organic phase (heptane). Electron microscopic data indicated that the size distribution of the nanoparticles was uniform with an average diameter between 3 ÷ 5 nm. The prepared hydrophobic nanocrystals were transferred in aqueous phase by surface cap exchange of AOT with biotin-dihydrolipoic ligands. This substitution allows the nanoparticles solubility in aqueous solutions and confer their bioactivity. In addition, we report the conjugation procedure between α-Lipoic acid (LA) and biotin (abbreviated as biotin-LA). The biotin-LA structure was characterized by 1D and 2D NMR spectroscopy. The biotinylated vanadium and chromium sulfide nanoparticles were tested as probes for colocalization of glutamate receptors on sodium-dodecyl-sulfate-digested replica prepared from rat hippocampus. The method suggests their high labeling efficiency for study of membrane biological macromolecules. Microsc. Res. Tech. 79:799-805, 2016. © 2016 Wiley Periodicals, Inc. © 2016 Wiley Periodicals, Inc.

Nanocarrier-based hydrogel of betamethasone dipropionate and salicylic acid for treatment of psoriasis

PubMed Central

Baboota, Sanjula; Alam, Md Sarfaraz; Sharma, Shrestha; Sahni, Jasjeet K; Kumar, Anil; Ali, Javed

2011-01-01

Introduction: Betamethasone dipropionate (BD) has anti-inflammatory, immunomodulatory, and antiproliferative activity. The aim of the current work was to test the hypothesis that the addition of corticosteroid such as BD and a keratolytic agent such as salicylic acid in nanocarrier based microemulsions formulation would result in enhancement and sustaining of corticosteroid delivery rate leading to better anti-psoriatic activity. Clinical use of BD is restricted to some extent due to its poor permeability across the skin. So to increase its permeation across the skin, microemulsion-based gel formulations were prepared and characterised. Materials and Methods: Microemulsions were prepared by aqueous phase titration method, using oleic acid:sefsol (1.5:1), Tween 20, isopropyl alcohol, and distilled water as the oil phase, surfactant, cosurfactant and aqueous phase, respectively. Selected formulations were subjected to physical stability studies and consequently in vitro skin permeation studies. Surface studies of optimized formulation were done by transmission electron microscopy. In vivo anti-inflammatory activity was done by carageenan-induced raw paw edema method. Results: The droplet size of microemulsions ranged from 60 to 190 nm. The optimized formulation exhibited viscosity 28.55 ± 2.03 mP, refractive index 1.409, pH 6.4, and conductivity 10-4 scm-1. The optimized microemulsion was converted into hydrogel using carbopol 934, and salicylic acid was incorporated into it. Drug deposition in skin was found to be 29.73 μg/mg. Assessment of skin permeation was done by histopathology studies which indicated changes in the structure of epidermal membrane of skin. In vivo anti-inflammatory activity indicated 72.11% and 43.96% inhibition of inflammation in case of developed microemulsion gel and marketed gel, respectively. Conclusions: The developed microemulsion gel containing BD and salicylic acid provided sustained and good anti-inflammatory activity for the treatment of psoriasis. PMID:23071936

Determination of drug lipophilicity by phosphatidylcholine-modified microemulsion high-performance liquid chromatography.

PubMed

Xuan, Xueyi; Xu, Liyuan; Li, Liangxing; Gao, Chongkai; Li, Ning

2015-07-25

A new biomembrane-mimetic liquid chromatographic method using a C8 stationary phase and phosphatidylcholine-modified (PC-modified) microemulsion mobile phase was used to estimate unionized and ionized drugs lipophilicity expressed as an n-octanol/water partition coefficient (logP and logD). The introduction of PC into sodium dodecyl sulfate (SDS) microemulsion yielded a good correlation between logk and logD (R(2)=0.8). The optimal composition of the PC-modified microemulsion liquid chromatography (PC-modified MELC) mobile phase was 0.2% PC-3.0% SDS-6.0% n-butanol-0.8% ethyl acetate-90.0% water (pH 7.0) for neutral and ionized molecules. The interactions between the analytes and system described by this chromatographic method is more similar to biological membrane than the n-octanol/water partition system. The result in this paper suggests that PC-modified MELC can serve as a possible alternative to the shake-flask method for high-throughput unionized and ionized drugs lipophilicity determination and simulation of biological processes. Copyright © 2015 Elsevier B.V. All rights reserved.

Oral bioavailability enhancement of raloxifene by developing microemulsion using D-optimal mixture design: optimization and in-vivo pharmacokinetic study.

PubMed

Shah, Nirmal; Seth, Avinashkumar; Balaraman, R; Sailor, Girish; Javia, Ankur; Gohil, Dipti

2018-04-01

The objective of this work was to utilize a potential of microemulsion for the improvement in oral bioavailability of raloxifene hydrochloride, a BCS class-II drug with 2% bioavailability. Drug-loaded microemulsion was prepared by water titration method using Capmul MCM C8, Tween 20, and Polyethylene glycol 400 as oil, surfactant, and co-surfactant respectively. The pseudo-ternary phase diagram was constructed between oil and surfactants mixture to obtain appropriate components and their concentration ranges that result in large existence area of microemulsion. D-optimal mixture design was utilized as a statistical tool for optimization of microemulsion considering oil, S mix , and water as independent variables with percentage transmittance and globule size as dependent variables. The optimized formulation showed 100 ± 0.1% transmittance and 17.85 ± 2.78 nm globule size which was identically equal with the predicted values of dependent variables given by the design expert software. The optimized microemulsion showed pronounced enhancement in release rate compared to plain drug suspension following diffusion controlled release mechanism by the Higuchi model. The formulation showed zeta potential of value -5.88 ± 1.14 mV that imparts good stability to drug loaded microemulsion dispersion. Surface morphology study with transmission electron microscope showed discrete spherical nano sized globules with smooth surface. In-vivo pharmacokinetic study of optimized microemulsion formulation in Wistar rats showed 4.29-fold enhancements in bioavailability. Stability study showed adequate results for various parameters checked up to six months. These results reveal the potential of microemulsion for significant improvement in oral bioavailability of poorly soluble raloxifene hydrochloride.

Dynamic and spectroscopic studies of nano-micelles comprising dye in water/ dioctyl sodium sulfosuccinate /decane droplet microemulsion at constant water content

NASA Astrophysics Data System (ADS)

Rahdar, Abbas; Almasi-Kashi, Mohammad

2017-01-01

In the present work, the dynamic and spectroscopic properties of water-in-decane dioctyl sodium sulfosuccinate (AOT) microemulsions comprising dye, Rhodamine B (RB), were studied by varying content of decane at the constant water content (W = 20), by using dynamic light scattering (DLS), UV/visible, and fluorescence techniques. The characterization results of DLS of AOT micelles showed that by decreasing concentration of Rhodamine B in the water/AOT/decane microemulsion, the inter-droplet interactions changed from attractive to repulsive as the mass fraction of nano-droplets (MFD) increased. A deviation in the absorption spectra of Rhodamine B from the Beer's law at the high Rhodamine B concentration (0.001) was observed in the AOT reversed micelles. The Quenching in the emission intensity of AOT droplets comprising Rhodamine B and red shift in λmax of fluorescence of dye was observed as a function of concentration of RB in AOT RMs. The Stokes shift of AOT droplets containing the high concentration of RB, increased with mass fraction of nano-droplet (MFD), whereas at the low Rhodamine B concentration, its variation remained constant up to MFD = 0.07, and then increased.

Enantioseparation of dopa and related compounds by cyclodextrin-modified microemulsion electrokinetic chromatography.

PubMed

Borst, Claudia; Holzgrabe, Ulrike

2008-09-19

A chiral microemulsion electrokinetic chromatography method has been developed for the enantiomeric separation of 3,4-dihydroxyphenylalanine (dopa), its precursors phenylalanine and tyrosine, and the structurally related substance methyldopa. The separations were achieved using an oil-in-water microemulsion, which consisted of the oil-compound ethyl acetate, the surfactant sodium dodecylsulfate (SDS), the co-surfactant 1-butanol, the organic modifier propan-2-ol and 20mM phosphate buffer pH 2.5 or 2.0 as aqueous phase. For enantioseparation sulfated beta-cyclodextrin was added. The resolution of each racemate was optimized by varying the concentration of the buffer and all components of the microemulsion. Enantioseparation could be achieved for dl-dopa, dl-phenylalanine and dl-tyrosine within 13 min with a resolution of 4.3, 3.1 and 3.3, respectively, and for methyldopa in 17 min (Rs: 1.4). The established methods allowed the detection of dopa, phenylalanine, tyrosine and methyldopa with a limit at 0.5, 1.0, 0.2 and 2.0 microg/ml.

Antitumor efficacy of a novel CLA-PTX microemulsion against brain tumors: in vitro and in vivo findings

PubMed Central

Li, Dan; Yang, Ke; Li, Jie-Si; Ke, Xi-Yu; Duan, Yu; Du, Ruo; Song, Ping; Yu, Ke-Fu; Ren, Wei; Huang, Dan; Li, Xing-Huo; Hu, Xin; Zhang, Xuan; Zhang, Qiang

2012-01-01

Background Considering the observations that linoleic acid conjugated with paclitaxel (CLA-PTX) possesses antitumor activity against brain tumors, is able to cross the blood–brain barrier, but has poor water solubility, the purpose of this study was to prepare a novel CLA-PTX microemulsion and evaluate its activity against brain tumors in vitro and in vivo. Methods The in vitro cytotoxicity of a CLA-PTX microemulsion was investigated in C6 glioma cells. The in vivo antitumor activity of the CLA-PTX microemulsion was evaluated in tumor-bearing nude mice and rats. The pharmacokinetics of the CLA-PTX microemulsion were investigated in rats, and its safety was also evaluated in mice. Results The average droplet size of the CLA-PTX microemulsion was approximately 176.3 ± 0.8 nm and the polydispersity index was 0.294 ± 0.024. In vitro cytotoxicity results showed that the IC50 of the CLA-PTX microemulsion was 1.61 ± 0.83 μM for a C6 glioma cell line, which was similar to that of free paclitaxel and CLA-PTX solution (P > 0.05). The antitumor activity of the CLA-PTX microemulsion against brain tumors was confirmed in our in vivo C6 glioma tumor-bearing nude mice as well as in a rat model. In contrast, Taxol® had almost no significant antitumor effect in C6 glioma tumor-bearing rats, but could markedly inhibit growth of C6 tumors in C6 glioma tumor-bearing nude mice. The pharmacokinetic results indicated that CLA-PTX in solution has a much longer circulation time and produces higher drug plasma concentrations compared with the CLA-PTX microemulsion. The results of the acute toxicity study showed that the LD50 of CLA-PTX solution was 103.9 mg/kg. In contrast, the CLA-PTX microemulsion was well tolerated in mice when administered at doses up to 200 mg/kg. Conclusion CLA-PTX microemulsion is a novel formulation with significant antitumor efficacy in the treatment of brain tumors, and is safer than CLA-PTX solution. PMID:23269869

Environmentally friendly ionic liquid-in-water microemulsions for extraction of hydrophilic and lipophilic components from Flos Chrysanthemi.

PubMed

Chen, Jue; Cao, Jun; Gao, Wen; Qi, Lian-Wen; Li, Ping

2013-10-21

Ionic liquids (ILs) have numerous chemical applications as environmentally green solvents that are extending into microemulsion applications. In this work, a novel benign IL-in-water microemulsion system modified by an IL surfactant has been proposed for simultaneous extraction of hydrophilic and lipophilic constituents from Flos Chrysanthemi (Chrysanthemum morifolium). Constituents were analyzed by rapid-resolution liquid chromatography coupled with quadrupole time-of-flight mass spectrometry. A mixture-design approach was used to optimize the IL surfactant and the IL oil phase in the microemulsion system. Microemulsions consisting of 6.0% 1-dodecyl-3-methylimidazolium hydrogen sulfate, 0.1% 1-vinyl-3-methylimidazolium hexafluorophosphate and 93.9% water offered the acceptable extract efficiency that are comparable to or even better than conventional volatile organic solvents. This assay was fully validated with respect to the linearity of response (r(2) > 0.999 over two orders of magnitude), precision (intra-RSD < 0.49 and inter-day RSD < 2.21), and accuracy (recoveries ranging from 93.73% to 101.84%). The proposed IL-in-water microemulsion method provided an environmentally friendly alternative for efficient extraction of compounds from Flos Chrysanthemi and could be extended to complex environmental and pharmaceutical samples.

Pressure-Responsive, Surfactant-Free CO2-Based Nanostructured Fluids

PubMed Central

2017-01-01

Microemulsions are extensively used in advanced material and chemical processing. However, considerable amounts of surfactant are needed for their formulation, which is a drawback due to both economic and ecological reasons. Here, we describe the nanostructuration of recently discovered surfactant-free, carbon dioxide (CO2)-based microemulsion-like systems in a water/organic-solvent/CO2 pressurized ternary mixture. “Water-rich” nanodomains embedded into a “water-depleted” matrix have been observed and characterized by the combination of Raman spectroscopy, molecular dynamics simulations, and small-angle neutron scattering. These single-phase fluids show a reversible, pressure-responsive nanostructuration; the “water-rich” nanodomains at a given pressure can be instantaneously degraded/expanded by increasing/decreasing the pressure, resulting in a reversible, rapid, and homogeneous mixing/demixing of their content. This pressure-triggered responsiveness, together with other inherent features of these fluids, such as the absence of any contaminant in the ternary mixture (e.g., surfactant), their spontaneous formation, and their solvation capability (enabling the dissolution of both hydrophobic and hydrophilic molecules), make them appealing complex fluid systems to be used in molecular material processing and in chemical engineering. PMID:28846386

Microemulsion-based lycopene extraction: Effect of surfactants, co-surfactants and pretreatments.

PubMed

Amiri-Rigi, Atefeh; Abbasi, Soleiman

2016-04-15

Lycopene is a potent antioxidant that has received extensive attention recently. Due to the challenges encountered with current methods of lycopene extraction using hazardous solvents, industry calls for a greener, safer and more efficient process. The main purpose of present study was application of microemulsion technique to extract lycopene from tomato pomace. In this respect, the effect of eight different surfactants, four different co-surfactants, and ultrasound and enzyme pretreatments on lycopene extraction efficiency was examined. Experimental results revealed that application of combined ultrasound and enzyme pretreatments, saponin as a natural surfactant, and glycerol as a co-surfactant, in the bicontinuous region of microemulsion was the optimal experimental conditions resulting in a microemulsion containing 409.68±0.68 μg/glycopene. The high lycopene concentration achieved, indicates that microemulsion technique, using a low-cost natural surfactant could be promising for a simple and safe separation of lycopene from tomato pomace and possibly from tomato industrial wastes. Copyright © 2015 Elsevier Ltd. All rights reserved.

Nose to brain microemulsion-based drug delivery system of rivastigmine: formulation and ex-vivo characterization.

PubMed

Shah, Brijesh M; Misra, Manju; Shishoo, Chamanlal J; Padh, Harish

2015-01-01

Alzheimer's disease (AD) is a progressive neurodegenerative disorder leading to irreversible loss of neurons, cognition and formation of abnormal protein aggregates. Rivastigmine, a reversible cholinesterase inhibitor used for the treatment of AD, undergoes extensive first-pass metabolism, thus limiting its absolute bioavailability to only 36% after 3-mg dose. Due to extreme aqueous solubility, rivastigmine shows poor penetration and lesser concentration in the brain thus requiring frequent oral dosing. This investigation was aimed to formulate microemulsion (ME) and mucoadhesive microemulsions (MMEs) of rivastigmine for nose to brain delivery and to compare percentage drug diffused for both systems using in-vitro and ex-vivo study. Rivastigmine-loaded ME and MMEs were prepared by titration method and characterized for drug content, globule size distribution, zeta potential, pH, viscosity and nasal ciliotoxicity study. Rivastigmine-loaded ME system containing 8% w/w Capmul MCM EP, 44% w/w Labrasol:Transcutol-P (1:1) and 48% w/w distilled water was formulated, whereas 0.3% w/w chitosan (CH) and cetyl trimethyl ammonium bromide (as mucoadhesive agents) were used to formulate MMEs, respectively. ME and MMEs formulations were transparent with drug content, globule size and zeta potential in the range of 98.59% to 99.43%, 53.8 nm to 55.4 nm and -2.73 mV to 6.52 mV, respectively. MME containing 0.3% w/w CH followed Higuchi model (r(2) = 0.9773) and showed highest diffusion coefficient. It was free from nasal ciliotoxicity and stable for three months. However, the potential of developed CH-based MME for nose to brain delivery of rivastigmine can only be established after in-vivo and biodistribution study.

Facile preparation of highly-dispersed cobalt-silicon mixed oxide nanosphere and its catalytic application in cyclohexane selective oxidation

PubMed Central

2011-01-01

Highly dispersed cobalt-silicon mixed oxide [Co-SiO2] nanosphere was successfully prepared with a modified reverse-phase microemulsion method. This material was characterized in detail by X-ray diffraction, transmission electron microscopy, Fourier transform infrared, ultraviolet-visible diffuse reflectance spectra, X-ray absorption spectroscopy near-edge structure, and N2 adsorption-desorption measurements. High valence state cobalt could be easily obtained without calcination, which is fascinating for the catalytic application for its strong oxidation ability. In the selective oxidation of cyclohexane, Co-SiO2 acted as an efficient catalyst, and good activity could be obtained under mild conditions. PMID:22067075

Surfactant-free microemulsion electrokinetic chromatography (SF-MEEKC) with UV and MS detection - a novel approach for the separation and ESI-MS detection of neutral compounds.

PubMed

Mohorič, Urška; Beutner, Andrea; Krickl, Sebastian; Touraud, Didier; Kunz, Werner; Matysik, Frank-Michael

2016-12-01

Microemulsion electrokinetic chromatography (MEEKC) is a powerful tool to separate neutral species based on differences in their hydrophobic and hydrophilic properties. However, as a major drawback the conventionally used SDS based microemulsions are not compatible with electrospray ionization mass spectrometry (ESI-MS). In this work, a surfactant-free microemulsion (SFME) consisting of water, ethanol, and 1-octanol is used for surfactant-free microemulsion electrokinetic chromatography (SF-MEEKC). Ammonium acetate was added to the SFME enabling electrophoretic separations. The stability of SFMEs containing ammonium acetate was investigated using small-angle X-ray scattering and dynamic light scattering. A method for the separation of a model system of hydrophobic and hydrophilic neutral vitamins, namely the vitamins B 2 and D 3 , and the cationic vitamin B 1 was developed using UV/VIS detection. The influence of the ammonium acetate concentration on the separation performance was studied in detail. The method was characterized concerning reproducibility of migration times and peak areas and concerning the linearity of the calibration data. Furthermore, SF-MEEKC was coupled to ESI-MS investigating the compatibility between SFMEs and the ESI process. The signal intensities of ESI-MS measurements of the model analytes were comparable for SFMEs and aqueous systems. Finally, the vitamin D 3 content of a drug treating vitamin D 3 deficiency was determined by SF-MEEKC coupled to ESI-MS using 25-hydroxycholecalciferol as an internal standard. Graphical abstract The concept of surfactant-free microemulsion electrokinetic chromatography coupled to electrospray ionization mass spectrometry.

Formation, thermodynamic properties, microstructures and antimicrobial activity of mixed cationic/non-ionic surfactant microemulsions with isopropyl myristate as oil.

PubMed

Bardhan, Soumik; Kundu, Kaushik; Das, Sajal; Poddar, Madhumita; Saha, Swapan K; Paul, Bidyut K

2014-09-15

Modification of the interface by blending of surfactants produces considerable changes in the elastic rigidity of the interface, which in turn affects the physicochemical properties of w/o microemulsions. Hence, it could be possible to tune the thermodynamic properties, microstructures and antimicrobial activity of microemulsions by using ionic/non-ionic mixed surfactants and polar lipophilic oil, which are widely used in biologically relevant systems. The present report was aimed at precise characterization of mixed cetyltrimethylammonium bromide and polyoxyethylene (23) lauryl ether microemulsions stabilized in 1-pentanol (Pn) and isopropyl myristate at different physicochemical conditions by employing phase studies, the dilution method, conductivity, DLS, FTIR (with HOD probing) and (1)H NMR measurements. Further, microbiological activities at different compositions were examined against two bacterial strains Bacillus subtilis and Escherichia coli at 303 K. The formation of mixed surfactant microemulsions was found to be spontaneous at all compositions, whereas it was endothermic at equimolar composition. FTIR and (1)H NMR measurements showed the existence of bulk-like, bound and trapped water molecules in confined environments. Interestingly, composition dependence of both highest and lowest inhibitory effects was observed against the bacterial strains, whereas similar features in spontaneity of microemulsion formation were also evidenced. These results suggested a close relationship between thermodynamic stability and antimicrobial activities. Such studies on polar lipophilic oil derived mixed surfactant microemulsions have not been reported earlier. Copyright © 2014 Elsevier Inc. All rights reserved.

Enhanced Solubility and Permeability of Salicis cortex Extract by Formulating as a Microemulsion.

PubMed

Piazzini, Vieri; Bigagli, Elisabetta; Luceri, Cristina; Bilia, Anna Rita; Bergonzi, Maria Camilla

2018-04-24

A microemulsion system was developed and investigated as a novel oral formulation to increase the solubility and absorption of Salicis cortex extract. This extract possesses many pharmacological activities, in particular, it is beneficial for back pain and osteoarthritic and rheumatic complaints. In this work, after qualitative and quantitative characterization of the extract and the validation of an HPLC/diode array detector analytical method, solubility studies were performed to choose the best components for microemulsion formulation. The optimized microemulsion consisted of 2.5 g of triacetin, as the oil phase, 2.5 g of Tween 20 as the surfactant, 2.5 g of labrasol as the cosurfactant, and 5 g of water. The microemulsion was visually checked, characterized by light scattering techniques and morphological observations. The developed formulation appeared transparent, the droplet size was around 40 nm, and the ζ -potential result was negative. The maximum loading content of Salicis cortex extract resulted in 40 mg/mL. Furthermore, storage stability studies and an in vitro digestion assay were performed. The advantages offered by microemulsion were evaluated in vitro using artificial membranes and cells, i.e., parallel artificial membrane permeability assay and a Caco-2 model. Both studies proved that the microemulsion was successful in enhancing the permeation of extract compounds, so it could be useful to ameliorate the bioefficacy of Salicis cortex. Georg Thieme Verlag KG Stuttgart · New York.

CUTANEOUS DELIVERY OF α-TOCOPHEROL AND LIPOIC ACID USING MICROEMULSIONS: INFLUENCE OF COMPOSITION AND CHARGE

PubMed Central

Cichewicz, Allie; Pacleb, Chelsea; Connors, Ashley; Hass, Martha A.; Lopes, Luciana B.

2013-01-01

Objectives To assess whether the composition and charge of microemulsions affect their ability to simultaneously deliver α-tocopherol and lipoic acid into viable skin layers. Methods α-tocopherol and lipoic acid were added (1.1 and 0.5% w/w, respectively) to decylglucoside-based microemulsions containing mono-dicaprylin. Microemulsions containing surfactant:oil:water (w/w/w) at 60:30:10 (ME-O) and 46:23:31 (ME-W), as well as a cationic form of ME-W containing 1% phytosphingosine (ME-Wphy) were characterized, and their ability to disrupt the skin barrier and deliver the antioxidants in vitro in the skin was evaluated. Antioxidant activity in ME-Wphy-treated skin was assessed using the thiobarbituric acid-reactive substances (TBARS) assay. Key findings internal phase diameters of microemulsions ranged between 47.0–53.2 nm; phytosphingosine addition and pH adjustment to 5.0 increased zeta potential from −4.3 to +29.1 mV. ME-O displayed w/o structure, whereas ME-W and ME-Wphy were consistent with o/w. Microemulsions affected skin electrical resistance and transepidermal water loss, but did not affect lipoic acid penetration. α-Tocopherol delivery increased following the order ME-O

Xingnaojing mPEG2000-PLA modified microemulsion for transnasal delivery: pharmacokinetic and brain-targeting evaluation.

PubMed

Wen, Ran; Zhang, Qing; Xu, Pan; Bai, Jie; Li, Pengyue; Du, Shouying; Lu, Yang

2016-01-01

Xingnaojing microemulsion (XNJ-M) administered intranasally is used for stroke treatment. In order to decrease the XNJ-M-induced mucosal irritation, XNJ-M modified by mPEG2000-PLA (XNJ-MM) were prepared in a previous work. The present work aimed to assess the impact of mPEG2000-PLA on pharmacokinetic features and brain-targeting ability of XNJ-M. The bioavailability and brain-target effects of borneol and geniposide in XNJ-M and XNJ-MM were compared in mice after intravenous (i.v.) and intranasal (i.n.) administrations. Gas chromatography, high-performance liquid chromatography, and ultra-performance liquid chromatography/tandem mass spectrometry methods were developed for the quantification of borneol and geniposide. Blood and brain samples were collected from mice at different time points after i.v. and i.n. treatments with borneol at 8.0 mg/kg, geniposide at 4.12 mg/kg. In addition, near-infrared fluorescence dye, 1,1'-dioctadecyl-3,3,3',3'-tetramethyl indotricarbocyanine iodide was loaded into microemulsions to evaluate the brain-targeting ability of XNJ-M and XNJ-MM by near-infrared fluorescence imaging in vivo and ex vivo. For XNJ-M and XNJ-MM, the relative brain targeted coefficients (Re) were 134.59% and 198.09% (borneol), 89.70% and 188.33% (geniposide), respectively. Besides, significant near-infrared fluorescent signal was detected in the brain after i.n. administration of microemulsions, compared with that of groups for i.v. administration. These findings indicated that mPEG2000-PLA modified microemulsion improved drug entry into blood and brain compared with normal microemulsion: the introduction of mPEG2000-PLA in microemulsion resulted in brain-targeting enhancement of both fat-soluble and water-soluble drugs. These findings provide a basis for the significance of mPEG2000-PLA addition in microemulsion, defining its effects on the drugs in microemulsion.

A theoretical approach for estimation of ultimate size of bimetallic nanocomposites synthesized in microemulsion systems

NASA Astrophysics Data System (ADS)

Salabat, Alireza; Saydi, Hassan

2012-12-01

In this research a new idea for prediction of ultimate sizes of bimetallic nanocomposites synthesized in water-in-oil microemulsion system is proposed. In this method, by modifying Tabor Winterton approximation equation, an effective Hamaker constant was introduced. This effective Hamaker constant was applied in the van der Waals attractive interaction energy. The obtained effective van der Waals interaction energy was used as attractive contribution in the total interaction energy. The modified interaction energy was applied successfully to predict some bimetallic nanoparticles, at different mass fraction, synthesized in microemulsion system of dioctyl sodium sulfosuccinate (AOT)/isooctane.

Study on nanomagnets supported TiO2 photocatalysts prepared by a sol-gel process in reverse microemulsion combining with solvent-thermal technique.

PubMed

Li, Hansheng; Zhang, Yaping; Wang, Shiying; Wu, Qin; Liu, Changhao

2009-09-30

A sol-gel process in reverse microemulsion combined with solvent-thermal technique was developed for synthesizing a series of nanomagnets supported TiO(2) (TiO(2)/NMs) photocatalysts in this study. The structure of TiO(2)/NMs photocatalysts was characterized by Fourier transform infrared (FTIR), TG-DSC, X-ray diffraction (XRD), Raman spectrometry, TEM, BET, and VSM. The influence of CoFe(2)O(4) dosage on the photocatalytic activity and magnetism of TiO(2)/NMs photocatalysts was investigated. The results showed that nanosized anatase TiO(2) were uniformly coated on spinel CoFe(2)O(4) in the prepared TiO(2)/NMs photocatalysts. They possessed typical ferromagnetic hysteresis and performed better photocatalytic activity in degradation of methylene blue than TiO(2) prepared by the same method. The existence of CoFe(2)O(4) nanomagnets played an important role on the crystalline grain size of TiO(2) and the specific surface area of the prepared TiO(2)/NMs photocatalysts, thus had an important influence on its photocatalytic performance and magnetism. The photocatalytic performance of TiO(2)/NMs photocatalysts is related to their specific surface area, crystalline grain sizes of TiO(2) and particle size, as well as the doping effect of Fe(3+). The highest photocatalytic activity in degradation of methylene blue for TiO(2)/NMs photocatalysts at the CoFe(2)O(4) content of 20wt.% was achieved, with k(p) 28.32% higher than that of pure TiO(2) photocatalyst. Moreover, the experiments on recycled use of TiO(2)/NMs photocatalyst demonstrated a good repeatability of the photocatalytic activity.

Oil-in-water nanocontainers as low environmental impact cleaning tools for works of art: two case studies.

PubMed

Carretti, Emiliano; Giorgi, Rodorico; Berti, Debora; Baglioni, Piero

2007-05-22

A novel class of p-xylene-in-water microemulsions mainly based on nonionic surfactants and their application as low impact cleaning tool in cultural heritage conservation is presented. Alkyl polyglycosides (APG) and Triton X-100 surfactants allow obtaining very effective low impact oil-in-water (o/w) microemulsions as alternatives to pure organic solvents for the removal of polymers (particularly Paraloid B72 and Primal AC33) applied during previous conservation treatments. The ternary APG/p-xylene/water microemulsions have been characterized by quasi elastic light scattering to obtain the hydrodynamic radius and the polydispersity of the microemulsion droplets. Laplace inversion of the correlation function CONTIN analysis provided evidence of acrylic copolymers solubilization into the oil nanodroplets. Contact angle, Fourier transform infrared (FTIR), and scanning electron microscopy/energy-dispersive spectroscopy (SEM/EDS) data confirmed that microemulsions were effective in removing polymer coatings. The phase diagram of APG microemulsions showed that a reduction >90% (compared to the conventional cleaning methods) of the organic solvent can be achieved by using o/w microemulsions. The microemulsions were successfully tested in two real cases: (1) the APG based microemulsion was used in a Renaissance painting by Vecchietta in Santa Maria della Scala, Siena, Italy, degraded by the presence of a polyacrylate coating applied during a previous restoration and (2) a Triton X-100 oil-in-water microemulsion containing (NH4)2CO3 in the water continuous phase. The association of ammoniun carbonate to the microemusion led to the swelling of an organic deposit (mainly asphaltenes deposited on the fresco in the Oratorio di San Nicola al Ceppo in Florence, still contamined by the water of the Arno river during the 1966 flood) and a very efficient removal of highly insoluble inorganic deposits (mainly gypsum) strongly associated to asphaltenes. These innovative systems are very attractive for the low amount of organic solvent used to extract the polymers or highly insoluble substances as the asphaltene and the very efficient and mild impact of the cleaning procedure on the fragile painted surfaces.

Ultrasound-assisted Micro-emulsion Synthesis of a Highly Active Nano-particle Catalyst

DTIC Science & Technology

2010-03-01

saturated calomel electrode [SCE]). 15. SUBJECT TERMS Microemulsion synthesis, Nano particles, Catalysts, Ultrasound, Oxygen reduction, Rotating disk...30 40 50 60 ω1/2 (rpm 1/2) i ( m A .c m -2 ) Ultrasound Assisted Microemulsion Microemulsion non- Microemulsion O2 4e Redc by Diff. Figure 17. Levich...2.0 2.4 0 0.02 0.04 0.06 0.08 0.1 0.12 ω-1/2(rpm-1/2) i-1 (m A -1 cm 2 ) non- Microemulsion Microemulsion Ultrasound Assisted Microemulsion O2 4-e Redc

Dielectric analysis of the APG/n-butanol/cyclohexane/water nonionic microemulsions.

PubMed

He, K J; Zhao, K S; Chai, J L; Li, G Z

2007-09-15

The nonionic APG/n-butanol/cyclohexane/water microemulsions with different microstructure, which is induced by the variation of water contents, are investigated by the dielectric spectroscopy. An appropriate dielectric theory, Hanai theory and the corresponding analytical method are applied to obtain the internal properties of the constituent phases of microemulsions, such as the relative permittivity and conductivity of continuous and dispersed phases and the volume fraction of dispersed phase. Using these parameters, the distribution of n-butanol in constituent phases, which is of important in the study field of the microstructure of microemulsion, is obtained quantitatively. It is found that the n-butanol molecules not only distribute in the interfacial APG layer but also in the continuous and dispersed phases. In addition, the percolation threshold is interpreted by using the dynamic percolation model. The structural and dynamic information are obtained, for instance, the critical volume fraction of water when percolation occurs and the characteristic time for the rearrangement of clusters. These parameters are intimately related to the properties of microemulsions, especially the characteristics of the interfacial layer.

Preparation of starch nanoparticles in water in oil microemulsion system and their drug delivery properties.

PubMed

Wang, Xinge; Chen, Haiming; Luo, Zhigang; Fu, Xiong

2016-03-15

In this research, 1-hexadecyl-3-methylimidazolium bromide C16mimBr/butan-1-ol/cyclohexane/water ionic liquid microemulsion was prepared. The effects of n-alkyl alcohols, alkanes, water content and temperature on the properties of microemulsion were studied by dilution experiment. The microregion of microemulsion was identified by pseudo-ternary phase diagram and conductivity measurement. Then starch nanoparticles were prepared by water in oil (W/O) microemulsion-cross-linking methods with C16mimBr as surfactant. Starch nanoparticles with a mean diameter of 94.3nm and narrow size distribution (SD=3.3) were confirmed by dynamic light scattering (DLS). Scanning electron microscope (SEM) data revealed that starch nanoparticles were spherical granules with the size about 60nm. Moreover the results of Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) demonstrated the formation of cross-linking bonds in starch molecules. Finally, the drug loading and releasing properties of starch nanoparticles were investigated with methylene blue (MB) as drug model. This work may provide an efficient pathway to synthesis starch nanoparticles. Copyright © 2015 Elsevier Ltd. All rights reserved.

Synthesis of MSnO{sub 3} (M = Ba, Sr) nanoparticles by reverse micelle method and particle size distribution analysis by whole powder pattern modeling

DOE Office of Scientific and Technical Information (OSTI.GOV)

Ahmed, Jahangeer; Blakely, Colin K.; Bruno, Shaun R.

2012-09-15

Highlights: ► BaSnO{sub 3} and SrSnO{sub 3} nanoparticles synthesized using the reverse micelle method. ► Particle size and size distribution studied by whole powder pattern modeling. ► Nanoparticles are of optimal size for investigation in dye-sensitized solar cells. -- Abstract: Light-to-electricity conversion efficiency in dye-sensitized solar cells critically depends not only on the dye molecule, semiconducting material and redox shuttle selection but also on the particle size and particle size distribution of the semiconducting photoanode. In this study, nanocrystalline BaSnO{sub 3} and SrSnO{sub 3} particles have been synthesized using the microemulsion method. Particle size distribution was studied by whole powdermore » pattern modeling which confirmed narrow particle size distribution with an average size of 18.4 ± 8.3 nm for SrSnO{sub 3} and 15.8 ± 4.2 nm for BaSnO{sub 3}. These values are in close agreement with results of transmission electron microscopy. The prepared materials have optimal microstructure for successive investigation in dye-sensitized solar cells.« less

Effect of water content on partial ternary phase diagram water-in-diesel microemulsion fuel

NASA Astrophysics Data System (ADS)

Mukayat, Hastinatun; Badri, Khairiah Haji; Raman, Ismail Ab.; Ramli, Suria

2014-09-01

Introduction of water in the fuel gave a significant effect to the reduction of pollutant such as NOx emission. In this work, water/diesel microemulsion fuels were prepared using compositional method by mixing water and diesel in the presence of non-ionic surfactant and co-surfactant. The effects of water composition on the partial ternary phase diagram were studied at 5%, 10%, 15% and 20% (w/w). The physical stability of the microemulsion was investigated at 45°C over a period of one month. The optimum formulae obtained were diesel/T80/1-penthanol/water 60:20:15:5 wt% (System 1), 55:20:15:10 wt% (System 2), 50:20:15:15 wt% (System 3) and 45:20:15:20 wt% (System 4). Physicochemical characterizations of optimum formulae were studied. The results showed that water content has a significant effect to the formation of microemulsion, its stability, droplet size and viscosity.

Effect of hexadecyltrimethylammonium bromide-based microemulsions on the rate of decomposition of the beta-lactam antibiotic cephaclor.

PubMed

De Oliveira, A G; Scarpa, M V; Chaimovich, H

1997-05-01

Microemulsions of hexadecyltrimethylammonium bromide (HTAB)/n-butanol/hexadecane/water catalyze the intramolecular degradation of cephaclor. The rate increase is a sensitive function of the microemulsion volume fraction and salt concentration. The effects of microemulsions, analyzed quantitatively using a pseudophase ion-exchange model, assumed that the extent of ion dissociation from the microemulsions varies with volume fraction. Comparison of micellar and microemulsion effects on the same reaction shows that microemulsions are less effective catalysts. Acceleration decreased significantly by increasing the relative proportion of n-butanol ratio in microemulsions and by addition of n-butanol in HTAB micelles. Comparison of the activation parameters of the reaction in aqueous solution, microemulsions, and micelles suggests that catalysis by both aggregates is driven mainly by entropic contributions.

New method to access hyperbranched polymers with uniform structure via one-pot polymerization of inimer in microemulsion.

PubMed

Min, Ke; Gao, Haifeng

2012-09-26

A facile approach is presented for successful synthesis of hyperbranched polymers with high molecular weight and uniform structure by a one-pot polymerization of an inimer in a microemulsion. The segregated space in the microemulsion confined the inimer polymerization and particularly the polymer-polymer reaction within discrete nanoparticles. At the end of polymerization, each nanoparticle contained one hyperbranched polymer that had thousands of inimer units and low polydispersity. The hyperbranched polymers were used as multifunctional macroinitiators for synthesis of "hyper-star" polymers. When a degradable inimer was applied, the hyper-stars showed fast degradation into linear polymer chains with low molecular weight.

Predicting solubilisation features of ternary phase diagrams of fully dilutable lecithin linker microemulsions.

PubMed

Nouraei, Mehdi; Acosta, Edgar J

2017-06-01

Fully dilutable microemulsions (μEs), used to design self-microemulsifying delivery system (SMEDS), are formulated as concentrate solutions containing oil and surfactants, without water. As water is added to dilute these systems, various μEs are produced (water-swollen reverse micelles, bicontinuous systems, and oil-swollen micelles), without the onset of phase separation. Currently, the formulation dilutable μEs follows a trial and error approach that has had a limited success. The objective of this work is to introduce the use of the hydrophilic-lipophilic-difference (HLD) and net-average-curvature (NAC) frameworks to predict the solubilisation features of ternary phase diagrams of lecithin-linker μEs and the use of these predictions to guide the formulation of dilutable μEs. To this end, the characteristic curvatures (Cc) of soybean lecithin (surfactant), glycerol monooleate (lipophilic linker) and polyglycerol caprylate (hydrophilic linker) and the equivalent alkane carbon number (EACN) of ethyl caprate (oil) were obtained via phase scans with reference surfactant-oil systems. These parameters were then used to calculate the HLD of lecithin-linkers-ethyl caprate microemulsions. The calculated HLDs were able to predict the phase transitions observed in the phase scans. The NAC was then used to fit and predict phase volumes obtained from salinity phase scans, and to predict the solubilisation features of ternary phase diagrams of the lecithin-linker formulations. The HLD-NAC predictions were reasonably accurate, and indicated that the largest region for dilutable μEs was obtained with slightly negative HLD values. The NAC framework also predicted, and explained, the changes in microemulsion properties along dilution lines. Copyright © 2017 Elsevier Inc. All rights reserved.

Formulation and evaluation of microemulsion-based hydrogel for topical delivery.

PubMed

Sabale, Vidya; Vora, Sejal

2012-07-01

The purpose of this study was to develop microemulsion-based hydrogel formulation for topical delivery of bifonazole with an objective to increase the solubility and skin permeability of the drug. Oleic acid was screened as the oil phase of microemulsions, due to a good solubilizing capacity of the microemulison systems. The pseudo-ternary phase diagrams for microemulsion regions were constructed using oleic acid as the oil, Tween 80 as the surfactant and isopropyl alcohol (IPA) as the cosurfactant. Various microemulsion formulations were prepared and optimized by 3(2) factorial design on the basis of percentage (%) transmittance, globule size, zeta potential, drug release, and skin permeability. The abilities of various microemulsions to deliver bifonazole through the skin were evaluated ex vivo using Franz diffusion cells fitted with rat skins. The Hydroxy Propyl Methyl Cellulose (HPMC) K100 M as a gel matrix was used to construct the microemulsion-based hydrogel for improving the viscosity of microemulsion for topical administration. The optimized microemulsion-based hydrogel was evaluated for viscosity, spreadability, skin irritancy, skin permeability, stability, and antifungal activity by comparing it with marketed bifonazole cream. The mechanism of drug release from microemulsion-based hydrogel was observed to follow zero order kinetics. The studied optimized microemulsion-based hydrogel showed a good stability over the period of 3 months. Average globule size of optimized microemulsion (F5) was found to be 18.98 nm, zeta potential was found to be -5.56 mv, and permeability of drug from microemulsion within 8 h was observed 84%. The antifungal activity of microemulsion-based hydrogel was found to be comparable with marketed cream. The results indicate that the studied microemulsion-based hydrogel (F5) has a potential for sustained action of drug release and it may act as promising vehicle for topical delivery of ibuprofen.

Characterization of potent anticholinesterase plant oil based microemulsion.

PubMed

Chaiyana, Wantida; Saeio, Kiattisak; Hennink, Wim E; Okonogi, Siriporn

2010-11-30

In the present study, essential oils of three edible Thai plants, Cymbopogon citratus (Gramineae), Citrus hystrix (Rutaceae) and Zingiber cassumunar (Zingiberaceae) were comparatively tested for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities using Ellman's colorimetric method. C. citratus oil exhibited the highest activity with IC(50) values of 0.34±0.07μl/ml and 2.14±0.18μl/ml against BChE and AChE activity, respectively. It was further investigated whether microemulsions of this oil could be obtained. The effects of type of surfactant and co-surfactant as well as pH and ionic strength on the phase behavior of the oil/water system were investigated. Brij 97, Triton X-114, Tween 20 and Tween 85 were employed as surfactant whereas ethanol and hexanol were used as cosurfactants. The size analysis, electrical conductivity measurements and cholinesterase inhibition assays were done in selected microemulsion. The results revealed that the type and concentration of surfactant and co-surfactant exhibited a distinct influence on the C. citratus oil microemulsions. Moreover, the inhibitory activities of the microemulsion formulation were remarkable. Copyright © 2010 Elsevier B.V. All rights reserved.

Formulation and characterization of lipid-based drug delivery system of raloxifene-microemulsion and self-microemulsifying drug delivery system

PubMed Central

Thakkar, Hetal; Nangesh, Jitesh; Parmar, Mayur; Patel, Divyakant

2011-01-01

Background: Raloxifene, a second-generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women is administered orally in the form of a tablet. The absolute bioavailability of the drug is only 2% because of extensive hepatic first-pass metabolism. Lipid-based formulations are reported to reduce the first-pass metabolism by promoting its lymphatic uptake. Materials and Methods: In the present investigation, microemulsion and Self-Microemulsifying Drug Delivery System (SMEDDS) formulations of Raloxifene were prepared. The prepared formulations were characterized for drug loading, size, transparency, zeta potential, Transmission Electron Microscopy (TEM) and in vitro intestinal permeability. Results: The results indicated that high drug loading, optimum size and desired zeta potential and transparency could be achieved with both SMEDDS and microemulsion. The TEM studies indicated the absence of aggregation with both the systems. The in vitro intestinal permeability results showed that the permeation of the drug from the microemulsion and SMEDDs was significantly higher than that obtained from the drug dispersion and marketed formulation. Conclusion: Lipid based formulations such as microemulsion and Self Microemulsifying drug delivery systems are expected to increase the oral bioavailability as evidenced by the increased intestinal permeation. PMID:21966167

Use of micro-emulsion technology for the directed evolution of antibodies.

PubMed

Buhr, Diane L; Acca, Felicity E; Holland, Erika G; Johnson, Katie; Maksymiuk, Gail M; Vaill, Ada; Kay, Brian K; Weitz, David A; Weiner, Michael P; Kiss, Margaret M

2012-09-01

Affinity reagents, such as antibodies, are needed to study protein expression patterns, sub-cellular localization, and post-translational modifications in complex mixtures and tissues. Phage Emulsion, Secretion, and Capture (ESCape) is a novel micro-emulsion technology that utilizes water-in-oil (W/O) emulsions for the identification and isolation of cells secreting phage particles that display desirable antibodies. Using this method, a large library of antibody-displaying phage will bind to beads in individual compartments. Rather than using biopanning on a large mixed population, phage micro-emulsion technology allows us to individually query clonal populations of amplified phage against the antigen. The use of emulsions to generate microdroplets has the promise of accelerating phage selection experiments by permitting fine discrimination of kinetic parameters for binding to targets. In this study, we demonstrate the ability of phage micro-emulsion technology to distinguish two scFvs with a 300-fold difference in binding affinities (100nM and 300pM, respectively). In addition, we describe the application of phage micro-emulsion technology for the selection of scFvs that are resistant to elevated temperatures. Copyright © 2012. Published by Elsevier Inc.

Structure and Solvent Properties of Microemulsions

ERIC Educational Resources Information Center

Katz, Civia A.; Calzola, Zachary J.; Mbindyo, Jeremiah K. N.

2008-01-01

A microscale laboratory experiment to investigate the formation and utility of microemulsions is described. Microemulsions are technologically important fluids that can reduce the use of toxic organic solvents. In the experiment, students prepare a microemulsion and compare the solubility of sudan III dye in the microemulsion and in dodecane. They…

Development of a novel microemulsion for oral absorption enhancement of all-trans retinoic acid

PubMed Central

Subongkot, Thirapit; Ngawhirunpat, Tanasait

2017-01-01

This study was aimed to develop a novel microemulsion that contained oleth-5 as a surfactant to enhance the oral absorption of all-trans retinoic acid (ATRA). The prepared microemulsion was evaluated for its particle size, shape, zeta potential, in vitro release, in vitro intestinal absorption, intestinal membrane cytotoxicity and stability. The obtained microemulsion was spherical in shape with a particle size of <200 nm and a negative surface charge. The in vitro release of the ATRA-loaded microemulsion was best fit with the zero-order model. This microemulsion significantly improved the intestinal absorption of ATRA. Confocal laser scanning microscopy analysis using a fluorescent dye-loaded microemulsion also confirmed the intestinal absorption result. The intestinal membrane cytotoxicity of the ATRA-loaded microemulsion did not differ from an edible oil (fish oil). Stability testing showed that the ATRA-loaded microemulsion was more stable at 25°C than 40°C. PMID:28831254

Development of a novel microemulsion for oral absorption enhancement of all-trans retinoic acid.

PubMed

Subongkot, Thirapit; Ngawhirunpat, Tanasait

2017-01-01

This study was aimed to develop a novel microemulsion that contained oleth-5 as a surfactant to enhance the oral absorption of all-trans retinoic acid (ATRA). The prepared microemulsion was evaluated for its particle size, shape, zeta potential, in vitro release, in vitro intestinal absorption, intestinal membrane cytotoxicity and stability. The obtained microemulsion was spherical in shape with a particle size of <200 nm and a negative surface charge. The in vitro release of the ATRA-loaded microemulsion was best fit with the zero-order model. This microemulsion significantly improved the intestinal absorption of ATRA. Confocal laser scanning microscopy analysis using a fluorescent dye-loaded microemulsion also confirmed the intestinal absorption result. The intestinal membrane cytotoxicity of the ATRA-loaded microemulsion did not differ from an edible oil (fish oil). Stability testing showed that the ATRA-loaded microemulsion was more stable at 25°C than 40°C.

Structure and dynamics of reverse micelles containing supercooled water investigated by neutron scattering

NASA Astrophysics Data System (ADS)

Spehr, Tinka; Frick, Bernhard; Grillo, Isabelle; Falus, Peter; Müller, Martin; Stühn, Bernd

2009-03-01

We present a detailed neutron scattering study of the structure, shape fluctuations, and translational diffusion of microemulsion droplets at low temperatures. We investigate the ternary microemulsion D2O , AOT [bis(2-ethyl-hexyl) sulfosuccinate], and toluene-d8 (or heptane-d16) which forms spherical water droplets surrounded by a monolayer of AOT dispersed in oil around room temperature. At T=290K , varying the molar ratio ω of water to AOT between 3 and 12, we find using small angle neutron scattering water core radii Rc between 7 and 18Å , respectively. We characterize the structure at low temperatures down to T=220K . Upon cooling the droplet structure is maintained and Rc stays roughly constant down to temperatures where the confined water is deeply supercooled. At an ω -dependent temperature Ts we observe for all compositions a shrinking of the droplets, which depends on the initial droplet size: the smaller the initial radii, the lower the Ts is. At the lowest investigated temperature T=220K we find an ω -independent remaining water core corresponding to a number of about 2 water molecules per AOT molecule. Neutron spin-echo spectroscopy is used to monitor shape fluctuations and translational diffusion for one microemulsion ( ω=8 , Rw=12Å ) from T=300K down to temperatures below the corresponding shrinking temperature Ts . Thereby we determine the bending elasticity to be κ=0.3kBT over the whole investigated temperature range where the droplets are stable. From these results we cannot establish a link between surfactant membrane elasticity and low temperature structural instability of the droplets. Moreover, our results show that reverse AOT micelles are an excellent tool for the study of soft confined water over a broad range of confining sizes and temperatures down to the supercooled state.

Microemulsions based transdermal drug delivery systems.

PubMed

Vadlamudi, Harini C; Narendran, Hyndavi; Nagaswaram, Tejeswari; Yaga, Gowri; Thanniru, Jyotsna; Yalavarthi, Prasanna R

2014-01-01

Since the discovery of microemulsions by Jack H Schulman, there has been huge progress made in applying microemulsion systems in plethora of research and industrial process. Microemulsions are optically isotropic systems consisting of water, oil and amphiphile. These systems are beneficial due to their thermodynamic stability, optical clarity, ease of preparation, higher diffusion and absorption rates. Moreover, it has been reported that the ingredients of microemulsion can effectively overcome the diffusion barrier and penetrate through the stratum corneum of the skin. Hence it becomes promising for both transdermal and dermal drug delivery. However, low viscosity of microemulsion restrains its applicability in pharmaceutical industry. To overcome the above drawback, the low viscous microemulsions were added to viscous gel bases to potentiate its applications as topical drug delivery systems so that various drug related toxic effects and erratic drug absorption can be avoided. The present review deals with the microemulsions, various techniques involved in the development of organic nanoparticles. The review emphasized on microemulsion based systems such as hydrogels and organogels. The physicochemical characteristics, mechanical properties, rheological and stability principles involved in microemulsion based viscous gels were also explored.

A propofol microemulsion with low free propofol in the aqueous phase: formulation, physicochemical characterization, stability and pharmacokinetics.

PubMed

Cai, WeiHui; Deng, WanDing; Yang, HuiHui; Chen, XiaoPing; Jin, Fang

2012-10-15

The purpose of this study was to develop a propofol microemulsion with a low concentration of free propofol in the aqueous phase. Propofol microemulsions were prepared based on single-factor experiments and orthogonal design. The optimal microemulsion was evaluated for pH, osmolarity, particle size, zeta potential, morphology, free propofol in the aqueous phase, stability, and pharmacokinetics in beagle dogs, and comparisons made with the commercial emulsion, Diprivan(®). The pH and osmolarity of the microemulsion were similar to those of Diprivan(®). The average particle size was 22.6±0.2 nm, and TEM imaging indicated that the microemulsion particles were spherical in appearance. The concentration of free propofol in the microemulsion was 21.3% lower than that of Diprivan(®). Storage stability tests suggested that the microemulsion was stable long-term under room temperature conditions. The pharmacokinetic profile for the microemulsion showed rapid distribution and elimination compared to Diprivan(®). We conclude that the prepared microemulsion may be clinically useful as a potential carrier for propofol delivery. Copyright © 2012 Elsevier B.V. All rights reserved.

Tc-99m Radiolabeled Alendronate Sodium Microemulsion: Characterization and Permeability Studies Across Caco-2 Cells.

PubMed

Elitez, Yetkin; Ekinci, Meliha; Ilem-Ozdemir, Derya; Gundogdu, Evren; Asikoglu, Makbule

2018-01-01

Alendronate sodium (ALD) is used orally but it is poorly absorbed from the gastrointestinal (GI) tract. For this reason, microemulsion system was chosen to evaluate ALD from the GI tract after oral delivery. This study was aimed to prepare water-in-oil (w/o) microemulsion formulation of ALD and evaluate the permeability of ALD microemulsion from Caco-2 cell lines with radioactive and nonradioactive studies. The ALD microemulsion was developed by using pseudo-ternary phase diagram and composed of Soybean oil, Colliphor EL, Tween 80, Transcutol and distilled water. The prepared ALD microemulsion was characterized by physical appearance, droplet size, viscosity, pH, electrical conductivity and refractive index. The stability of the formulation was investigated for 6 months at 25±2°C/60±5% of relative humidity (RH) as well as at 40±2°C/75±5% RH. After that 1 mg of ALD was radiolabeled with 99mTc and added to microemulsion. The permeability studies were performed with both 99mTc-ALD microemulsion and ALD microemulsion. The experimental results suggested that ALD microemulsion presented adequate stability with droplet size varying from 37.8±0.9 to 39.9±1.2 nm during incubation time. In addition, ALD microemulsion was radiolabeled with high labeling efficiency (>95%). In a non-radioactive study, ALD permeability was found to be 45 µg.mL-1 and microemulsion has high permeability percentage when compared to another study. The novel w/o microemulsion formulation has been developed for oral delivery of ALD. Based on the results, permeability of ALD could be significantly improved by the microemulsion formulation. In addition, 99mTc-ALD microemulsion in capsule can be used for bone disease treatment and diagnosis. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Lower irritation microemulsion-based rotigotine gel: formulation optimization and in vitro and in vivo studies.

PubMed

Wang, Zheng; Mu, Hong-Jie; Zhang, Xue-Mei; Ma, Peng-Kai; Lian, Sheng-Nan; Zhang, Feng-Pu; Chu, Sheng-Ying; Zhang, Wen-Wen; Wang, Ai-Ping; Wang, Wen-Yan; Sun, Kao-Xiang

2015-01-01

Rotigotine is a potent and selective D1, D2, and D3 dopaminergic receptor agonist. Due to an extensive first-pass effect, it has a very low oral bioavailability (approximately 0.5% in rats). The present investigation aimed to develop a microemulsion-based hydrogel for transdermal rotigotine delivery with lower application site reactions. Pseudoternary phase diagrams were constructed to determine the region of oil in water (o/w)-type microemulsion. Central composite design was used to support the pseudoternary phase diagrams and to select homogeneous and stable microemulsions with an optimal amount of rotigotine permeation within 24 hours. In vitro skin permeation experiments were performed, using Franz diffusion cells, to compare rotigotine-loaded microemulsions with rotigotine solutions in oil. The optimized formulation was used to prepare a microemulsion-based hydrogel, which was subjected to bioavailability and skin irritancy studies. The selected formulations of rotigotine-loaded microemulsions had enhanced flux and permeation coefficients compared with rotigotine in oil. The optimum microemulsion contained 68% water, 6.8% Labrafil(®), 13.44% Cremophor(®) RH40, 6.72% Labrasol(®), and 5.04% Transcutol(®) HP; the drug-loading rate was 2%. To form a microemulsion gel, 1% Carbomer 1342 was added to the microemulsion. The bioavailability of the rotigotine-loaded microemulsion gel was 105.76%±20.52% with respect to the marketed rotigotine patch (Neupro(®)). The microemulsion gel irritated the skin less than Neupro. A rotigotine microemulsion-based hydrogel was successfully developed, and an optimal formulation for drug delivery was identified. This product could improve patient compliance and have broad marketability.

Microemulsion based approach for nanospheres assembly into anisotropic nanostructures of NiMnO3 and their magnetic properties

NASA Astrophysics Data System (ADS)

Jha, Menaka; Kumar, Sandeep; Garg, Neha; Ramanujachary, Kandalam V.; Lofland, Samuel E.; Ganguli, Ashok K.

2018-02-01

The present study focuses on synthesis of anisotropic nanostructures of nickel manganese oxide (NiMnO3) obtained by thermal decomposition of nanocrystalline nickel manganese oxalate precursor, Ni0.5Mn0.5(C2O4)·2H2O which crystallized as nanorods. The synthesis of the oxalate precursor has been carried out via microemulsion-mediated process with cationic and non-ionic surfactants. The microemulsion led to reverse micelles, and the film flexibility of the micelle in presence of non-ionic surfactant (Tergitol) was reduced by increasing the chain length of the co-surfactant (1-butanol, 1-hexanol and 1-octanol) which led to the increase in reaction rate and hence increase in the aspect ratio of the nickel manganese oxalate by up to four times. However, in the presence of cationic surfactant, highly uniform nickel manganese oxalate nanorods were obtained. Further, the decomposition of the oxalate precursor was optimized to maintain the anisotropy of the rods of ternary metal oxide (NiMnO3). An electron microscopy study showed that the rods were made up of an assembly of ultrafine nanospheres. The NiMnO3 nanostructures were all ferrimagnetic with Curie temperature ranging between 437 and 467 K showing increasing saturation magnetization with increase in aspect ratio of the nanorods.

Mixture experiment methods in the development and optimization of microemulsion formulations

DOE Office of Scientific and Technical Information (OSTI.GOV)

Furlanetto, Sandra; Cirri, Marzia; Piepel, Gregory F.

2011-06-25

Microemulsion formulations represent an interesting delivery vehicle for lipophilic drugs, allowing for improving their solubility and dissolution properties. This work developed effective microemulsion formulations using glyburide (a very poorly-water-soluble hypoglycaemic agent) as a model drug. First, the area of stable microemulsion (ME) formations was identified using a new approach based on mixture experiment methods. A 13-run mixture design was carried out in an experimental region defined by constraints on three components: aqueous, oil, and surfactant/cosurfactant. The transmittance percentage (at 550 nm) of ME formulations (indicative of their transparency and thus of their stability) was chosen as the response variable. Themore » results obtained using the mixture experiment approach corresponded well with those obtained using the traditional approach based on pseudo-ternary phase diagrams. However, the mixture experiment approach required far less experimental effort than the traditional approach. A subsequent 13-run mixture experiment, in the region of stable MEs, was then performed to identify the optimal formulation (i.e., having the best glyburide dissolution properties). Percent drug dissolved and dissolution efficiency were selected as the responses to be maximized. The ME formulation optimized via the mixture experiment approach consisted of 78% surfactant/cosurfacant (a mixture of Tween 20 and Transcutol, 1:1 v/v), 5% oil (Labrafac Hydro) and 17% aqueous (water). The stable region of MEs was identified using mixture experiment methods for the first time.« less

A novel liquid template corrosion approach for layered silica with various morphologies and different nanolayer thicknesses

NASA Astrophysics Data System (ADS)

Yang, Wanliang; Li, Baoshan

2014-01-01

A novel liquid template corrosion (LTC) method has been developed for the synthesis of layered silica materials with a variety of morphologies, including hollow nanospheres, trilobite-like nanoparticles, spherical particles and a film resembling the van Gogh painting `Starry Night'. Lamellar micelles and microemulsion droplets are first formed in an oil-water (O/W) mixture of ethyl acetate (EA), cetyltrimethylammonium bromide (CTAB) and water. After adding aqueous ammonia the EA becomes hydrolyzed, which results in corrosion of microemulsion droplets. These droplets subsequently act as templates for the synthesis of silica formed by hydrolysis of tetraethyl orthosilicate. The morphological evolution of silica can be tuned by varying the concentration of aqueous ammonia which controls the degree of corrosion of the microemulsion droplet templates. A possible mechanism is proposed to explain why the LTC approach affords layered silica nanostructured materials with various morphologies and nanolayer thickness (2.6-4.5 nm), rather than the usual ordered mesostructures formed in the absence of EA. Our method provides a simple way to fabricate a variety of building blocks for assembling nanomaterials with novel structures and functionality, which are not available using conventional template methods.A novel liquid template corrosion (LTC) method has been developed for the synthesis of layered silica materials with a variety of morphologies, including hollow nanospheres, trilobite-like nanoparticles, spherical particles and a film resembling the van Gogh painting `Starry Night'. Lamellar micelles and microemulsion droplets are first formed in an oil-water (O/W) mixture of ethyl acetate (EA), cetyltrimethylammonium bromide (CTAB) and water. After adding aqueous ammonia the EA becomes hydrolyzed, which results in corrosion of microemulsion droplets. These droplets subsequently act as templates for the synthesis of silica formed by hydrolysis of tetraethyl orthosilicate. The morphological evolution of silica can be tuned by varying the concentration of aqueous ammonia which controls the degree of corrosion of the microemulsion droplet templates. A possible mechanism is proposed to explain why the LTC approach affords layered silica nanostructured materials with various morphologies and nanolayer thickness (2.6-4.5 nm), rather than the usual ordered mesostructures formed in the absence of EA. Our method provides a simple way to fabricate a variety of building blocks for assembling nanomaterials with novel structures and functionality, which are not available using conventional template methods. Electronic supplementary information (ESI) available. See DOI: 10.1039/c3nr04733d

[Preparation of Ganoderma lucidum polysaccharides and triterpenes microemulsion and its anticancer effect in mice with transplant Heps tumors].

PubMed

Chen, Yan; Lu, Hui; Song, Shihua; Jia, Xiaobin

2010-10-01

To research the microemulsion preparation of Ganoderma lucidum polysaccharides and triterpenes and investigate its properities. Evaluate the effects of polysaccharides and triterpenes microemulsions against transplant tumor growth. The microemulsion formula was optimized by constructing the pseudo-ternary phase diagrams of blank microemulsion. The polysaccharides and triterpenes microemulsions were prepared on the blank microemulsions. The appearance, particle distribution and Zeta potential were investigated by transmission electron microscope and grain size analyzer. The Heps mice were randomly administered with polysaccharides and triterpenes microemulsions (114.5, 57.25 mg x kg(-1) x d(-1)) for 7 days. The effectiveness was assessed based on tumor inhibitory ratio of mice with Heps tumors. The toxicity was evaluated by measurements of the mice weight, immune organ weight. The optimal microemulsion formula was composed of tween 20, dimethyl carbinol, water and 9-octadecenoic acid with the ratio of 14.3: 14.3: 33. 3:2. Polysaccharides and triterpenes microemulsions in transmission electron microscope were consisted of small spherical drop. The average particle size was 32.43 nm and the Zeta potential was -3.41 mV. The polysaccharides and triterpenes microemulsions showed an inhibition rate of 37.66% (57.25 mg x kg(-1) x d(-1)) and 52.34% (114.5 mg x kg(-1) x d(-1)) respectively against Heps tumor growth. The acquired microemulsion with small particle size is stable. It significantly inhibits the tumor growth in Heps mice.

Adapalene microemulsion for transfollicular drug delivery.

PubMed

Bhatia, Gaurav; Zhou, Yingcong; Banga, Ajay K

2013-08-01

The aim of this study was to develop a microemulsion formulation of adapalene for transfollicular delivery. A pseudoternary phase diagram was developed for microemulsion consisting of oleic acid as oil phase, tween 20 as surfactant, Transcutol® as cosurfactant, and deionized water. Differential tape stripping and confocal laser scanning microscopy were performed to determine the penetration of microemulsion through hair follicles. Transmission electron microscopy, dynamic light scattering, polarizing light microscopy, and differential scanning calorimetry were performed to characterize the microstructures of microemulsion. The pH and viscosity of the microemulsions were also determined. Permeation studies were carried out in vitro on porcine ear skin over a period of 24 h using Franz diffusion cells. The drug penetration in the hair follicles increased from 0.109 ± 0.03 to 0.292 ± 0.094 μg, as the microstructure of microemulsion shifted from oil-in-water to bi-continuous, with increase in water content of microemulsion. Confocal laser scanning microscopy images suggested that hair follicles provided the path for transfollicular permeation of adapalene microemulsion. These results suggest that microemulsion penetrated through hair follicles and are promising for transfollicular drug delivery. Copyright © 2013 Wiley Periodicals, Inc.

Development of cyclosporine A microemulsion for parenteral delivery.

PubMed

Yuan, Yue; Che, Xin; Zhao, Mingyi; Wang, Yan; Liu, Yajun; Schwendeman, Anna; Li, Sanming

2015-01-01

The goal of this study was to develop a parenteral microemulsion formulation of cyclosporine A (CyA). The CyA solubility in caprylic capric triglyceride (GTCC), ethyl oleate and soybean oil were determined. The pseudo-ternary diagrams of oil (GTCC), surfactant (Solutol® HS-15), cosurfactants (ethanol/polyethylene glycol 400 [PEG 400] mixture) and water were constructed to identify boundaries for microemulsion existence. The CyA was added at 3, 6 and 9% w/w to the optimal microemulsion composition. Microemulsion particle size, solution viscosity and conductivity were examined. The microemulsion stability and haemolytic potential were examined after dilution in 5% dextrose solution for injection to 1 mg/mL CyA. Microemulsion stability was examined after a three-month storage at 4 and 25 °C. The GTCC was selected as an oil phase for CyA microemulsion based on solubility results. The optimum CyA microemulsion formulation consisted of 2.5% CyA, 9% GTCC, 24% Solutol® HS 15, 8% PEG 400, 4% ethanol and 52.5% water based on weight percent. The average particle sizes of the optimized blank and drug-loaded microemulsions were 68.7 nm and 71.6 nm, respectively and remained unchanged upon 25-fold dextrose dilution. The results of microemulsion physical and CyA chemical were confirmed by a three-month stability study at 4 and 25 °C. In vitro haemolysis studies indicated that CyA microemulsions were well tolerated by erythrocytes. The novel microemulsion formulation of CyA was developed that is suitable for parenteral administration. This new formulation could potentially have less vehicle-associated side effects that current commercial formulation of CyA based on Cremophor® EL and ethanol solution.

Optimized mixed oils remarkably reduce the amount of surfactants in microemulsions without affecting oral bioavailability of ibuprofen by simultaneously enlarging microemulsion areas and enhancing drug solubility.

PubMed

Chen, Yizhen; Tuo, Jue; Huang, Huizhi; Liu, Dan; You, Xiuhua; Mai, Jialuo; Song, Jiaqi; Xie, Yanqi; Wu, Chuanbin; Hu, Haiyan

2015-06-20

The toxicity and irritation associated with high amounts of surfactants restrict the extensive utilization of microemulsions. To address these shortcomings, employing mixed oils to enlarge microemulsion areas therefore reducing surfactant contents is a promising strategy. However, what kinds of mixed oils are more efficient in enlarging microemulsion areas still remains unclear. In this research, we found that the chain length and degree of unsaturation of oils play a key role in enlarging microemulsion areas. The combination of moderate chain saturated oil caprylic/capric triglyceride (GTCC) with long chain unsaturated oil glycerol trioleate significantly increased the microemulsion areas. Solubility of ibuprofen in the mixed oils was unexpectedly and remarkably increased (almost 300mg/mL) compared with that (around 100mg/mL) of the single oil (GTCC), which also resulted in greatly increased solubility of ibuprofen in mixed oils-containing microemulsions. By optimizing the mixed oil formulation, the absolute amount of surfactant in drug-loaded microemulsions was reduced but increased drug oral bioavailability in rats was maintained. It could be concluded that the combined use of moderate chain oils and long chain unsaturated oils could not only acquire enlarged microemulsion areas but also enhanced drug solubility, therefore doubly reducing surfactant amount, which is extremely beneficial for developing safe microemulsions. Copyright © 2015. Published by Elsevier B.V.

Unusually large acrylamide induced effect on the droplet size in AOT/Brij30 water-in-oil microemulsions.

PubMed

Poulsen, Allan K; Arleth, Lise; Almdal, Kristoffer; Scharff-Poulsen, Anne Marie

2007-02-01

Droplet microemulsions are widely used as templates for controlled synthesis of nanometer sized polymer gel beads for use as, e.g., nanobiosensors. Here we examine water-in-oil microemulsions typically used for preparation of sensors. The cores of the microemulsion droplets are constituted by an aqueous component consisting of water, reagent monomer mixture, buffer salts, and the relevant dyes and/or enzymes. The cores are encapsulated by a mixture of the surfactants Brij30 and AOT and the resulting microemulsion droplets are suspended in a continuous hexane phase. The size of the final polymer particles may be of great importance for the applications of the sensors. Our initial working hypothesis was that the size of the droplet cores and therefore the size of the synthesized polymer gel beads could be controlled by the surfactant-to-water ratio of the template microemulsion. In the present work we have tested this hypothesis and investigated how the monomers and the ratio between the two surfactants affect the size of the microemulsion droplets and the microemulsion domain. We find that the monomers in water have a profound effect on the microemulsion domain as well as on the size of the microemulsion droplets. The relation between microemulsion composition and droplet size is in this case more complicated than assumed in standard descriptions of microemulsions [R. Strey, Colloid Polym. Sci. 272 (1994) 1005-1019; I. Danielsson, B. Lindman, Colloids Surf. 3 (1981) 391-392; Y. Chevalier, T. Zemb, Rep. Progr. Phys. 53 (1990) 279-371].

Microemulsion formulation of clonixic acid: solubility enhancement and pain reduction.

PubMed

Lee, Jung-Mi; Park, Kyung-Mi; Lim, Soo-Jeong; Lee, Mi-Kyung; Kim, Chong-Kook

2002-01-01

Clonixic acid is currently marketed as a salt form because of its poor water-solubility. However, the commercial dosage form causes severe pain after intramuscular or intravenous injection. To improve the solubility of clonixic acid and to reduce pain on injection, clonixic acid was incorporated into oil-in-water microemulsions prepared from pre-microemulsion concentrate composed of varying ratios of oil and surfactant mixture. As an oil phase for drug incorporation, up to 14% castor oil could be included in the pre-microemulsion concentrate without a significant increase in droplet size. Both drug contents and droplet size increased as the weight ratio of Tween 20 to Tween 85 decreased. Taken together, when microemulsions were prepared from pre-microemulsion concentrate composed of 5:12:18 weight ratio of castor oil:Tween 20:Tween 85, clonixic acid could be incorporated at 3.2 mg mL(-1) in the microemulsion with a droplet size of less than 120 nm. The osmotic pressure of this microemulsion was remarkably lower than the commercial formulation, irrespective of the dilution ratios. The rat paw-lick test was used to compare pain responses among formulations. The microemulsion formulation significantly reduced the number of rats licking their paws as well as the total licking time, suggesting less pain induction by the microemulsion formulation. The pharmacokinetic parameters of clonixic acid after intravenous administration of the clonixic acid microemulsion to rats were not significantly different from those of the commercial formulation, lysine clonixinate. The present study suggests that microemulsion is an alternative formulation for clonixic acid with improved characteristics.

Determination of drug and fatty acid binding capacity to pluronic f127 in microemulsions.

PubMed

James-Smith, Monica A; Shekhawat, Dushyant; Moudgil, Brij M; Shah, Dinesh O

2007-02-13

We propose that one can deduce very insightful information regarding the drug and fatty acid binding capacity of microemulsions through simple turbidity experiments. Pluronic F127-based oil-in-water microemulsions of various compositions were synthesized and titrated to turbidity with concentrated amitriptyline, an antidepressant drug. We observed that, above certain Pluronic F127 concentrations, turbidity was never observed, irrespective of how much amitriptyline was added to the microemulsion. We also observed that whenever sodium caprylate fatty acid was not included in the microemulsion formulation, turbidity never occurred. On the basis of these findings, we were able to determine the point at which all sodium caprylate present in the microemulsion formulation was bound to the F127 in the microemulsion (i.e., no fatty acid was free in the bulk in monomer form). By the same logic we were also able to determine how much amitriptyline was binding to the microemulsions. We also measured the dynamic surface tension, foamability, and fabric wetting time of the microemulsion formulations to further prove the hypothesis that all fatty acid is bound to the F127 in the microemulsion above a critical Pluronic F127 concentration. On the basis of this research, we have concluded that there are approximately 11 molecules of sodium caprylate fatty acid bound per molecule of Pluronic F127 and approximately 12 molecules of amitriptyline bound per molecule of Pluronic F127 in the optimal microemulsion formulation. These findings give us valuable information about the charge density at the oil/water interface and about the mechanism of binding of the drug to the microemulsion.

AC electrokinetic manipulation of selenium nanoparticles for potential nanosensor applications

DOE Office of Scientific and Technical Information (OSTI.GOV)

Mahmoodi, Seyed Reza; Bayati, Marzieh, E-mail: m-bayati@tums.ac.ir; Hosseinirad, Somayeh

2013-03-15

Highlights: ► Se nanoparticles were synthesized using a reverse-microemulsion process. ► AC osmotic fluid flow repulses the particles from electrode edges. ► Dielectrophoretic force attracts the particles to electrode edges. ► Dielectrophoresis electrode showed non-ohmic behavior. ► The device can potentially be used as a nanosensor. - Abstract: We report the AC electrokinetic behavior of selenium (Se) nanoparticles for electrical characterization and possible application as micro/nano devices. selenium Se nanoparticles were successfully synthesized using a reverse-microemulsion process and investigated structurally using X-ray diffraction and transmission electron microscope. Interdigitated castellated ITO and non-castellated platinum electrodes were employed for manipulation of suspendedmore » materials in the fluid. Using ITO electrodes at low frequency limits resulted in deposition of Se particles on electrode surface. When Se particles exposed to platinum electrodes in the 10 Hz–1 kHz range and V {sub p−p}> 8, AC osmotic fluid flow repulses the particles from electrode edges. However, in 10 kHz–10 MHz range and V {sub p−p}> 5, dielectrophoretic force attracts the particles to electrode edges. As the Se particle concentration increased, the trapped Se particles were aligned along the electric field line and bridged the electrode gap. The device was characterized and can potentially be useful in making micro/nano electronic devices.« less

Novel Fluorescent Microemulsion: Probing Properties, Investigating Mechanism, and Unveiling Potential Application.

PubMed

Hou, Mengna; Dang, Leping; Liu, Tiankuo; Guo, Yun; Wang, Zhanzhong

2017-08-09

Nanoscale microemulsions have been utilized as delivery carriers for nutraceuticals and active biological drugs. Herein, we designed and synthesized a novel oil in water (O/W) fluorescent microemulsion based on isoamyl acetate, polyoxyethylene castor oil EL (CrEL), and water. The microemulsion emitted bright blue fluorescence, thus exhibiting its potential for active drug detection with label-free strategy. The microemulsion exhibited excitation-dependent emission and distinct red shift with longer excitation wavelengths. Lifetime and quantum yield of fluorescent microemulsion were 2.831 ns and 5.0%, respectively. An excellent fluorescent stability of the microemulsion was confirmed by altering pH, ionic strength, temperature, and time. Moreover, we proposed a probable mechanism of fluorochromic phenomenon, in connection with the aromatic ring structure of polyoxyethylene ether substituent in CrEL. Based on our findings, we concluded that this new fluorescent microemulsion is a promising drug carrier that can facilitate active drug detection with a label-free strategy. Although further research is required to understand the exact mechanism behind its fluorescence property, this work provided valuable guidance to develop new biosensors based on fluorescent microemulsion.

Preparation and evaluation of cilnidipine microemulsion

PubMed Central

Tandel, Hemal; Raval, Krunal; Nayani, Anil; Upadhay, Manish

2012-01-01

Cilnidipine, a calcium channel blocker having neuroprotective action and BCS Class II drug, hence formulating in Microemulsion will increase solubility, absorption and bioavailability. The formulation was prepared using titration method by tocotrienol, tween 20 and transcutol HP as oil, surfactant and co-surfactant and characterized for dilutability, dye solubility, assay (98.39±0.06), pH (6.6±1.5), Viscosity (98±1.0 cps) and Conductivity (0.2±0.09 μS/cm). The formulation was optimized on basis of percentage transmittance (99.269±0.23 at 700 nm), Globule size (13.31±4.3 nm) and zeta potential (–11.4±2.3 mV). Cilnidipine microemulsion was found to be stable for 3 months. PMID:23066184

Investigation of microemulsion system for transdermal delivery of itraconazole

PubMed Central

Chudasama, Arpan; Patel, Vineetkumar; Nivsarkar, Manish; Vasu, Kamala; Shishoo, Chamanlal

2011-01-01

A new oil-in-water microemulsion-based (ME) gel containing 1% itraconazole (ITZ) was developed for topical delivery. The solubility of ITZ in oils and surfactants was evaluated to identify potential excipients. The microemulsion existence ranges were defined through the construction of the pseudoternary phase diagrams. The optimized microemulsion was characterized for its morphology and particle size distribution. The optimized microemulsion was incorporated into polymeric gels of Lutrol F127, Xanthan gum, and Carbopol 934 for convenient application and evaluated for pH, drug content, viscosity, and spreadability. In vitro drug permeation of ME gels was determined across excised rat skins. Furthermore, in vitro antimycotic inhibitory activity of the gels was conducted using agar-cup method and Candida albicans as a test organism. The droplet size of the optimized microemulsion was found to be <100 nm. The optimized Lutrol F 127 ME gel showed pH in the range of 5.68±0.02 and spreadability of 5.75±1.396 gcm/s. The viscosity of ME gel was found to be 1805.535±542.4 mPa s. The permeation rate (flux) of ITZ from prepared ME gel was found to be 4.234 μg/cm/h. The release profile exhibited diffusion controlled mechanism of drug release from ME ITZ gel. The developed ME gels were nonirritant and there was no erythema or edema. The antifungal activity of ITZ showed the widest zone of inhibition with Lutrol F127 ME gel. These results indicate that the studied ME gel may be a promising vehicle for topical delivery of ITZ. PMID:22171289

Tacrolimus loaded biocompatible lecithin-based microemulsions with improved skin penetration: Structure characterization and in vitro/in vivo performances.

PubMed

Savić, Vedrana; Todosijević, Marija; Ilić, Tanja; Lukić, Milica; Mitsou, Evgenia; Papadimitriou, Vassiliki; Avramiotis, Spyridon; Marković, Bojan; Cekić, Nebojša; Savić, Snežana

2017-08-30

In order to improve skin penetration of tacrolimus we aimed to develop potentially non-irritant, lecithin-based microemulsions containing ethanol, isopropanol and/or propylene glycol as cosurfactants, varying caprylic/capric triglycerides and propylene glycol monocaprylate as oil phase. The influence of excipients on the size of microemulsion region in pseudo-ternary phase diagrams and their ability to form different types of microemulsions was evaluated. The comprehensive physicochemical characterization of microemulsions and the evaluation of their structure was performed, while the localization of tacrolimus in microemulsions was further investigated using electron paramagnetic resonance spectroscopy. Moreover, stability studies proved no change in tacrolimus content during one year of storage at room temperature. In addition, in vivo skin performance indicated no skin irritation potential of blank microemulsions, whereas in vitro release testing using Franz diffusion cells showed superior release rate of tacrolimus from microemulsions (0.98±0.10 and 0.92±0.11μg/cm 2 /h for two bicontinuous and 1.00±0.24μg/cm 2 /h for oil-in-water microemulsion) compared to referent Protopic ointment (0.15±0.08μg/cm 2 /h). Furthermore, ex vivo penetration assessed through porcine ear skin using tape stripping, confirmed superiority of two microemulsions related to the reference, implying developed microemulsions as promising carriers for dermal delivery of tacrolimus. Copyright © 2017 Elsevier B.V. All rights reserved.

Preparation and evaluation of topical microemulsion system containing metronidazole for remission in rosacea.

PubMed

Tirnaksiz, Figen; Kayiş, Ayşegül; Çelebi, Nevin; Adişen, Esra; Erel, Arzu

2012-01-01

The aim of this study was to prepare a topical water-in-oil type microemulsion containing metronidazole and to compare its effectiveness with a commercial gel product in the treatment of rosacea. A pseudo-ternary phase diagram (K(m)=2:1) was constructed using lecithin/butanol/isopropyl myristate/water. The microemulsion was chosen from the microemulsion region in the phase diagram. The formulation was a water-in-oil type microemulsion (droplet size: 11.6 nm, viscosity: 457.3 mPa·s, conductivity: 1.5 µs/cm, turbidity: 6.89 NTU) and the addition of the metronidazole did not alter the properties of the system. The release experiment showed that the release rate of metronidazole from the commercial gel product was higher than that of the microemulsion. Stability experiments showed that the metronidazole microemulsion remained stable for at least 6 months; none of the characteristic properties of the microemulsion had changed, the system retained its clarity and there was no sign that crystallization of metronidazole has occurred. Microemulsion was compared to a gel product in a randomized, double-blind, baseline-controlled, split-face clinical trial for the treatment of patients. After the 6-week treatment period there was a statistically significant difference in reduction of the main symptoms of rosacea. Of the patients treated with the microemulsion, 17% experienced complete relief from inflammatory lesions, and 50% from erythema. The microemulsion resulted in complete relief in 38% of the patients with telangiectasia while the commercial product did not provide any relief of telangiectasia symptoms. In conclusion, the microemulsion containing metronidazole was found to be more effective in reducing the symptoms of rosacea compared to the commercial gel product.

Microemulsion-based oxyresveratrol for topical treatment of herpes simplex virus (HSV) infection: physicochemical properties and efficacy in cutaneous HSV-1 infection in mice.

PubMed

Sasivimolphan, Pattaraporn; Lipipun, Vimolmas; Ritthidej, Garnpimol; Chitphet, Khanidtha; Yoshida, Yoshihiro; Daikoku, Tohru; Sritularak, Boonchoo; Likhitwitayawuid, Kittisak; Pramyothin, Pornpen; Hattori, Masao; Shiraki, Kimiyasu

2012-12-01

The physicochemical properties of the optimized microemulsion and the permeating ability of oxyresveratrol in microemulsion were evaluated, and the efficacy of oxyresveratrol microemulsion in cutaneous herpes simplex virus type 1 (HSV-1) infection in mice was examined. The optimized microemulsion was composed of 10% w/w of isopropyl myristate, 35% w/w of Tween 80, 35% w/w of isopropyl alcohol, and 20% w/w of water. The mean particle diameter was 9.67 ± 0.58 nm, and the solubility of oxyresveratrol in the microemulsion was 196.34 ± 0.80 mg/ml. After accelerated and long-term stability testing, the microemulsion base and oxyresveratrol-loaded microemulsion were stable. The cumulative amount of oxyresveratrol permeating through shed snake skin from microemulsion at 6 h was 93.04 times compared to that of oxyresveratrol from Vaseline, determined at 20% w/w concentration. In cutaneous HSV-1 infection in mice, oxyresveratrol microemulsion at 20%, 25%, and 30% w/w, topically applied five times daily for 7 days after infection, was significantly effective in delaying the development of skin lesions and protecting from death (p < 0.05) compared with the untreated control. Oxyresveratrol microemulsion at 25% and 30% w/w was significantly more effective than that of 30% w/w of oxyresveratrol in Vaseline (p < 0.05) and was as effective as 5% w/w of acyclovir cream, topically applied five times daily (p > 0.05). These results demonstrated that topical oxyresveratrol microemulsion at 20-30% w/w was suitable for cutaneous HSV-1 mouse infection.

Mixture experiment methods in the development and optimization of microemulsion formulations.

PubMed

Furlanetto, S; Cirri, M; Piepel, G; Mennini, N; Mura, P

2011-06-25

Microemulsion formulations represent an interesting delivery vehicle for lipophilic drugs, allowing for improving their solubility and dissolution properties. This work developed effective microemulsion formulations using glyburide (a very poorly-water-soluble hypoglycaemic agent) as a model drug. First, the area of stable microemulsion (ME) formations was identified using a new approach based on mixture experiment methods. A 13-run mixture design was carried out in an experimental region defined by constraints on three components: aqueous, oil and surfactant/cosurfactant. The transmittance percentage (at 550 nm) of ME formulations (indicative of their transparency and thus of their stability) was chosen as the response variable. The results obtained using the mixture experiment approach corresponded well with those obtained using the traditional approach based on pseudo-ternary phase diagrams. However, the mixture experiment approach required far less experimental effort than the traditional approach. A subsequent 13-run mixture experiment, in the region of stable MEs, was then performed to identify the optimal formulation (i.e., having the best glyburide dissolution properties). Percent drug dissolved and dissolution efficiency were selected as the responses to be maximized. The ME formulation optimized via the mixture experiment approach consisted of 78% surfactant/cosurfacant (a mixture of Tween 20 and Transcutol, 1:1, v/v), 5% oil (Labrafac Hydro) and 17% aqueous phase (water). The stable region of MEs was identified using mixture experiment methods for the first time. Copyright © 2011 Elsevier B.V. All rights reserved.

PREPARATION AND PROPERTIES OF COMPOUND ARNEBIAE RADIX MICROEMULSION GEL.

PubMed

Chen, Jing; He, Yanping; Gao, Ting; Zhang, Licheng; Zhao, Yuna

2017-01-01

Compound Arnebiae radix oil has been clinically applied to treat burns and scalds for a long time. However, it is unstable and inconvenient to use. The aim of this study was to prepare a compound Arnebiae radix microemulsion gel for transdermal delivery system and evaluate its characteristics. Based on the solubility of Shikonin, the active component of Arnebiae radix and the results of phase studies, adequate ratio of each component in microemulsion was determined. The optimized microemulsion gel was prepared using Carbomer 940. The gels were characterized in terms of appearance, preliminary stability test and the content of Shikonin in the compound Arnebiae radix microemulsion gel with HPLC analysis. The optimized conditions for preparing microemulsion were Tween-80, glycerin, isopropyl myristate (IPM) with the ratio of 6:3:2. The optimal microemulsion gel was obtained with Carbomer 940 (1.0%). The prepared compound Arnebiae radix microemulsion gel showed good stability over time. It is more convenience in application than the previous used formulations.

In-site synthesis of monodisperse, oleylamine-capped Ag nanoparticles through microemulsion approach

NASA Astrophysics Data System (ADS)

Chen, Shun; Ju, Yanyun; Guo, Yi; Xiong, Chuanxi; Dong, Lijie

2017-03-01

Ag NPs were in-site synthesized through microemulsion method by reducing silver acetate with oleylamine-mediated at 70 °C with highly monodisperse and narrow size from 10 to 20 nm. The synthesis of Ag NPs was aided by oleylamine and the role of oleylamine was researched. This in-site synthesis approach to Ag NPs was reproducibility and high yield more than 80% with stable store about 6 months.

Formulation and evaluation of flurbiprofen microemulsion.

PubMed

Ambade, K W; Jadhav, S L; Gambhire, M N; Kurmi, S D; Kadam, V J; Jadhav, K R

2008-01-01

The purpose of the present study was to investigate the microemulsion formulations for topical delivery of Flurbiprofen (FP) in order to by pass its gastrointestinal adverse effects. The pseudoternary phase diagrams were developed and various microemulsion formulations were prepared using Isopropyl Myristate (IPM), Ethyl Oleate (EO) as oils, Aerosol OT as surfactant and Sorbitan Monooleate as cosurfactant. The transdermal permeability of flurbiprofen from microemulsions containing IPM and EO as two different oil phases was analyzed using Keshary-Chien diffusion cell through excised rat skin. Flurbiprofen showed higher in vitro permeation from IPM as compared to that of from EO microemulsion. Thus microemulsion containing IPM as oil phase were selected for optimization. The optimization was carried out using 2(3) factorial design. The optimized formula was then subjected to in vivo anti-inflammatory study and the performance of flurbiprofen from optimized formulation was compared with that of gel cream. Flurbiprofen from optimized microemulsion formulation was found to be more effective as compared to gel cream in inhibiting the carrageenan induced rat paw edema at all time intervals. Histopathological investigation of rat skin revealed the safety of microemulsion formulation for topical use. Thus the present study indicates that, microemulsion can be a promising vehicle for the topical delivery of flurbiprofen.

Evaluation of cinnamon essential oil microemulsion and its vapor phase for controlling postharvest gray mold of pears (Pyrus pyrifolia).

PubMed

Wang, Yifei; Zhao, Ruipeng; Yu, Ling; Zhang, Yunbin; He, Yan; Yao, Jie

2014-03-30

Essential oil of cinnamon (CM) is a potential alternative to chemical fungicides. Thus this work aimed to investigate the possible effects of CM microemulsions on decay developments and qualitative properties of pears. The decay incidence of samples treated with 500 µg L⁻¹ microemulsion was significantly reduced by 18.7% in comparison to that of 500 µg L⁻¹ non-microemulsion after 4 days' storage at 20 °C. In the vapor phase, the CM microemulsion with the lowest concentration had the best control for decay incidence and lesion diameter. The interval between inoculations also influenced decay development. Pears treated with Botrytis cinerea and immediately followed by CM microemulsion showed the lowest decay incidence. Moreover, in the natural decay experiment, the percentage of rotted pears was 3.8% in the CM microemulsion treatment and 5.8% in the control. CM microemulsion delayed the loss of ascorbic acid, yet it had no significant influence on pear qualities such as firmness and color. CM microemulsion may be an alternative way to control the gray mold of pears without a negative influence on its qualities. © 2013 Society of Chemical Industry.

Development and in vitro-in vivo evaluation of a water-in-oil microemulsion formulation for the oral delivery of troxerutin.

PubMed

Xu, Man; Yu, Qing; Zhao, Qianru; Chen, Wei; Lin, Yuanjie; Jin, Yong

2016-01-01

The main objective of this study was to develop and evaluate a W/O microemulsion formulation of troxerutin to improve its oral bioavailability. The W/O microemulsion was optimized using a pseudo-ternary phase diagram and evaluated for physical properties. In vitro MDCK cell permeability studies were carried out to evaluate the permeability enhancement effect of microemulsion, and in vivo absorption of troxerutin microemulsion in the intestine was compared with that of solution after single-dose administration (56.7 mg/kg) in male Wistar rats. The optimal formulation consisted of lecithin, ethanol, isopropyl myristate and water (23.30/11.67/52.45/12.59 w/w) was physicochemical stable and the mean droplet size was about 50.20 nm. In vitro study, the troxerutin-loaded microemulsion showed higher intestinal membrane permeability across MDCK monolayer when compared with the control solution. The W/O microemulsion can significantly promote the intestinal absorption of troxerutin in rats in vivo, and the relative bioavailability of the microemulsion was about 205.55% compared to control solution. These results suggest that novel W/O microemulsion could be used as an effective formulation for improving the oral bioavailability of troxerutin.

Influence of vitamin E acetate and other lipids on the phase behavior of mesophases based on unsaturated monoglycerides.

PubMed

Sagalowicz, L; Guillot, S; Acquistapace, S; Schmitt, B; Maurer, M; Yaghmur, A; de Campo, L; Rouvet, M; Leser, M; Glatter, O

2013-07-02

The phase behavior of the ternary unsaturated monoglycerides (UMG)-DL-α-tocopheryl acetate-water system has been studied. The effects of lipid composition in both bulk and dispersed lyotropic liquid crystalline phases and microemulsions were investigated. In excess water, progressive addition of DL-α-tocopheryl acetate to a binary UMG mixture results in the following phase sequence: reversed bicontinuous cubic phase, reversed hexagonal (H(II)) phase, and a reversed microemulsion. The action of DL-α-tocopheryl acetate is then compared to that of other lipids such as triolein, limonene, tetradecane, and DL-α-tocopherol. The impact of solubilizing these hydrophobic molecules on the UMG-water phase behavior shows some common features. However, the solubilization of certain molecules, like DL-α-tocopherol, leads to the presence of the reversed micellar cubic phase (space group number 227 and symmetry Fd3m) while the solubilization of others does not. These differences in phase behavior are discussed in terms of physical-chemical characteristics of the added lipid molecule and its interaction with UMG and water. From an applications point of view, phase behavior as a function of the solubilized content of guest molecules (lipid additive in our case) is crucial since macroscopic properties such as molecular release depend strongly on the phase present. The effect of two hydrophilic emulsifiers, used to stabilize the aqueous dispersions of UMG, was studied and compared. Those were Pluronic F127, which is the most commonly used stabilizer for these kinds of inverted type structures, and the partially hydrolyzed emulsifier lecithin (Emultop EP), which is a well accepted food-grade emulsifier. The phase behavior of particles stabilized by the partially hydrolyzed lecithin is similar to that of bulk sample at full hydration, but this emulsifier interacts significantly with the internal structure and affects it much more than F127.

Chemical and Photochemical Reactivity in Microemulsions and Waterless Microemulsions.

DTIC Science & Technology

1988-02-10

virtually the same as that found in the alcohol rich microemulsion A. This value is also close to that found in pure butanol (= 5.0 - table I). It would...formamide or alcohol rich). RESEARCH PATTERN -Supplementing the physical chemical study of the microemulsion medium involving ionic surfactants with density...SAMII (1/02/1988) Ii&N 3 Part II - OXYDATIONS BY HYDROPEROXIDES IN MICROEMULSIONS E. OLIVEROS and M.T. MAURETTE During the past six months, the financial

Microemulsion and Microemulsion-Based Gels for Topical Antifungal Therapy with Phytochemicals.

PubMed

Boonme, Prapaporn; Kaewbanjong, Jarika; Amnuaikit, Thanaporn; Andreani, Tatiana; Silva, Amélia M; Souto, Eliana B

2016-01-01

Skin fungal infections are regular injuries suffered by people living in tropical areas. Most common pathogens are Trichophyton, Microsporum and Epidermophyton which can cause skin lesions in many parts of body. Topical antifungal phytochemicals are commonly used to avoid systemic adverse events and are more convenient for patient application than those administered by other routes. However, the effectiveness of topical treatments in eradicating fungal infection is more limited since the stratum corneum acts as the skin barrier, resulting in long treatment duration and low patient's compliance. The goal of this work is to identify optimized drug delivery systems to improve topic clinical efficacy. Microemulsions i.e. liquid dispersions of oil and water stabilized with an interfacial film of surfactant are well known drug delivery systems. A thickening agent may be included to form microemulsion-based gels to increase skin adhesion. Microemulsions and microemulsion-based gels can be loaded with several hydrophilic and lipophilic drugs because they are composed of both water and oil phases. Microemulsions and microemulsion-based gels can also be used for the delivery of many drugs including antifungal drugs through stratum corneum due to their capacity to act as skin penetration enhancement. In addition to a comprehensive review of microemulsion and microemulsion-based gels as suitable carriers for skin delivery of various antifungal drugs, this review also aims to discuss the delivery of antifungal phytochemicals.

Microemulsions containing long-chain oil ethyl oleate improve the oral bioavailability of piroxicam by increasing drug solubility and lymphatic transportation simultaneously.

PubMed

Xing, Qiao; Song, Jia; You, Xiuhua; Xu, Dongling; Wang, Kexin; Song, Jiaqi; Guo, Qin; Li, Pengyu; Wu, Chuanbin; Hu, Haiyan

2016-09-25

Drug solubility and lymphatic transport enhancements are two main pathways to improve drug oral bioavailability for microemulsions. However, it is not easy to have both achieved simultaneously because excipients used for improving lymphatic transport were usually insufficient in forming microemulsions and solubilizing drugs. Our research is to explore whether ethyl oleate, an oil effective in developing microemulsions with desired solubilizing capability, could increase bioavailability to a higher extent by enhancing lymphatic transport. As a long-chain oil, ethyl oleate won larger microemulsion area than short-chain tributyrin and medium-chain GTCC. In contrast, long-chain soybean oil failed to prepare microemulsions. The solubility of piroxicam in ethyl oleate microemulsions (ME-C) increased by about 30 times than in water. ME-C also won significantly higher AUC0-t compared with tributyrin microemulsions (ME-A) and GTCC microemulsions (ME-B). Oral bioavailability in ME-C decreased by 38% after lymphatic transport was blocked by cycloheximide, severer than those in ME-A and ME-B (8% and 34%). These results suggest that improving lymphatic transport and solubility simultaneously might be a novel strategy to increase drug oral bioavailability to a higher extent than increasing solubility only. Ethyl oleate is a preferred oil candidate due to its integrated advantages of high solubilizing capability, large microemulsion area and effective lymphatic transport. Copyright © 2016 Elsevier B.V. All rights reserved.

Pluronic Microemulsions as Nanoreservoirs for Extraction of Bupivacaine from Normal Saline

PubMed Central

Varshney, Manoj; Morey, Timothy E.; Shah, Dinesh O.; Flint, Jason A.; Moudgil, Brij M.; Seubert, Christoph N.

2013-01-01

We hypothesized that custom-designed microemulsions would effectively scavenge compounds from bulk media. Pluronic-based oil-in-water microemulsions were synthesized that efficiently reduced the free concentration of the local anesthetic bupivacaine in 0.9% NaCl. Both the molecular nature and concentration of the constituents in the microemulsions significantly affected extraction efficiencies. Pluronic F127-based microemulsions extracted bupivacaine more efficiently than microemulsions synthesized using other Pluronic surfactants (L44, L62, L64, F77, F87, F88, P104). Extraction was markedly increased by addition of fatty acid sodium salts due to greater oil/water interface area, increased columbic interaction between bupivacaine and fatty acids sodium salt, and greater surface activity. These data suggest that oil-in-water microemulsions may be an effective agent to treat cardiotoxicity caused by bupivacaine or other lipophilic drugs. PMID:15099093

Improvement of effect of water-in-oil microemulsion as an oral delivery system for fexofenadine: in vitro and in vivo studies

PubMed Central

Gundogdu, E; Alvarez, I Gonzalez; Karasulu, E

2011-01-01

Fexofenadine (FEX) has high solubility and low permeability (BCS, Class III). In this work, novel FEX loaded water in oil microemulsion (w/o) was designed to improve bioavailability and compared with Fexofen® syrup in in vitro and in vivo studies. In addition, pharmacokinetic parameters in permeability studies were estimated by using WinNonLin software program. w/o microemulsion system was optimized using a pseudoternary phase diagram, composed of span 80/lutrol F 68 (9.5:0.5 w/w), oleic acide, isopropyl alcohol and water as surfactant mixture; oil and cosurfactant was developed for oral drug delivery. w/o microemulsion systems were characterized by phase behavior, particle size, viscosity and solubilization capacity. In vitro studies were studied using Caco-2 cell monolayer. Pharmacokinetic parameters of w/o microemulsion were investigated in rabbits and compared to Fexofen® syrup. Fexofen® syrup and microemulsion were administered by oral gavage at 6 mg/kg of the same concentration. The experimental results indicated that microemulsion (HLB = 5.53) formed nanometer sized droplets (33.29 ± 1.76) and had good physical stability. This microemulsion increased the oral bioavailability of FEX which was highly water-soluble but fairly impermeable. The relative bioavailability of FEX microemulsion was about 376.76% compared with commercial syrup in rabbits. In vitro experiments were further employed for the enhanced effect of the microemulsion for FEX. These results suggest that novel w/o microemulsion plays an important role in enhancing oral bioavailability of low permeability drugs. PMID:21904453

Synthesis and characterization of nano-sized zirconia powder synthesized by single emulsion-assisted direct precipitation.

PubMed

Chandra, Navin; Singh, Deepesh Kumar; Sharma, Meenakshi; Upadhyay, Ravi Kant; Amritphale, S S; Sanghi, S K

2010-02-15

For the first time, single reverse microemulsion-assisted direct precipitation route has been successfully used to synthesize tetragonal zirconia nanoparticles in narrow size range. The synthesized powder was characterized using FT-IR, XRD and HRTEM techniques. The zirconia nanoparticles obtained were spherical in shape and has narrow particle size distribution in the range of 13-31nm and crystallite size in the range of 13-23nm. Copyright 2009 Elsevier Inc. All rights reserved.

Fine tuning of size and morphology of magnetite nanoparticles synthesized by microemulsion

NASA Astrophysics Data System (ADS)

Singh, Pinki; Upadhyay, Chandan

2018-05-01

The synthesis parameters crucially affect the physical and chemical parameters of nanoparticles. Magnetite (Fe3O4) nanoparticles were synthesized using microemulsion method. This method does not require high temperature synthesis, nitrogen environment and/or pH regulation during synthesis process. We are presenting here a systematic study on role of different associated parameters of microemulsion synthesis method on the formation of Fe3O4 nanoparticles. From X-ray Diffraction and Transmission Electron Micoscopy data analysis the size of synthesized particles were observed to be <10 nm. The critical concentration of ferrous-ferric solution to obtain particles in single phase has been found to be ≤0.09 M and ≤0.184 M, respectively. The variation of molar concentration (0.01 M ≤x≤ 0.1 M) of CTAB leads to formation of Fe3O4 nano-scale particles of distinct morphologies e.g. nano-cubes, pentagons and spheres. The number of ferrous and ferric ions involved in the formation decides the size of the nanoparticles. The single crystallographic phase is obtained in reaction temperature range of 65° C

Microemulsion Liquid Chromatographic Method for Simultaneous Determination of Simvastatin and Ezetimibe in Their Combined Dosage Forms

PubMed Central

Hammouda, Mohammed E. A.; Abu El-Enin, Mohamed A.; El-Sherbiny, Dina T.; El-Wasseef, Dalia R.; El-Ashry, Saadia M.

2013-01-01

A rapid HPLC procedure using a microemulsion as an eluent was developed and validated for analytical quality control of antihyperlipidemic mixture containing simvastatin (SIM) and ezetimibe (EZT) in their pharmaceutical preparations. The separation was performed on a column packed with cyano bonded stationary phase adopting UV detection at 238 nm using a flow rate of 1 mL/min. The optimized microemulsion mobile phase consisted of 0.2 M sodium dodecyl sulphate, 1% octanol, 10% n-propanol, and 0.3% triethylamine in 0.02 M phosphoric acid at pH 5.0. The developed method was validated in terms of specificity, linearity, lower limit of quantification (LOQ), lower limit of detection (LOD), precision, and accuracy. The proposed method is rapid (8.5 min), reproducible (RSD < 2.0%) and achieves satisfactory resolution between SIM and EZT (resolution factor = 2.57). The mean recoveries of the analytes in pharmaceutical preparations were in agreement with those obtained from a reference method, as revealed by statistical analysis of the obtained results using Student's t-test and the variance ratio F-test. PMID:24282651

Investigation of surfactant/cosurfactant synergism impact on ibuprofen solubilization capacity and drug release characteristics of nonionic microemulsions.

PubMed

Djekic, Ljiljana; Primorac, Marija; Filipic, Slavica; Agbaba, Danica

2012-08-20

The current study investigates the performances of the multicomponent mixtures of nonionic surfactants regarding the microemulsion stabilisation, drug solubilization and in vitro drug release kinetic. The primary surfactant was PEG-8 caprylic/capric glycerides (Labrasol). The cosurfactants were commercially available mixtures of octoxynol-12 and polysorbate 20 without or with the addition of PEG-40 hydrogenated castor oil (Solubilisant gamma 2421 and Solubilisant gamma 2429, respectively). The oil phase of microemulsions was isopropyl myristate. Phase behaviour study of the pseudo-ternary systems Labrasol/cosurfactant/oil/water at surfactant-to-cosurfactant weight ratios (K(m)) 40:60, 50:50 and 60:40, revealed a strong synergism in the investigated tensides mixtures for stabilisation of microemulsions containing up to 80% (w/w) of water phase at surfactant +cosurfactant-to-oil weight ratio (SCoS/O) 90:10. Solubilization of a model drug ibuprofen in concentration common for topical application (5%, w/w) was achieved at the water contents below 50% (w/w). Drug free and ibuprofen-loaded microemulsions M1-M6, containing 45% (w/w) of water phase, were prepared and characterized by polarized light microscopy, conductivity, pH, rheological and droplet size measurements. In vitro ibuprofen release kinetics from the microemulsions was investigated using paddle-over-enhancer cell method and compared with the commercial 5% (w/w) ibuprofen hydrogel product (Deep Relief, Mentholatum Company Ltd., USA). The investigated microemulsions were isotropic, low viscous Bingham-type liquids with the pH value (4.70-6.61) suitable for topical application. The different efficiency of the tensides mixtures for microemulsion stabilisation was observed, depending on the cosurfactant type and K(m) value. Solubilisant gamma 2429 as well as higher K(m) (i.e., lower relative content of the cosurfactant) provided higher surfactant/cosurfactant synergism. The drug molecules were predominantly solubilized within the interface film. The amount of drug released from the formulations M3 (10.75%, w/w) and M6 (13.45%, w/w) (K(m) 60:40) was limited in comparison with the reference (22.22%, w/w) and follows the Higuchi model. Microemulsions M2 and M5 (K(m) 50:50) gave zero order drug release pattern and ∼15% (w/w) ibuprofen released. The release profiles from microemulsions M1 and M4 (K(m) 40:60) did not fit well with the models used for analysis, although the amounts of ibuprofen released (24.47%, w/w) and 17.99% (w/w), respectively) were comparable to that of the reference hydrogel. The drug release mechanism was related with the surfactant/cosurfactant synergism, thus the lower efficiency of the tensides corresponded to the faster drug release. Copyright © 2012 Elsevier B.V. All rights reserved.

Preparation and enhancement of oral bioavailability of curcumin using microemulsions vehicle.

PubMed

Hu, Liandong; Jia, Yanhong; Niu, Feng; Jia, Zheng; Yang, Xun; Jiao, Kuiliang

2012-07-25

A new microemulsions system of curcumin (CUR-MEs) was successfully developed to improve the solubility and bioavailability of curcumin. Several formulations of the microemulsions system were prepared and evaluated using different ratios of oils, surfactants, and co-surfactants (S&CoS). The optimal formulation, which consists of Capryol 90 (oil), Cremophor RH40 (surfactant), and Transcutol P aqueous solution (co-surfactant), could enhance the solubility of curcumin up to 32.5 mg/mL. The pharmacokinetic study of microemulsions was performed in rats compared to the corresponding suspension. The stability of microemulsions after dilution was excellence. Microemulsions have significantly increased the C(max) and area under the curve (AUC) in comparison to that in suspension (p < 0.05). The relative bioavailability of curcumin in microemulsions was 22.6-fold higher than that in suspension. The results indicated that the CUR-MEs could be used as an effective formulation for enhancing the oral bioavailability of curcumin.

Food grade microemulsion systems: canola oil/lecithin:n-propanol/water.

PubMed

Abbasi, Soleiman; Radi, Mohsen

2016-03-01

In this study, the capability of a natural surfactant, lecithin, and the influence of ionic strength, pH, and temperature on some properties of a food grade microemulsion system were evaluated. For this purpose, the pseudoternary phase diagrams of canola oil/lecithin:n-propanol/water microemulsions in the presence of different salts (NaCl and CaCl2), ionic strengths, pHs, and temperatures were constructed. Our findings showed that the presence of salts slightly increased the W/O areas on the phase diagrams, whereas pH variation was not effective on the microemulsion formation. The expansion of microemulsion areas with temperature indicated the greater triglycerides solubilization capacity of lecithin based microemulsions at higher temperatures. These findings revealed the efficiency of lecithin-based microemulsion system for solubilization of triglycerides which can potentially be used for extraction of edible vegetable oils particularly canola oil. Copyright © 2015 Elsevier Ltd. All rights reserved.

Microemulsions for Colorectal Cancer Treatments. General Considerations and Formulation of Methotrexate.

PubMed

Flores, Sergio E; Rial-Hermida, M Isabel; Ramirez, Jorge C; Pazos, Alejandro; Concheiro, Angel; Alvarez-Lorenzo, Carmen; Peralta, René D

2016-01-01

Microemulsions combine the advantages of emulsions with those of nanocarriers, overcoming the stability problems of the former and providing facile scalable systems with compartments adequate for high drug loadings. Recently, microemulsions are gaining attention in the formulation of anticancer drugs not only for topical treatment, but also for systemic delivery as well as for the development of theranostic systems. The aim of this paper is two-fold. First, an updated review about general features, preparation, characterization and pharmaceutical applications, with a special focus on colorectal cancer, is provided. Second, a case study of formulation of methotrexate in microemulsions is presented. Various essential oils (menthol, trans-anethole, α-tocopherol) and surfactants (TPGS-1000, Maxemul 6112, Noigen RN-20) were investigated for the preparation of o/w microemulsions for the delivery of methotrexate, and the ability of methotrexate-loaded microemulsions to inhibit cancer cell growth was then evaluated. Disregarding the surfactants used, menthol and trans-anethole led to cytotoxic microemulsions, whereas α-tocopherol based-formulations induced cell proliferation. These findings highlight the role that the oily component may play in the efficacy and safety of the microemulsions.

Formulation, physicochemical characterization and stability study of lithium-loaded microemulsion system.

PubMed

Mouri, Abdelkader; Legrand, Philippe; El Ghzaoui, Abdeslam; Dorandeu, Christophe; Maurel, Jean Claude; Devoisselle, Jean-Marie

2016-04-11

Lithium biocompatible microemulsion based on Peceol(®), lecithin, ethanol and water was studied in attempt to identify the optimal compositions in term of drug content, physicochemical properties and stability. Lithium solubilization in microemulsion was found to be compatible with a drug-surfactant binding model. Lithium ions were predominantly solubilized within lecithin head group altering significantly the interfacial properties of the system. Pseudo-ternary phase diagrams of drug free and drug loaded microemulsions were built at constant ethanol/lecithin weight ratio (40/60). Lithium loaded microemulsion has totally disappeared in the Peceol(®) rich part of phase diagram; critical fractions of lecithin and ethanol were required for the formation of stable microemulsion. The effect of lithium concentration on the properties and physical stability of microemulsions were studied using microscopy, Karl Fischer titrations, rheology analyses, conductivity measurements and centrifugation tests. The investigated microemulsions were found to be stable under accelerated storage conditions. The systems exhibited low viscosity and behaved as Newtonian fluid and no structural transition was shown. Copyright © 2016 Elsevier B.V. All rights reserved.

Characterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid.

PubMed

Lu, Yingnian; Wu, Kefeng; Li, Li; He, Yuhui; Cui, Liao; Liang, Nianci; Mu, Bozhong

2013-01-01

The objective of this study was to develop an oral microemulsion formulation of the antitumor diterpenoid agent, ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic-acid (henceforth referred to as 5F), to enhance its bioavailability and evaluate its hepatotoxicity. Pseudoternary phase diagrams showed that the optimal microemulsion formulation contained 45% water, 10% castor oil as the oil phase, 15% Cremophor EL as the surfactant, and 30% as a cosurfactant mixture of 1,2-propanediol and polyethylene glycol (PEG)-400 (2:1, w/w). The microemulsion preparation was characterized and its droplet diameter was within 50 nm. Release of 5F in vitro from the microemulsion was slightly increased compared with a suspension containing the same amount of active drug. Pharmacokinetic parameters in vivo indicated that bioavailability was markedly improved, with the relative bioavailability being 616.15% higher for the microemulsion than for the suspension. Toxicity tests showed that the microemulsion had no hepatotoxicity in mice. These results suggest the potential for 5F microemulsion to be administered by the oral route.

Evaluation of Ocular Irritation and Bioavailability of Voriconazole Loaded Microemulsion.

PubMed

Kumar, Rakesh; Sinha, Vivek Ranjan

2017-01-01

Voriconazole (VCZ), a second-generation antifungal with excellent attributes like, broad-spectrum activity, targeted delivery, and tolerability. VCZ loaded microemulsion could be an effective strategy for efficient ocular delivery of the drug. To perform corneal irritation studies and in vivo delivery of VCZ microemulsion to establish its potential as an efficient ocular delivery system. Ocular irritancy was performed by HETCAM (Hen's Egg Test Chorio Allantoic Membrane) assay, corneal histopathology and Draize test. Ex vivo and in vivo studies were performed to determine permeation efficiency of VCZ microemulsion. The irritation studies suggested the non-irritant nature of the microemulsion. The ex vivo studies performed on excised cornea displayed significant enhancement in drug permeation/penetration from microemulsion in contrast to the drug suspension. Further, the in vivo study confirmed the higher availability of VCZ (from microemulsion) in aqueous humor with minimal nasolacrimal drainage (lower plasma drug content) when compared with the drug suspension. The non-irritant nature and high corneal permeation of VCZ encourages the role of microemulsion as a potential ocular delivery system. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Microemulsion of babassu oil as a natural product to improve human immune system function.

PubMed

Pessoa, Rafael Souza; França, Eduardo Luzia; Ribeiro, Elton Brito; Lanes, Patrícia Kelly Dias; Chaud, Natalina Galdeano Abud; Moraes, Lucélia Campelo Albuquerque; Honorio-França, Adenilda Cristina

2015-01-01

The aim of this study was to develop and characterize a babassu oil microemulsion system and determine the effect of this microemulsion on the functional activity of phagocytes. The microemulsion was formulated using distilled water, babassu as the oil phase component, Sorbitan monooleate-Span 80(®) (SP), Polysorbate 80-Tween 80(®) (TW), and 1-butanol (BT). Pseudoternary diagrams were prepared, and microemulsion diagram regions were preselected. Rheological characterization and preliminary and accelerated stability tests were performed. The effect of the microemulsion on the interactions between leukocytes and bacteria was determined by superoxide release, phagocytosis, and microbicidal activity. The developed formulation SP/TW/BT (4.2/4.8/1.0) was classified as oil/water, showed a Newtonian profile, and had linear viscosity. When we assessed the interaction of the microemulsion or babassu oil with phagocytes, we observed an increase in superoxide, phagocytosis, and microbicidal activity. The babassu oil microemulsion system is an option for future applications, including for vaccine delivery systems. Babassu oil is a natural product, so is an alternative for future immunotherapy strategies, in particular for infectious diseases.

Microemulsions containing lecithin and sugar-based surfactants: nanoparticle templates for delivery of proteins and peptides.

PubMed

Graf, Anja; Ablinger, Elisabeth; Peters, Silvia; Zimmer, Andreas; Hook, Sarah; Rades, Thomas

2008-02-28

Two pseudo-ternary systems comprising isopropyl myristate, soybean lecithin, water, ethanol and either decyl glucoside (DG) or capryl-caprylyl glucoside (CCG) as surfactant were investigated for their potential to form microemulsion templates to produce nanoparticles as drug delivery vehicles for proteins and peptides. All microemulsion and nanoparticle compounds used were pharmaceutically acceptable and biocompatible. Phase diagrams were established and characterized using polarizing light microscopy, viscosity, conductivity, electron microscopy, differential scanning calorimetry and self-diffusion NMR. An area in the phase diagrams containing optically isotropic, monophasic systems was designated as the microemulsion region and systems therein identified as solution-type microemulsions. Poly(alkylcyanoacrylate) nanoparticles prepared by interfacial polymerisation from selected microemulsions ranged from 145 to 660nm in size with a unimodal size distribution depending on the type of monomer (ethyl (2) or butyl (2) cyanoacrylate) and microemulsion template. Generally larger nanoparticles were formed by butyl (2) cyanoacrylate. Insulin was added as a model protein and did not alter the physicochemical behaviour of the microemulsions or the morphology of the nanoparticles. However, insulin-loaded nanoparticles in the CCG containing system decreased in size when using butyl (2) cyanoacrylate. This study shows that microemulsions containing sugar-based surfactants are suitable formulation templates for the formation of nanoparticles to deliver peptides.

Design and Evaluation of Microemulsion Gel System of Nadifloxacin

PubMed Central

Shinde, Ujwala; Pokharkar, Sharda; Modani, Sheela

2012-01-01

Topical microemulsion systems for the antiacne agent, nadifloxacin were designed and developed to overcome the problems associated with the cutaneous delivery due to poor water solubility. The solubility of nadifloxacin in oils, surfactants and cosurfactants was evaluated to screen the components of the microemulsion. Various surfactants and cosurfactants were screened for their ability to emulsify the selected oily phase. The pseudoternary diagrams were constructed to identify the area of microemulsion existence. The influence of km (surfactant/cosurfactant) ratio on the microemulsion existence region was determined and optimum systems were designed. The systems were assessed for drug-loading efficiency and characterised for optical birefringence, pH and refractive index, robustness to dilution, globule size, drug content and thermodynamic stability. Optimised microemulsion systems were formulated into gel form and evaluated for viscosity, spreadability, drug content, ex vivo skin permeation and antibacterial activity. The maximum solubility of nadifloxacin in the microemulsion system was found to be 0.25%. The nadifloxacin microemulsions had a small and uniform globule size (67.3-121.23 nm). The stability results revealed that all formulations showed a stable globule size and the polydispersity index under stress conditions. Incorporation of nadifloxacin in microemulsion gel increased the ex vivo skin permeation and antibacterial activity when compared to marketed cream. PMID:23439454

Transdermal delivery of diclofenac using water-in-oil microemulsion: formulation and mechanistic approach of drug skin permeation.

PubMed

Thakkar, Priyanka J; Madan, Parshotam; Lin, Senshang

2014-05-01

The objective of the present investigation was to enhance skin permeation of diclofenac using water-in-oil microemulsion and to elucidate its skin permeation mechanism. The w/o microemulsion formulations were selected based on constructed pseudoternary phase diagrams depending on water solubilization capacity and thermodynamic stability. These formulations were also subjected to physical characterization based on droplet size, viscosity, pH and conductivity. Permeation of diclofenac across rat skin using side-by-side permeation cells from selected w/o microemulsion formulations were evaluated and compared with control formulations. The selected w/o microemulsion formulations were thermodynamically stable, and incorporation of diclofenac sodium into microemulsion did not affect the phase behavior of system. All microemulsion formulations had very low viscosity (11-17 cps) and droplet size range of 30-160 nm. Microemulsion formulations exhibited statistically significant increase in diclofenac permeation compared to oily solution, aqueous solution and oil-Smix solution. Higher skin permeation of diclofenac was observed with low Smix concentration and smaller droplet size. Increase in diclofenac loading in aqueous phase decreased the partition of diclofenac. Diclofenac from the oil phase of microemulsion could directly partition into skin, while diclofenac from the aqueous droplets was carried through skin by carrier effect.

A Novel Paclitaxel Microemulsion Containing a Reduced Amount of Cremophor EL: Pharmacokinetics, Biodistribution, and In Vivo Antitumor Efficacy and Safety

PubMed Central

Wang, Ying; Wu, Ke-Chun; Zhao, Bing-Xiang; Zhao, Xin; Wang, Xin; Chen, Su; Nie, Shu-Fang; Pan, Wei-San; Zhang, Xuan; Zhang, Qiang

2011-01-01

The purpose of this study was to prepare a novel paclitaxel (PTX) microemulsion containing a reduced amount of Cremophor EL (CrEL) which had similar pharmacokinetics and antitumor efficacy as the commercially available PTX injection, but a significantly reduced allergic effect due to the CrEL. The pharmacokinetics, biodistribution, in vivo antitumor activity and safety of PTX microemulsion was evaluated. The results of pharmacokinetic and distribution properties of PTX in the microemulsion were similar to those of the PTX injection. The antitumor efficacy of the PTX microemulsion in OVCRA-3 and A 549 tumor-bearing animals was similar to that of PTX injection. The PTX microemulsion did not cause haemolysis, erythrocyte agglutination or simulative reaction. The incidence and degree of allergic reactions exhibited by the PTX microemulsion group, with or without premedication, were significantly lower than those in the PTX injection group (P < .01). In conclusion, the PTX microemulsion had similar pharmacokinetics and anti-tumor efficacy to the PTX injection, but a significantly reduced allergic effect due to CrEL, indicating that the PTX microemulsion overcomes the disadvantages of the conventional PTX injection and is one way of avoiding the limitations of current injection product while providing suitable therapeutic efficacy. PMID:21331356

Photoionization of oxidized coenzyme Q in microemulsion: laser flash photolysis study in biomembrane-like system.

PubMed

Li, Kun; Wang, Mei; Wang, Jin; Zhu, Rongrong; Sun, Dongmei; Sun, Xiaoyu; Wang, Shi-Long

2013-01-01

Photoexcitation to generate triplet state has been proved to be the main photoreaction in homogeneous system for many benzoquinone derivatives, including oxidized coenzyme Q (CoQ) and its analogs. In the present study, microemulsion of CoQ, a heterogeneous system, is employed to mimic the distribution of CoQ in biomembrane. The photochemistry of CoQ(10) in microemulsion and cyclohexane is investigated and compared using laser flash photolysis and results show that CoQ(10) undergoes photoionization via a monophotonic process to generate radical cation of CoQ(10) in microemulsion and photoexcitation to generate excited triplet state in cyclohexane. Meanwhile, photoreactions of duroquinone (DQ) and CoQ(0) in microemulsion are also investigated to analyze the influence of molecular structure on the photochemistry of benzoquinone derivatives in microemulsion. Results suggest that photoexcitation, which is followed by excited state-involved hydrogen-abstraction reaction, is the main photoreaction for DQ and CoQ(0) in microemulsion. However, photoexcited CoQ(0) also leads to the formation of hydrated electrons. The isoprenoid side chain-involved high resonance stabilization is proposed to explain the difference in photoreactions of CoQ(0) and CoQ(10) in microemulsion. Considering that microemulsion is close to biomembrane system, its photoionization in microemulsion may be helpful to understand the real photochemistry of biological quinones in biomembrane system. © 2012 Tongji University. Photochemistry and Photobiology © 2012 The American Society of Photobiology.

Pore Scale Dynamics of Microemulsion Formation.

PubMed

Unsal, Evren; Broens, Marc; Armstrong, Ryan T

2016-07-19

Experiments in various porous media have shown that multiple parameters come into play when an oleic phase is displaced by an aqueous solution of surfactant. In general, the displacement efficiency is improved when the fluids become quasi-miscible. Understanding the phase behavior oil/water/surfactant systems is important because microemulsion has the ability to generate ultralow interfacial tension (<10(-2) mN m(-1)) that is required for miscibility to occur. Many studies focus on microemulsion formation and the resulting properties under equilibrium conditions. However, the majority of applications where microemulsion is present also involve flow, which has received relatively less attention. It is commonly assumed that the characteristics of an oil/water/surfactant system under flowing conditions are identical to the one under equilibrium conditions. Here, we show that this is not necessarily the case. We studied the equilibrium phase behavior of a model system consisting of n-decane and an aqueous solution of olefin sulfonate surfactant, which has practical applications for enhanced oil recovery. The salt content of the aqueous solution was varied to provide a range of different microemulsion compositions and oil-water interfacial tensions. We then performed microfluidic flow experiments to study the dynamic in situ formation of microemulsion by coinjecting bulk fluids of n-decane and surfactant solution into a T-junction capillary geometry. A solvatochromatic fluorescent dye was used to obtain spatially resolved compositional information. In this way, we visualized the microemulsion formation and the flow of it along with the excess phases. A complex interaction between the flow patterns and the microemulsion properties was observed. The formation of microemulsion influenced the flow regimes, and the flow regimes affected the characteristics of the microemulsion formation. In particular, at low flow rates, slug flow was observed, which had profound consequences on the pore scale mixing behavior and resulting microemulsion properties.

Effect of surfactant chain length on drug release kinetics from microemulsion-laden contact lenses.

PubMed

Maulvi, Furqan A; Desai, Ankita R; Choksi, Harsh H; Patil, Rahul J; Ranch, Ketan M; Vyas, Bhavin A; Shah, Dinesh O

2017-05-30

The effect of surfactant chain lengths [sodium caprylate (C 8 ), Tween 20 (C 12 ), Tween 80 (C 18 )] and the molecular weight of block copolymers [Pluronic F68 and Pluronic F 127] were studied to determine the stability of the microemulsion and its effect on release kinetics from cyclosporine-loaded microemulsion-laden hydrogel contact lenses in this work. Globule size and dilution tests (transmittance) suggested that the stability of the microemulsion increases with increase in the carbon chain lengths of surfactants and the molecular weight of pluronics. The optical transmittance of direct drug-laden contact lenses [DL-100] was low due to the precipitation of hydrophobic drugs in the lenses, while in microemulsion-laden lenses, the transmittance was improved when stability of the microemulsion was achieved. The results of in vitro release kinetics revealed that drug release was sustained to a greater extent as the stability of microemulsion was improved as well. This was evident in batch PF127-T80, which showed sustained release for 15days in comparison to batch DL-100, which showed release up to 7days. An in vivo drug release study in rabbit tear fluid showed significant increase in mean residence time (MRT) and area under curve (AUC) with PF-127-T80 lenses (stable microemulsion) in comparison to PF-68-SC lenses (unstable microemulsion) and DL-100 lenses. This study revealed the correlation between the stability of microemulsion and the release kinetics of drugs from contact lenses. Thus, it was inferred that the stable microemulsion batches sustained the release of hydrophobic drugs, such as cyclosporine from contact lenses for an extended period of time without altering critical lens properties. Copyright © 2017 Elsevier B.V. All rights reserved.

Systemic delivery of insulin via the nasal route using a new microemulsion system: In vitro and in vivo studies.

PubMed

Sintov, Amnon C; Levy, Haim V; Botner, Shafir

2010-12-01

The main purpose of this study was to investigate the nasal absorption of insulin from a new microemulsion spray preparation in rabbits. The bioavailability of insulin lispro via the nasal route using a W/O microemulsion was found to reach 21.5% relative to subcutaneous administration, whereas the use of an inverse microemulsion as well as a plain solution yielded less than 1% bioavailability. The profile of plasma glucose levels obtained after nasal spray application of the microemulsion (1IU/kg lispro) was similar to the subcutaneous profile of 0.5IU/kg at the first 90min after application and resulted in a 30-40% drop in glucose levels. The microemulsion system was characterized by DLS, TEM, viscosity measurements, and by construction of pseudo-ternary phase diagram. The average droplet size of an insulin-unloaded and insulin-loaded microemulsions containing 20% aqueous phase (surfactants-to-oil ratio=87:13) was 2nm and 2.26nm in diameter, respectively. In addition, the effect of the microemulsion on FITC-labeled insulin permeation was examined across the porcine nasal mucosa in vitro. The permeability coefficient of FITC-insulin via the microemulsion was 0.210±0.048cm/h with a lag time of 10.9±6.5min, whereas the permeability coefficient from a plain solution was 0.082±0.043cm/h with a lag time of 36.3±10.1min. In view of the absorption differences of insulin between 20%, 50% water-containing microemulsions and an aqueous solution obtained in vitro and in vivo, it has been concluded that the acceleration in the intramucosal transport process is the result of encapsulating insulin within the nano-droplet clusters of a W/O microemulsion, while the microemulsion ingredients seems to have no direct role. Copyright © 2010 Elsevier B.V. All rights reserved.

Gold decorated NaYF4:Yb,Er/NaYF4/silica (core/shell/shell) upconversion nanoparticles for photothermal destruction of BE(2)-C neuroblastoma cells

NASA Astrophysics Data System (ADS)

Qian, Li Peng; Zhou, Li Han; Too, Heng-Phon; Chow, Gan-Moog

2011-02-01

Gold decorated NaYF4:Yb,Er/NaYF4/silica (core/shell/shell) upconversion (UC) nanoparticles ( 70-80 nm) were synthesized using tetraethyl orthosilicate and chloroauric acid in a one-step reverse microemulsion method. Gold nanoparticles ( 6 nm) were deposited on the surface of silica shell of these core/shell/shell nanoparticles. The total upconversion emission intensity (green, red, and blue) of the core/shell/shell nanoparticles decreased by 31% after Au was deposited on the surface of silica shell. The upconverted green light was coupled with the surface plasmon of Au leading to rapid heat conversion. These UC/silica/Au nanoparticles were very efficient to destroy BE(2)-C cancer cells and showed strong potential in photothermal therapy.

Water-in-Supercritical CO2 Microemulsion Stabilized by a Metal Complex.

PubMed

Luo, Tian; Zhang, Jianling; Tan, Xiuniang; Liu, Chengcheng; Wu, Tianbin; Li, Wei; Sang, Xinxin; Han, Buxing; Li, Zhihong; Mo, Guang; Xing, Xueqing; Wu, Zhonghua

2016-10-17

Herein we propose for the first time the utilization of a metal complex for forming water-in-supercritical CO 2 (scCO 2 ) microemulsions. The water solubility in the metal-complex-stabilized microemulsion is significantly improved compared with the conventional water-in-scCO 2 microemulsions stabilized by hydrocarbons. Such a microemulsion provides a promising route for the in situ CO 2 reduction catalyzed by a metal complex at the water/scCO 2 interface. © 2016 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Studies on the kinetics of killing and the proposed mechanism of action of microemulsions against fungi.

PubMed

Al-Adham, Ibrahim S I; Ashour, Hana; Al-Kaissi, Elham; Khalil, Enam; Kierans, Martin; Collier, Phillip J

2013-09-15

Microemulsions are physically stable oil/water clear dispersions, spontaneously formed and thermodynamically stable. They are composed in most cases of water, oil, surfactant and cosurfactant. Microemulsions are stable, self-preserving antimicrobial agents in their own right. The observed levels of antimicrobial activity associated with microemulsions may be due to the direct effect of the microemulsions themselves on the bacterial cytoplasmic membrane. The aim of this work is to study the growth behaviour of different microbes in presence of certain prepared physically stable microemulsion formulae over extended periods of time. An experiment was designed to study the kinetics of killing of a microemulsion preparation (17.3% Tween-80, 8.5% n-pentanol, 5% isopropyl myristate and 69.2% sterile distilled water) against selected test microorganisms (Candida albicans, Aspergillus niger, Schizosaccharomyces pombe and Rhodotorula spp.). Secondly, an experiment was designed to study the effects of the microemulsion preparation on the cytoplasmic membrane structure and function of selected fungal species by observation of 260 nm component leakage. Finally, the effects of the microemulsion on the fungal membrane structure and function using S. pombe were studied using transmission electron microscopy. The results showed that the prepared microemulsions are stable, effective antimicrobial systems with effective killing rates against C. albicans, A. niger, S. pombe and Rhodotorula spp. The results indicate a proposed mechanism of action of significant anti-membrane activity, resulting in the gross disturbance and dysfunction of the cytoplasmic membrane structure which is followed by cell wall modifications, cytoplasmic coagulation, disruption of intracellular metabolism and cell death. Copyright © 2013 Elsevier B.V. All rights reserved.

The effect of water on the microstructure of 1-butyl-3-methylimidazolium tetrafluoroborate/TX-100/benzene ionic liquid microemulsions.

PubMed

Gao, Yan'an; Li, Na; Zheng, Liqiang; Zhao, Xueyan; Zhang, Jin; Cao, Quan; Zhao, Mingwei; Li, Zhen; Zhang, Gaoyong

2007-01-01

The ionic liquid (IL) 1-butyl-3-methylimidazolium tetrafluoroborate ([bmim][BF4]) forms nonaqueous microemulsions with benzene with the aid of nonionic surfactant TX-100. The phase diagram of the ternary system was prepared, and the microstructures of the microemulsion were recognized. On the basis of the phase diagram, a series of ionic liquid-in-oil (IL/O) microemulsions were chosen and characterized by dynamic light scattering (DLS), which shows a similar swelling behavior to typical water-in-oil (W/O) microemulsions. The existence of IL pools in the IL/O microemulsion was confirmed by UV/Vis spectroscopic analysis with CoCl2 and methylene blue (MB) as the absorption probes. A constant polarity of the IL pool is observed, even if small amounts of water are added to the microemulsion, thus suggesting that the water molecules are solubilized in the polar outer shell of the microemulsion, as confirmed by FTIR spectra. 1H NMR spectroscopic analysis shows that these water molecules interact with the electronegative oxygen atoms of the oxyethylene (OE) units of TX-100 through hydrogen-bonding interactions, and the electronegative oxygen atoms of the water molecules attract the electropositive imidazolium rings of [bmim][BF4]. Hence, the water molecules are like a glue that stick the IL and OE units more tightly together and thus make the microemulsion system more stable. Considering the unique solubilization behavior of added water molecules, the IL/O microemulsion system may be used as a medium to prepare porous or hollow nanomaterials by hydrolysis reactions.

Small-angle neutron scattering study of a dense microemulsion system formed with an ionic liquid

DOE PAGES

Kang, T.; Qian, S.; Smith, G. S.; ...

2017-09-07

Mixtures of water, octane and 1-octanol with 1-tetradecyl-3-methylimidazolium chloride (C14MIM·Cl), often referred to as a surface active ionic liquid (SAIL), form water-in-oil microemulsions that have potential application as extraction media for various metal ions. Here in this work, we present a structural study by small-angle neutron scattering (SANS) of dense microemulsions formed by surfactant-rich mixtures of these four compounds to understand how the SAIL can be used to tune the structures and properties of the microemulsions. The SANS experiments revealed that the microemulsions formed are composed of two phases, a water-in-oil microemulsion and a bicontinuous microemulsion, which becomes the dominantmore » phase at high surfactant concentration. In this concentration regime, the surfactant film becomes more rigid, having a higher bending modulus that results from the parallel stacking of the imidazolium ring of the SAIL. At lower surfactant concentrations, the molecular packing of the SAIL does not change with the water content of the microemulsion. Finally, the results presented here correlate well with previously observed changes in the interaction between the IL cation and metal ions (Y. Tong, L. Han and Y. Yang, Ind. Eng. Chem. Res., 2012, 51, 16438–16443), while the capacity of the microemulsion system for water remains high enough for using the system as an extraction medium.« less

Small-angle neutron scattering study of a dense microemulsion system formed with an ionic liquid

DOE Office of Scientific and Technical Information (OSTI.GOV)

Kang, T.; Qian, S.; Smith, G. S.

Mixtures of water, octane and 1-octanol with 1-tetradecyl-3-methylimidazolium chloride (C14MIM·Cl), often referred to as a surface active ionic liquid (SAIL), form water-in-oil microemulsions that have potential application as extraction media for various metal ions. Here in this work, we present a structural study by small-angle neutron scattering (SANS) of dense microemulsions formed by surfactant-rich mixtures of these four compounds to understand how the SAIL can be used to tune the structures and properties of the microemulsions. The SANS experiments revealed that the microemulsions formed are composed of two phases, a water-in-oil microemulsion and a bicontinuous microemulsion, which becomes the dominantmore » phase at high surfactant concentration. In this concentration regime, the surfactant film becomes more rigid, having a higher bending modulus that results from the parallel stacking of the imidazolium ring of the SAIL. At lower surfactant concentrations, the molecular packing of the SAIL does not change with the water content of the microemulsion. Finally, the results presented here correlate well with previously observed changes in the interaction between the IL cation and metal ions (Y. Tong, L. Han and Y. Yang, Ind. Eng. Chem. Res., 2012, 51, 16438–16443), while the capacity of the microemulsion system for water remains high enough for using the system as an extraction medium.« less

Characterization and evaluation of an oral microemulsion containing the antitumor diterpenoid compound ent-11alpha-hydroxy-15-oxo-kaur-16-en-19-oic-acid

PubMed Central

Lu, Yingnian; Wu, Kefeng; Li, Li; He, Yuhui; Cui, Liao; Liang, Nianci; Mu, Bozhong

2013-01-01

The objective of this study was to develop an oral microemulsion formulation of the antitumor diterpenoid agent, ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic-acid (henceforth referred to as 5F), to enhance its bioavailability and evaluate its hepatotoxicity. Pseudoternary phase diagrams showed that the optimal microemulsion formulation contained 45% water, 10% castor oil as the oil phase, 15% Cremophor EL as the surfactant, and 30% as a cosurfactant mixture of 1,2-propanediol and polyethylene glycol (PEG)-400 (2:1, w/w). The microemulsion preparation was characterized and its droplet diameter was within 50 nm. Release of 5F in vitro from the microemulsion was slightly increased compared with a suspension containing the same amount of active drug. Pharmacokinetic parameters in vivo indicated that bioavailability was markedly improved, with the relative bioavailability being 616.15% higher for the microemulsion than for the suspension. Toxicity tests showed that the microemulsion had no hepatotoxicity in mice. These results suggest the potential for 5F microemulsion to be administered by the oral route. PMID:23690685

Bicontinuous microemulsions as a biomembrane mimetic system for melittin

DOE Office of Scientific and Technical Information (OSTI.GOV)

Hayes, Douglas G.; Ye, Ran; Dunlap, Rachel N.

Antimicrobial peptides effectively kill antibiotic-resistant bacteria by forming pores in prokaryotes' biomembranes via penetration into the biomembranes' interior. Bicontinuous microemulsions, consisting of interdispersed oil and water nanodomains separated by flexible surfactant monolayers, are potentially valuable for hosting membrane-associated peptides and proteins due to their thermodynamic stability, optical transparency, low viscosity, and high interfacial area. Here, we show that bicontinuous microemulsions formed by negatively-charged surfactants are a robust biomembrane mimetic system for the antimicrobial peptide melittin. When encapsulated in bicontinuous microemulsions formed using three-phase (Winsor-III) systems, melittin's helicity increases greatly due to penetration into the surfactant monolayers, mimicking its behavior inmore » biomembranes. But, the threshold melittin concentration required to achieve these trends is lower for the microemulsions. The extent of penetration was decreased when the interfacial fluidity of the microemulsions was increased. In conclusion, these results suggest the utility of bicontinuous microemulsions for isolation, purification, delivery, and host systems for antimicrobial peptides.« less

Bicontinuous microemulsions as a biomembrane mimetic system for melittin

DOE PAGES

Hayes, Douglas G.; Ye, Ran; Dunlap, Rachel N.; ...

2017-11-12

Antimicrobial peptides effectively kill antibiotic-resistant bacteria by forming pores in prokaryotes' biomembranes via penetration into the biomembranes' interior. Bicontinuous microemulsions, consisting of interdispersed oil and water nanodomains separated by flexible surfactant monolayers, are potentially valuable for hosting membrane-associated peptides and proteins due to their thermodynamic stability, optical transparency, low viscosity, and high interfacial area. Here, we show that bicontinuous microemulsions formed by negatively-charged surfactants are a robust biomembrane mimetic system for the antimicrobial peptide melittin. When encapsulated in bicontinuous microemulsions formed using three-phase (Winsor-III) systems, melittin's helicity increases greatly due to penetration into the surfactant monolayers, mimicking its behavior inmore » biomembranes. But, the threshold melittin concentration required to achieve these trends is lower for the microemulsions. The extent of penetration was decreased when the interfacial fluidity of the microemulsions was increased. In conclusion, these results suggest the utility of bicontinuous microemulsions for isolation, purification, delivery, and host systems for antimicrobial peptides.« less

Behavior of microemulsion systems of virgin coconut oil (VCO) using igepal CO-520 and tween 80 surfactant

NASA Astrophysics Data System (ADS)

Safuan, A.; Hamdan, S.; Laili, C. R.

2017-09-01

Virgin Coconut Oil (VCO) has been applied in many application and products. Formation of microemulsion region with surfactant was investigated by using phase diagram. The surfactants used are igepal CO-520 and tween 80. The studies showed that formation of microemulsion region were dependent on the behaviour of the surfactant toward VCO. The result showed that microemulsion regions were present in igepal CO-520 system formed a larger water-in-oil microemulsion region compared to tween 80 system. Certain weight ratios of VCO to surfactants were studied by using evaporation test in order to study the water loss of the microemulsion in ambient condition. The evaporation rate of samples was varies depending their compositon of VCO, surfactant and water.

A comprehensive strategy in the development of a cyclodextrin-modified microemulsion electrokinetic chromatographic method for the assay of diclofenac and its impurities: Mixture-process variable experiments and quality by design.

PubMed

Orlandini, S; Pasquini, B; Caprini, C; Del Bubba, M; Squarcialupi, L; Colotta, V; Furlanetto, S

2016-09-30

A comprehensive strategy involving the use of mixture-process variable (MPV) approach and Quality by Design principles has been applied in the development of a capillary electrophoresis method for the simultaneous determination of the anti-inflammatory drug diclofenac and its five related substances. The selected operative mode consisted in microemulsion electrokinetic chromatography with the addition of methyl-β-cyclodextrin. The critical process parameters included both the mixture components (MCs) of the microemulsion and the process variables (PVs). The MPV approach allowed the simultaneous investigation of the effects of MCs and PVs on the critical resolution between diclofenac and its 2-deschloro-2-bromo analogue and on analysis time. MPV experiments were used both in the screening phase and in the Response Surface Methodology, making it possible to draw MCs and PVs contour plots and to find important interactions between MCs and PVs. Robustness testing was carried out by MPV experiments and validation was performed following International Conference on Harmonisation guidelines. The method was applied to a real sample of diclofenac gastro-resistant tablets. Copyright © 2016 Elsevier B.V. All rights reserved.

Theory of microemulsions in a gravitational field

NASA Technical Reports Server (NTRS)

Jeng, J. F.; Miller, Clarence A.

1989-01-01

A theory of microemulsions developed previously is extended to include the effect of a gravitational field. It predicts variation with position of drop size, drop volume fraction, and area per molecule in the surfactant films within a microemulsion phase. Variation in volume fraction is greatest and occurs in such a way that oil content increases with increasing elevation, as has been found experimentally. Large composition variations are predicted within a middle phase microemulsion near optimal conditions because inversion from the water-continuous to the oil-continuous arrangement occurs with increasing elevation. Generally speaking, gravity reduces solubilization within microemulsions and promotes separation of excess phases.

Development and characterization of morin hydrate loaded microemulsion for the management of Alzheimer's disease.

PubMed

Sharma, Dheeraj; Singh, Manpreet; Kumar, Punnet; Vikram, Vir; Mishra, Neeraj

2017-12-01

The aim of this study is to prepare and characterize intranasal delivery of morin hydrate loaded microemulsion for the management of Alzheimer's diseases. After intranasal delivery, brain and blood drug concentrations were found to be higher for optimized morin hydrate loaded microemulsion as compared to plain morin hydrate. Significant (P < 0.05) reduction in assessed pharmacodynamic parameters was observed after intranasal administration of morin hydrate loaded microemulsion as compared to sham control group. Daily chronic treatment with morin loaded microemulsion till the 21st day significantly increased the memory in wistar rats with STZ-induced dementia.

Ionic liquid-in-oil microemulsions composed of double chain surface active ionic liquid as a surfactant: temperature dependent solvent and rotational relaxation dynamics of coumarin-153 in [Py][TF2N]/[C4mim][AOT]/benzene microemulsions.

PubMed

Rao, Vishal Govind; Mandal, Sarthak; Ghosh, Surajit; Banerjee, Chiranjib; Sarkar, Nilmoni

2012-07-19

In the recent past, nonaqueous microemulsions containing ionic liquids (ILs) have been utilized for performing chemical reactions, preparation of nanomaterials, and synthesis of nanostructured polymers and in drug delivery systems. The most promising fact about IL-in-oil microemulsions is their high thermal stability compared to that of aqueous microemulsions. In our earlier publication (Rao, V. G.; Ghosh, S.; Ghatak, C.; Mandal, S.; Brahmachari, U.; Sarkar, N. J. Phys. Chem. B 2012, 116, 2850-2855), we presented for the first time the possibility of creating huge number of IL-in-oil microemulsions, just by replacing the inorganic cation, Na(+), of NaAOT by any organic cation and using different ionic liquids as the polar core. In this manuscript we are interested in exploring the effect of temperature on such systems. We have characterized the phase diagram of the [Py][TF2N]/[C4mim][AOT]/benzene ternary system at 298 K. We have shown that in the experimental temperature range employed in this study, the microemulsions remain stable and a slight decrease in the size of the microemulsions is observed with increasing temperature. We have reported the detailed study of solvent and rotational relaxation of coumarin 153 (C-153) in neat IL, N-methyl-N-propylpyrrolidinium bis((trifluoromethyl)sulfonyl)imide ([Py][TF2N]), and in [Py][TF2N]/[C4mim][AOT]/benzene microemulsions using steady state and picosecond time-resolved spectroscopy. We have monitored the effect of (i) varying the [Py][TF2N]/[C4mim][AOT] molar ratio (R value) and (ii) temperature on solvent and rotational relaxation of C-153. The features observed in absorption and emission spectra clearly indicate that (i) the probe molecules reside at the polar interfacial region of the [Py][TF2N]/[C4mim][AOT]/benzene microemulsions and (ii) with increasing R value the probe molecules move toward the polar IL-pool of the microemulsion. We have shown that the increase in solvation time on going from neat [Py][TF2N] to [Py][TF2N]-containing microemulsions is very small compared to the increase in solvation time on going from pure water to water-containing microemulsions. The average solvation time decreases with increasing R values at 298 K, but it shows only a small R dependence compared to microemulsions containing solvents capable of forming hydrogen bonds. We have also shown that the temperature has substantial effect on the solvent and rotational relaxation of C-153 in neat [Py][TF2N] compared to that of [Py][TF2N]/[C4mim][AOT]/benzene microemulsions at R = 0.69.

Effect of molecular structure of tartrates on chiral recognition of tartrate-boric acid complex chiral selectors in chiral microemulsion electrokinetic chromatography.

PubMed

Hu, Shao-Qiang; Chen, Yong-Lei; Zhu, Hua-Dong; Shi, Hai-Jun; Yan, Na; Chen, Xing-Guo

2010-08-20

Eight l-tartrates and a d-tartrate with different alcohol moieties were used as chiral oils to prepare chiral microemulsions, which were utilized in conjunction with borate buffer to separate the enantiomers of beta-blockers or structurally related compounds by the chiral microemulsion electrokinetic chromatography (MEEKC) method. Among them, six were found to have a relatively good chiral separation performance and their chiral recognition effect in terms of both enantioselectivity and resolution increases linearly with the number of carbon atoms in the alkyl group of alcohol moiety. The tartrates containing alkyl groups of different structures but the same number of carbon atoms, i.e. one of straight chain and one of branched chain, provide similar enantioseparations. The trend was elucidated according to the changes in the difference of the steric matching between the molecules of two enantiomers and chiral selector. Furthermore, it was demonstrated for the first time that a water insoluble solid compound, di-i-butyl l-tartrate (mp. 73.5 degrees C), can be used as an oil to prepare a stable microemulsion to be used in the chiral MEEKC successfully. And a critical effect of the microemulsion for chiral separation, which has never been reported before, was found in this experiment, namely providing a hydrophobic environment to strengthen the interactions between the chiral selector and enantiomers. Copyright 2010 Elsevier B.V. All rights reserved.

Bioprobes Based on Aptamer and Silica Fluorescent Nanoparticles for Bacteria Salmonella typhimurium Detection

NASA Astrophysics Data System (ADS)

Wang, Qiu-Yue; Kang, Yan-Jun

2016-03-01

In this study, we have developed an efficient method based on single-stranded DNA (ssDNA) aptamers along with silica fluorescence nanoparticles for bacteria Salmonella typhimurium detection. Carboxyl-modified Tris(2,2'-bipyridyl)dichlororuthenium(II) hexahydrate (RuBPY)-doped silica nanoparticles (COOH-FSiNPs) were prepared using reverse microemulsion method, and the streptavidin was conjugated to the surface of the prepared COOH-FSiNPs. The bacteria S. typhimurium was incubated with a specific ssDNA biotin-labeled aptamer, and then the aptamer-bacteria conjugates were treated with the synthetic streptavidin-conjugated silica fluorescence nanoprobes (SA-FSiNPs). The results under fluorescence microscopy show that SA-FSiNPs can be applied effectively for the labeling of bacteria S. typhimurium with great photostable property. To further verify the specificity of SA-FSiNPs out of multiple bacterial conditions, variant concentrations of bacteria mixtures composed of bacteria S. typhimurium, Escherichia coli, and Bacillus subtilis were treated with SA-FSiNPs.

In vitro and in vivo evaluation of a water-in-oil microemulsion system for enhanced peptide intestinal delivery.

PubMed

Liu, Dongyun; Kobayashi, Taku; Russo, Steven; Li, Fengling; Plevy, Scott E; Gambling, Todd M; Carson, Johnny L; Mumper, Russell J

2013-01-01

Peptide and protein drugs have become the new generation of therapeutics, yet most of them are only available as injections, and reports on oral local intestinal delivery of peptides and proteins are quite limited. The aim of this work was to develop and evaluate a water-in-oil (w/o) microemulsion system in vitro and in vivo for local intestinal delivery of water-soluble peptides after oral administration. A fluorescent labeled peptide, 5-(and-6)-carboxytetramethylrhodamine labeled HIV transactivator protein TAT (TAMRA-TAT), was used as a model peptide. Water-in-oil microemulsions consisting of Miglyol 812, Capmul MCM, Tween 80, and water were developed and characterized in terms of appearance, viscosity, conductivity, morphology, and particle size analysis. TAMRA-TAT was loaded and its enzymatic stability was assessed in modified simulated intestinal fluid (MSIF) in vitro. In in vivo studies, TAMRA-TAT intestinal distribution was evaluated using fluorescence microscopy after TAMRA-TAT microemulsion, TAMRA-TAT solution, and placebo microemulsion were orally gavaged to mice. The half-life of TAMRA-TAT in microemulsion was enhanced nearly three-fold compared to that in the water solution when challenged by MSIF. The treatment with TAMRA-TAT microemulsion after oral administration resulted in greater fluorescence intensity in all intestine sections (duodenum, jejunum, ileum, and colon) compared to TAMRA-TAT solution or placebo microemulsion. The in vitro and in vivo studies together suggested TAMRA-TAT was better protected in the w/o microemulsion in an enzyme-containing environment, suggesting that the w/o microemulsions developed in this study may serve as a potential delivery vehicle for local intestinal delivery of peptides or proteins after oral administration.

Preparation and characterization of cyanocobalamin (vit B12) microemulsion properties and structure for topical and transdermal application.

PubMed

Salimi, Anayatollah; Sharif Makhmal Zadeh, Behzad; Moghimipour, Eskandar

2013-07-01

The objective of this study was to design a topical microemulsion of Vit B12 and to study the correlation between internal structure and physicochemical properties of the microemulsions. Microemulsions are thermodynamically stable mixtures of water, oil, surfactants and usually cosurfactants with several advantages for topical and transdermal drug delivery. The formulation of microemulsions for pharmaceutical use requires a clear understanding of the properties and microstructures of the microemulsions. In this study, phase behavior and microstructure of traditional and novel microemulsions of Vit B12 have been investigated by Small-angle X-ray (SAXS), differential scanning calorimetery (DSC) and measuring density, particle size, conductivity and surface tension. WO and bicontinuous microemulsion with different microstructures were found in novel and traditional formulations. In this study, amount of water, surfactant concentration, oil/ surfactant ratio and physicochemical properties of cosurfactants influenced the microstructures. In both formulations, water behavior was affected by the concentration of the surfactant. Water Solubilization capacity and enthalpy of exothermic peak of interfacial and free water of traditional formulations were more than novel ones. This means that the affinity of water to interfacial film is dependent on the surfactant properties.   This study showed that both microemulsions provided good solubility of Vit B12 with a wide range of internal structure. Low water solubilization capacity is a common property of microemulsions that can affect drug release and permeability through the skin.  Based on Vit B12 properties, specially, intermediate oil and water solubility, better drug partitioning into the skin may be obtained by traditional formulations with wide range of structure and high amount of free and bounded water.    

Enhancement of transdermal delivery of ibuprofen using microemulsion vehicle.

PubMed

Hu, Liandong; Hu, Qiaofeng; Yang, Jianxue

2014-10-01

The objective of this study was to find a stable microemulsion vehicle for transdermal delivery of ibuprofen to improve the skin permeability. Microemulsion was prepared using different sorts of oils, surfactants and co-surfactants. Pseudo-ternary phase diagrams were used to evaluate the microemulsion domain. The effects of oleic acid and surfactant mixture on skin permeation of ibuprofen were evaluated with excised skins. The optimum formulation F3 consisting of 6% oleic acid, 30% Cremophor RH40/Transcutol P (2:1, w/w) and 59% water phase, showed a high permeation rate of 42.98 µg/cm(2)/hr. The mean droplet size of microemulsion was about 43 nm and no skin irritation signs were observed on the skin of rabbits. These results indicated that this novel microemulsion is a useful formulation for the transdermal delivery of ibuprofen.

Development of w/o microemulsion for transdermal delivery of iodide ions.

PubMed

Lou, Hao; Qiu, Ni; Crill, Catherine; Helms, Richard; Almoazen, Hassan

2013-03-01

The objective of this study was to develop a water-in-oil (w/o) microemulsion which can be utilized as a transdermal delivery for iodide ions. Several w/o microemulsion formulations were prepared utilizing Span 20, ethanol, Capryol 90®, and water. The selected formulations had 5%, 10%, 15%, 20%, and a maximum of 23% w/w water content. Potassium iodide (KI) was incorporated in all formulations at 5% w/v. Physicochemical characterizations were conducted to evaluate the structure and stability. These studies included: mean droplet size, pH, viscosity, conductivity, and chemical stability tests. In vitro human skin permeation studies were conducted to evaluate the diffusion of the iodide ion through human skin. The w/o microemulsion formulations were stable and compatible with iodide ions with water content ranging from 5% to 23% w/w. The addition of KI influenced the physicochemical properties of microemulsion as compared to blank microemulsion formulations. In vitro human skin permeation studies indicated that selected formulations improved iodide ion diffusion significantly as compared to control (KI solution; P value<0.05). Iodide ions were entrapped within the aqueous core of w/o microemulsion. Span 20, ethanol and Capryol 90 protected the iodide ions against oxidation and formed a stable microemulsion. It is worth to note that according to Hofmeister series, iodide ions tend to lower the interfacial tension between water and oil and consequently enhance overall stability. This work illustrates that microemulsion system can be utilized as a vehicle for the transdermal administration of iodide.

Novel microemulsion-based gels for topical delivery of indomethacin: Formulation, physicochemical properties and in vitro drug release studies.

PubMed

Froelich, Anna; Osmałek, Tomasz; Snela, Agnieszka; Kunstman, Paweł; Jadach, Barbara; Olejniczak, Marta; Roszak, Grzegorz; Białas, Wojciech

2017-12-01

Microemulsion-based semisolid systems may be considered as an interesting alternative to the traditional dosage forms applied in topical drug delivery. Mechanical properties of topical products are important both in terms of application and dosage form effectiveness. In this study we designed and evaluated novel microemulsion-based gels with indomethacin and analyzed the factors affecting their mechanical characteristics and drug release. The impact of the microemulsion composition on the extent of isotropic region was investigated with the use of pseudoternary phase diagrams. Selected microemulsions were analyzed in terms of electrical conductivity and surface tension in order to determine the microemulsion type. Microemulsions were transformed into polymer-based gels and subjected to rheological and textural studies. Finally, the indomethacin release from the analyzed gels was studied and compared to commercially available product. The extent of isotropic domain in pseudoternary phase diagrams seems to be dependent on the polarity of the oil phase. The surface tension and conductivity monitored as a function of water content in microemulsion systems revealed possible structural transformations from w/o through bicontinuous systems into o/w. The mechanical properties of semisolid microemulsion-based systems depended on the composition of surface active agents and the drug presence. The drug release profiles observed in the case of the investigated gels differed from those recorded for the commercially available product which was most probably caused by the different structure of both systems. Copyright © 2017 Elsevier Inc. All rights reserved.

A facile construction strategy of stable lipid nanoparticles for drug delivery using a hydrogel-thickened microemulsion system

NASA Astrophysics Data System (ADS)

Chen, Huabing; Xiao, Ling; Du, Danrong; Mou, Dongsheng; Xu, Huibi; Yang, Xiangliang

2010-01-01

We report a novel facile method for preparing stable nanoparticles with inner spherical solid spheres and an outer hydrogel matrix using a hot O/W hydrogel-thickened microemulsion with spontaneous stability. The nanoparticles with average diameters of about 30.0 nm and 100.0 nm were constructed by cooling the hot hydrogel-thickened microemulsion at different temperatures, respectively. We explained the application of these nanoparticles by actualizing the cutaneous delivery of drug-loaded nanoparticles. The in vitro skin permeation studies showed that the nanoparticles could significantly reduce the penetration of model drugs through skin and resulted in their dermal uptakes in skin. The sol-gel process of TEOS was furthermore used in the template of HTM to regulate the particle size of nanoparticles. The coating of silica on the surface of nanoparticles could regulate the penetration of drug into skin from dermal delivery to transdermal delivery. This strategy provides a facile method to produce nanoparticles with long-term stability and ease of manufacture, which might have a promising application in drug delivery.

Decontamination of materials contaminated with Francisella philomiragia or MS2 bacteriophage using PES-Solid, a solid source of peracetic acid.

PubMed

Buhr, T L; Young, A A; Johnson, C A; Minter, Z A; Wells, C M

2014-08-01

The aim of the study was to develop test methods and evaluate survival of Francisella philomiragia cells and MS2 bacteriophage after exposure to PES-Solid (a solid source of peracetic acid) formulations with or without surfactants. Francisella philomiragia cells (≥7·6 log10 CFU) or MS2 bacteriophage (≥6·8 log10 PFU) were deposited on seven different test materials and treated with three different PES-Solid formulations, three different preneutralized samples and filter controls at room temperature for 15 min. There were 0-1·3 log10 CFU (<20 cells) of cell survival, or 0-1·7 log10 (<51 PFU) of bacteriophage survival in all 21 test combinations (organism, formulation and substrate) containing reactive PES-Solid. In addition, the microemulsion (Dahlgren Surfactant System) showed ≤2 log10 (100 cells) of viable F. philomiragia cells, indicating the microemulsion achieved <2 log10 CFU on its own. Three PES-Solid formulations and one microemulsion system (DSS) inactivated F. philomiragia cells and/or MS2 bacteriophage that were deposited on seven different materials. A test method was developed to show that reactive PES-Solid formulations and a microemulsion system (DSS) inactivated >6 log10 CFU/PFU F. philomiragia cells and/or MS2 bacteriophage on different materials. Published 2014. This article is a U.S. Government work and is in the public domain in the USA.

Lecithin-based microemulsion of a peptide for oral administration: preparation, characterization, and physical stability of the formulation.

PubMed

Cilek, Ayşe; Celebi, Nevin; Tirnaksiz, Figen

2006-01-01

The objective of our study was to prepare and characterize a stable microemulsion formulation for oral administration of a peptide, e.g., rh-insulin. The microemulsions were prepared using Labrafil M 1944 CS, Phospholipon 90G (lecithin), absolute alcohol, and bidistilled water. Commercially available soybean lecithins (namely, Phospholipon 80, phosphatidylcholine purity 76 +/- 3%, and Phospholipon 90G, phosphatidylcholine purity 93 +/- 3%) were used in the study. The results showed that the phase diagram obtained using a low purity lecithin was not similar to that obtained with a high purity lecithin. We observed that the microemulsion area was wider at the phase diagram obtained with the higher purity lecithin. We found that the extent of the microemulsion region depended upon both the purity of the lecithin and the surfactant/co-surfactant (s/co-s) mixing ratios (K(m)). The rheological studies showed that microemulsions followed a Newtonian behavior. Such physical characteristics as viscosity, turbidity, density, conductivity, refractive index, droplet size, physical appearance, and phase separation of the microemulsion were measured at different temperatures (4 degrees C, 25 degrees C, and 40 degrees C) during 6 months. The results indicated that the physical characteristics of the developed microemulsions did not change under different storage temperatures (p > 0.05).

Evaluation of nicotinamide microemulsion on the skin penetration enhancement.

PubMed

Boonme, Prapaporn; Boonthongchuay, Chalida; Wongpoowarak, Wibul; Amnuaikit, Thanaporn

2016-01-01

This study purposed to evaluate a microemulsion containing nicotinamide for its characteristics, stability, and skin penetration and retention comparing with a solution of nicotinamide in 2:1 mixture of water and isopropyl alcohol (IPA). The microemulsion system was composed of 1:1 mixture of Span80 and Tween80 as a surfactant mixture, isopropyl palmitate (IPP) as an oil phase, and 2:1 mixture of water and IPA as an aqueous phase. Nicotinamide microemulsion was prepared by dissolving the active in the aqueous phase before simply mixing with the other components. It was determined for its characteristics and stability under various conditions. The skin penetration and retention studies of nicotinamide microemulsion and solution were performed by modified Franz diffusion cells, using newborn pig skin as the membrane. The results showed that nicotinamide microemulsion could be obtained as clear yellowish liquid, was water-in-oil (w/o) type, possessed Newtonian flow, and exhibited physicochemical stability when kept at 4 °C and room temperature (≈30 ± 2 °C) during 3 months. From the skin penetration data, the microemulsion could enhance the skin penetration of nicotinamide comparing with the solution. Additionally, nicotinamide microemulsion could provide much higher amount of skin retention than that of skin penetration, resulting in suitability for a cosmeceutical product.

Design of microemulsion system suitable for the oral delivery of poorly aqueous soluble beta-carotene.

PubMed

Peng, Cheng; Svirskis, Darren; Lee, Sung Je; Oey, Indrawati; Kwak, Hae-Soo; Chen, Guanyu; Bunt, Craig; Wen, Jingyuan

2017-02-14

Beta-carotene is a potent antioxidant for maintaining human health. However, its oral absorption is low due to poor aqueous solubility of less than 1 μg/ml. A microemulsion delivery system was designed to solubilize beta-carotene toward enhancing its oral bioavailability. From seven pseudoternary diagrams constructed, three systems were selected with large microemulsion areas suitable for oral administration and dilution in the predominately aqueous gastrointestinal fluids. Conductivity and rheology characterization were conducted along four dilution lines within the selected systems. Three pseudoternary-phase diagrams were selected with large microemulsion regions, >60% of the total phase diagram area, which provide microemulsions with higher drug-loading capacity. A phenomenon was observed by which both propylene glycol and Capmul MCM EP stabilize the microstructure of the microemulsions has been proposed based on the characterization studies. An optimal bicontinuous microemulsion formulation was selected comprising 12% orange oil, 24% Capmul MCM, 18% Tween 20, 6% Labrasol, 20% propylene glycol and 20% water, with a high beta-carotene loading capacity of 140.8 μg/ml and droplet size of 117.4 nm. In conclusion, the developed novel microemulsion formulation allows solubilizing beta-carotene and is a promising basis for further development as a functional beverage.

Application of electrochemical impedance spectroscopy: A phase behavior study of babassu biodiesel-based microemulsions.

PubMed

Pereira, Thulio C; Conceição, Carlos A F; Khan, Alamgir; Fernandes, Raquel M T; Ferreira, Maira S; Marques, Edmar P; Marques, Aldaléa L B

2016-11-05

Microemulsions are thermodynamically stable systems of two immiscible liquids, one aqueous and the other of organic nature, with a surfactant and/or co-surfactant adsorbed in the interface between the two phases. Biodiesel-based microemulsions, consisting of alkyl esters of fatty acids, open a new means of analysis for the application of electroanalytical techniques, and is advantageous as it eliminates the required pre-treatment of a sample. In this work, the phase behaviours of biodiesel-based microemulsions were investigated through the electrochemical impedance spectroscopy (EIS) technique. We observed thatan increase in the amount of biodiesel in the microemulsion formulation increases the resistance to charge transfer at the interface. Also, the electrical conductivity measurements revealed that a decrease or increase in electrical properties depends on the amount of biodiesel. EIS studies of the biodiesel-based microemulsion samples showed the presence of two capacitive arcs: one high-frequency and the other low-frequency. Thus, the formulation of microemulsions plays an important role in estimating the electrical properties through the electrochemical impedance spectroscopy technique. Copyright © 2016 Elsevier B.V. All rights reserved.

Enhanced UV protection of ketoconazole using Hyptis suaveolens micro emulsion.

PubMed

Khonkarn, Ruttiros; Kittipongpatana, Ornanong S; Boasouna, Vilai; Okonogi, Siriporn

2018-05-01

Ketoconazole is photolabile antifungal drug. Photochemical reactions may decrease its therapeutic effect or induce toxic compounds. The aim of this study was to prepare ketoconazole loaded microemulsion containing H. suaveolens oil with antifungal and antioxidant powers in order to obtain effective antifungal formulation. The release study, antifungal activity and photostability test, were then evaluated. The results showed that optimized Hyptis suaveolens microemulsion for ketoconazole loading was selected through construction of pseudo-ternary phase diagrams. It consisted of 12.5% H. suaveolens oil, 12.5% capryol, 25% tween 80, 25% ethanol and 25% water. Mean globule size was 153 nm, as analyzed by photon correlation spectroscopy. Ketoconazole-loaded Hyptis suaveolens microemulsion and Hyptis suaveolens microemulsion had antifungal activity against Candida albican, Microsporum gypseum and Trichophyton mentagrophyte, showing inhibition zone ranged from 28-37 mm and 23-32 mm, respectively. Ketoconazole was released from Hyptis suaveolens microemulsion more than 90% within 5 days. In the results of photostability test, ketoconazole-loaded Hyptis suaveolens microemulsion gave significantly higher remaining ketoconazole than ketoconazole solution. This study demonstrated that Hyptis suaveolens microemulsion could be used to improve the photoprotection of photolabile drug.

Application of electrochemical impedance spectroscopy: A phase behavior study of babassu biodiesel-based microemulsions

NASA Astrophysics Data System (ADS)

Pereira, Thulio C.; Conceição, Carlos A. F.; Khan, Alamgir; Fernandes, Raquel M. T.; Ferreira, Maira S.; Marques, Edmar P.; Marques, Aldaléa L. B.

2016-11-01

Microemulsions are thermodynamically stable systems of two immiscible liquids, one aqueous and the other of organic nature, with a surfactant and/or co-surfactant adsorbed in the interface between the two phases. Biodiesel-based microemulsions, consisting of alkyl esters of fatty acids, open a new means of analysis for the application of electroanalytical techniques, and is advantageous as it eliminates the required pre-treatment of a sample. In this work, the phase behaviours of biodiesel-based microemulsions were investigated through the electrochemical impedance spectroscopy (EIS) technique. We observed thatan increase in the amount of biodiesel in the microemulsion formulation increases the resistance to charge transfer at the interface. Also, the electrical conductivity measurements revealed that a decrease or increase in electrical properties depends on the amount of biodiesel. EIS studies of the biodiesel-based microemulsion samples showed the presence of two capacitive arcs: one high-frequency and the other low-frequency. Thus, the formulation of microemulsions plays an important role in estimating the electrical properties through the electrochemical impedance spectroscopy technique.

Encapsulation artocarpanone and ascorbic acid in O/W microemulsions: Preparation, characterization, and antibrowning effects in apple juice.

PubMed

Dong, Xue; Zhu, Qin; Dai, Yaqing; He, Jianfei; Pan, Hongyang; Chen, Jie; Zheng, Zong-Ping

2016-02-01

The aim of this study is to improve artocarpanone solubility by developing an O/W microemulsion with the evaluation of its antibrowning effects. The chemical and physical stabilities as well as antibrowning effects in apple juice were also evaluated. The formulation of artocarpanone microemulsion consisted of 4% w/w of ethyl butyrate, 10.67% w/w of Tween 80, 5.33% w/w of polyethylene glycol 400, and 80% w/w of water, with a maximum solubility of artocarpanone up to 10.54 ± 0.01 mg/mL, at least 3000-folds increase in solubility compared that in water. Encapsulating artocarpanone and ascorbic acid (VC) into microemulsion simultaneously decreased modest artocarpanone solubility whereas improving its stability in long-term storage. Blank, artocarpanone and artocarpanone-Vc-loaded microemulsions demonstrated steadily during accelerated and long-term storage. Artocarpanone-Vc-loaded microemulsion showed strong antibrowning effects in apple juice at room temperature in 24h, suggesting that artocarpanone-Vc-loaded microemulsion is a good antibrowning agent for apple juices. Copyright © 2015 Elsevier Ltd. All rights reserved.

Superswollen microemulsions stabilized by shear and trapped by a temperature quench.

PubMed

Roger, Kevin; Olsson, Ulf; Zackrisson-Oskolkova, Malin; Lindner, Peter; Cabane, Bernard

2011-09-06

We studied the solubilization of oil in the C(16)E(8)/hexadecane/H(2)O system. Close to the phase inversion temperature (PIT), the system, at equilibrium, can form either homogeneous states (i.e., microemulsions) at high surfactant concentrations or three-phase states at lower concentrations. We show that, under gentle shear, at a line we named the clearing boundary (CB), located a few degrees below the PIT, the system is homogeneous regardless of the surfactant concentration. We relate this shift of the microemulsion boundary to shear-induced disruption of the asymmetric bicontinuous structure. Although this state quickly relaxes to equilibrium when shear is stopped, we show that it is still possible to trap it into a metastable state through a temperature quench. This method is the sub-PIT emulsification that we described in a previous work (Roger Langmuir 2010, 26, 3860-3867). © 2011 American Chemical Society

A new dispersive liquid-liquid microextraction using ionic liquid based microemulsion coupled with cloud point extraction for determination of copper in serum and water samples.

PubMed

Arain, Salma Aslam; Kazi, Tasneem Gul; Afridi, Hassan Imran; Arain, Mariam Shahzadi; Panhwar, Abdul Haleem; Khan, Naeemullah; Baig, Jameel Ahmed; Shah, Faheem

2016-04-01

A simple and rapid dispersive liquid-liquid microextraction procedure based on ionic liquid assisted microemulsion (IL-µE-DLLME) combined with cloud point extraction has been developed for preconcentration copper (Cu(2+)) in drinking water and serum samples of adolescent female hepatitits C (HCV) patients. In this method a ternary system was developed to form microemulsion (µE) by phase inversion method (PIM), using ionic liquid, 1-butyl-3-methylimidazolium hexafluorophosphate ([C4mim][PF6]) and nonionic surfactant, TX-100 (as a stabilizer in aqueous media). The Ionic liquid microemulsion (IL-µE) was evaluated through visual assessment, optical light microscope and spectrophotometrically. The Cu(2+) in real water and aqueous acid digested serum samples were complexed with 8-hydroxyquinoline (oxine) and extracted into IL-µE medium. The phase separation of stable IL-µE was carried out by the micellar cloud point extraction approach. The influence of of different parameters such as pH, oxine concentration, centrifugation time and rate were investigated. At optimized experimental conditions, the limit of detection and enhancement factor were found to be 0.132 µg/L and 70 respectively, with relative standard deviation <5%. In order to validate the developed method, certified reference materials (SLRS-4 Riverine water) and human serum (Sero-M10181) were analyzed. The resulting data indicated a non-significant difference in obtained and certified values of Cu(2+). The developed procedure was successfully applied for the preconcentration and determination of trace levels of Cu(2+) in environmental and biological samples. Copyright © 2015 Elsevier Inc. All rights reserved.

Ultra-small and anionic starch nanospheres: formation and vitro thrombolytic behavior study.

PubMed

Huang, Yinjuan; Ding, Shenglong; Liu, Mingzhu; Gao, Chunmei; Yang, Jinlong; Zhang, Xinjie; Ding, Bin

2013-07-25

This paper is considered as the first report on the investigation of nattokinase (NK) release from anionic starch nanospheres. The ultra-small and anionic starch nanospheres were prepared by the method of reverse micro-emulsion crosslinking in this work. Starch nanospheres were characterized through Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), transmission electron microscopy (TEM) and dynamic light scattering (DLS). Effects of preparation conditions on particle size were studied. The cytotoxicity, biodegradable and vitro thrombolytic behaviors of nattokinase (NK) loaded anionic starch nanospheres were also studied. The results showed that the anionic starch nanospheres are non-toxic, biocompatible and biodegradable. Moreover, the anionic starch nanospheres can protect NK from fast biodegradation hence prolongs the circulation in vivo and can reduce the risk of acute hemorrhage complication by decreasing the thrombolysis rate. Copyright © 2013 Elsevier Ltd. All rights reserved.

Augmented bioavailability of felodipine through an α-linolenic acid-based microemulsion.

PubMed

Singh, Mahendra; Kanoujia, Jovita; Parashar, Poonam; Arya, Malti; Tripathi, Chandra B; Sinha, V R; Saraf, Shailendra K; Saraf, Shubhini A

2018-02-01

The oral bioavailability of felodipine, a dihydropyridine calcium channel antagonist, is about 15%. This may be due to poor water solubility, and a lower intestinal permeability than a BCS class I drug, and hepatic first-pass metabolism of the drug. Many drugs are unpopular due to solubility issues. The goal of this study was to develop and optimize a felodipine-containing microemulsion to improve the intestinal permeability and bioavailability of the drug. The felodipine microemulsions were developed with the selected components, i.e., α-linolenic acid as the oil phase, Tween 80 as a surfactant, and isopropyl alcohol as co-surfactant using Box-Behnken design and characterized for in vitro release and particle size. The optimized felodipine-loaded microemulsion was investigated for physicochemical interaction, surface morphology, intestinal permeability, rheology, cytotoxicity, cellular uptake, pharmacodynamic (electrocardiogram and heart rate variability), and pharmacokinetic studies to explore its suitability as a promising oral drug delivery system for the treatment of hypertension. The optimized felodipine-loaded microemulsion showed significantly higher (P < 0.05) apparent permeability coefficients (Papp) at 7.918 × 10 -5  cm/s after 1 h, when compared with conventional formulations that are marketed tablet, drug oily solution, and drug emulsion, which showed a maximum Papp of 3.013, 4.428, and 5.335 × 10 -5  cm/s, respectively. The optimized felodipine-loaded microemulsion showed biocompatibility and no cytotoxicity. Cellular uptake studies confirmed payload delivery to a cellular site on the J774.A1 cell line. The rheology study of the optimized felodipine-loaded microemulsion revealed Newtonian-type flow behavior and discontinuous microemulsion formation. In pharmacodynamic studies, significant differences in parameters were observed between the optimized felodipine-loaded microemulsion and marketed formulation. The optimized felodipine-loaded microemulsion showed significantly higher (p < 0.01) C max (7.12 ± 1.04 μg/ml) than marketed tablets (2.44 ± 1.03 μg/ml). It was found that AUC last obtained from the optimized felodipine-loaded microemulsion (84.53 ± 10.73 μg h/ml) was significantly higher (p < 0.01) than the marketed tablet (27.41 ± 5.54 μg h/ml). The relative bioavailability (Fr) of the optimized felodipine-loaded microemulsion was about 308.3% higher than that of the marketed formulation. The results demonstrate that the prepared microemulsion is an advanced and efficient oral delivery system of felodipine for the management of hypertension.

KDP Aqueous Solution-in-Oil Microemulsion for Ultra-Precision Chemical-Mechanical Polishing of KDP Crystal

PubMed Central

Dong, Hui; Wang, Lili; Gao, Wei; Li, Xiaoyuan; Wang, Chao; Ji, Fang; Pan, Jinlong; Wang, Baorui

2017-01-01

A novel functional KH2PO4 (KDP) aqueous solution-in-oil (KDP aq/O) microemulsion system for KDP crystal ultra-precision chemical-mechanical polishing (CMP) was prepared. The system, which consisted of decanol, Triton X-100, and KH2PO4 aqueous solution, was available at room temperature. The functional KDP aq/O microemulsion system was systematically studied and applied as polishing solution to KDP CMP technology. In this study, a controlled deliquescent mechanism was proposed for KDP polishing with the KDP aq/O microemulsion. KDP aqueous solution, the chemical etchant in the polishing process, was caged into the micelles in the microemulsion, leading to a limitation of the reaction between the KDP crystal and KDP aqueous solution only if the microemulsion was deformed under the effect of the external force. Based on the interface reaction dynamics, KDP aqueous solutions with different concentrations (cKDP) were applied to replace water in the traditional water-in-oil (W/O) microemulsion. The practicability of the controlled deliquescent mechanism was proved by the decreasing material removal rate (MRR) with the increasing of the cKDP. As a result, the corrosion pits on the KDP surface were avoided to some degree. Moreover, the roughnesses of KDP with KDP aq/O microemulsion (cKDP was changed from 10 mM to 100 mM) as polishing solutions were smaller than that with the W/O microemulsion. The smallest surface root-mean-square roughness of 1.5 nm was obtained at a 30 mmol/L KDP aq solution, because of the most appropriate deliquescent rate and MRR. PMID:28772632

KDP Aqueous Solution-in-Oil Microemulsion for Ultra-Precision Chemical-Mechanical Polishing of KDP Crystal.

PubMed

Dong, Hui; Wang, Lili; Gao, Wei; Li, Xiaoyuan; Wang, Chao; Ji, Fang; Pan, Jinlong; Wang, Baorui

2017-03-09

A novel functional KH₂PO₄ (KDP) aqueous solution-in-oil (KDP aq/O) microemulsion system for KDP crystal ultra-precision chemical-mechanical polishing (CMP) was prepared. The system, which consisted of decanol, Triton X-100, and KH₂PO₄ aqueous solution, was available at room temperature. The functional KDP aq/O microemulsion system was systematically studied and applied as polishing solution to KDP CMP technology. In this study, a controlled deliquescent mechanism was proposed for KDP polishing with the KDP aq/O microemulsion. KDP aqueous solution, the chemical etchant in the polishing process, was caged into the micelles in the microemulsion, leading to a limitation of the reaction between the KDP crystal and KDP aqueous solution only if the microemulsion was deformed under the effect of the external force. Based on the interface reaction dynamics, KDP aqueous solutions with different concentrations ( c KDP ) were applied to replace water in the traditional water-in-oil (W/O) microemulsion. The practicability of the controlled deliquescent mechanism was proved by the decreasing material removal rate (MRR) with the increasing of the c KDP . As a result, the corrosion pits on the KDP surface were avoided to some degree. Moreover, the roughnesses of KDP with KDP aq/O microemulsion ( c KDP was changed from 10 mM to 100 mM) as polishing solutions were smaller than that with the W/O microemulsion. The smallest surface root-mean-square roughness of 1.5 nm was obtained at a 30 mmol/L KDP aq solution, because of the most appropriate deliquescent rate and MRR.

Improvement of lindane removal by Streptomyces sp. M7 by using stable microemulsions.

PubMed

Saez, Juliana Maria; Casillas García, Verena; Benimeli, Claudia Susana

2017-10-01

Lindane is an organochlorine pesticide which persists in the environment and can cause serious health problems due to its chlorinated and hydrophobic nature. Microemulsions are isotropic and macroscopically homogeneous systems with high solubilization capacity of hydrophilic and hydrophobic compounds. The aim of this study was to evaluate the removal of high concentrations of lindane by the actinobacterium Streptomyces sp. M7 in aqueous and soil systems in the presence of stable microemulsions. Three stable microemulsions were successfully formed with Tween 80, 1-pentanol and three vegetable oils. In most cases, an increase in the cosurfactant/surfactant ratio in the microemulsions favored the solubilization of lindane, while an increase in the oil/surfactant ratio negatively affected the stability of the system. The microemulsion prepared with soybean oil allowed the solubilization of 66% of lindane added to the aqueous medium and 4.5 times more than the surfactant solution at the same concentration. This microemulsion increased the bioavailability of lindane in the aqueous medium and hence enhanced its removal by Streptomyces sp. M7 almost two times respect to the achieved with the surfactant solution. In loam soil system, the addition of the microemulsion allowed an 87% of lindane removal by Streptomyces sp. M7, increasing almost 50% the removal respect to the obtained without the addition of surfactant agents, although it did not present significant difference respect to the obtained with the surfactant solution. This is the first report on enhanced lindane removal by actinobacteria by using direct microemulsions as bioremediation tools. Copyright © 2017 Elsevier Inc. All rights reserved.

Development of Microemulsion Based Nabumetone Transdermal Delivery For Treatment of Arthritis.

PubMed

Jagdale, Swati; Deore, Gokul; Chabukswar, Anuruddha

2018-02-26

Background Nabumetone is biopharmaceutics classification system (BCS) class II drug, widely used in the treatment of osteoarthritis and rheumatoid arthritis. The most frequently reported adverse reactions for the drug involve disturbance in gastrointestinal tract , diarrhea, dyspepsia and abdominal pain. Microemulgel has advantages of microemulsion for improving solubility for hydrophobic drug. Patent literature had shown that the work for drug has been carried on spray chilling, enteric coated tablet, and topical formulation which gave idea for present research work for development of transdermal delivery. Objective Objective of the present research work was to optimize transdermal microemulgel delivery for Nabumetone for treatment of arthritis. Method Oil, surfactant and co-surfactant were selected based on solubility study for the drug. Gelling agents used were Carbopol 934 and HPMC K100M. Optimization was carried out using 32 factorial design. Characterization and evaluation were carried out for microemulsion and microemulsion based gel. Results Field emission-scanning electron microscopy (FE-SEM) study of the microemulsion revealed globules of 50-200 nm size . Zeta potential -9.50 mV indicated good stability of microemulsion. Globule size measured by dynamic light scattering (zetasizer) was 160 nm. Design expert gave optimized batch as F7 which contain 0.2% w/w drug, 4.3% w/w liquid paraffin, 0.71% w/w tween 80, 0.35% w/w propylene glycol, 0.124% w/w Carbopol 934, 0.187% w/w HPMC K100M and 11.68% w/w water. In-vitro diffusion study for F7 batch showed 99.16±2.10 % drug release through egg membrane and 99.15±2.73% drug release in ex-vivo study. Conclusion Nabumetone microemulgel exhibiting good in-vitro and ex-vivo controlled drug release was optimized. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Properties of surfactant films in water-in-CO2 microemulsions obtained by small-angle neutron scattering.

PubMed

Yan, Ci; Sagisaka, Masanobu; James, Craig; Rogers, Sarah; Alexander, Shirin; Eastoe, Julian

2014-12-01

The formation, stability and structural properties of normal liquid phase microemulsions, stabilized by hydrocarbon surfactants, comprising water and hydrocarbon oils can be interpreted in terms of the film bending rigidity (energy) model. Here, this model is tested for unusual water-in-CO2 (w/c) microemulsions, formed at high pressure with supercritical CO2 (sc-CO2) as a solvent and fluorinated surfactants as stabilizers. Hence, it is possible to explore the generality of this model for other types of microemulsions. High Pressure Small-Angle Neutron Scattering (HP-SANS) has been used to study w/c microemulsions, using contrast variation to highlight scattering from the stabilizing fluorinated surfactant films: these data show clear evidence for spherical core-shell structures for the microemulsion droplets. The results extend understanding of w/c microemulsions since previous SANS studies are based only on scattering from water core droplets. Here, detailed structural parameters for the surfactant films, such as thickness and film bending energy, have been extracted from the core-shell SANS profiles revealed by controlled contrast variation. Furthermore, at reduced CO2 densities (∼0.7gcm(-3)), elongated cylindrical droplet structures have been observed, which are uncommon for CO2 microemulsions/emulsions. The implications of the presence of cylindrical micelles and droplets for applications of CO2, and viscosity enhancements are discussed. Copyright © 2014 Elsevier Inc. All rights reserved.

Microemulsion-loaded hydrogel formulation of butenafine hydrochloride for improved topical delivery.

PubMed

Pillai, Anilkumar B; Nair, Jyothilaksmi V; Gupta, Nishant Kumar; Gupta, Swati

2015-09-01

Topical microemulsion systems for the antifungal drug, butenafine hydrochloride (BTF) were designed and developed to overcome the problems associated with the cutaneous delivery due to poor water solubility. The solubility of BTF in oils, surfactants and co-surfactants was evaluated to screen the components of the microemulsion. Isopropyl palmitate was used as the oil phase, aerosol OT as the surfactant and sorbitan monooleate as co-surfactant. The pseudoternary diagrams were constructed to identify the area of microemulsion existence and optimum systems were designed. The systems were assessed for drug-loading efficiency and characterized for pH, robustness to dilution, globule size, drug content and stability. Viscosity analysis, spreadability, drug content assay, ex vivo skin permeation study and antifungal activity assay were performed for the optimized microemulsion-loaded hydrogel. The optimized BTF microemulsion had a small and uniform globule size. The incorporation of microemulsion system into Carbopol 940 gel was found to be better as compared to sodium alginate or hydroxyl propyl methyl cellulose (HPMC K4 M) gel. The developed gel has shown better ex vivo skin permeation and antifungal activity when compared to marketed BTF cream. Thus, the results provide a basis for the successful delivery of BTF from microemulsion-loaded hydrogel formulation, which resulted in improved penetration of drug and antifungal activity in comparison with commercial formulation of BTF.

Determination of in vivo behavior of mitomycin C-loaded o/w soybean oil microemulsion and mitomycin C solution via gamma camera imaging.

PubMed

Kotmakçı, Mustafa; Kantarcı, Gülten; Aşıkoğlu, Makbule; Ozkılıç, Hayal; Ertan, Gökhan

2013-09-01

In this study, a microemulsion system was evaluated for delivery of mitomycin C (MMC). To track the distribution of the formulated drug after intravenous administration, radiochemical labeling and gamma scintigraphy imaging were used. The aim was to evaluate a microemulsion system for intravenous delivery of MMC and to compare its in vivo behavior with that of the MMC solution. For microemulsion formulation, soybean oil was used as the oil phase. Lecithin and Tween 80 were surfactants and ethanol was the cosurfactant. To understand the whole body localization of MMC-loaded microemulsion, MMC was labeled with radioactive technetium and gamma scintigraphy was applied for visualization of drug distribution. Radioactivity in the bladder 30 minutes after injection of the MMC solution was observed, according to static gamma camera images. This shows that urinary excretion of the latter starts very soon. On the other hand, no radioactivity appeared in the urinary bladder during the 90 minutes following the administration of MMC-loaded microemulsion. The unabated radioactivity in the liver during the experiment shows that the localization of microemulsion formulation in the liver is stable. In the light of the foregoing, it is suggested that this microemulsion formulation may be an appropriate carrier system for anticancer agents by intravenous delivery in hepatic cancer chemotherapy.

Antitumor efficacy of a novel CLA-PTX microemulsion against brain tumors: in vitro and in vivo findings.

PubMed

Li, Dan; Yang, Ke; Li, Jie-Si; Ke, Xi-Yu; Duan, Yu; Du, Ruo; Song, Ping; Yu, Ke-Fu; Ren, Wei; Huang, Dan; Li, Xing-Huo; Hu, Xin; Zhang, Xuan; Zhang, Qiang

2012-01-01

Considering the observations that linoleic acid conjugated with paclitaxel (CLA-PTX) possesses antitumor activity against brain tumors, is able to cross the blood-brain barrier, but has poor water solubility, the purpose of this study was to prepare a novel CLA-PTX microemulsion and evaluate its activity against brain tumors in vitro and in vivo. The in vitro cytotoxicity of a CLA-PTX microemulsion was investigated in C6 glioma cells. The in vivo antitumor activity of the CLA-PTX microemulsion was evaluated in tumor-bearing nude mice and rats. The pharmacokinetics of the CLA-PTX microemulsion were investigated in rats, and its safety was also evaluated in mice. The average droplet size of the CLA-PTX microemulsion was approximately 176.3 ± 0.8 nm and the polydispersity index was 0.294 ± 0.024. In vitro cytotoxicity results showed that the IC(50) of the CLA-PTX microemulsion was 1.61 ± 0.83 μM for a C6 glioma cell line, which was similar to that of free paclitaxel and CLA-PTX solution (P > 0.05). The antitumor activity of the CLA-PTX microemulsion against brain tumors was confirmed in our in vivo C6 glioma tumor-bearing nude mice as well as in a rat model. In contrast, Taxol(®) had almost no significant antitumor effect in C6 glioma tumor-bearing rats, but could markedly inhibit growth of C6 tumors in C6 glioma tumor-bearing nude mice. The pharmacokinetic results indicated that CLA-PTX in solution has a much longer circulation time and produces higher drug plasma concentrations compared with the CLA-PTX microemulsion. The results of the acute toxicity study showed that the LD(50) of CLA-PTX solution was 103.9 mg/kg. In contrast, the CLA-PTX microemulsion was well tolerated in mice when administered at doses up to 200 mg/kg. CLA-PTX microemulsion is a novel formulation with significant antitumor efficacy in the treatment of brain tumors, and is safer than CLA-PTX solution.

In vitro release of diclofenac diethylamine from caprylocaproyl macrogolglycerides based microemulsions.

PubMed

Djordjevic, Ljiljana; Primorac, Marija; Stupar, Mirjana

2005-05-30

The purpose of the present study was to determine the influence of both formulation parameters and vehicle structure on in vitro release rate of amphiphilic drug diclofenac diethylamine (DDA) from microemulsion vehicles containing PEG-8 caprylic/capric glycerides (surfactant), polyglyceryl-6 dioleate (cosurfactant), isopropyl myristate and water. From the constructed pseudo-ternary phase diagram at surfactant-cosurfactant mass ratio (K(m) 1:1), the optimum oil-to-surfactant-cosurfactant mass ratio values (O/SC 0.67-1.64) for formulation of microemulsions with similar concentrations of hydrophilic, lipophilic and amphiphilic phases (balanced microemulsions) were found. The results of characterization experiments indicated bicontinuous or nonspherical water-continuous internal structure of the selected microemulsion vehicles. Low water/isopropyl myristate apparent partition coefficient for DDA as well as elevated electrical conductivity and apparent viscosity values for the investigated microemulsion formulations containing 1.16% (w/w) of DDA, suggested that the drug molecules was predominantly partitioned in the water phase and most likely selfaggregate and interact with interfacial film. Release of DDA from the selected water-continuous (W/O), oil-continuous (O/W) and balanced microemulsions was investigated using rotating paddle dissolution apparatus modified by addition of enhancer cell. A linear diffusion of DDA through regenerated cellulose membrane was observed for the W/O and O/W formulations with the low content of dispersed phase. Non-linearity of the drug release profile in the case of bicontinuous formulations was related to the more complex distribution of DDA including interactions between the drug and vehicle. The membrane flux value increases from 25.02 microgcm(-2)h(-1) (W/O microemulsion) to 117.94 microgcm(-2)h(-1) (O/W microemulsion) as the water phase concentration increases. Moreover, the obtained flux values for balanced microemulsions (29.38-63.70 microgcm(-2)h(-1)) suggested that bicontinuous microstructure hampers the release of the amphiphilic drug.

Water/oil type microemulsion systems containing lidocaine hydrochloride: in vitro and in vivo evaluation.

PubMed

Dogrul, Ahmet; Arslan, Seyda Akkus; Tirnaksiz, Figen

2014-01-01

The purpose of this study was to develop a water/oil microemulsion containing lidocaine hydrochloride (4%) and to compare its local anaesthetic efficacy with commercial products. A pseudoternary diagram (Km:1/1 or 1/2) was constructed using lecithin/ethanol/oil/water. The droplet size, viscosity and release of the microemulsions were evaluated. Tail flick tests were conducted for in vivo effectiveness; the initiation time of effect, maximum effect, time to reach maximum effect, and relative efficacy were evaluated. The drug caused a significant increase in droplet size. The use of olive oil resulted in a decrease in the solubilisation parameter, as well as a reduction in the release. The droplet size and viscosity of the microemulsion composed of Miglyol/lecithin/ethanol/water/drug (Km:1/2) was lower than other microemulsions (8.38 nm, 6.9 mPa), and its release rate (1.61 mg/h) was higher. This system had a faster and more efficient anaesthetic effect than the other microemulsions and commercial products. Results indicate that a water/oil type microemulsion (Miglyol/lecithin/ethanol/water) has promising potential to increase the local anaesthetic effect.

Microemulsion formulation design and evaluation for hydrophobic compound: Catechin topical application.

PubMed

Lin, Yu-Hsiang; Tsai, Ming-Jun; Fang, Yi-Ping; Fu, Yaw-Syan; Huang, Yaw-Bin; Wu, Pao-Chu

2018-01-01

The aim of the present study was to design a microemulsion for catechin topical application. A mixture experimental design with five independent variables (X 1 : oil, X 2 : surfactant, X 3 : catechin, X 4 : cosurfactant and X 5 : water) was developed, and the response surface methodology was used to study the effect of formulation components on physiochemical characteristics and penetration capacity of a catechin-loaded microemulsion, and to obtain an optimal microemulsion formulation. The results showed that the drug-loaded microemulsion formation and characteristics were related to many parameters of the components. The transdermal amounts in receiver cells and skin deposition amount remarkably increased about 4.1-111.6-fold and 0.6-7.6-fold respectively. The lag time was significantly shortened from 10h to 1.0-6.7h. The optimal formulation with 20% surfactant, 30% cosurfactant and 2.6% Catechin was subjected to stability and irritation tests. The results showed that the physicochemical characteristics and catechin level of the drug-loaded microemulsion did not show significant degradation after 3 months of storage at 25°C.The catechin-loaded microemulsion did not cause significant irritation compared to the water-treated group. Copyright © 2017 Elsevier B.V. All rights reserved.

Duloxetine loaded-microemulsion system to improve behavioral activities by upregulating serotonin and norepinephrine in brain for the treatment of depression.

PubMed

Sindhu, Pardeep; Kumar, Shobhit; Iqbal, Babar; Ali, Javed; Baboota, Sanjula

2018-04-01

Duloxetine is a well-known antidepressant molecule which is used in the treatment of depression but due to poor solubility it suffers with the drawback of low oral bioavailability. The objective of present work was to formulate and characterize duloxetine loaded microemulsion to enhance the oral bioavailability. Prepared microemulsion was studied for droplet size, zeta potential, refractive index, polydispersity index (PDI), percentage transmittance, viscosity and in vitro release study. Optimized microemulsion (D1) showed spherical droplets with mean diameter of 35.40 ± 3.11 nm, PDI of 0.170 and zeta potential values of -25.8 mV. Formulation showed good transmittance (greater than 99%), viscosity (0.205 Pa s) and refractive index (1.43 ± 0.01). Increased duloxetine release was obtained with microemulsion in comparison to drug suspension. Behavioral tests like mobility test, tail suspension test and forced swimming test performed in depressed and treated rats with duloxetine microemulsion significantly improved the behavioral activities in comparison to duloxetine suspension. Pharmacokinetic studies showed that microemulsion exhibited 1.8 times increment in bioavailability in comparison to duloxetine suspension. Copyright © 2018 Elsevier Ltd. All rights reserved.

Effect of oil substitution in chiral microemulsion electrokinetic chromatography.

PubMed

Mertzman, Melissa D; Foley, Joe P

2004-02-01

In a previous publication (Pascoe, R., Foley, J. P., Analyst 2002, 127, 710-714), a novel chiral microemulsion based on 1.0% w/v dodecoxycarbonylvaline (DDCV), 0.50% v/v ethyl acetate and 1.2% v/v 1-butanol, was shown to provide rapid enantiomeric separations of various pharmaceutical compounds. The two deficiencies noted with this method were that the peak shapes obtained were asymmetric and the efficiencies were lower than those previously obtained using DDCV micelles (Peterson, A. G., Ahuja, E. S., Foley, J. P., J. Chromatogr. B 1996, 683, 15-28). This study examines the use of three alternative low-interfacial-tension oils (methyl acetate, methyl propionate, and methyl formate), in combination with DDCV, to characterize their effect on the elution range, efficiency, resolution, and enantioselectivity of various pharmaceutical enantiomers. The oils were evaluated in both the same volume percentage and the same molar concentration as ethyl acetate in the original DDCV microemulsion system. Including ethyl acetate, a total of seven microemulsion systems were examined. For the compounds that were separated, average enantioselectivities ranged from 1.09 to 1.28, with corresponding efficiencies of 14,000-20,000. While some interesting differences were observed, ethyl acetate still proved to be the most advantageous in terms of enantioselectivity, resolution, and elution range.

Bending moduli of microemulsions; comparison of results from small angle neutron scattering and neutron spin-echo spectroscopy

NASA Astrophysics Data System (ADS)

Monkenbusch, M.; Holderer, O.; Frielinghaus, H.; Byelov, D.; Allgaier, J.; Richter, D.

2005-08-01

The properties of bicontinuous microemulsions, consisting of water, oil and a surfactant, depend to a large extent on the bending moduli of the surfactant containing oil-water interface. In systems with CiEj as surfactant these moduli can be modified by the addition of diblock copolymers (boosting effect) and homopolymers (inverse boosting effect) or a combination of both. The influence of the addition of homopolymers (PEPX and PEOX, X = 5 or 10 kg/mol molecular weight) on the structure, bending modulus and dynamics of the surfactant layer is studied with small angle neutron scattering (SANS) and neutron spin-echo spectroscopy (NSE). Besides providing information on the microemulsion structure, neutron scattering is a microscopic probe that can be used to measure the local bending modulus κ. The polymer addition gives access to a homologous series of microemulsions with changing κ values. We relate the results obtained by analysis of SANS to those from NSE experiments. Comparison of the bending moduli obtained sheds light on the different renormalization length scales for NSE and SANS. Comparison of SANS and NSE derived κ values yields a consistent picture if renormalization properties are observed. Finally a ready to use method for converting NSE data into reliable values for κ is presented.

Rapid determination of water- and fat-soluble vitamins with microemulsion electrokinetic chromatography.

PubMed

Yin, Changna; Cao, Yuhua; Ding, Shaodong; Wang, Yun

2008-06-06

A rapid, reliable and reproducible method based on microemulsion electrokinetic chromatography (MEEKC) for simultaneous determination of 13 kinds of water- and fat-soluble vitamins has been developed in this work. A novel microemulsion system consisting of 1.2% (w/w) sodium lauryl sulphate (SDS), 21% (v/v) 1-butanol, 18% (v/v) acetonitrile, 0.8% (w/w) n-hexane, 20mM borax buffer (pH 8.7) was applied to improve selectivity and efficiency, as well as shorten analysis time. The composition of microemulsion used as the MEEKC running buffer was investigated thoroughly to obtain stable separation medium, as well as the optimum determination conditions. Acetonitrile as the organic solvent modifier, pH of the running buffer and 1-butanol as the co-surfactant played the most important roles for the separation of the fat-soluble vitamins, water-soluble vitamins and stabilization of system, respectively. The 13 water- and fat-soluble vitamins were baseline separated within 30 min. The system was applied to determine water- and fat-soluble vitamins in commercial multivitamin pharmaceutical formulation, good accuracy and precision were obtained with recoveries between 97% and 105%, relative standard derivations (RSDs) less than 1.8% except vitamin C, and acceptable quantitative results corresponding to label claim.

Nanostructured lipid carriers versus microemulsions for delivery of the poorly water-soluble drug luteolin.

PubMed

Liu, Ying; Wang, Lan; Zhao, Yiqing; He, Man; Zhang, Xin; Niu, Mengmeng; Feng, Nianping

2014-12-10

Nanostructured lipid carriers and microemulsions effectively deliver poorly water-soluble drugs. However, few studies have investigated their ability and difference in improving drug bioavailability, especially the factors contributed to the difference. Thus, this study was aimed at investigating their efficiency in bioavailability enhancement based on studying two key processes that occur in NLC and ME during traverse along the intestinal tract: the solubilization process and the intestinal permeability process. The nanostructured lipid carriers and microemulsions had the same composition except that the former were prepared with solid lipids and the latter with liquid lipids; both were evaluated for particle size and zeta potential. Transmission electron microscopy, differential scanning calorimetry, and X-ray diffraction were performed to characterize their properties. Furthermore, in vitro drug release, in situ intestinal absorption, and in vitro lipolysis were studied. The bioavailability of luteolin delivered using nanostructured lipid carriers in rats was compared with that delivered using microemulsions and suspensions. The in vitro analysis revealed different release mechanisms for luteolin in nanostructured lipid carriers and microemulsions, although the in situ intestinal absorption was similar. The in vitro lipolysis data indicated that digestion speed and extent were higher for microemulsions than for nanostructured lipid carriers, and that more of the former partitioned to the aqueous phase. The in vivo bioavailability analysis in rats indicated that the oral absorption and bioavailability of luteolin delivered using nanostructured lipid carriers and microemulsions were higher than those of luteolin suspensions. Nanostructured lipid carriers and microemulsions improved luteolin's oral bioavailability in rats. The rapid lipid digestion and much more drug solubilized available for absorption in microemulsions may contribute to better absorption and higher bioavailability. Copyright © 2014 Elsevier B.V. All rights reserved.

The influence of surfactant HLB and oil/surfactant ratio on the formation and properties of self-emulsifying pellets and microemulsion reconstitution.

PubMed

Matsaridou, Irini; Barmpalexis, Panagiotis; Salis, Andrea; Nikolakakis, Ioannis

2012-12-01

Self-emulsifying oil/surfactant mixtures can be incorporated into pellets that have the advantages of the oral administration of both microemulsions and a multiple-unit dosage form. The purpose of this work was to study the effects of surfactant hydrophilic-lipophilic balance (HLB) and oil/surfactant ratio on the formation and properties of self-emulsifying microcrystalline cellulose (MCC) pellets and microemulsion reconstitution. Triglycerides (C(8)-C(10)) was the oil and Cremophor ELP and RH grades and Solutol the surfactants. Pellets were prepared by extrusion/spheronization using microemulsions with fixed oil/surfactant content but with different water proportions to optimize size and shape parameters. Microemulsion reconstitution from pellets suspended in water was evaluated by turbidimetry and light scattering size analysis, and H-bonding interactions of surfactant with MCC from FT-IR spectra. It was found that water requirements for pelletization increased linearly with increasing HLB. Crushing load decreased and deformability increased with increasing oil/surfactant ratio. Incorporation of higher HLB surfactants enhanced H-bonding and resulted in faster and more extensive disintegration of MCC as fibrils. Reconstitution was greater at high oil/surfactant ratios and the droplet size of the reconstituted microemulsions was similar to that in the wetting microemulsions. The less hydrophilic ELP with a double bond in the fatty acid showed weaker H-bonding and greater microemulsion reconstitution. Purified ELP gave greater reconstitution than the unpurified grade. Thus, the work demonstrates that the choice of type and quantity of the surfactant used in the formulation of microemulsions containing pellets has an important influence on their production and performance.

Processes for microemulsion polymerization employing novel microemulsion systems

DOEpatents

Beckman, Eric J.; Smith, Richard D.; Fulton, John L.

1990-06-12

This invention is directed to a microemulsion system comprising a first phase including a low-polarity fluid material which is a gas at standard temperature and pressure, and which has a cloud-point density. It also includes a second phase including a polar fluid, typically water, a monomer, preferably a monomer soluble in the polar fluid, and a microemulsion promoter for facilitating the formation of micelles including the monomer in the system. In the subject process, micelles including the monomer are formed in the first phase. A polymerization initiator is introduced into the micelles in the microemulsion system. The monomer is then polymerized in the micelles, preferably in the core of the micelle, to produce a polymeric material having a relatively high molecular weight.

Comparison of chiral electrophoretic separation methods for phenethylamines and application on impurity analysis.

PubMed

Borst, Claudia; Holzgrabe, Ulrike

2010-12-15

A chiral microemulsion electrokinetic chromatography method has been developed for the separation of the enantiomers of the phenethylamines ephedrine, N-methylephedrine, norephedrine, pseudoephedrine, adrenaline (epinephrine), 2-amino-1-phenylethanol, diethylnorephedrine, and 2-(dibutylamino)-1-phenyl-1-propanol, respectively. The separations were achieved using an oil-in-water microemulsion consisting of the oil-component ethyl acetate, the surfactant sodium dodecylsulfate, the cosurfactant 1-butanol, the organic modifier propan-2-ol and 20mM phosphate buffer pH 2.5 as aqueous phase. For enantioseparation sulfated beta-cyclodextrin was added. The method was compared to an already described CZE method, which made use of heptakis(2,3-di-O-diacetyl-6-O-sulfo)-beta-cyclodextrin (HDAS) as chiral selector. Additionally, the developed method was successfully applied to the related substances analysis of noradrenaline, adrenaline, dipivefrine, ephedrine and pseudoephedrine monographed in the European Pharmacopoeia 6. Copyright 2010 Elsevier B.V. All rights reserved.

Development of capillary electrophoresis methods for quantitative determination of taurine in vehicle system and biological media.

PubMed

da Silva, Dayse L P; Rüttinger, Hans H; Mrestani, Yahia; Baum, Walter F; Neubert, Reinhard H H

2006-06-01

CE methods have been developed for the determination of taurine in pharmaceutical formulation (microemulsion) and in biological media such as sweat. The CE system with end-column pulsed amperometric detection has been found to be an interesting method in comparison with UV and fluorescence detection for its simplicity and rapidity. A gold-disk electrode of 100 mm diameter was used as the working electrode. The effects of a field decoupler at the end of the capillary, separation voltage, injection and pressure times were investigated. A detection limit of 4 x 10(-5) mol/L was reached using integrated pulsed amperometric detection, a method successfully applied to taurine analysis of the biological samples such as sweat. For taurine analysis of oil-in-water microemulsion, fluorescence detector was the favored method, the detection limit of which was 4 x 10(-11) mol/L.

Supercooling of water confined in reverse micelles

NASA Astrophysics Data System (ADS)

Spehr, T.; Frick, B.; Grillo, I.; Stühn, B.

2008-03-01

We report on the temperature dependence of the nanosecond-timescale dynamics of the ternary mixture water/AOT/oil with deuterated heptane, toluene or decane as the oil. Water-swollen reverse micelles as formed in such microemulsions allow us to investigate the freezing behaviour of water confined in a soft environment. We report here on the first neutron scattering studies in which the freezing of the confined water and of the oil is followed down to temperatures at which the whole system is frozen. We focus on studies of water confined in three different droplet sizes: by means of small-angle neutron scattering we have determined the radii to be 46, 18, and 7 Å for water to surfactant ratios ω = 40, 12, and 3. From elastic temperature scans by neutron backscattering we deduce a strong supercooling of water confined in the reverse swollen micelles which increases with decreasing droplet size. For the smallest droplets we find a supercooling of more than 45 K compared to bulk water.

Enhanced skin delivery of quercetin by microemulsion.

PubMed

Kitagawa, Shuji; Tanaka, Yuko; Tanaka, Manami; Endo, Kanako; Yoshii, Akiko

2009-07-01

For topical application of quercetin it is necessary to improve the low efficiency of its intradermal delivery as well as its low solubility in aqueous and organic vesicles. The aim of this study was to determine the usefulness of a microemulsion for that purpose. A microemulsion consisting of isopropyl myristate, 150 mM NaCl solution, Tween 80 and ethanol was prepared. The skin delivery of quercetin by microemulsion using excised guinea-pig and Yucatan micropig skin in Franz diffusion cells was examined. Lipid peroxidation in skin was also tested using iron(II) and citrate. Using a w/o microemulsion as a vehicle, intradermal delivery of quercetin was significantly increased, as was its solubility. Quercetin penetrated deep into the skin, but no transfer was observed into the receptor compartment. It was confirmed that quercetin retained in the skin dose-dependently inhibited lipid peroxidation. The findings indicate the potential use of microemulsions for the skin delivery of quercetin, where it exerts antioxidative effects.

Collagen and hyaluronic acid hydrogel in water-in-oil microemulsion delivery systems.

PubMed

Kupper, Sylwia; Kłosowska-Chomiczewska, Ilona; Szumała, Patrycja

2017-11-01

The increase in skin related health issues has promoted interest in research on the efficacy of microemulsion in dermal and transdermal delivery of active ingredients. Here, we assessed the water-in-oil microemulsion capacity to incorporate two natural polymers, i.e. collagen and hyaluronic acid with low and high molecular weight. Systems were extensively characterized in terms of conductivity, phase inversion studies, droplet diameter, polydispersity index and rheological properties. The results of this research indicate that the structure and extent of water phase in microemulsions is governed by ratio and amount of surfactant mixture (sorbitan ester derivatives). However, results have also shown that collagen, depending upon the weight of the molecule and its surface activity, influence the droplet size of the microemulsions. While the hyaluronic acid, especially with high molecular weight, due to the water-binding ability and hydrogel formation alters the rheological properties of the microemulsion, thus providing viscous consistency of the formulation. Copyright © 2017 Elsevier Ltd. All rights reserved.

Co-surfactant free microemulsions: Preparation, characterization and stability evaluation for food application.

PubMed

Xu, Zhenbo; Jin, Jun; Zheng, Minying; Zheng, Yan; Xu, Xuebing; Liu, Yuanfa; Wang, Xingguo

2016-08-01

The aim of the study is to prepare co-surfactant free microalgal oil microemulsions and investigate their properties as well as processing stability for food application. The physicochemical characteristics of the microemulsions were investigated by dynamic light scattering (DLS), turbidity, conductivity, rheological measurements and transmission electron microscopy (TEM). Within the microemulsion region, when the surfactant to oil ratio was 9:1, the hydrodynamic diameter (Dh) was 18nm; when the surfactant to oil ratio was 7.5:1, the hydrodynamic diameter (Dh) was 50nm. Rheological studies proved that the microemulsion system was a pseudoplastic fluid, which followed a shear thinning flow behavior. The loss rate of docosahexaenoic acid (DHA) was less than 5%wt after ultra high temperature (UHT) and high temperature short time (HTST) thermal treatments. A high content of CaCl2 (10.0%wt) could not destroy the microemulsion system, and it could be stored at 4°C for two years. Copyright © 2016 Elsevier Ltd. All rights reserved.

The novel oral imatinib microemulsions: physical properties, cytotoxicity activities and improved Caco-2 cell permeability.

PubMed

Gundogdu, Evren; Karasulu, Hatice Yesim; Koksal, Cinel; Karasulu, Ercüment

2013-01-01

The objective of this study was to formulate imatinib (IM) loaded to water-in-oil (w/o) microemulsions as an alternative formulation for cancer therapy and to evaluate the cytotoxic effect of microemulsions Caco-2 and MCF-7. Moreover, permeability studies were also performed with Caco-2 cells. W/o microemulsion systems were developed by using pseudo-ternary phase diagram. According to cytotoxicity studies, all formulations did not exert a cytotoxic effect on Caco-2 cells. Furthermore, all formulations had a significant cytotoxic effect on MCF-7 cells and the cytotoxic effect of M3IM was significantly more than that of other microemulsions and IM solution (p < 0.05). The permeability studies of IM across Caco-2 cells showed that permeability value from apical to basolateral was higher than permeability value of other formulations. In conclusion, the microemulsion formulations as a drug carrier, especially M3IM formulation, may be used as an effective alternative breast cancer therapy for oral delivery of IM.

Application of Complex Fluids in Lignocellulose Processing

NASA Astrophysics Data System (ADS)

Carrillo Lugo, Carlos A.

Complex fluids such as emulsions, microemulsions and foams, have been used for different applications due to the multiplicity of properties they possess. In the present work, such fluids are introduced as effective media for processing lignocellulosic biomass. A demonstration of the generic benefits of complex fluids is presented to enhance biomass impregnation, to facilitate pretreatment for fiber deconstruction and to make compatible cellulose fibrils with hydrophobic polymers during composite manufacture. An improved impregnation of woody biomass was accomplished by application of water-continuous microemulsions. Microemulsions with high water content, > 85%, were formulated and wood samples were impregnated by wicking and capillary flooding at atmospheric pressure and temperature. Formulations were designed to effectively impregnate different wood species during shorter times and to a larger extent compared to the single components of the microemulsions (water, oil or surfactant solutions). The viscosity of the microemulsions and their interactions with cell wall constituents in fibers were critical to define the extent of impregnation and solubilization. The relation between composition and formulation variables and the extent of microemulsion penetration in different woody substrates was studied. Formulation variables such as salinity content of the aqueous phase and type of surfactant were elucidated. Likewise, composition variables such as the water-to-oil ratio and surfactant concentration were investigated. These variables affected the characteristics of the microemulsion and determined their effectiveness in wood treatment. Also, the interactions between the surfactant and the substrate had an important contribution in defining microemulsion penetration in the capillary structure of wood. Microemulsions as an alternative pretreatment for the manufacture of cellulose nanofibrils (CNFs) was also studied. Microemulsions were applied to pretreat lignin-free and lignin-containing fibers obtained from various processes. Incorporation of active agents in the microemulsion facilitated fiber pretreatment before deconstruction via grinding and microfluidization. The energy consumed during the manufacture of cellulose nanofibrils was reduced by up to 55 and 32% in the case of lignin-containing and lignin-free fibers. Moreover, such pre-treatment did not affect negatively the mechanical properties of films prepared with the produced CNF. CNF was also used to enhance the stability of normal and multiple emulsions of the water-in-oil-in-water (W/O/W) type and to prevent their creaming. This was achieved by the marked increase in viscosity of the aqueous phase in the presence CNF. Finally, water-continuous emulsions were used to prepare nanocomposite fibers containing polystyrene and CNF. The morphology of composite fibers obtained after electrospinning of emulsions incorporating polystyrene and CNF was affected by parameters such the concentration of surfactant additives present in the microemulsion and the conductivity of the aqueous phase. Overall, emulsions and microemulsions are presented as a convenient platform to improve the compatibility between polymers of different hydrophilicity, to facilitate their processing and integration in composites.

Intravenous microemulsion of docetaxel containing an anti-tumor synergistic ingredient (Brucea javanica oil): formulation and pharmacokinetics.

PubMed

Ma, Shilin; Chen, Fen; Ye, Xiaohui; Dong, Yingjie; Xue, Yingna; Xu, Heming; Zhang, Wenji; Song, Shuangshuang; Ai, Li; Zhang, Naixian; Pan, Weisan

2013-01-01

The purpose of this study was to develop a docetaxel microemulsion containing an anti-tumor synergistic ingredient (Brucea javanica oil) and to investigate the characteristics of the microemulsion. Brucea javanica oil contains oleic acid and linoleic acids that have been shown by animal and human studies to inhibit tumor formation. The microemulsion containing Brucea javanica oil, medium-chain triglyceride, soybean lecithin, Solutol®HS 15, PEG 400, and water was developed for docetaxel intravenous administration. A formulation with higher drug content, lower viscosity, and smaller particle size was developed. The droplet size distribution of the dispersed phase of the optimized microemulsion was 13.5 nm, determined using a dynamic light scattering technique. The small droplet size enabled the microemulsion droplets to escape from uptake and phagocytosis by the reticuloendothelial system and increased the circulation time of the drug. The zeta potential was -41.3 mV. The optimized microemulsion was pale yellow, transparent, and non-opalescent in appearance. The value of the combination index was 0.58, showing that there was a synergistic effect when docetaxel was combined with Brucea javanica oil. After a single intravenous infusion dose (10 mg/kg) in male Sprague Dawley rats, the area under the curve of the microemulsion was higher and the half-time was longer compared with that of docetaxel solution alone, and showed superior pharmacokinetic characteristics. These results indicate that this preparation of docetaxel in emulsion is likely to provide an excellent prospect for clinical tumor treatment.

Synthesis of FeCoB amorphous nanoparticles and application in ferrofluids

NASA Astrophysics Data System (ADS)

Zhao, Shuchun; Bian, Xiufang; Yang, Chuncheng; Yu, Mengchun; Wang, Tianqi

2018-03-01

Magnetic FeCoB amorphous nanoparticles were successfully synthesized by borohydride reduction in water/n-hexane (W/He) microemulsions. The as-prepared FeCoB alloys are amorphous and spherical nanoparticles with an average particle size about 10.7 nm, compared to FeCoB alloys with an average particle size about 304.2 nm which were synthesized by a conventional aqua-solution method. Furthermore, three kinds of FeCoB ferrofluids (FFs) were prepared by dispersing FeCoB particles into W/He microemulsion, water and silicone oil respectively. Results show that the W/He-based FeCoB FFs are superparamagnetic with saturation magnetization (Ms) reaching to 12.4 emu/g. Besides, compared to water-based and silicone oil-based FFs, W/He-based FeCoB FFs exhibit high stability, with magnetic weights decreasing slightly even under the magnetic field intensity of H = 210 mT. In the W/He-based FeCoB FFs, interfacial tensions of water phase and oil phase are supposed to prevent the agglomeration and sedimentation of FeCoB nanoparticles dispersed in different water droplets of the microemulsion, compared to the current stabilizing method of directly modifying the surface of particles.

Analysis of plant hormones by microemulsion electrokinetic capillary chromatography coupled with on-line large volume sample stacking.

PubMed

Chen, Zongbao; Lin, Zian; Zhang, Lin; Cai, Yan; Zhang, Lan

2012-04-07

A novel method of microemulsion electrokinetic capillary chromatography (MEEKC) coupled with on-line large volume sample stacking was developed for the analysis of six plant hormones including indole-3-acetic acid, indole-3-butyric acid, indole-3-propionic acid, 1-naphthaleneacetic acid, abscisic acid and salicylic acid. Baseline separation of six plant hormones was achieved within 10 min by using the microemulsion background electrolyte containing a 97.2% (w/w) 10 mM borate buffer at pH 9.2, 1.0% (w/w) ethyl acetate as oil droplets, 0.6% (w/w) sodium dodecyl sulphate as surfactant and 1.2% (w/w) 1-butanol as cosurfactant. In addition, an on-line concentration method based on a large volume sample stacking technique and multiple wavelength detection was adopted for improving the detection sensitivity in order to determine trace level hormones in a real sample. The optimal method provided about 50-100 fold increase in detection sensitivity compared with a single MEEKC method, and the detection limits (S/N = 3) were between 0.005 and 0.02 μg mL(-1). The proposed method was simple, rapid and sensitive and could be applied to the determination of six plant hormones in spiked water samples, tobacco leaves and 1-naphthylacetic acid in leaf fertilizer. The recoveries ranged from 76.0% to 119.1%, and good reproducibilities were obtained with relative standard deviations (RSDs) less than 6.6%.

Tulane/Xavier Vaccine Peptide Program

DTIC Science & Technology

2013-07-01

include a dry powder formulation, microemulsions , nonspherical liposomes, ceramic shell vesicles, and nanometer-sized silk particles. Nasal...pulmonary delivery: dry powder formulation, microemulsions , nonspherical liposomes, ceramic shell vesicles, and nanometer-sized silk particles. (3) Confirm...include a dry powder formulation, microemulsions , nonspherical liposomes, ceramic shell vesicles, and nanometer-sized silk particles. Nasal

Improving the Isotretinoin Photostability by Incorporating in Microemulsion Matrix

PubMed Central

Patel, Mrunali R.; Patel, Rashmin B.; Parikh, Jolly R.; Patel, Bharat G.

2011-01-01

The present paper demonstrates the increased photostability of isotretinoin when loaded in microemulsion. The photodegradation of isotretinoin, in methanol and microemulsion formulation was studied under direct sun light. The photodegradation process was monitored by UV spectrophotometry. In methanol solution, isotretinoin undergoes complete photodegradation just within a few minutes of light exposure. Isotretinoin incorporated in microemulsion formulation showed an increased stability in comparison to the methanol solutions. In particular for isotretinoin, a residual concentration of 75% was still present after a light irradiance versus a residual value of just 16% measured at the same time in methanol solution. Further, degradation kinetic parameters of isotretinoin-loaded microemulsion formulation were demonstrated increase isotretinoin half-life about five-times in comparison with a methanol solution under a direct sun light. PMID:22389863

Formulation and In-vitro Evaluation of Tretinoin Microemulsion as a Potential Carrier for Dermal Drug Delivery

PubMed Central

Mortazavi, Seyed Alireza; Pishrochi, Sanaz; Jafari azar, Zahra

2013-01-01

In this study, tretinoin microemulsion has been formulated based on phase diagram studies by changing the amounts and proportions of inactive ingredients, such as surfactants, co-surfactants and oils. The effects of these variables have been determined on microemulsion formation, particle size of the dispersed phase and release profile of tretinoin from microemulsion through dialysis membrane. In released studies, static Franz diffusion cells mounted with dialysis membrane were used. Sampling was conducted every 3 h at room temperature over a period of 24 h. The amount of released drug was measured with UV-spectrophotometer and the percentage of drug released was calculated. Based on the results obtained, the oil phase concentration had a proportional effect on particle size which can consequently influence on drug release. The particle size and the amount of released drug were affected by the applied surfactants. The components of the optimized microemulsion formulation were 15% olive oil, 12% propylene glycol (as co-surfactant), 33% Tween®80 (as surfactant) and 40% distilled water, which was tested for viscosity and rheological behavior. The prepared tretinoin microemulsion showed pseudoplastic-thixotropic behavior. The profile of drug release follows zero order kinetics. The optimized tretinoin microemulsion showed enhanced in-vitro release profile compared to the commercial gels and creams. PMID:24523740

Polyprenols of Ginkgo biloba Enhance Antibacterial Activity of Five Classes of Antibiotics.

PubMed

Tao, Ran; Wang, Chengzhang; Ye, Jianzhong; Zhou, Hao; Chen, Hongxia

2016-01-01

Polyprenol (GBP) from Ginkgo biloba Leaves (GBL) is an important lipid with many bioactive effects. The effect of GBP on antibacterial properties of five antibiotics belonging to different classes was through analysis of inhibition halos, MIC, and FIC index. And we studied the time-killing curves and Ca(2+) mobilization assay in Staphylococcus aureus cells treated with GBP microemulsion and gentamicin sulfate under MIC/2 conditions. These results showed that the GBP microemulsion (average diameter 90.2 nm) combining with gentamicin sulfate had the highest enhancing antibacterial effect against Staphylococcus aureus, and the MIC value was 33.0 μg/mL. The increase of the antibacterial effect of tested antibiotics was positively correlated with the decrease of the average diameter of GBP microemulsion. Moreover, GBP microemulsion enhanced antibacterial effect and prolonged antibacterial time of GBP combining with gentamicin sulfate against Staphylococcus aureus. GBP microemulsion could enhance the ability of gentamicin inducing an increase in intracellular calcium concentrations to Staphylococcus aureus. GBP microemulsion could help some classes of antibiotics to inhibit or kill bacteria. This study supports the fact that GBP microemulsion obviously can not only reduce the dosage of some classes of antibiotics, but also reduce the frequency of the antibiotic use in vitro.

Efficient topical delivery of chlorogenic acid by an oil-in-water microemulsion to protect skin against UV-induced damage.

PubMed

Kitagawa, Shuji; Yoshii, Kenta; Morita, Shin-ya; Teraoka, Reiko

2011-01-01

We examined the intradermal delivery of a hydrophilic polyphenol chlorogenic acid by in vitro study using excised guinea pig dorsal skin and Yucatan micropig skin. Skin accumulation as well as the solubility of chlorogenic acid in aqueous vehicles was much greater than for other polyphenols such as quercetin and genistein. However, since enhancement of skin delivery seemed to be necessary to exhibit its protective effects against oxidative damage of skin, we examined the effects of microemulsions as vehicles. Using microemulsions consisting of 150 mM NaCl solution, isopropyl myristate, polyoxyethylene sorbitan monooleate (Tween 80) and ethanol, skin accumulation as well as solubility of chlorogenic acid further increased. Enhancement effect of an oil-in-water (o/w-type) microemulsion was greater than that of a water-in-oil (w/o-type) microemulsion possibly due to the greater increase in solubility. This finding was quite different from previous findings on relatively hydrophobic polyphenols such as quercetin and genistein. Pretreatment of guinea pig dorsal skin with chlorogenic acid containing microemulsion gel prevented erythema formation induced by UV irradiation. These findings indicate the potential use of hydrophilic chlorogenic acid with o/w-type microemulsion as a vehicle to protect skin against UV-induced oxidative damage.

Formulation and In-vitro Evaluation of Tretinoin Microemulsion as a Potential Carrier for Dermal Drug Delivery.

PubMed

Mortazavi, Seyed Alireza; Pishrochi, Sanaz; Jafari Azar, Zahra

2013-01-01

In this study, tretinoin microemulsion has been formulated based on phase diagram studies by changing the amounts and proportions of inactive ingredients, such as surfactants, co-surfactants and oils. The effects of these variables have been determined on microemulsion formation, particle size of the dispersed phase and release profile of tretinoin from microemulsion through dialysis membrane. In released studies, static Franz diffusion cells mounted with dialysis membrane were used. Sampling was conducted every 3 h at room temperature over a period of 24 h. The amount of released drug was measured with UV-spectrophotometer and the percentage of drug released was calculated. Based on the results obtained, the oil phase concentration had a proportional effect on particle size which can consequently influence on drug release. The particle size and the amount of released drug were affected by the applied surfactants. The components of the optimized microemulsion formulation were 15% olive oil, 12% propylene glycol (as co-surfactant), 33% Tween(®)80 (as surfactant) and 40% distilled water, which was tested for viscosity and rheological behavior. The prepared tretinoin microemulsion showed pseudoplastic-thixotropic behavior. The profile of drug release follows zero order kinetics. The optimized tretinoin microemulsion showed enhanced in-vitro release profile compared to the commercial gels and creams.

Nitroxide delivery system for Nrf2 activation and skin protection.

PubMed

Ben Yehuda Greenwald, Maya; Frušić-Zlotkin, Marina; Soroka, Yoram; Sasson, Shmuel Ben; Bianco-Peled, Havazelet; Bitton, Ronit; Kohen, Ron

2015-08-01

Cyclic nitroxides are a large group of compounds composed of diverse stable radicals also known as synthetic antioxidants. Although nitroxides are valuable for use in several skin conditions, in in vivo conditions they have several drawbacks, such as nonspecific dispersion in normal tissue, preferential renal clearance and rapid reduction of the nitroxide to the corresponding hydroxylamine. However, these drawbacks can be easily addressed by encapsulating the nitroxides within microemulsions. This approach would allow nitroxide activity and therefore their valuable effects (e.g. activation of the Keap1-Nrf2-EpRE pathway) to continue. In this work, nitroxides were encapsulated in a microemulsion composed of biocompatible ingredients. The nanometric size and shape of the vehicle microemulsion and nitroxide microemulsion displayed high similarity, indicating that the stability of the microemulsions was preserved. Our studies demonstrated that nitroxide microemulsions were more potent inducers of the Keap1-Nrf2-EpRE pathway than the free nitroxides, causing the activation of phase II enzymes. Moreover, microemulsions containing nitroxides significantly reduced UVB-induced cytotoxicity in the skin. Understanding the mechanism of this improved activity may expand the usage of many other Nrf2 modulating molecules in encapsulated form, as a skin protection strategy against oxidative stress-related conditions. Copyright © 2015 Elsevier B.V. All rights reserved.

Physicochemical, in vitro and in vivo evaluation of flurbiprofen microemulsion.

PubMed

Naeem, Muhammad; Ur Rahman, Nisar; Tavares, Guilherme D; Barbosa, Sávio F; Chacra, Nádia B; Löbenberg, Raimar; Sarfraz, Muhammad K

2015-09-01

Flurbiprofen, a potent nonsteroidal anti-inflammatory drug, is widely used for relief of pain in patients suffering from rheumatic diseases, migraine, sore throat and primary dysmenorrheal. However, this drug has many gastrointestinal side effects produced by its oral administration, such as gastric bleeding and peptic ulcer. These effects were responsible for non-compliance among patients, which ultimately results in treatment failure. The physicochemical properties of flurbiprofen, make it a suitable candidate for transdermal drug delivery, which can overcome the drawbacks of oral administration. In this sense, microemulsions have been proved to increase the cutaneous absorption of lipophilic drugs when compared to conventional drug delivery systems. The purpose of this study was to formulate and characterize gel based microemulsions, for topical delivery of flurbiprofen. Different gel bases, containing microemulsion and hydro-alcoholic solution of flurbiprofen, were developed and compared. In vitro study showed that gels containing microemulsion had a higher permeation rate than those containing hydro-alcoholic solutions. Additionally, formulation of Carbopol-I (microemulsion) showed higher percent of inhibition of inflammation than others bases. Further, skin irritation study demonstrated that Carbopol-I was none irritating. Flurbiprofen microemulsion incorporated on Carbopol-I showed physicochemical, in vitro and in vivo characteristics suitable for the development of alternative transdermal delivery formulation.

Enzyme-Catalyzed Regioselective Modification of Starch Nanoparticles

DOE Office of Scientific and Technical Information (OSTI.GOV)

Chakraborty, Soma; Sahoo, Bishwabhusan; Teraoka, Iwao

The selective esterification of starch nanoparticles was performed using as catalyst Candida antartica Lipase B (CAL-B) in its immobilized (Novozym 435) and free (SP-525) forms. The starch nanoparticles were made accessible for acylation reactions by formation of Aerosol-OT (AOT, bis(2-ethylhexyl)sodium sulfosuccinate) stabilized microemulsions. Starch nanoparticles in microemulsions were reacted with vinyl stearate, ε-caprolactone, and maleic anhydride at 40 °C for 48 h to give starch esters with degrees of substitution (DS) of 0.8, 0.6, and 0.4, respectively. Substitution occurred regioselectively at the C-6 position of the glucose repeat units. Infrared microspectroscopy (IRMS) revealed that AOT-coated starch nanoparticles diffuse into themore » outer 50 μm shell of catalyst beads. Thus, even though CAL-B is immobilized within a macroporous resin, CAL-B is sufficiently accessible to the starch nanoparticles. When free CAL-B was incorporated along with starch within AOT-coated reversed micelles, CAL-B was also active and catalyzed the acylation with vinyl stearate (24 h, 40 °C) to give DS = 0.5. After removal of surfactant from the modified starch nanoparticles, they were dispersed in DMSO or water and were shown to retain their nanodimensions.« less

Crystallization from microemulsions ? a novel method for the preparation of new crystal forms of aspartame

NASA Astrophysics Data System (ADS)

Füredi-Milhofer, Helga; Garti, N.; Kamyshny, A.

1999-03-01

Solubilization and crystallization of the artificial sweetener aspartame (APM), in water/isooctane microemulsions stabilized with sodium diisooctyl sulfosuccinate (AOT) has been investigated. The amount of aspartame that could be solubilized depended primarily on the amount of surfactant and on the temperature. The maximum AOT/aspartame molar ratio at the w/o interface is shown to be 6.2 at 25°C. It was concluded that the dipeptide is located at the w/o interface interspersed between surfactant molecules and that it acts as a cosurfactant. A new crystal form, APM III, was obtained by cooling of hot w/isooctane/AOT microemulsions containing solubilized aspartame. The new crystal form exhibits a distinct X-ray diffraction powder pattern, as well as changes in the FTIR spectra, thermogravimetric and DSC patterns. H-NMR spectra of APM III dissolved in D 2O were identical to the spectrum of commercial aspartame recorded under the same conditions. The new crystal form has greatly improved dissolution kinetics.

Microemulsion-Based Topical Hydrogels of Tenoxicam for Treatment of Arthritis.

PubMed

Goindi, Shishu; Narula, Manleen; Kalra, Atin

2016-06-01

Tenoxicam (TNX) is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, backache and pain. However, prolonged oral use of this drug is associated with gastrointestinal adverse events like peptic ulceration, thus necessitating its development as topical formulation that could obviate the adverse effects and improve patient compliance. The present study was aimed at development of microemulsion-based formulations of TNX for topical delivery at the affected site. The pseudoternary phase diagrams were developed and microemulsion formulations were prepared using Captex 300/oleic acid as oil, Tween 80 as surfactant and n-butanol/ethanol as co-surfactant. Optimized microemulsions were characterized for drug content, droplet size, viscosity, pH and zeta potential. The ex vivo permeation studies through Laca mice skin were performed using Franz diffusion cell assembly, and the permeation profile of the microemulsion formulation was compared with aqueous suspension of drug and drug incorporated in conventional cream. Microemulsion formulations of TNX showed significantly higher (p < 0.001) mean cumulative percent permeation values in comparison to conventional cream and suspension of drug. In vivo anti-arthritic and anti-inflammatory activity of the developed TNX formulations was evaluated using various inflammatory models such as air pouch model, xylene-induced ear edema, cotton pellet granuloma and carrageenan-induced inflammation. Microemulsion formulations were found to be superior in controlling inflammation as compared to conventional topical dosage forms and showed efficacy equivalent to oral formulation. Results suggest that the developed microemulsion formulations may be used for effective topical delivery of TNX to treat various inflammatory conditions.

Microemulsions based on a sunflower lecithin-Tween 20 blend have high capacity for dissolving peppermint oil and stabilizing coenzyme Q10.

PubMed

Chen, Huaiqiong; Guan, Yongguang; Zhong, Qixin

2015-01-28

The objectives of the present study were to improve the capability of microemulsions to dissolve peppermint oil by blending sunflower lecithin with Tween 20 and to study the possibility of codelivering lipophilic bioactive compounds. The oil loading in microemulsions with 20% (w/w) Tween 20 increased from 3% (w/w) to 20% (w/w) upon gradual supplementation of 6% (w/w) lecithin. All microemulsions had particles of <12 nm that did not change over 70 d of storage at 21 °C. They had relatively low Newtonian viscosities and were physically and chemically stable after 50-200-fold dilution in water, resulting from similar hydrophile-lipophile-balance values of the surfactant mixture and peppermint oil. Furthermore, the microemulsions were capable of dissolving coenzyme Q10 and preventing its degradation at UV 302 nm, more significant for the microemulsion with lecithin. Therefore, natural surfactant lecithin can reduce the use of synthetic Tween 20 to dissolve peppermint oil and protect the degradation of dissolved lipophilic bioactive components in transparent products.

Thermal and UV stability of β-carotene dissolved in peppermint oil microemulsified by sunflower lecithin and Tween 20 blend.

PubMed

Chen, Huaiqiong; Zhong, Qixin

2015-05-01

Microemulsions are suitable for simultaneous delivery of flavour oils and lipophilic bioactive compounds in transparent beverages. In the present study, the feasibility of delivering β-carotene in microemulsions formulated with peppermint oil and a blend of Tween® 20 and various amounts of sunflower lecithin was investigated. The poorly water- and oil-soluble β-carotene was dissolved in the transparent microemulsions that had particles smaller than 10nm and were stable during ambient storage for 65 d. The inclusion of β-carotene did not change the flow-behaviour and Newtonian viscosity. The degradation of β-carotene in microemulsions during ambient storage, ultraviolet radiation, and thermal treatments at 60 and 80 °C followed first order kinetics and was greatly suppressed when compared to the solution control. The antioxidant potential of peppermint oil and a greater content of lecithin in microemulsions enabled the better protection of β-carotene. The studied microemulsions may find various applications in manufacturing transparent beverages. Copyright © 2014 Elsevier Ltd. All rights reserved.

The preparation of neem oil microemulsion (Azadirachta indica) and the comparison of acaricidal time between neem oil microemulsion and other formulations in vitro.

PubMed

Xu, Jiao; Fan, Qiao-Jia; Yin, Zhong-Qiong; Li, Xu-Ting; Du, Yong-Hua; Jia, Ren-Yong; Wang, Kai-Yu; Lv, Cheng; Ye, Gang; Geng, Yi; Su, Gang; Zhao, Ling; Hu, Ting-Xiu; Shi, Fei; Zhang, Li; Wu, Chang-Long; Tao, Cui; Zhang, Ya-Xue; Shi, Dong-Xia

2010-05-11

The preparation of neem oil microemulsion and its acaricidal activity in vitro was developed in this study. In these systems, the mixture of Tween-80 and the sodium dodecyl benzene sulfonate (SDBS) (4:1, by weight) was used as compound surfactant; the mixture of compound surfactant and hexyl alcohol (4:1, by weight) was used as emulsifier system; the mixture of neem oil, emulsifier system and water (1:3.5:5.5, by weight) was used as neem oil microemulsion. All the mixtures were stired in 800 rpm for 15 min at 40 degrees C. The acaricidal activity was measured by the speed of kill. The whole lethal time value of 10% neem oil microemulsion was 192.50 min against Sarcoptes scabiei var. cuniculi larvae in vitro. The median lethal time value was 81.7463 min with the toxicity regression equations of Y=-6.0269+3.1514X. These results demonstrated that neem oil microemulsion was effective against Sarcoptes scabie var. cuniculi larvae in vitro. (c) 2010. Published by Elsevier B.V. All rights reserved.

Biocompatible microemulsions for fabrication of glyceryl monostearate solid lipid nanoparticles (SLN) of tretinoin.

PubMed

Shah, Kumar A; Joshi, Medha D; Patravale, Vandana B

2009-08-01

The objective of the present investigation was to fabricate glyceryl monostearate SLN by employing a biocompatible microemulsion as a template. Biocompatible excipients such as Tween 20 (as a surfactant) and Transcutol P (a cosourfactant) (at different K(m) ratios) were selected for the fabrication of microemulsions. Pseudo-ternary phase diagrams were plotted to identify the area of the microemulsion existence. Glyceryl monostearate SLN were fabricated by dispersing the microemulsion (maintained at 65 degrees C) into cold water (maintained at 2-3 degrees C). The particle size of the SLN was determined by photon correlation spectroscopy. Tretinoin, a lipophilic anti-acne agent was incorporated into SLN as a model drug. The encapsulation efficiency of tretinoin in the SLN was determined by using Nanosep ultrafilteration device at different lipid loads viz. 1%, 1.5% and 2%. Glyceryl monostearate SLN fabricated from biocompatible microemulsion template exhibited average particle size of 175 nm and polydispersity index of 0.833. Tretinoin could be successfully incorporated into SLN and the encapsulation efficiency ranged from 37-48% at different lipid loads.

Influence of alkyl chain length compatibility on microemulsion structure and solubilization

DOE Office of Scientific and Technical Information (OSTI.GOV)

Bansal, V.K.; O'Connell, J.P.; Shah, D.O.

1980-06-01

The water solubilization capacity of water/oil microemulsions is studied as a function of alkyl chain length of oil (C/sub 8/ to C/sub 16/), surfactant (C/sub 14/ and C/sub 18/ fatty acid soaps), and alcohol (C/sub 4/ to C/sub 7/). Sodium stearate and sodium myristate were used as surfactants. For n-butanol microemulsions the maximum amount of water solubilized in the microemulsion decreased continuously with increasing oil chain length; for n-heptanol it increased continuously. For n-pentanol and n-hexanol systems, water solubilization reached a maximum when the oil chain length plus alcohol chain length was equal to that of the surfactant. The electricmore » resistance and dielectric constant of the microemulsions also are measured as a function of alkyl chain length of the oil. 48 references.« less

Transdermal delivery of curcumin via microemulsion.

PubMed

Sintov, Amnon C

2015-03-15

The objective of this study was to evaluate the transdermal delivery potential of a new curcumin-containing microemulsion system. Three series of experiments were carried out to comprehend the system characteristics: (a) examining the influence of water content on curcumin permeation, (b) studying the effect of curcumin loading on its permeability, and (c) assessing the contribution of the vesicular nature of the microemulsion on permeability. The skin permeability of curcumin from microemulsions, which contained 5%, 10%, and 20% of water content (1% curcumin), was measured in vitro using excised rat skin. It has been shown that the permeability coefficient of CUR in a formulation containing 10% aqueous phase (ME-10) was twofold higher than the values obtained for formulations with 5% and 20% water (Papp=0.116 × 10(-3)± 0.052 × 10(-3)vs. 0.043 × 10(-3)± 0.022 × 10(-3) and 0.047 × 10(-3)± 0.025 × 10(-3)cm/h, respectively. A reasonable explanation for this phenomenon may be the reduction of both droplet size and droplets' concentration in the microemulsion as the aqueous phase decreased from 20% to 5%. It has also been shown that a linear correlation exists between the decrease in droplet size and the increase of curcumin loading in the microemulsion. In addition, it has been demonstrated that a micellar system, S/O-mix, and a plain solution of curcumin resulted in a significantly lower curcumin permeation relative to that presented by the microemulsion, Papp=0.018 × 10(-3)± 0.011 × 10(-3), 0.005 × 10(-3)± 0.002 × 10(-3), and 0.002 × 10(-3)± 0.000 × 10(-3)cm/h, respectively, vs. 0.110 × 10(-3)± 0.021 × 10(-3)cm/h for the microemulsion. The enhancement ratio (ER=Jss-ME/Jss-solution) of CUR permeated via 1% loaded microemulsion was 55. Copyright © 2015 Elsevier B.V. All rights reserved.

Clotrimazole microemulsion and microemulsion-based gel: evaluation of buccal drug delivery and irritancy using chick chorioallantoic membrane as the model.

PubMed

Kaewbanjong, Jarika; Wan Sia Heng, Paul; Boonme, Prapaporn

2017-12-01

To investigate the efficacy of clotrimazole microemulsion (CTZ-ME) and its gel form, clotrimazole microemulsion-based gel (CTZ-MBG), for the treatment of oral candidiasis. CTZ-ME and CTZ-MBG were characterized for droplet size and texture, respectively. The ex-vivo permeation study and irritancy assessment of CTZ-ME and CTZ-MBG were performed using chick chorioallantoic membrane (CAM) as the model. Antifungal activity against Candida albicans ATCC 10 231 of CTZ-ME and CTZ-MBG was determined by agar diffusion method compared to the blank counterparts. CTZ-ME contained nano-sized droplets and CTZ-MBG had acceptable firmness and spreadability. CTZ-ME exhibited faster CAM permeation of the drug and larger inhibition zone than CTZ-MBG as the increased viscosity of CTZ-MBG resulted in more retardation and higher fluctuations in drug diffusion. As there were no detectable visual changes in CAM blood vessels after applying CTZ-ME or CTZ-MBG, both formulations were non-irritants. CTZ-ME and CTZ-MBG could deliver the drug through CAM, the model for buccal delivery. Additionally, they did not cause irritancy and had effective antifungal activity against C. albicans. The results indicated that CTZ-ME and CTZ-MBG were potential effective antifungal formulations to treat oral candidiasis. © 2017 Royal Pharmaceutical Society.

Neuroprotective effects and UPLC-Q-TOF/MS-based active components identification of external applied a novel Wen-Luo-Tong microemulsion.

PubMed

Lin, Hong-Mei; Lin, Long-Fei; Xia, Zhen-Zhen; Mao, Yong; Liu, Jia; Xu, Ling-Yan; Wu, Qing

2017-11-13

Chemotherapy induced neuropathy causes excruciating pain to cancer patients. Wen-Luo-Tong (WLT), a traditional Chinese medicinal compound, has been used to alleviate anti-cancer drug such as oxaliplatin-induced neuropathic pain for many years. However, the current route of administration of WLT is inconvenient and the active ingredients and mechanism of action of WLT are still unclear. To address these issues, we developed a novel formulation of WLT (W/O microemulsion) for the ease of application. New ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS) methods were employed for analysis of the ingredients. We identified seven ingredients that penetrated through the skin into the Franz cell receptor solution and four of those ingredients were retained in skin tissue when WLT microemulsion was applied. We tested the microemulsion formulation on an oxaliplatin-induced neuropathy rat model and showed that this formulation significantly decreased oxaliplatin-induced mechanical hyperalgesia responses. Schwann cells (SCs) viability experiment in vitro was studied to test the protective effect of the identified seven ingredients. The result showed that Hydroxysafflor Yellow A, icariin, epimedin B and 4-dihydroxybenzoic acid significantly increased the viability of SCs after injured by Oxaliplatin. Our report presents the first novel formulation of WLT with neuroprotective effect and ease of use, which has potential for clinical applications.

Formulation Optimization and Ex Vivo and In Vivo Evaluation of Celecoxib Microemulsion-Based Gel for Transdermal Delivery.

PubMed

Cao, Mengyuan; Ren, Lili; Chen, Guoguang

2017-08-01

Celecoxib (CXB) is a poorly aqueous solubility sulfonamide non-steroidal anti-inflammatory drug (NSAID). Hence, the formulation of CXB was selected for solubilization and bioavailability. To find out suitable formulation for microemulsion, the solubility of CXB in triacetin (oil phase), Tween 80 (surfactant), and Transcutol-P (co-surfactant) was screened respectively and optimized by using orthogonal experimental design. The Km value and concentration of oil, S mix , and water were confirmed by pseudo-ternary phase diagram studies and central composite design. One percent carbopol 934 was added to form CXB microemulsion-based gel. The final formulation was evaluated for its appearance, pH, viscosity, stability, drug content determination, globule size, and zeta potential. Its ex vivo drug permeation and the in vivo pharmacokinetic was investigated. Further research was performed to ensure the safety and validity by skin irritation study and in vivo anti-inflammatory activity study. Ex vivo permeation study in mice was designed to compare permeation and transdermal ability between microemulsion formulation and conventional gel. The results revealed that optimized microemulsion-based gel gained higher permeation based on smaller globule size and high drug loading of microemulsion. Transdermal ability was also greatly improved. Bioavailability was compared to market Celebrex® by the in vivo pharmacokinetic study in rabbits. The results indicated that CXB microemulsion-based gel had better bioavailability than Celebrex®.

Water-in-Oil Microemulsions for Protein Delivery: Loading Optimization and Stability.

PubMed

Perinelli, Diego R; Cespi, Marco; Pucciarelli, Stefania; Vincenzetti, Silvia; Casettari, Luca; Lam, Jenny K W; Logrippo, Serena; Canala, Elisa; Soliman, Mahmoud E; Bonacucina, Giulia; Palmieri, Giovanni F

2017-01-01

Microemulsions are attractive delivery systems for therapeutic proteins and peptides due to their ability to enhance bioavailability. Although different proteins and peptides have been successfully delivered through such ternary systems, no information can be found about protein loading and the formulation stability when such microemulsions are prepared with pharmaceuticallyapproved oils and surfactants. The aim of this work was to optimise a ternary system consisting of water/ ethyl oleate/Span® 80-Tween® 80 and to determine its protein loading capacity and stability, using bovine serum albumin (BSA) as a model of biomolecule. The optimization was carried out using a Central Composite Design and all the prepared formulations were characterised through dynamic light scattering, rheology, optical and polarized microscopy. Subsequently, the maximum loading capacity was determined and the stability of the final microemulsion with the highest content of protein was followed over six months. To investigate the structural features of the protein, BSA was recovered from the microemulsion and analysed through fluorescence spectroscopy. After incorporation of the protein in the microemulsion, a decrease of its aqueous solubility was observed. However, the formulation remained stable over six months and the native-like state of the recovered protein was demonstrated by fluorescence spectroscopy Conclusion: This study demonstrated the feasibility of preparing microemulsions with the highest content of protein and their long-term stability. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Development and characterization of acrylated palm oil nanoparticles using ionizing radiation

DOE Office of Scientific and Technical Information (OSTI.GOV)

Tajau, Rida; Yunus, Wan Md Zin Wan; Dahlan, Khairul Zaman Mohd

2012-11-27

In this study, the utilization of radiation crosslinking methods which are known as intermolecular and intramolecular crosslinking for the formation of nanoparticles of Acrylated Palm Oil (APO) in the microemulsion system that also consists of Pluronic F-127 (PF-127) surfactant was demonstrated. This microemulsion system was subjected to the ionizing radiation i.e. gamma irradiation at different doses to form the crosslinked APO nanoparticles. The effects of radiation doses on the size of APO nanoparticles were investigated using the Dynamic Light Scattering (DLS) method and their images were viewed using the Transmission Electron Microcrospy (TEM). The Fourier Transform Infra-Red (FTIR) spectroscopy wasmore » used to characterize the chemical structure and the crosslinking conversion of carbon-carbon double bond (-C = C-) of the APO nanoparticles after irradiation. As a result, the size of the APO nanoparticle decreased when the irradiation dose increased. Reduce in size might be due to the effect of intramolecular crosslinking reaction of the APO nanoparticles during irradiation process. Meanwhile, the intramolecular -C C- crosslinking conversion percentage was increased at doses below 1kGy before decreasing at the higher dose that might due to the intermolecular crosslinking of the macromolecules. This study showed that radiation crosslinking methods of polymerization and crosslinking in the microemulsion were found to be promising for the synthesis of nanoparticles.« less

Simultaneous determination of enalapril and hydrochlorothiazide in pharmaceutical preparations using microemulsion liquid chromatography.

PubMed

Hammouda, Mohammed E A; Abu El-Enin, Mohamed A; El-Sherbiny, Dina T; El-Wasseef, Dalia R; El-Ashry, Saadia M

2015-01-01

A rapid high-performance liquid chromatography procedure for analytical quality control of mixture containing enalapril maleate (ENM) and hydrochlorothiazide (HCT) in their pharmaceutical preparations was developed using a microemulsion as an eluent. The separation was performed on a column packed with cyano-bonded stationary phase adopting UV detection at 210 nm using a flow rate of 1 mL/min. The optimized microemulsion mobile phase consisted of 0.2 M sodium dodecyl sulfate, 1% octanol, 10% n-propanol and 0.3% triethylamine in 0.02 M phosphoric acid, and pH was adjusted at 3.5. The proposed method was found to be linear over the concentration ranges 1-100 and 0.05-5 μg/mL for ENM and HCT, respectively with a correlation coefficient of 0.9999 for both drugs. The developed method was validated in terms of specificity, linearity, lower limit of quantification, lower limit of detection, precision and accuracy. The proposed method is rapid (5 min), reproducible (relative standard deviation <2.0%) and achieves a satisfactory resolution between ENM and HCT (resolution factor = 3.62). The mean recoveries of the analytes in tablets were in agreement with those obtained from a comparison method, as revealed by statistical analysis of the obtained results using Student's t-test and the variance ratio F-test. © The Author [2014]. Published by Oxford University Press. All rights reserved. For Permissions, please email: journals.permissions@oup.com.

Kinetic studies of Chromobacterium viscosum lipase in AOT water in oil microemulsions and gelatin microemulsion-based organogels.

PubMed

Jenta, T R; Batts, G; Rees, G D; Robinson, B H

1997-06-05

Kinetic studies have shown that octyl decanoate synthesis by Chromobacterium viscosum (CV) lipase in sodium bis-2-(ethylhexyl) sulfosuccinate (AOT) water in oil (w/o) microemulsions occurs via the nonsequential (ping-pong) bi bi mechanism. There was evidence of single substrate inhibition by decanoic acid at high concentrations. Initial rate data yielded estimates for acid and alcohol Michaelis constants of ca. 10(-1) mol dm(-3) and a maximum rate under saturation conditions of ca. 10(-3) mol dm(-3) s(-1) for a lipase concentration of 0.36 mg cm(-3). CV lipase immobilized in AOT microemulsion-based organogels (MBGs) was also found to catalyze the synthesis of octyl decanoate according to the ping-pong bi bi mechanism. Reaction rates were similar in the free and immobilized systems under comparable conditions. Initial rates at saturating (but noninhibiting) substrate concentrations were first order with respect to CV lipase concentration in both w/o microemulsions and the MBG/oil systems. Gradients yielded an apparent k(cat) = 4.4 x 10(-4) mol g(-1) s(-1) in the case of w/o microemulsions, and 6.1 x 10(-4) mol g(-1) s(-1) for CV lipase immobilized in the MBGs. A third system comprising w/o microemulsions containing substrates and gelatin at concentrations comparable to those employed in the MBG formulations, provided a useful link between the conventional liquid microemulsion medium and the solid organogels. The nongelation of these intermediate systems stems from the early inclusion of substrate during a modified preparative protocol. The presence of substrate appears to prevent the development of a percolated microstructure that is thought to be a prerequisite for MBG formation. FT-NMR was employed as a semicontinuous in situ assay procedure. The apparent activity expressed by CV lipase in compositionally equivalent liquid and solid phase gelatin-containing systems was similar. An apparent activation energy of 24 +/- 2 kJ mol(-1) was determined by (1)H-NMR for esterification in gelatin-containing w/o microemulsions. This value agrees with previous determinations for CV lipase-catalyzed synthesis of octyl decanoate in "conventional" w/o microemulsions and MBG/oil systems. The similarities in lipase behavior are consistent with the claim, based largely on structural measurements, that the physico-chemical properties of the lipase-containing w/o microemulsion are to a large extent preserved on transformation to the daughter organogel. The close agreement of apparrent activation energies suggests that substrate mass transfer is not rate determining in the three studied systems.

Enhanced biodegradation of lindane using oil-in-water bio-microemulsion stabilized by biosurfactant produced by a new yeast strain, Pseudozyma VITJzN01.

PubMed

Abdul Salam, Jaseetha; Das, Nilanjana

2013-11-28

Organochlorine pesticide residues continue to remain as a major environmental threat worldwide. Lindane is an organochlorine pesticide widely used as an acaricide in medicine and agriculture. In the present study, a new lindane-degrading yeast strain, Pseudozyma VITJzN01, was identified as a copious producer of glycolipid biosurfactant. The glycolipid structure and type were elucidated by FTIR, NMR spectroscopy, and GC-MS analysis. The surface activity and stability of the glycolipid was analyzed. The glycolipids, characterized as mannosylerythritol lipids (MELs), exhibited excellent surface active properties and the surface tension of water was reduced to 29 mN/m. The glycolipid was stable over a wide range of pH, temperature, and salinity, showing a very low CMC of 25 mg/l. Bio-microemulsion of olive oil-in-water (O/W) was prepared using the purified biosurfactant without addition of any synthetic cosurfactants, for lindane solubilization and enhanced degradation assay in liquid and soil slurry. The O/W bio-microemulsions enhanced the solubility of lindane up to 40-folds. Degradation of lindane (700 mg/l) by VITJzN01 in liquid medium amended with bio-microemulsions was found to be enhanced by 36% in 2 days, compared with degradation in 12 days in the absence of bio-microemulsions. Lindane-spiked soil slurry incubated with bio-microemulsions also showed 20-40% enhanced degradation compared with the treatment with glycolipids or yeast alone. This is the first report on lindane degradation by Pseudozyma sp., and application of bio-microemulsions for enhanced lindane degradation. MEL-stabilized bio-microemulsions can serve as a potential tool for enhanced remediation of diverse lindanecontaminated environments.

Microemulsion Using Polyoxyethylene Sorbitan Trioleate and its Usage for Skin Delivery of Resveratrol to Protect Skin against UV-Induced Damage.

PubMed

Yutani, Reiko; Teraoka, Reiko; Kitagawa, Shuji

2015-01-01

We examined the phase behavior of various polyoxyethylene sorbitan fatty acid ester (polysorbates)/ethanol/isopropyl myristate (IPM)/150 mM NaCl solution (NaClaq) systems in order to prepare a microemulsion containing a low ratio of ethanol, which is more suitable for in vivo application. Using polyoxyethylene sorbitan trioleate (Tween 85), which has a large lipophilic moiety, as a surfactant component, single-phase domain of the phase diagram was the largest of all the polysorbates examined, and in particular a large oil-rich single-phase domain was obtained. When the ratio of Tween 85 to ethanol was changed from 1 : 1 to 3 : 1, the oil-rich single-phase domain further expanded, which led to a reduced ethanol concentration in the preparation. Thus, we determined the composition of the microemulsion to be Tween 85 : ethanol : IPM : NaClaq=30 : 10 : 53 : 7, and used it for skin delivery of resveratrol. Microemulsion gel was also prepared by adding 6.5% Aerosil) 200 into the microemulsion for ease of topical application. When applied with each vehicle, delivery of resveratrol into guinea pig skin in vitro was significantly enhanced compared with that by IPM, and resveratrol incorporated into the skin by microemulsion gel decreased lipid peroxidation to 29.5% compared with that of the control. Pretreatment of guinea pig dorsal skin with the microemulsion gel containing resveratrol almost completely prevented UV-B-induced erythema formation in vivo. These findings demonstrate that the microemulsion using Tween 85 containing a minimal concentration of ethanol enhanced the skin delivery of resveratrol and the incorporated resveratrol exhibited a protective effect against UV-induced oxidative damage.

Preparation of Essential Oil-Based Microemulsions for Improving the Solubility, pH Stability, Photostability, and Skin Permeation of Quercetin.

PubMed

Lv, Xia; Liu, Tiantian; Ma, Huipeng; Tian, Yan; Li, Lei; Li, Zhen; Gao, Meng; Zhang, Jianbin; Tang, Zeyao

2017-11-01

Quercetin can bring many benefits to skin based on its various bioactivities. However, the therapeutic effect of quercetin is limited due to the poor water solubility, pH instability, light instability, and skin permeation. The aim of the present work was applying essential oil-based microemulsions to improve the solubility, pH stability, photostability, and skin permeation of quercetin for topical application. Peppermint oil (PO-ME), clove oil (CO-ME), and rosemary oil (RMO-ME) were selected as model essential oils. Microemulsions composed of Cremophor EL/1,2-propanediol/essential oils (47:23:30, w/w) were selected as model formulations, based on the pseudo-ternary phase diagram and the characterizations. In the solubility study, the solubility of quercetin was improved dozens of times by microemulsions. Quercetin was found instable under alkaline condition, with 50% degraded in the solution of pH 13. However, PO-ME, CO-ME, and RMO-ME could protect quercetin from the hydroxide ions, with 47, 9, and 12% of quercetin degraded. In the photostability study, the essential oil-based microemulsions showed the capability of protecting quercetin from degradation under UV radiation. Where more than 67% of quercetin was degraded in aqueous solution, while less than 7% of quercetin degraded in microemulsions. At last, the in vitro skin permeation study showed that the essential oil-based microemulsions could enhance the permeation capacity of quercetin by 2.5-3 times compared to the aqueous solution. Hence, the prepared essential oil microemulsions could improve the solubility, pH stability, photostability, and skin permeation of quercetin, which will be beneficial for its topical application.

Testing of resveratrol microemulsion photostability and protective effect against UV induced oxidative stress.

PubMed

Juškaitė, Vaida; Ramanauskienė, Kristina; Briedis, Vitalis

2017-06-27

Resveratrol is well known for its antioxidant activity and susceptibility to ultraviolet radiation. Development of formulations providing improved stability and relevant drug delivery of resveratrol is still a challenging task. The aim of this study was to determine protective characteristics of formulated microemulsions by evaluating photoisomerization of resveratrol and to investigate the effects of resveratrol on human keratinocyte cells under oxidative stress caused by ultraviolet radiation. Incorporation of resveratrol into microemulsions resulted in increased photostability of active compounds and the results demonstrated that photodegradation of resveratrol was significantly delayed. Results of biopharmaceutical evaluation in vitro demonstrated that up to 60 % of resveratrol was released from microemulsions within 6 hours under a constant release rate profile. In vivo biological testing confirmed the ability of resveratrol to protect cells from oxidative stress and to increase cell viability. It was concluded that microemulsions might be considered in the development of UV light sensitive compounds.

CO2-Reactive Ionic Liquid Surfactants for the Control of Colloidal Morphology.

PubMed

Brown, Paul; Sresht, Vishnu; Eral, Burak H; Fiore, Andrew; de la Fuente-Núñez, César; O'Mahony, Marcus; Mendes, Gabriel P; Heller, William T; Doyle, Patrick S; Blankschtein, Daniel; Hatton, T Alan

2017-08-08

This article reports on a new class of stimuli-responsive surfactant generated from commercially available amphiphiles such as dodecyltrimethylammmonium bromide (DTAB) by substitution of the halide counterion with counterions such as 2-cyanopyrrolide, 1,2,3-triazolide, and L-proline that complex reversibly with CO 2 . Through a combination of small-angle neutron scattering (SANS), electrical conductivity measurements, thermal gravimetric analysis, and molecular dynamics simulations, we show how small changes in charge reorganization and counterion shape and size induced by complexation with CO 2 allow for fine-tunability of surfactant properties. We then use these findings to demonstrate a range of potential practical uses, from manipulating microemulsion droplet morphology to controlling micellar and vesicular aggregation. In particular, we focus on the binding of these surfactants to DNA and the reversible compaction of surfactant-DNA complexes upon alternate bubbling of the solution with CO 2 and N 2 .

CO 2 -Reactive Ionic Liquid Surfactants for the Control of Colloidal Morphology

DOE Office of Scientific and Technical Information (OSTI.GOV)

Brown, Paul; Sresht, Vishnu; Eral, Burak H.

Here, this article reports on a new class of stimuli-responsive surfactant generated from commercially available amphiphiles such as dodecyltrimethylammmonium bromide (DTAB) by substitution of the halide counterion with counterions such as 2-cyanopyrrolide, 1,2,3-triazolide, and L-proline that complex reversibly with CO 2. Through a combination of small-angle neutron scattering (SANS), electrical conductivity measurements, thermal gravimetric analysis, and molecular dynamics simulations, we show how small changes in charge reorganization and counterion shape and size induced by complexation with CO 2 allow for fine-tunability of surfactant properties. Additionally, we then use these findings to demonstrate a range of potential practical uses, from manipulatingmore » microemulsion droplet morphology to controlling micellar and vesicular aggregation. In particular, we focus on the binding of these surfactants to DNA and the reversible compaction of surfactant–DNA complexes upon alternate bubbling of the solution with CO 2 and N 2.« less

CO 2 -Reactive Ionic Liquid Surfactants for the Control of Colloidal Morphology

DOE PAGES

Brown, Paul; Sresht, Vishnu; Eral, Burak H.; ...

2017-07-12

Here, this article reports on a new class of stimuli-responsive surfactant generated from commercially available amphiphiles such as dodecyltrimethylammmonium bromide (DTAB) by substitution of the halide counterion with counterions such as 2-cyanopyrrolide, 1,2,3-triazolide, and L-proline that complex reversibly with CO 2. Through a combination of small-angle neutron scattering (SANS), electrical conductivity measurements, thermal gravimetric analysis, and molecular dynamics simulations, we show how small changes in charge reorganization and counterion shape and size induced by complexation with CO 2 allow for fine-tunability of surfactant properties. Additionally, we then use these findings to demonstrate a range of potential practical uses, from manipulatingmore » microemulsion droplet morphology to controlling micellar and vesicular aggregation. In particular, we focus on the binding of these surfactants to DNA and the reversible compaction of surfactant–DNA complexes upon alternate bubbling of the solution with CO 2 and N 2.« less

Effect of microemulsions on cell viability of human dermal fibroblasts

NASA Astrophysics Data System (ADS)

Li, Juyi; Mironava, Tatsiana; Simon, Marcia; Rafailovich, Miriam; Garti, Nissim

Microemulsions are optically clear, thermostable and isotropic mixture consisting of water, oil and surfactants. Their advantages of ease preparation, spontaneous formation, long-term stability and enhanced solubility of bioactive materials make them great potentials as vehicles in food and pharmaceutical applications. In this study, comparative in vitro cytotoxicity tests were performed to select a best formulation of microemulsion with the least toxicity for human dermal fibroblasts. Three different kinds of oils and six different kinds of surfactants were used to form microemulsions by different ratios. The effect of oil type and surfactant type as well as their proportions on cell proliferation and viability were tested.

Self-assembly of phosphate fluorosurfactants in carbon dioxide.

PubMed

Keiper, Jason S; Behles, Jacqueline A; Bucholz, Tracy L; Simhan, Ruma; DeSimone, Joseph M; Lynn, Gary W; Wignall, George D; Melnichenko, Yuri B; Frielinghaus, Henrich

2004-02-17

Anionic phosphodiester surfactants, possessing either two fluorinated chains (F/F) or one hydrocarbon chain and one fluorinated chain (H/F), were synthesized and evaluated for solubility and self-assembly in liquid and supercritical carbon dioxide. Several surfactants, of both F/F and H/F types and having varied counterions, were found to be capable of solubilizing water-in-CO2 (W/C), via the formation of microemulsions, expanding upon the family of phosphate fluorosurfactants already found to stabilize W/C microemulsions. Small-angle neutron scatteringwas used to directly characterize the microemulsion particles at varied temperatures, pressures, and water loadings, revealing behavior consistent with previous results on W/C microemulsions.

Co-delivery of evodiamine and rutaecarpine in a microemulsion-based hyaluronic acid hydrogel for enhanced analgesic effects on mouse pain models.

PubMed

Zhang, Yong-Tai; Li, Zhe; Zhang, Kai; Zhang, Hong-Yu; He, Ze-Hui; Xia, Qing; Zhao, Ji-Hui; Feng, Nian-Ping

2017-08-07

The aim of this study was to improve the analgesic effect of evodiamine and rutaecarpine, using a microemulsion-based hydrogel (ME-Gel) as the transdermal co-delivery vehicle, and to assess hyaluronic acid as a hydrogel matrix for microemulsion entrapment. A microemulsion was formulated with ethyl oleate as the oil core to improve the solubility of the alkaloids and was loaded into a hyaluronic acid-structured hydrogel. Permeation-enhancing effects of the microemulsion enabled evodiamine and rutaecarpine in ME-Gel to achieve 2.60- and 2.59-fold higher transdermal fluxes compared with hydrogel control (p<0.01). The hyaluronic acid hydrogel-containing microemulsion exhibited good skin biocompatibility, whereas effective ME-Gel co-delivery of evodiamine and rutaecarpine through the skin enhanced the analgesic effect in mouse pain models compared with hydrogel. Notably, evodiamine and rutaecarpine administered using ME-Gel effectively down-regulated serum levels of prostaglandin E 2 , interleukin 6, and tumor necrosis factor α in formaldehyde-induced mouse pain models, possibly reflecting the improved transdermal permeability of ME-Gel co-delivered evodiamine and rutaecarpine, particularly with hyaluronic acid as the hydrogel matrix. Copyright © 2017 Elsevier B.V. All rights reserved.

Phase behavior, microstructural transition, antimicrobial and antioxidant activities of a water-dilutable thymol microemulsion.

PubMed

Deng, Lingli; Taxipalati, Maierhaba; Sun, Ping; Que, Fei; Zhang, Hui

2015-12-01

Pseudo ternary phase diagrams were constructed to assess the dilutability of thymol microemulsions using non-ionic (Tween 80), cationic (CTAB), and anionic (SDS) surfactants. We successfully constructed a thymol U-type microemulsion system using Tween 80 as surfactant and studied the microstructural transition along the dilution line at a 90/10 surfactant/oil mass ratio, with thymol and ethanol (3:1, w/w) as the oil phase. Differential scanning calorimetry analysis suggested that the microemulsions gradually inverted from the water-in-oil (W/O) (0-20% water) to the bicontinuous (25-35% water), and finally to the oil-in-water (O/W) (40-90% water) microstructures upon dilution, in good agreement with the conductivity measurements, while the rheological results indicated the collapse of rod-like micelles followed by formation of spherical micelles in the O/W region. The activities of the U-type thymol microemulsions are structural dependent. The antimicrobial activity against Escherichia coli and Staphylococcus aureus decreased when the microemulsions transformed from W/O to bicontinuous and O/W structures, while the DPPH scavenging activity increased. Copyright © 2015 Elsevier B.V. All rights reserved.

Oral microemulsions of paclitaxel: in situ and pharmacokinetic studies.

PubMed

Nornoo, Adwoa O; Zheng, Haian; Lopes, Luciana B; Johnson-Restrepo, Boris; Kannan, Kurunthachalam; Reed, Rachel

2009-02-01

The overall goal of this study was to develop cremophor-free oral microemulsions of paclitaxel (PAC) to enhance its permeability and oral absorption. The mechanism of this enhancement, as well as characteristics of the microemulsions relevant to the increase in permeability and absorption of the low solubility, low permeability PAC was investigated. Phase diagrams were used to determine the macroscopic phase behavior of the microemulsions and to compare the efficiency of different surfactant-oil mixtures to incorporate water. The microemulsion region on the phase diagrams utilizing surfactant-myvacet oil combinations was in decreasing order: lecithin: butanol: myvacet oil (LBM, 48.5%)>centromix CPS: 1-butanol: myvacet oil (CPS, 45.15%)>capmul MCM: polysorbate 80: myvacet oil (CPM, 27.6%)>capryol 90: polysorbate 80: myvacet oil (CP-P80, 23.9%)>capmul: myvacet oil (CM, 20%). Oil-in-water (o/w) microemulsions had larger droplet sizes (687-1010 nm) than the water-in-oil (w/o) microemulsions (272-363 nm) when measured using a Zetasizer nano series particle size analyzer. Utilizing nuclear magnetic resonance spectroscopy (NMR), the self-diffusion coefficient (D) of PAC in CM, LBM and CPM containing 10% of deuterium oxide (D(2)O) was 2.24x10(-11), 1.97x10(-11) and 0.51x10(-11) m(2)/s, respectively. These values indicate the faster molecular mobility of PAC in the two w/o microemulsions (CM and LBM) than the o/w microemulsion--CPM. The in situ permeability of PAC through male CD-IGS rat intestine was 3- and 11-fold higher from LBM and CM, respectively, than that from the control clinical formulation, Taxol (CE, cremophor: ethanol) in a single pass perfusion study. PAC permeability was significantly increased in the presence of the pgp/CYP3A4 inhibitor cyclosporine A (CsA). This enhancement may be attributed to the pgp inhibitory effect of the surfactants, oil and/or the membrane perturbation effect of the surfactants. The oral disposition of PAC in CM, LBM and CPM compared to CE was studied in male CD-IGS rats after a single oral dose (20 mg/kg). The area-under-the-curve of PAC in CM was significantly larger than LBM, CPM and CE. Oral microemulsions of PAC were developed that increased both the permeability and AUC of PAC as compared to CE.

Peroxyl radical reactions with carotenoids in microemulsions: Influence of microemulsion composition and the nature of peroxyl radical precursor.

PubMed

El-Agamey, Ali; McGarvey, David J

2016-01-01

The reactions of acetylperoxyl radicals with different carotenoids (7,7'-dihydro-β-carotene and ζ-carotene) in SDS and CTAC microemulsions of different compositions were investigated using laser flash photolysis (LFP) coupled with kinetic absorption spectroscopy. The primary objective of this study was to explore the influence of microemulsion composition and the type of surfactant used on the yields and kinetics of various transients formed from the reaction of acetylperoxyl radicals with carotenoids. Also, the influence of the site (hydrocarbon phases or aqueous phase) of generation of the peroxyl radical precursor was examined by using 4-acetyl-4-phenylpiperidine hydrochloride (APPHCl) and 1,1-diphenylacetone (11DPA) as water-soluble and lipid-soluble peroxyl radical precursors, respectively. LFP of peroxyl radical precursors with 7,7'-dihydro-β-carotene (77DH) in different microemulsions gives rise to the formation of three distinct transients namely addition radical (λmax=460 nm), near infrared transient1 (NIR, λmax=700 nm) and 7,7'-dihydro-β-carotene radical cation (77DH(•+), λmax=770 nm). In addition, for ζ-carotene (ZETA) two transients (near infrared transient1 (NIR1, λmax=660 nm) and ζ-carotene radical cation (ZETA(•+), λmax=730-740 nm)) are generated following LFP of peroxyl radical precursors in the presence of ζ-carotene (ZETA) in different microemulsions. The results show that the composition of the microemulsion strongly influences the observed yield and kinetics of the transients formed from the reactions of peroxyl radicals (acetylperoxyl radicals) with carotenoids (77DH and ZETA). Also, the type of surfactant used in the microemulsions influences the yield of the transients formed. The dependence of the transient yields and kinetics on microemulsion composition (or the type of surfactant used in the microemulsion) can be attributed to the change of the polarity of the microenvironment of the carotenoid. Furthermore, the nature of the peroxyl radical precursor used (water-soluble or lipid-soluble peroxyl radical precursors) has little influence on the yields and kinetics of the transients formed from the reaction of peroxyl radicals with carotenoids. In the context of the interest in carotenoids as radical scavenging antioxidants, the fates of the addition radicals (formed from the reaction of carotenoid with peroxyl radicals) and carotenoid radical cations are discussed. Copyright © 2015 Elsevier Inc. All rights reserved.

Characteristics of Nano-emulsion for Cold Thermal Storage

NASA Astrophysics Data System (ADS)

Fumoto, Koji; Kawaji, Masahiro; Kawanami, Tsuyoshi

Phase change emulsion (PCE) is novel kind of heat storage and heat transfer fluids. It has characteristics as follows; greater apparent specific heat and higher heat transfer abilities in the phase change temperature range than conventional single phase heat transfer fluid. In this paper, a phase change emulsion, which has droplet diameter distribution of nanometer, were prepared. The Nano-emulsion was formed by low energy emulsification methods, as known the phase inversion temperature (PIT) method. Physical properties, such as viscosity, diameter and its distribution of emulsion were investigated. Especially, the relationships between preparation method and the concentration of surfactant have been discussed in detail. The results show that the viscosity of the Nano-emulsion is lower than the micro-emulsion, which was made by same mixing ratio of surfactant and concentration of phase change material. In addition, the Nano-emulsion clarified that stability was higher than microemulsions.

Physicochemical and pharmacological investigation of water/oil microemulsion of non-selective beta blocker for treatment of glaucoma.

PubMed

Hegde, Rahul Rama; Bhattacharya, Shiv Sankar; Verma, Anurag; Ghosh, Amitava

2014-02-01

Ocular drug delivery system always remained associated with lots of difficulties and faced issues of poor drug absorption and poor bioavailability. Timolol maleate is a nonspecific beta blocker used for reduction of elevated intraocular pressure in glaucoma. Timolol maleate is absorbed systemically and is contraindicated in asthmatic patients. This study is focused to deliver Timolol maleate by a water/oil microemulsion to extend the time of reduced intraocular pressure of glaucomatous rabbit's eye measured by using a Schoetz tonometer. The microemulsion is prepared by mixing the oily components with two nonionic surfactants, drug and water, and evaluated for the physicochemical, in vitro and in vivo parameters. The colloidal system demonstrates monodisperse distribution behavior and exhibits a uniform size distribution of finite width. In vitro drug release from microemulsion was found to follow Higuchi's pattern followed by a zero-order drug release by the emulsion. Ex vivo permeation through goat cornea revealed delayed release of Timolol maleate from microemulsion as compared with its aqueous solution. A reduction in intraocular pressure is seen lasting for 12 h compared to aqueous eye drop that lasted for only 5 h. CONCLUSION. In vivo reduction of intraocular pressure revealed a similar efficacy for once daily dosed 0.3% Timolol maleate in microemulsion formulation compared to 0.5% concentration in both microemulsion as well as aqueous formulation. The possible outcome of dose reduction will reduce the cardiovascular side effects generally reported with Timolol maleate eye drops.

New vehicle based on a microemulsion for topical ocular administration of dexamethasone.

PubMed

Fialho, Sílvia Ligório; da Silva-Cunha, Armando

2004-12-01

Eye drops are the most used dosage form by the ocular route, in spite of their low bioavailability. Due to their properties and numerous advantages, microemulsions are promising systems for topical ocular drug delivery. They can increase water solubility of the drug and enhance drug absorption into the eye. The present study describes the development and characterization of an oil-in-water microemulsion containing dexamethasone and the evaluation of its pharmacokinetics in rabbits after topical ocular application. The microemulsion was prepared by the titration technique. Its physico-chemical characteristics and stability were determined. The ocular irritation test and the pharmacokinetics of this system were studied in white rabbits. The developed system showed an acceptable physico-chemical behaviour and presented good stability for 3 months. The ocular irritation test used suggested that the microemulsion did not provide significant alteration to eyelids, conjunctiva, cornea and iris. This formulation showed greater penetration of dexamethasone in the anterior segment of the eye and also release of the drug for a longer time when compared with a conventional preparation. The area under the curve obtained for the microemulsion system was more than twofold higher than that of the conventional preparation (P < 0.05). The microemulsion-based dexamethasone eye drop is advantageous for ophthalmic use because it is well-tolerated in the eye and seemed to provide a higher degree of bioavailability. The developed system shows greater penetration in the eye, allowing the possibility of decreasing the number of applications of eye drops per day.

Biocompatible microemulsions of a model NSAID for skin delivery: A decisive role of surfactants in skin penetration/irritation profiles and pharmacokinetic performance.

PubMed

Todosijević, Marija N; Savić, Miroslav M; Batinić, Bojan B; Marković, Bojan D; Gašperlin, Mirjana; Ranđelović, Danijela V; Lukić, Milica Ž; Savić, Snežana D

2015-12-30

To elaborate the decisive role of surfactants in promotion of aceclofenac' skin absorption, potentially avoiding irritation, we developed non-ionic microemulsions varying natural or synthetic surfactants: sucrose esters (laurate or myristate) vs. polysorbate 80. A comprehensive physicochemical characterization indicated no significant influence of the solubilized nonsteroidal anti-inflammatory drug on the bicontinuous structure of blank formulations. To evaluate skin tolerability of isopropyl alcohol, a sucrose ester-based microemulsion containing transcutol P as a cosurfactant was also developed. The measured skin parameters strongly depended on the (co)surfactant type, showing higher compatibility of the microemulsions containing sucrose ester and isopropyl alcohol. In vitro release results, in vivo tape stripping and pharmacokinetics in rats confirmed superiority of the sucrose ester- over polysorbate-based microemulsions (total amounts of aceclofenac penetrated 60.81±5.97 and 60.86±3.67 vs. 27.00±5.09μg/cm(2), and its maximum plasma concentrations 275.57±109.49 and 281.31±76.76 vs. 150.23±69.74ng/ml for sucrose laurate- and myristate- vs. polysorbate 80-based microemulsions, respectively). Hence, sugar-based excipients increased delivery of aceclofenac through stratum corneum by increasing its fluidity, showing overall more satisfying safety profiles. In conclusion, sucrose ester-based microemulsions proved to be promising carriers for dermal/transdermal aceclofenac delivery. Copyright © 2015 Elsevier B.V. All rights reserved.

Preparation and photocatalytic properties of nanometer-sized magnetic TiO2/SiO2/CoFe2O4 composites.

PubMed

Li, Hansheng; Zhang, Yaping; Wu, Qin; Wang, Xitao; Liu, Changhao

2011-11-01

Magnetic TiO2/SiO2/CoFe2O4 nanoparticles (TiO2/SCFs) were prepared by a sol-gel process in a reverse microemulsion combined with solvent-thermal technique. TiO2/SCFs were characterized by Fourier transform infrared spectrometry, thermogravimetric analysis-differential scanning calorimetry, X-ray diffraction, Raman spectrometry, TEM, BET specific surface area measurement, and magnetic analysis. Structure analyses indicated that TiO2/SCFs presented a core-shell structure with TiO2 uniformly coating on SiO2/CoFe2O4 nanomagnets (SCFs) and typical ferromagnetic hysteresis. TiO2/SCFs showed larger specific surface area and better photocatalytic activities than TiO2 and TiO2/CoFe2O4 photocatalysts prepared by the same method. The doping interaction between TiO2 and CoFe2O4 reduced thanks to the inert SiO2 mesosphere.

Synthesis and characterization of chitosan-coated magnetite nanoparticles and their application in curcumin drug delivery

NASA Astrophysics Data System (ADS)

Nui Pham, Xuan; Phuoc Nguyen, Tan; Nhung Pham, Tuyet; Thuy Nga Tran, Thi; Van Thi Tran, Thi

2016-12-01

In this work anti-cancer drug curcumin-loaded superparamagnetic iron oxide (Fe3O4) nanoparticles was modified by chitosan (CS). The magnetic iron oxide nanoparticles were synthesized by using reverse micro-emulsion (water-in-oil) method. The magnetic nanoparticles without loaded drug and drug-loaded magnetic nanoparticles were characterized by XRD, FTIR, TG-DTA, SEM, TEM, and VSM techniques. These nanoparticles have almost spherical shape and their diameter varies from 8 nm to 17 nm. Measurement of VSM at room temperature showed that iron oxide nanoparticles have superparamagnetic properties. In vitro drug loading and release behavior of curcumin drug-loaded CS-Fe3O4 nanoparticles were studied by using UV-spectrophotometer. In addition, the cytotoxicity of the modified nanoparticles has shown anticancer activity against A549 cell with IC50 value of 73.03 μg/ml. Therefore, the modified magnetic nanoparticles can be used as drug delivery carriers on target in the treatment of cancer cells.

Improving the Thermoelectric Properties of Polyaniline by Introducing Poly(3,4-ethylenedioxythiophene)

NASA Astrophysics Data System (ADS)

Wang, Xiao Yang; Liu, Cheng Yan; Miao, Lei; Gao, Jie; Chen, Yu

2016-03-01

By using the parent monomers, 3,4-ethylenedioxythiophene and aniline, a series of nanocomposites consisting of different mass ratios of polyaniline (PANI) to poly(3,4-ethylenedioxythiophene) (PEDOT) have been successfully prepared in hydrochloric acid solution through oxidative polymerization, then redoped with p-toluenesulfonic acid ( p-TSA). Firstly, PEDOT nanoparticles were fabricated via chemical oxidation polymerization in reverse (water-in-oil) microemulsions. Then, PANI-doped PEDOT nanoparticles were formed by oxidative polymerization of aniline to form PANI/PEDOT nanofibers. The resulting nanostructured components were characterized by scanning electron microscopy (SEM) and a series of spectroscopic methods. The presence of PEDOT increased the room-temperature electrical conductivity of the PANI/PEDOT nanocomposites by more than two orders of magnitude in comparison with the parent PANI. Moreover, the PANI/PEDOT nanocomposites showed better thermoelectric properties than PANI. Different concentrations of p-TSA also affected the electrical conductivity and Seebeck coefficient of the nanocomposites. With increasing temperature, both the electrical conductivity and Seebeck coefficient increased.

A micrometer-sized europium(iii)-organic framework for selective sensing of the Cr2O72- anion and picric acid in water systems.

PubMed

He, Hongming; Chen, Si-Hang; Zhang, De-Yu; Hao, Rui; Zhang, Chao; Yang, En-Cui; Zhao, Xiao-Jun

2017-10-10

A micrometer-sized europium(iii)-organic framework with asymmetric binuclear metal subunits extended by 4,5-dichlorophthalaten (DCPA), [Eu 2 (H 2 O)(DCPA) 3 ] n , was easily obtained using a reverse microemulsion method. The framework exhibits good dispersibility, excellent thermal and environmental stability and easy regeneration ability. More importantly, the complex displays strong red emission and can selectively and sensitively detect both inorganic Cr 2 O 7 2- anions (K sv = 8.7 × 10 3 M -1 ) and organic picric acid contaminants (K sv = 1.07 × 10 4 M -1 ) in water systems through fluorescence quenching. A luminescent film of 1 was further prepared and successfully used to detect the Cr 2 O 7 2- anion in an aqueous system. These interesting results indicate that the well-dispersed europium(iii)-organic framework can serve as a promising dual-responsive luminescent sensor for environmental pollutant monitoring.

Silica nanoparticles with a substrate switchable luminescence

NASA Astrophysics Data System (ADS)

Bochkova, O. D.; Mustafina, A. R.; Fedorenko, S. V.; Konovalov, A. I.

2011-04-01

Silica nanoparticles with visible (Tb and Ru doped), near IR (Yb doped) and dual visible-near IR luminescence (Ru-Yb doped) were obtained by reverse w/o microemulsion procedure. Plenty of luminescent complexes (from 4900 to 10000) encapsulated into each nanoparticle ensures the intensive luminescence of nanoparticles and their applicability as biomarkers. The silica surface decoration by definite anchor groups is the required step for the gaining to these nanoparticles marking and sensing functions. Thus covalent and non-covalent surface modification of these nanoparticles was developed to provide the binding with biotargets and sensing of anions. The dicationic surfactant coating of negatively charged Tb(III)-TCAS doped silica nanoparticles was chosen as the basis for the anion responsible system. The reversible insertion of the quenching anions (namely phenol red) into the surfactant based layer at the surface of luminescent nanoparticles switches off the Tb-centered luminescence. In turn the reversible reestablishment of the luminescence results from the competitive insertion of the non-quenching anions into the surfactant layer at the silica/water interface. The hydrophobic anions exemplified by dodecylsulfates versus hydrophilic ones (hydrophosphates) are preferable in the competition with phenol red anions.

Nanoscale Hollow Spheres: Microemulsion-Based Synthesis, Structural Characterization and Container-Type Functionality

PubMed Central

Gröger, Henriette; Kind, Christian; Leidinger, Peter; Roming, Marcus; Feldmann, Claus

2010-01-01

A wide variety of nanoscale hollow spheres can be obtained via a microemulsion approach. This includes oxides (e.g., ZnO, TiO2, SnO2, AlO(OH), La(OH)3), sulfides (e.g., Cu2S, CuS) as well as elemental metals (e.g., Ag, Au). All hollow spheres are realized with outer diameters of 10−60 nm, an inner cavity size of 2−30 nm and a wall thickness of 2−15 nm. The microemulsion approach allows modification of the composition of the hollow spheres, fine-tuning their diameter and encapsulation of various ingredients inside the resulting “nanocontainers”. This review summarizes the experimental conditions of synthesis and compares them to other methods of preparing hollow spheres. Moreover, the structural characterization and selected properties of the as-prepared hollow spheres are discussed. The latter is especially focused on container-functionalities with the encapsulation of inorganic salts (e.g., KSCN, K2S2O8, KF), biomolecules/bioactive molecules (e.g., phenylalanine, quercetin, nicotinic acid) and fluorescent dyes (e.g., rhodamine, riboflavin) as representative examples. PMID:28883333

Optimization of processing parameters for the preparation of phytosterol microemulsions by the solvent displacement method.

PubMed

Leong, Wai Fun; Che Man, Yaakob B; Lai, Oi Ming; Long, Kamariah; Misran, Misni; Tan, Chin Ping

2009-09-23

The purpose of this study was to optimize the parameters involved in the production of water-soluble phytosterol microemulsions for use in the food industry. In this study, response surface methodology (RSM) was employed to model and optimize four of the processing parameters, namely, the number of cycles of high-pressure homogenization (1-9 cycles), the pressure used for high-pressure homogenization (100-500 bar), the evaporation temperature (30-70 degrees C), and the concentration ratio of microemulsions (1-5). All responses-particle size (PS), polydispersity index (PDI), and percent ethanol residual (%ER)-were well fit by a reduced cubic model obtained by multiple regression after manual elimination. The coefficient of determination (R(2)) and absolute average deviation (AAD) value for PS, PDI, and %ER were 0.9628 and 0.5398%, 0.9953 and 0.7077%, and 0.9989 and 1.0457%, respectively. The optimized processing parameters were 4.88 (approximately 5) homogenization cycles, homogenization pressure of 400 bar, evaporation temperature of 44.5 degrees C, and concentration ratio of microemulsions of 2.34 cycles (approximately 2 cycles) of high-pressure homogenization. The corresponding responses for the optimized preparation condition were a minimal particle size of 328 nm, minimal polydispersity index of 0.159, and <0.1% of ethanol residual. The chi-square test verified the model, whereby the experimental values of PS, PDI, and %ER agreed with the predicted values at a 0.05 level of significance.

Curcumin Protects Skin against UVB-Induced Cytotoxicity via the Keap1-Nrf2 Pathway: The Use of a Microemulsion Delivery System.

PubMed

Ben Yehuda Greenwald, Maya; Frušić-Zlotkin, Marina; Soroka, Yoram; Ben Sasson, Shmuel; Bitton, Ronit; Bianco-Peled, Havazelet; Kohen, Ron

2017-01-01

Curcumin was found to be beneficial in treating several skin pathologies and diseases, providing antioxidant protection due to its reducing properties and its electrophilic properties (the ability to activate the Nrf 2 pathway and induce phase II cytoprotective enzymes). Nevertheless, clinical applications of curcumin are being hampered by its insufficient solubility, chemical instability, and poor absorption, leading to low efficacy in preventing skin pathologies. These limitations can be overcome by using a nanotechnology-based delivery system. Here, we elucidated the possibility of using curcumin encapsulated in a microemulsion preserving its unique chemical structure. We also examined whether curcumin microemulsion would reduce UVB-induced toxicity in skin. A significant curcumin concentration was found in the human skin dermis following topical application of a curcumin microemulsion. Moreover, curcumin microemulsion enhanced the reduction of UV-induced cytotoxicity in epidermal cells, paving the way for other incorporated electrophiles in encapsulated form protecting skin against stress-related diseases.

Curcumin Protects Skin against UVB-Induced Cytotoxicity via the Keap1-Nrf2 Pathway: The Use of a Microemulsion Delivery System

PubMed Central

Ben Yehuda Greenwald, Maya; Frušić-Zlotkin, Marina; Soroka, Yoram; Ben Sasson, Shmuel; Bitton, Ronit; Bianco-Peled, Havazelet

2017-01-01

Curcumin was found to be beneficial in treating several skin pathologies and diseases, providing antioxidant protection due to its reducing properties and its electrophilic properties (the ability to activate the Nrf2 pathway and induce phase II cytoprotective enzymes). Nevertheless, clinical applications of curcumin are being hampered by its insufficient solubility, chemical instability, and poor absorption, leading to low efficacy in preventing skin pathologies. These limitations can be overcome by using a nanotechnology-based delivery system. Here, we elucidated the possibility of using curcumin encapsulated in a microemulsion preserving its unique chemical structure. We also examined whether curcumin microemulsion would reduce UVB-induced toxicity in skin. A significant curcumin concentration was found in the human skin dermis following topical application of a curcumin microemulsion. Moreover, curcumin microemulsion enhanced the reduction of UV-induced cytotoxicity in epidermal cells, paving the way for other incorporated electrophiles in encapsulated form protecting skin against stress-related diseases. PMID:28757910

Simulated formation and flow of microemulsions during surfactant flushing of contaminated soil.

PubMed

Ouyan, Ying; Cho, Jong Soo; Mansell, Robert S

2002-01-01

Contamination of groundwater resources by non-aqueous phase liquids (NAPLs) has become an issue of increasing environmental concern. This study investigated the formation and flow of microemulsions during surfactant flushing of NAPL-contaminated soil using the finite difference model UTCHEM, which was verified with our laboratory experimental data. Simulation results showed that surfactant flushing of NAPLs (i.e., trichloroethylene and tetrachloroethylene) from the contaminated soils was an emulsion-driven process. Formation of NAPL-in-water microemulsions facilitated the removal of NAPLs from contaminated soils. Changes in soil saturation pressure were used to monitor the mobilization and entrapment of NAPLs during surface flushing process. In general, more NAPLs were clogged in soil pores when the soil saturation pressure increased. Effects of aquifer salinity on the formation and flow of NAPL-in-water microemulsions were significant. This study suggests that the formation and flow of NAPL-in-water microemulsions through aquifer systems are complex physical-chemical phenomena that are critical to effective surfactant flushing of contaminated soils.

Extraction of trace elements by ultrasound-assisted emulsification from edible oils producing detergentless microemulsions.

PubMed

Kara, Derya; Fisher, Andrew; Hill, Steve

2015-12-01

The aim of this study is to develop a new method for the extraction and preconcentration of trace elements from edible oils via an ultrasound-assisted extraction using ethylenediaminetetraacetic acid (EDTA) producing detergentless microemulsions. These were then analyzed using ICP-MS against matrix matched standards. Optimum experimental conditions were determined and the applicability of the proposed ultrasound-assisted extraction method was investigated. Under the optimal conditions, the detection limits (μg kg(-1)) were 2.47, 2.81, 0.013, 0.037, 1.37, 0.050, 0.049, 0.47, 0.032 and 0.087 for Al, Ca, Cd, Cu, Mg, Mn, Ni, Ti, V and Zn respectively for edible oils (3Sb/m). The accuracy of the developed method was checked by analyzing certified reference material. The proposed method was applied to different edible oils such as sunflower seed oil, rapeseed oil, olive oil and cod liver oil. Copyright © 2015 Elsevier Ltd. All rights reserved.

Post-Self-Assembly Cross-Linking to Integrate Molecular Nanofibers with Copolymers in Oscillatory Hydrogels

DTIC Science & Technology

2013-05-09

The BZ reaction provides a model system to mimic a variety of complex processes, such as biological morphogenesis, in monodisperse microemulsions .15...surfaces, ion-exchange resins, membranes, and microemulsions . For example, in addition to minimizing the hydrodynamic effects and formation of bubbles...Reaction-Diffusion Microemulsions Reveals Three-Dimensional Tu- ring Patterns. Science (Washington, DC, U.S.) 2011, 331, 1309−1312. (16) Agladze, K. I

Method of remediation of contaminants in porous media through minimization of bouyancy effects

DOEpatents

Shook, G. Michael; Pope, Gary A.

1999-01-01

A method for controlling vertical migration of contaminants in an aquifer includes introduction of a solubilizing solution having a surfactant and an alcohol or other light co-solvent. The surfactant is selected to solubilize the contaminant. The alcohol or other solvent is selected to provide the microemulsion with a substantially neutral buoyancy with respect to groundwater. The neutral buoyancy of the microemulsion prevents the normal downward movement which is typical of the solubilized dense non-aqueous phase liquid in surfactant-enhanced aquifer remediation. Thus, the risk that any significant amount of the solubilized dense non-aqueous contaminants will migrate vertically can be controlled. The relative tendency for vertical migration may also be reduced by increasing the injection rate or injected fluid viscosity (by adding polymer), or by reducing the well spacing.

Fluorescence quenching of protonated β-carbolines in water and microemulsions: evidence for heavy-atom and electron-transfer mechanisms.

PubMed

Mousa, Souad A; Douglas, Peter; Burrows, Hugh D; Fonseca, Sofia M

2013-09-01

The fluorescence quenching of protonated β-carbolines has been investigated in acidic aqueous solutions and in w/o microemulsions using I(-), Br(-), Cu(2+), SCN(-), and Pb(2+) as quenchers. It was found that fluorescence quenching by these compounds is much more efficient in water than in microemulsions since quenching in microemulsions depends on the simultaneous occupancy of the water droplets by both fluorophore and quencher. Linear Stern-Volmer plots were obtained in all cases, leading to quenching rate constants of ca. 10(8)-10(10) M(-1) s(-1) in water and ca. 10(7)-10(8) M(-1) s(-1) in microemulsions. In the case of quenching by SCN(-), ns flash photolysis studies indicate formation of (SCN)2(˙-) showing that at least part of the quenching process involves an electron transfer mechanism. This indicates that the singlet excited states of the protonated β-carbolines can act as relatively strong oxidants (E° > 1.6 V), capable of oxidizing many species, including the biologically relevant DNA base guanine. The observation of the (SCN)2(˙-) transient in microemulsions demonstrates that it is possible to have the protonated β-carboline and at least two thiocyanate ions in the same water pool.

Preparation and evaluation of novel microemulsion-based hydrogels for dermal delivery of benzocaine.

PubMed

Üstündağ Okur, Neslihan; Çağlar, Emre Şefik; Arpa, Muhammet Davut; Karasulu, H Yeşim

2017-06-01

The purpose of the current research was to prepare and evaluate the potential use of microemulsion-based hydrogel (MBH) formulations for dermal delivery of benzocaine (BZN). The pseudoternary-phase diagrams were constructed for various microemulsions composed of isopropyl myristate (IPM) as oil phase, Span 20, Tween 20, Tween 80, cremophor EL and cremophor RH40 as surfactants, ethanol as cosurfactant and distilled water as aqueous phase. Finally, concentration of BZN in microemulsions was 2% (w/w). The physicochemical properties, such as conductivity, viscosity, pH, droplet size, polydispersity index and zeta potential of microemulsions, were measured. Carbopol 940 was used to convert BZN-loaded microemulsions into gel form without affecting their structure. Furthermore, excised rat abdominal skin was used to compare permeation and penetration properties of BZN loaded M3 and M3BHs with BZN solution. According to ex vivo study results, BZN-loaded M3BH1 showed highest flux values and high release rate values, and furthermore, this gel formulation had low surfactant content. Finally, in order to learn the localization of formulations within the dermal penetration, formulations and BZN solution were labeled with red oil O and subjected to fluorescence observation. In conclusion, BZN-loaded MBHs could be offered as a promising strategy for dermal drug delivery.

Microemulsion-Based Mucoadhesive Buccal Wafers: Wafer Formation, In Vitro Release, and Ex Vivo Evaluation.

PubMed

Pham, Minh Nguyet; Van Vo, Toi; Tran, Van-Thanh; Tran, Phuong Ha-Lien; Tran, Thao Truong-Dinh

2017-10-01

Microemulsion has the potentials to enhance dissolution as well as facilitate absorption and permeation of poorly water-soluble drugs through biological membranes. However, its application to govern a controlled release buccal delivery for local treatment has not been discovered. The aim of this study is to develop microemulsion-based mucoadhesive wafers for buccal delivery based on an incorporation of the microemulsion with mucoadhesive agents and mannitol. Ratio of oil to surfactant to water in the microemulsion significantly impacted quality of the wafers. Furthermore, the combination of carbopol and mannitol played a key role in forming the desired buccal wafers. The addition of an extra 50% of water to the formulation was suitable for wafer formation by freeze-drying, which affected the appearance and distribution of carbopol in the wafers. The amount of carbopol was critical for the enhancement of mucoadhesive properties and the sustained drug release patterns. Release study presented a significant improvement of the drug release profile following sustained release for 6 h. Ex vivo mucoadhesive studies provided decisive evidence to the increased retention time of wafers along with the increased carbopol content. The success of this study indicates an encouraging strategy to formulate a controlled drug delivery system by incorporating microemulsions into mucoadhesive wafers.

In vitro and in vivo evaluation of capsaicin-loaded microemulsion for enhanced oral bioavailability.

PubMed

Zhu, Yuan; Zhang, Jiajia; Zheng, Qianfeng; Wang, Miaomiao; Deng, Wenwen; Li, Qiang; Firempong, Caleb Kesse; Wang, Shengli; Tong, Shanshan; Xu, Ximing; Yu, Jiangnan

2015-10-01

Capsaicin, as a food additive, has attracted worldwide concern owing to its pungency and multiple pharmacological effects. However, poor water solubility and low bioavailability have limited its application. This study aims to develop a capsaicin-loaded microemulsion to enhance the oral bioavailability of the anti-neuropathic-pain component, capsaicin, which is poorly water soluble. In this study, the microemulsion consisting of Cremophor EL, ethanol, medium-chain triglycerides (oil phase) and water (external phase) was prepared and characterized (particle size, morphology, stability and encapsulation efficiency). The gastric mucosa irritation test of formulated capsaicin was performed in rats to evaluate its oral feasibility, followed by the pharmacokinetic study in vivo. Under these conditions, the encapsulated capsaicin revealed a faster capsaicin release in vitro coupled with a greater absorption in vivo when compared to the free capsaicin. The oral bioavailability of the formulated capsaicin-loaded microemulsions was 2.64-fold faster than that of free capsaicin. No significant irritation was observed on the mucosa from the pathological section of capsaicin-loaded microemulsion treated stomach. These results indicate that the developed microemulsion represents a safe and orally effective carrier for poorly soluble substances. The formulation could be used for clinical trials and expand the application of capsaicin. © 2014 Society of Chemical Industry.

Development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability

PubMed Central

Sane, Ramola; Mittapalli, Rajendar K.; Elmquist, William F.

2014-01-01

The study objective was to develop a formulation of elacridar to overcome its dissolution-rate limited bioavailability. Elacridar is a P-gp and BCRP inhibitor that has been used to improve the brain distribution of drugs that are substrates of P-gp and BCRP. The chronic use of elacridar is restricted due to poor solubility leading to poor oral bioavailability. A microemulsion formulation using Cremophor EL, Carbitol and Captex 355 (6:3:1) was developed. The elacridar microemulsion was effective in the inhibition of P-gp and Bcrp in MDCKII-transfected cells. FVBn mice were used to determine the bioavailability of elacridar after a 10 mg/kg dose of elacridar in the microemulsion, intraperitoneally and orally; and the absolute bioavailability was determined to be 1.3 and 0.47, respectively. Co-administration of elacridar microemulsion intraperitoneally with oral erlotinib in FVBn mice improved the erlotinib brain penetration three-fold. The current study shows that a microemulsion formulation of elacridar is effective in improving the bioavailability of elacridar and is an effective inhibitor of P-gp and Bcrp; in-vitro and in-vivo. It offers an alternative to the suspension and allows a decrease in the dose required to achieve a significant inhibitory effect at the blood-brain barrier. PMID:23334925

Ultrasound mediates the release of curcumin from microemulsions.

PubMed

Lee, Mei-Hwa; Lin, Hung-Yin; Chen, Hsu-Chih; Thomas, James L

2008-03-04

Ultrasound is a powerful noninvasive modality for biomedical imaging, and holds much promise for noninvasive drug delivery enhancement and targeting. However, the optimal design of sound sensitive carriers is still poorly understood. In this study, curcumin, an important natural antioxidant and anticancer compound, was stably entrapped into microemulsion droplets with average size 20-35 nm. To release curcumin, low frequency (40 kHz) ultrasound at an intensity of 3.8 or 9.8 W/cm2 was applied to the microemulsions, using a probe sonicator. On insonation, much of the curcumin was released from the microemulsions and formed insoluble aggregates, as evidenced by decreased UV-vis absorption at 420 nm. The initial release rate (assayed by the rate of change of absorption) was as high as 0.11 microg/s (1.87%/sec) in phosphate buffered saline solution at neutral pH, but decreased at acidic pH. Interestingly, lower curcumin loading led to a more rapid release under insonation. Measurements of emulsion droplet size implicate droplet reorganization (fusion or fission) as an important contributing mechanism for the ultrasonic release of this compound. Although cargo in microemulsions is partitioned, rather than encapsulated (as in, for example, liposomes), these new results demonstrate that microemulsion carriers are feasible for some ultrasonic drug delivery applications.

Stability assessment of lycopene microemulsion prepared using tomato industrial waste against various processing conditions.

PubMed

Amiri-Rigi, Atefeh; Abbasi, Soleiman

2017-11-01

Green separation techniques are growing at a greater rate than solvent extraction as a result of the constant consumer drive to 'go natural'. Considering the increasing evidence of the health benefits of lycopene and massive tomato industrial waste, in the present study, lycopene was extracted from tomato industrial waste using microemulsion technique and its mean droplet size and size distribution was determined. Moreover, the effects of pasteurization, sterilization, freeze-thaw cycles and ultraviolet (UV) irradiation on the thermodynamic stability, turbidity and lycopene concentration of the lycopene microemulsion were monitored. Freeze-thaw cycles, pasteurization and short exposure to UV irradiation showed no or negligible influence on lycopene content and turbidity of the microemulsion. However, long exposure to UV (260 min) reduced the lycopene content and turbidity by 34% and 10%, respectively. HHST (higher-heat shorter-time) and sterilization also reduced lycopene content (25%) and increased turbidity (32%). The lycopene microemulsion showed satisfactory stability over a process where its monodispersity and nanosize could be of potential advantage to the food and related industries. Regarding the carcinogenicity of synthetic colourants, potential applications of the lycopene microemulsion include in soft drinks and minced meat, which would result in a better colour and well-documented health-promoting qualities. © 2017 Society of Chemical Industry. © 2017 Society of Chemical Industry.

Effect of chain length on binding of fatty acids to Pluronics in microemulsions.

PubMed

James-Smith, Monica A; Shekhawat, Dushyant; Cheung, Sally; Moudgil, Brij M; Shah, Dinesh O

2008-03-15

We investigated the effect of fatty acid chain length on the binding capacity of drug and fatty acid to Pluronic F127-based microemulsions. This was accomplished by using turbidity experiments. Pluronic-based oil-in-water microemulsions of various compositions were synthesized and titrated to turbidity with concentrated Amitriptyline, an antidepressant drug. Sodium salts of C(8), C(10), or C(12) fatty acid were used in preparation of the microemulsion and the corresponding binding capacities were observed. It has been previously determined that, for microemulsions prepared with sodium caprylate (C(8) fatty acid soap), a maximum of 11 fatty acid molecules bind to the microemulsion per 1 molecule of Pluronic F127 and a maximum of 12 molecules of Amitriptyline bind per molecule of F127. We have found that with increasing the chain length of the fatty acid salt component of the microemulsion, the binding capacity of both the fatty acid and the Amitriptyline to the microemulsion decreases. For sodium salts of C(8), C(10) and C(12) fatty acids, respectively, a maximum of approximately 11, 8.4 and 8.3 molecules of fatty acid molecules bind to 1 Pluronic F127 molecule. We propose that this is due to the decreasing number of free monomers with increasing chain length. As chain length increases, the critical micelle concentration (cmc) decreases, thus leading to fewer monomers. Pluronics are symmetric tri-block copolymers consisting of propylene oxide (PO) and ethylene oxide (EO). The polypropylene oxide block, PPO is sandwiched between two polyethylene oxide (PEO) blocks. The PEO blocks are hydrophilic while PPO is hydrophobic portion in the Pluronic molecule. Due to this structure, we propose that the fatty acid molecules that are in monomeric form most effectively diffuse between the PEO "tails" and bind to the hydrophobic PPO groups.

A Study of Chemical Reactions and Interactions in Microemulsion and Surfactant Phases.

DTIC Science & Technology

1982-07-19

purpose of this study was to continue in depth investigations of the utility of microemulsion systems for studies of interactions at microcopic oil...which contain one or more amphiphilic compounds and are mechanically stable. However, the crux of the problem concerning the definition of a...microemulsion is a "persistent translucent combination of oil and water that may contain electrolytes and one or more amphiphilic compounds ". The definition

Overcoming the Cutaneous Barrier with Microemulsions

PubMed Central

Lopes, Luciana B.

2014-01-01

Microemulsions are fluid and isotropic formulations that have been widely studied as delivery systems for a variety of routes, including the skin. In spite of what the name suggests, microemulsions are nanocarriers, and their use as topical delivery systems derives from their multiple advantages compared to other dermatological formulations, such as ease of preparation, thermodynamic stability and penetration-enhancing properties. Composition, charge and internal structure have been reported as determinant factors for the modulation of drug release and cutaneous and transdermal transport. This manuscript aims at reviewing how these and other characteristics affect delivery and make microemulsions appealing for topical and transdermal administration, as well as how they can be modulated during the formulation design to improve the potential and efficacy of the final system. PMID:24590260

Determination of arsenic species in solid matrices utilizing supercritical fluid extraction coupled with gas chromatography after derivatization with thioglycolic acid n-butyl ester.

PubMed

Wang, Zhifeng; Cui, Zhaojie

2016-12-01

A method using derivatization and supercritical fluid extraction coupled with gas chromatography was developed for the analysis of dimethylarsinate, monomethylarsonate and inorganic arsenic simultaneously in solid matrices. Thioglycolic acid n-butyl ester was used as a novel derivatizing reagent. A systematic discussion was made to investigate the effects of pressure, temperature, flow rate of the supercritical CO 2 , extraction time, concentration of the modifier, and microemulsion on extraction efficiency. The application for real environmental samples was also studied. Results showed that thioglycolic acid n-butyl ester was an effective derivatizing reagent that could be applied for arsenic speciation. Using methanol as modifier of the supercritical CO 2 can raise the extraction efficiency, which can be further enhanced by adding a microemulsion that contains Triton X-405. The optimum extraction conditions were: 25 MPa, 90°C, static extraction for 10 min, dynamic extraction for 25 min with a flow rate of 2.0 mL/min of supercritical CO 2 modified by 5% v/v methanol and microemulsion. The detection limits of dimethylarsinate, monomethylarsonate, and inorganic arsenic in solid matrices were 0.12, 0.26, and 1.1 mg/kg, respectively. The optimized method was sensitive, convenient, and reliable for the extraction and analysis of different arsenic species in solid samples. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Small-angle-neutron-scattering from giant water-in-oil microemulsion droplets. II. Polymer-decorated droplets in a quaternary system

NASA Astrophysics Data System (ADS)

Foster, Tobias; Sottmann, Thomas; Schweins, Ralf; Strey, Reinhard

2008-02-01

Amphiphilic block copolymers of the type poly(ethylenepropylene)-co-poly(ethyleneoxide) dramatically enhance the solubilisation efficiency of non-ionic surfactants in microemulsions that contain equal volumes of water in oil. Consequently, the length scale of the microstructure of such bicontinuous microemulsions is dramatically increased up to the order of a few 100nm. In this paper, we show that this so-called efficiency boosting effect can also be applied to water-in-oil microemulsions with droplet microstructure. Such giant water-in-oil microemulsions would provide confined compartments in which chemical reactions of biological macromolecules can be performed on a single molecule level. With this motivation we investigated the phase behavior and the microstructure of oil-rich microemulsions containing D2O, n-decane(d22), C10E4 and the amphiphilic block copolymer PEP5-PEO5 [poly(ethylenepropylene)-co-poly(ethyleneoxide), weight per block of 5000g/mol]. We found that 15wt% of water can be solubilised by 5wt% of surfactant and block copolymer when about 6wt% of surfactant is replaced by the block copolymer. Small-angle-neutron-scattering experiments were performed to determine the length scales and microstructure topologies of the oil-rich microemulsions. To analyze the scattering data, we derived a novel form factor that also takes into account the scattering contribution of the hydrophobic part of the block copolymer molecules that reside in the surfactant shell. The quantitative analysis of the scattering data with this form factor shows that the radius of the largest droplets amounts up to 30nm. The novel form factor also yielded qualitative information on the stretching of the polymer chains in dependence on the polymer surface density and the droplet radius.

A lecithin-based microemulsion of rh-insulin with aprotinin for oral administration: Investigation of hypoglycemic effects in non-diabetic and STZ-induced diabetic rats.

PubMed

Cilek, A; Celebi, N; Tirnaksiz, F; Tay, A

2005-07-14

The aim of this study was to develop a microemulsion formulation providing an improved efficacy of orally administered insulin. The microemulsions were prepared using Labrafil M 1944 CS, Phospholipon 90 G (lecithin), absolute alcohol and bi-distilled water. The microemulsions of recombinant human (rh)-insulin and aqueous solution (200 IU/kg) were administered intragastrically by a canulla to diabetic and non-diabetic rats. Aprotinin (2500 KIU/g) was added as the enzyme inhibitor to the formulation. Upon the administration of intragastric rh-insulin solution (IS) to non-diabetic rats, the plasma glucose and insulin levels were not changed significantly. Therefore, the hypoglycemic effect caused by subcutaneous rh-insulin solution (SC), microemulsion containing rh-insulin (IME) and microemulsion containing rh-insulin and aprotinin (IMEA) were analyzed in diabetic rats. The area above the plasma glucose levels time curves (AAC), minimum glucose concentration (Cmin) and time to Cmin (tmin) were derived from the plasma glucose profiles. IME and IMEA caused approximately 30% decrease in plasma glucose levels. The decrease in the plasma glucose levels continued after the 90th min. The highest AAC value was obtained when IMEA was administered to rats. The maximum plasma insulin concentration (Cmax), time to reach Cmax (tmax), terminal half-life (t(1/2)), area under the plasma concentration-time curve (AUC), mean residence time (MRT) and elimination rate constant (k(el)) values were also calculated. It was observed that t(1/2) values varied between 0.53 and 1.31h. No significant difference could be found between the pharmacokinetic parameters of the IME and IMEA administered groups. Addition of aprotinin to the microemulsion containing rh-insulin increased bioavailability when compared to those not containing it, although the difference is not significant.

Optimization of Microemulsion Based Transdermal Gel of Triamcinolone.

PubMed

Jagdale, Swati; Chaudhari, Bhagyashree

2017-01-01

Triamcinolone is a long acting corticosteroid used in the treatment of arthritis, eczema, psoriasis and similar conditions which cause inflammation. Triamcinolone has half-life of 88min. Prolonged oral use is associated with gastrointestinal adverse effects as peptic ulcer, abdominal distention and ulcerative esophagitis as described in various patents. Microemulgel offers advantage of better stability, better loading capacity and controlled release especially for drug with short half life. Objective of the present study was to optimize microemulgel based transdermal delivery of triamcinolone. Saturated solubility of triamcinolone in various oils, surfactants and co-surfactants is estimated. Pseudo-ternary phase diagrams were constructed to determine the region of transparent microemulsion. Microemulsion was evaluated for globule size (FE-SEM, zetasizer), % transmittance, pH, viscosity, conductivity etc. Design of experiment was used to optimize microemulsion based gel. Carbopol 971P and HPMC K100M were used as independent variables. Microemulsion based gel was evaluated for in-vitro as well as ex-vivo parameters. Microemulsion was formulated with oleic acid, lauroglycol FCC and propylene glycol. PDI 0.197 indicated microemulsion is mono-disperse. 32 factorial design gave batch F8 as optimized. Design expert suggested drug release; gel viscosity and bio-adhesive strength were three significant dependant factors affecting the transdermal delivery. F8 showed drug release 92.62.16±1.22% through egg membrane, 95.23±1.44% through goat skin after 8hr and Korsmeyer-Peppas release model was followed. It can be concluded that a stable, effective controlled release transdermal microemulgel was optimised for triamcinolone. This would be a promising tool to deliver triamcinolone with enhanced bioavailability and reduced dosing frequency. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Fabrication of a novel scaffold of clotrimazole-microemulsion-containing nanofibers using an electrospinning process for oral candidiasis applications.

PubMed

Tonglairoum, Prasopchai; Ngawhirunpat, Tanasait; Rojanarata, Theerasak; Kaomongkolgit, Ruchadaporn; Opanasopit, Praneet

2015-02-01

Clotrimazole (CZ)-loaded microemulsion-containing nanofiber mats were developed as an alternative for oral candidiasis applications. The microemulsion was composed of oleic acid (O), Tween 80 (T80), and a co-surfactant such as benzyl alcohol (BzOH), ethyl alcohol (EtOH) or isopropyl alcohol (IPA). The nanofiber mats were obtained by electrospinning a blended solution of a CZ-loaded microemulsion and a mixed polymer solution of 2% (w/v) chitosan (CS) and 10% (w/v) polyvinyl alcohol (PVA) at a weight ratio of 30:70. The nanofiber mats were characterized using various analytical techniques. The entrapment efficiency, drug release, antifungal activity and cytotoxicity were investigated. The average diameter of the nanofiber mats was in the range of 105.91-125.56 nm. The differential scanning calorimetry (DSC) and powder X-ray diffractometry (PXRD) results revealed the amorphous state of the CZ-loaded microemulsions incorporated into the nanofiber mats. The entrapment efficiency of CZ in the mats was approximately 72.58-98.10%, depended on the microemulsion formulation. The release experiment demonstrated different CZ release characteristics from nanofiber mats prepared using different CZ-loaded microemulsions. The extent of drug release from the fiber mats at 4h was approximately 64.81-74.15%. The release kinetics appeared to follow Higuchi's model. In comparison with CZ lozenges (10mg), the nanofiber mats exhibited more rapid killing activity. Moreover, the nanofiber mats demonstrated desirable mucoadhesive properties and were safe for 2h. Therefore, the nanofiber mats have the potential to be promising candidates for oral candidiasis applications. Copyright © 2014 Elsevier B.V. All rights reserved.

Ionizing power and nucleophilicity in water in oil AOT-based microemulsions.

PubMed

García-Río, Luis; Hervella, Pablo; Leis, José Ramón

2005-08-16

A study was carried out on the solvolysis of substituted phenyl chloroformates in AOT/isooctane/water microemulsions. (AOT is the sodium salt of bis(2-ethyhexyl)sulfosuccinate.) The results obtained have been interpreted by taking into account the distribution of the chloroformates between the continuous medium and the interface of the microemulsions, where the reactions take place. The values obtained for the rate constant in the interface, k(i), decreases as the water content of the microemulsions increases, as a consequence of the decrease in its nucleophilic capacity. This behavior is consistent with a rate-determining step of water addition to the carbonyl group. The values of k(i) allow us to obtain the slopes of the Hammett correlations at the interface of the microemulsions, rho = 2.25, whose values are greater than those obtained in an aqueous medium, rho = 0.82. This increase in the Hammett slope is similar to that observed in ethanol/water mixtures and is a consequence of a variation in the structure of the transition state of the reaction where there is a smaller extension of the expulsion of the leaving group. The values of the rate constants at the interface of the microemulsions have allowed us, by means of the Grunwald-Winstein equation, to obtain the solvent ionizing power and the nucleophilicity of the solvent. The values obtained for Y(Cl) increase together with the water content of the microemulsion, whereas the values of N(T) decrease. These variations are a consequence of the interaction between the AOT headgroups and the interfacial water, where the water molecules act like electronic acceptors. The intensity of this interaction is greater if the system has a small water content, which explains the variation of Y(Cl) and N(T).

Anomalies in, and Crystallization of Supercooled Water and Aqueous Solutions.

DTIC Science & Technology

1984-03-01

and to an extent novel situations, by D. L. Fields. The first study has been on water contained in the newly developed microemulsions in which there...feature of this microemulsion is March 8, 1984 ..... ...... ....... % *~.~- * -7- * •that the only-OH groups present derive from the water component. Our...interest in this subject has been two-fold. (1) To obtain information on the structure of water in the microemulsion form, (2) attempt to use the

Purification of Houttuynia cordata Thunb. Essential Oil Using Macroporous Resin Followed by Microemulsion Encapsulation to Improve Its Safety and Antiviral Activity.

PubMed

Pang, Jianmei; Dong, Wujun; Li, Yuhuan; Xia, Xuejun; Liu, Zhihua; Hao, Huazhen; Jiang, Lingmin; Liu, Yuling

2017-02-15

Essential oil extracted from Houttuynia cordata Thunb. ( H. cordata ) is widely used in traditional Chinese medicine due to its excellent biological activities. However, impurities and deficient preparations of the essential oil limit its safety and effectiveness. Herein, we proposed a strategy to prepare H. cordata essential oil (HEO) safely and effectively by combining the solvent extraction and the macroporous resin purification flexibly, and then encapsulating it using microemulsion. The extraction and purification process were optimized by orthogonal experimental design and adsorption-desorption tests, respectively. The average houttuynin content in pure HEO was then validated at 44.3% ± 2.01%, which presented a great potential for industrial application. Subsequently, pure HEO-loaded microemulsion was prepared by high-pressure homogenization and was then fully characterized. Results showed that the pure HEO-loaded microemulsion was successfully prepared with an average particle size of 179.1 nm and a high encapsulation rate of 94.7%. Furthermore, safety evaluation tests and in vitro antiviral testing indicated that the safety and activity of HEO were significantly improved after purification using D101 resin and were further improved by microemulsion encapsulation. These results demonstrated that the purification of HEO by macroporous resin followed by microemulsion encapsulation would be a promising approach for industrial application of HEO for the antiviral therapies.

Match of Solubility Parameters Between Oil and Surfactants as a Rational Approach for the Formulation of Microemulsion with a High Dispersed Volume of Copaiba Oil and Low Surfactant Content.

PubMed

Xavier-Junior, Francisco Humberto; Huang, Nicolas; Vachon, Jean-Jacques; Rehder, Vera Lucia Garcia; do Egito, Eryvaldo Sócrates Tabosa; Vauthier, Christine

2016-12-01

Aim was to formulate oil-in-water (O/W) microemulsion with a high volume ratio of complex natural oil, i.e. copaiba oil and low surfactant content. The strategy of formulation was based on (i) the selection of surfactants based on predictive calculations of chemical compatibility between their hydrophobic moiety and oil components and (ii) matching the HLB of the surfactants with the required HLB of the oil. Solubility parameters of the hydrophobic moiety of the surfactants and of the main components found in the oil were calculated and compared. In turn, required HLB of oils were calculated. Selection of surfactants was achieved matching their solubility parameters with those of oil components. Blends of surfactants were prepared with HLB matching the required HLB of the oils. Oil:water mixtures (15:85 and 25:75) were the titrated with surfactant blends until a microemulsion was formed. Two surfactant blends were identified from the predictive calculation approach. Microemulsions containing up to 19.6% and 13.7% of selected surfactant blends were obtained. O/W microemulsions with a high volume fraction of complex natural oil and a reasonable surfactant concentration were formulated. These microemulsions can be proposed as delivery systems for the oral administration of poorly soluble drugs.

Characterization of interaction between esculin and human serum albumin in membrane mimetic environments

NASA Astrophysics Data System (ADS)

Zhang, Yaheng; Li, Jiazhong; Dong, Lijun; Li, Ying; Chen, Xingguo

2008-10-01

In this study the interaction between esculin and human serum albumin (HSA) in AOT/isooctane/water microemulsions was studied for the first time using fluorescence quenching technique in combination with UV absorption spectroscopy, Fourier transform infrared (FT-IR) spectroscopy, circular dichroism (CD) spectroscopy and dynamic light scattering (DLS) technique. Fluorescence data in ω o 20 microemulsions revealed the presence of the binding site of esculin on HSA and its binding constants at four different temperatures were obtained. The affinities in microemulsions are similar to that in buffer solution. The alterations of protein secondary structure in the microemulsions in the absence and presence of esculin compared with the free form of HSA in buffer were qualitatively and quantitatively analyzed by the evidence from CD and FT-IR spectroscopes. The displacement experiments confirmed that esculin could bind to the site I of HSA, which was in agreement with the result of the molecular modeling study. Furthermore, the DLS data suggested that HSA may locate at the interface of the microemulsion and esculin could interact with them.

Food grade microemulsion systems: Sunflower oil/castor oil derivative-ethanol/water. Rheological and physicochemical analysis.

PubMed

Mori Cortés, Noelia; Lorenzo, Gabriel; Califano, Alicia N

2018-05-01

Microemulsions are thermodynamically stable systems that have attracted considerable attention in the food industry as delivery systems for many hydrophobic nutrients. These spontaneous systems are highly dependent on ingredients and composition. In this work phase diagrams were constructed using two surfactants (Kolliphor RH40 and ELP), water, sunflower oil, and ethanol as cosurfactant, evaluating their physicochemical properties. Stability of the systems was studied at 25 and 60 °C, monitoring turbidity at 550 nm for over a month to identify the microemulsion region. Conductivity was measured to classify between water-in-oil and oil-in-water microemulsions. The phase diagram constructed with Kolliphor RH40 exhibited a larger microemulsion area than that formulated with Kolliphor ELP. All formulations showed a monomodal droplet size distribution with low polydispersity index (<0.30) and a mean droplet size below 20 nm. Systems with higher water content presented a Newtonian behavior; increasing the dispersed phase content produced a weak gel-like structure with pseudoplastic behavior under flow conditions that was satisfactorily modeled to obtain structural parameters. Copyright © 2018 Elsevier Ltd. All rights reserved.

[Determination of lead in microemulsified rapeseed oil and bio-diesel oil by GFAAS].

PubMed

Li, Sheng-qing; He, Xiao-min; Du, Ping; Wang, Min; Chen, Hao; Wu, Mou-cheng

2008-10-01

Bio-diesel oil has attracted much attention as a substitutable energy sources for its renewable and eco-friendly property. However, problems of lead contamination in fuel are also emphasized increasingly at present. So it was of quite significance to determine the contents of lead in bio-diesel oil and its raw material rapeseed oil. An effective method was developed for the rapid determination of lead in rapeseed oil and bio-diesel oil by graphite furnace atomic absorption spectrometry (GFAAS) after their stabilization as microemulsions. In this research work, polyethyleneglycol octyl phenyl ether and n-butanol were used for emulsifier and auxiliary emulsifying agent, respectively. For Pb, efficient thermal stabilization was obtained using NH4H2PO4 as matrix modifier. Sample stabilization was necessary because of evident analyte losses that occurred immediately after sampling. Excellent long-term sample stabilization and the influence of the microemulsion composition on the GFAAS response were observed by mixing different organic solvents. The ashing and atomization temperature and ramp rate influenced the sensitivity obtained for Ph. Take this into account, the optimum conditions of the graphite furnace atomic absorption spectrometric determination of Pb in rapeseed oil and bio-diesel oil samples were investigated. The results showed that the microemulsion was quite stable when the value of V(20% polyethyleneglycol octyl phenyl ether), V(n-butanol), V(oil) and V(water) was 0.1: 8.9: 0.5: 0.5, without matrix interference effect. The determination limit of the proposed method was 126.2 microg x L(-1) for Pb, comfortably below the values found in the analyzed samples. The recoveries were from 81.8% to 109.0%, which performed using the addition of different concentrations of lead to bio-diesel oil, rapeseed oil and petrochemical diesel samples. The relative standard deviation of determination was 5.84%. This work showed the great efficiency of the microemulsion, indicating that it is possible to extract lead from the oil phase. The method was applied to the determination of lead in oil samples with satisfactory results.

Preparation of hollow silica nanospheres in O/W microemulsion system by hydrothermal temperature changes

NASA Astrophysics Data System (ADS)

Wang, Dandan; Li, Xiuyan; Liu, Zuohua; Shi, Xue; Zhou, Guowei

2017-01-01

Hollow silica nanospheres with wrinkled or smooth surfaces were successfully fabricated through a hydrothermal method. In this method, oil-in-water microemulsion (composed of cyclohexane, water, ethanol, and cetyltrimethylammonium bromide), and polyvinylpyrrolidone were utilized as template and capping agent, respectively. In such a facile synthesis, we can well realize the morphological transformation of spheres with radially oriented mesochannels to hollow structures of silica nanoparticle only by regulating the hydrothermal temperature from 100 °C to 200 °C. Synthesized samples with different mesostructures were then used as supports to immobilize Candida rugosa lipase (CRL). The immobilized CRL was employed as a new biocatalyst for biodiesel production through the esterification of heptanoic acid with ethanol. The conversion ratio of heptanoic acid with ethanol catalyzed by the immobilized CRL was also evaluated. Results of this study suggest that the prepared samples have potential applications in biocatalysis.

Food-grade microemulsions based on nonionic emulsifiers: media to enhance lycopene solubilization.

PubMed

Spernath, Aviram; Yaghmur, Anan; Aserin, Abraham; Hoffman, Roy E; Garti, Nissim

2002-11-06

Water-dilutable food-grade microemulsions consisting of ethoxylated sorbitan esters, and in some cases blended with other emulsifiers, water, (R)-(+)-limonene, ethanol, and propylene glycol, have been prepared. These microemulsions are of growing interest to the food industry as vehicles for delivering and enhancing solubilization of natural food supplements with nutritional and health benefits. Lycopene, an active natural lipophilic antioxidant from tomato, has solubilized in water-in-oil, bicontinuous, and oil-in-water types of microemulsions up to 10 times the oil [(R)-(+)-limonene] dissolution capacity. The effects of aqueous-phase dilution, nature of surfactant (hydrophilic-lypophilic balance), and mixed surfactant on solubilization capacity and solubilization efficiency were studied. Structural aspects studied by self-diffusion NMR were correlated to the solubilization capacity, and transformational structural changes were identified.

Microemulsion synthesis and magnetic properties of FexNi(1-x) alloy nanoparticles

NASA Astrophysics Data System (ADS)

Beygi, H.; Babakhani, A.

2017-01-01

This paper investigates synthesis of FexNi(1-x) bimetallic nanoparticles by microemulsion method. Through studying the mechanism of nanoparticles formation, it is indicated that synthesis of nanoparticles took placed by simultaneous reduction of metal ions and so nanoparticles structure is homogeneous alloy. FexNi(1-x) nanoparticles with different sizes, morphologies and compositions were synthesized by changing the microemulsion parameters such as water/surfactant/oil ratio, presence of co-surfactant and NiCl2·6H2O to FeCl2·4H2O molar ratio. Synthesized nanoparticles were characterized by transmission electron microscopy, particle size analysis, X-ray diffraction, atomic absorption and thermogravimetric analyses. The results indicated that, presence of butanol as co-surfactant led to chain-like arrangement of nanoparticles. Also, finer nanoparticles were synthesized by decreasing the amount of oil and water and increasing the amount of CTAB. The results of vibrating sample magnetometer suggested that magnetic properties of FexNi(1-x) alloy nanoparticles were affected by composition, size and morphology of the particles. Spherical and chain-like FexNi(1-x) alloy nanoparticles were superparamagnetic and ferromagnetic, respectively. Furthermore, higher iron in the composition of nanoparticles increases the magnetic properties.

Polymer loaded microemulsions: Changeover from finite size effects to interfacial interactions

NASA Astrophysics Data System (ADS)

Kuttich, B.; Ivanova, O.; Grillo, I.; Stühn, B.

2016-10-01

Form fluctuations of microemulsion droplets are observed in experiments using dielectric spectroscopy (DS) and neutron spin echo spectroscopy (NSE). Previous work on dioctyl sodium sulfosuccinate based water in oil microemulsions in the droplet phase has shown that adding a water soluble polymer (Polyethylene glycol M = 1500 g mol-1) modifies these fluctuations. While for small droplet sizes (water core radius rc < 37 Å) compared to the size of the polymer both methods consistently showed a reduction in the bending modulus of the surfactant shell as a result of polymer addition, dielectric spectroscopy suggests the opposite behaviour for large droplets. This observation is now confirmed by NSE experiments on large droplets. Structural changes due to polymer addition are qualitatively independent of droplet size. Dynamical properties, however, display a clear variation with the number of polymer chains per droplet, leading to the observed changes in the bending modulus. Furthermore, the contribution of structural and dynamical properties on the changes in bending modulus shifts in weight. With increasing droplet size, we initially find dominating finite size effects and a changeover to a system, where interactions between the confined polymer and the surfactant shell dominate the bending modulus.

Microporous crystals and synthesis schemes

DOEpatents

Tumas, William; Ott, Kevin C.; McCleskey, T. Mark; Yates, Matthew Z.; Birnbaum, Eva R.

2008-04-22

Novel zeolites are produced by combining a polar solute, a silicon or phosphorous source, and a structure directing agent. Surfactants and a hydrophobic solvent are added to the previously mixed three species and shaken to disperse the surfactants. The reverse microemulsion is stirred overnight, at about room temperature and then iced for five to ten minutes. A metal source is added vigorously shaken for about two minutes. The mixture is then aged for about two hours at about room temperature. A mineralizer is added and the resultant mixture aged for about two hours at about room temperature. The mixture is heated to about 180.degree. C., for a suitable time period. The final novel product is then isolated.

Microporous crystals and synthesis schemes

DOEpatents

Tumas, William; Ott, Kevin C.; McCleskey, T. Mark; Yates, Matthew Z.; Birnbaum, Eva R.

2005-09-27

Novel zeolites are produced by combining a polar solute, a silicon or phosphorous source, and a structure directing agent. Surfactants and a hydrophobic solvent are added to the previously mixed three species and shaken to disperse the surfactants. The reverse microemulsion is stirred overnight, at about room temperature and then iced for five to ten minutes. A metal source is added vigorously shaken for about two minutes. The mixture is then aged for about two hours at about room temperature. A mineralizer is added and the resultant mixture aged for about two hours at about room temperature. The mixture is heated to about 180.degree. C., for a suitable time period. The final novel product is then isolated.

Fluorescence probe studies of the interactions between poly(oxyethylene) and surfactant micelles and microemulsion droplets in aqueous solutions

DOE Office of Scientific and Technical Information (OSTI.GOV)

Zana, R.; Lianos, P.; Lang, J.

1985-01-03

The interaction between poly(ethylene oxide) (POE) and the aggregates present in micellar solutions of sodium dodecyl sulfate (SDS), mixed micellar solutions of SDS + 1-pentanol, and oil in water microemulsions made of SDS + 1-pentanol + oil (dodecane or toluene) has been investigated by means of fluorescence probing methods. It is shown that the addition of POE results in a decrease of the aggregation number of SDS in the aggregates present in all the systems investigated. Most likely this decrease is due to the adsorption of the POE chain in the micelle palisade layer and the ensuing increase of micellemore » ionization. 22 references, 5 figures, 2 tables.« less

Tuning aggregation of microemulsion droplets and silica nanoparticles using solvent mixtures.

PubMed

Salabat, Alireza; Eastoe, Julian; Mutch, Kevin J; Tabor, Rico F

2008-02-15

The effect of solvent on stability of water-in-oil microemulsions has been studied with AOT (sodium bis(2-ethylhexyl)sulfosuccinate) and different solvent mixtures of n-heptane, toluene and dodecane. Dynamic light scattering DLS was used to monitor the apparent diffusion coefficient D(A) and effective microemulsion droplet diameter on changing composition of the solvent. Interdroplet attractive interactions, as indicated by variations in D(A), can be tuned by formulation of appropriate solvent mixtures using heptane, toluene, and dodecane. In extreme cases, solvent mixtures can be used to induce phase transitions in the microemulsions. Aggregation and stability of model AOT-stabilized silica nanoparticles in different solvents were also investigated to explore further these solvent effects. For both systems the state of aggregation can be correlated with the effective molecular volume of the solvent V(mol)(eff) mixture.

Optimizing the dermal accumulation of a tazarotene microemulsion using skin deposition modeling.

PubMed

Nasr, Maha; Abdel-Hamid, Sameh

2016-01-01

It is well known that microemulsions are mainly utilized for their transdermal rather than their dermal drug delivery potential due to their low viscosity, and the presence of penetration enhancing surfactants and co-surfactants. Applying quality by design (QbD) principles, a tazarotene microemulsion formulation for local skin delivery was optimized by creating a control space. Critical formulation factors (CFF) were oil, surfactant/co-surfactant (SAA/CoS), and water percentages. Critical quality attributes (CQA) were globular size, microemulsion viscosity, tazarotene skin deposition, permeation, and local accumulation efficiency index. Increasing oil percentage increased globular size, while the opposite occurred regarding SAA/CoS, (p = 0.001). Microemulsion viscosity was reduced by increasing oil and water percentages (p < 0.05), due to the inherent high viscosity of the utilized SAA/CoS. Drug deposition in the skin was reduced by increasing SAA/CoS due to the increased hydrophilicity and viscosity of the system, but increased by increasing water due to hydration effect (p = 0.009). Models with very good fit were generated, predicting the effect of CFF on globular size, microemulsion viscosity, and drug deposition. A combination of 40% oil and 45% SAA/CoS showed the maximum drug deposition of 75.1%. Clinical skin irritation study showed that the aforementioned formula was safe for topical use. This article suggests that applying QbD tools such as experimental design is an efficient tool for drug product design.

Mercury removal from aqueous streams utilizing microemulsion liquid membranes

DOE Office of Scientific and Technical Information (OSTI.GOV)

Larson, K.A.; Wiencek, J.M.

1994-11-01

The goal of this work is the removal of mercury ion from wastewater using thermodynamically stable microemulsions as liquid membranes. The research focuses on identification and modeling of the appropriate aqueous and organic phase equilibrium reactions for mercury extraction and stripping, comparison of extraction kinetics between coarse emulsions and microemulsions, and demulsification and recovery of the emulsion components. An oleic acid microemulsion liquid membrane (water-in-oil) containing sulfuric acid as the internal phase reduces the feed phase mercury concentration from 460 mg/l to 0.84 mg/l in a single contacting. This compares favorably with a control extraction (oleic acid/no internal phase) whichmore » results in a final concentration of 20 mg/l Hg{sup +2}. Microemulsions can be demulsified using butanol as an additive. The demulsification kinetics are proportional to butanol concentration and temperature and inversely proportional to surfactant concentration. The demulsification rate is second order with respect to water concentration which implies that the rate-limiting step in the process is the rate of internal phase droplet encounters. Proof-of-principle experiments demonstrate the ability to extract mercury ion using microemulsions formulated with recycled organic phase, albeit at a somewhat reduced efficiency. The reduced efficiency is attributed to increased internal phase leakage due to residual butanol in the oil phase. Finally, the cycle is brought around full circle by recovering metallic mercury from the internal phase by electroplating. 27 refs., 11 figs., 1 tab.« less

Pressure effects on enzyme reactions in mainly organic media: alpha-chymotrypsin in reversed micelles of Aerosol OT in octane.

PubMed

Mozhaev, V V; Bec, N; Balny, C

1994-08-01

Biocatalytic transformations in reversed micelles formed by anionic surfactant Aerosol OT in octane have been studied at high pressures by an example of alpha-chymotrypsin-catalyzed hydrolysis of N-carbobenzoxy-L-tyrosine p-nitrophenyl ester and N-succinyl-L-phenylalanine p-nitroanilide. For the first time it has been found that the enzyme retains high activity in these water-in-oil microemulsions up to a pressure of 2 kbar. The value of the activation volume (delta V*) for the enzyme reactions shows a dependence on the water content in the system. When the size of the micellar aqueous inner cavity (as evaluated at 1 atm) approaches the molecular size of alpha-chymotrypsin, delta V* becomes significantly different from the value in aqueous solution and in the micelles with a larger size. Possibilities of regulating the enzyme activity by pressure in systems with a low content of water are discussed.

Sulfur Nanoparticles Synthesis and Characterization from H2S Gas, Using Novel Biodegradable Iron Chelates in W/O Microemulsion

NASA Astrophysics Data System (ADS)

Deshpande, Aniruddha S.; Khomane, Ramdas B.; Vaidya, Bhalchandra K.; Joshi, Renuka M.; Harle, Arti S.; Kulkarni, Bhaskar D.

2008-06-01

Sulfur nanoparticles were synthesized from hazardous H2S gas using novel biodegradable iron chelates in w/o microemulsion system. Fe3+ malic acid chelate (0.05 M aqueous solution) was studied in w/o microemulsion containing cyclohexane, Triton X-100 and n-hexanol as oil phase, surfactant, co-surfactant, respectively, for catalytic oxidation of H2S gas at ambient conditions of temperature, pressure, and neutral pH. The structural features of sulfur nanoparticles have been characterized by X-ray diffraction (XRD), transmission electron microscope (TEM), energy dispersive spectroscopy (EDS), diffused reflectance infra-red Fourier transform technique, and BET surface area measurements. XRD analysis indicates the presence of α-sulfur. TEM analysis shows that the morphology of sulfur nanoparticles synthesized in w/o microemulsion system is nearly uniform in size (average particle size 10 nm) and narrow particle size distribution (in range of 5 15 nm) as compared to that in aqueous surfactant systems. The EDS analysis indicated high purity of sulfur (>99%). Moreover, sulfur nanoparticles synthesized in w/o microemulsion system exhibit higher antimicrobial activity (against bacteria, yeast, and fungi) than that of colloidal sulfur.

Transungual Gel of Terbinafine Hydrochloride for the Management of Onychomycosis: Formulation, Optimization, and Evaluation.

PubMed

Thatai, Purva; Sapra, Bharti

2017-08-01

The present study was aimed to optimize, develop, and evaluate microemulsion and microemulsion-based gel as a vehicle for transungual drug delivery of terbinafine hydrochloride for the treatment of onychomycosis. D-optimal mixture experimental design was adopted to optimize the composition of microemulsion having amount of oil (X 1 ), Smix (mixture of surfactant and cosurfactant; X 2 ), and water (X 3 ) as the independent variables. The formulations were assessed for permeation (micrograms per square centimeter per hour; Y 1 ), particle size (nanometer; Y 2 ), and solubility of the drug in the formulation (milligrams per milliliter; Y 3 ). The microemulsion containing 3.05% oil, 24.98% Smix, and 71.96% water was selected as the optimized formulation. The microemulsion-based gel showed better penetration (∼5 folds) as well as more retention (∼9 fold) in the animal hoof as compared to the commercial cream. The techniques used to screen penetration enhancers (hydration enhancement factor, ATR-FTIR, SEM, and DSC) revealed the synergistic effect of combination of urea and n-acetyl cysteine in disruption of the structure of hoof and hence, leading to enhanced penetration of drug.

Microemulsion Electrokinetic Chromatography.

PubMed

Buchberger, Wolfgang

2016-01-01

Microemulsion electrokinetic chromatography (MEEKC) is a special mode of capillary electrophoresis employing a microemulsion as carrier electrolyte. Analytes may partition between the aqueous phase of the microemulsion and its oil droplets which act as a pseudostationary phase. The technique is well suited for the separation of neutral species, in which case charged oil droplets (obtained by addition of an anionic or cationic surfactant) are present. A single set of separation parameters may be sufficient for separation of a wide range of analytes belonging to quite different chemical classes. Fine-tuning of resolution and analysis time may be achieved by addition of organic solvents, by changes in the nature of the surfactants (and cosurfactants) used to stabilize the microemulsion, or by various additives that may undergo some additional interactions with the analytes. Besides the separation of neutral analytes (which may be the most important application area of MEEKC), it can also be employed for cationic and/or anionic species. In this chapter, MEEKC conditions are summarized that have proven their reliability for routine analysis. Furthermore, the mechanisms encountered in MEEKC allow an efficient on-capillary preconcentration of analytes, so that the problem of poor concentration sensitivity of ultraviolet absorbance detection is circumvented.

Evaluation of steady-state kinetic parameters for enzymes solubilized in water-in-oil microemulsion systems.

PubMed Central

Oldfield, C

1990-01-01

1. Equations are derived for the steady-state kinetics of substrate conversion by enzymes confined within the water-droplets of water-in-oil microemulsion systems. 2. Water-soluble substrates initially confined within droplets that do not contain enzyme are assumed to be converted into product only after they enter enzyme-containing droplets via the inter-droplet exchange process. 3. Hyperbolic (Michaelis-Menten) kinetics are predicted when the substrate concentration is varied in microemulsions of fixed composition. Both kcat. and Km are predicted to be dependent on the size and concentration of the water-droplets in the microemulsion. 4. The predicted behaviour is shown to be supported by published experimental data. A physical interpretation of the form of the rate equation is presented. 5. The rate equation for an oil-soluble substrate was derived assuming a pseudo-two-phase (oil & water) model for the microemulsion. Both kcat. and Km are shown to be independent of phi aq. Km is larger than the aqueous solution value by a factor approximately equal to the oil/water partition coefficient of the substrate. The validity of the rate equation is confirmed by published data. PMID:2264819

Sulfur Nanoparticles Synthesis and Characterization from H2S Gas, Using Novel Biodegradable Iron Chelates in W/O Microemulsion

PubMed Central

2008-01-01

Sulfur nanoparticles were synthesized from hazardous H2S gas using novel biodegradable iron chelates in w/o microemulsion system. Fe3+–malic acid chelate (0.05 M aqueous solution) was studied in w/o microemulsion containing cyclohexane, Triton X-100 andn-hexanol as oil phase, surfactant, co-surfactant, respectively, for catalytic oxidation of H2S gas at ambient conditions of temperature, pressure, and neutral pH. The structural features of sulfur nanoparticles have been characterized by X-ray diffraction (XRD), transmission electron microscope (TEM), energy dispersive spectroscopy (EDS), diffused reflectance infra-red Fourier transform technique, and BET surface area measurements. XRD analysis indicates the presence of α-sulfur. TEM analysis shows that the morphology of sulfur nanoparticles synthesized in w/o microemulsion system is nearly uniform in size (average particle size 10 nm) and narrow particle size distribution (in range of 5–15 nm) as compared to that in aqueous surfactant systems. The EDS analysis indicated high purity of sulfur (>99%). Moreover, sulfur nanoparticles synthesized in w/o microemulsion system exhibit higher antimicrobial activity (against bacteria, yeast, and fungi) than that of colloidal sulfur.

Evaluation of Sub-acute Oral Toxicity of Lithium Carbonate Microemulsion (Nano Size) on Liver and Kidney of Mice

PubMed Central

Kalantari, Heibatullah; Salimi, Anayatollah; Rezaie, Anahita; Jazayeri Shushtari, Fereshteh; Goudarzi, Mehdi

2015-01-01

Background: The development of drug delivery systems has improved the therapeutic and toxic properties of existing drugs in therapy. Microemulsion systems are novel vehicles for drug delivery, which have been developed in recent years. These systems are currently of interest to the pharmaceutical scientist because of their considerable potential to act as drug delivery vehicles by incorporating into a wide range of drug molecules. Although these systems improved solubility and bioavailability of drugs, they may have potential toxic effects on the body organs. Objectives: The purpose of this study was to examine a possible hepatotoxic and nephrotoxic effect of lithium carbonate microemulsion (LCME) in a mice model. Materials and Methods: Eighty male Swiss albino mice were randomly allocated to eight experimental groups, as follows: Group 1, as negative control group were treated orally with normal saline (0.9% NaCl); Group 2, received microemulsion base without drug as control group; Groups 3 to 5, received lithium carbonate (LC) solution in doses of 50, 100, and 200 mg/kg, respectively; Groups 6 to 8, received LCME orally in doses of 50, 100, and 200 mg/kg, respectively. All drugs were administered orally for ten consecutive days. Serum glutamate pyruvate aminotransferase (SGPT), serum glutamate oxaloacetate aminotransferase (SGOT), alkaline phosphatase (ALP), blood urea nitrogen (BUN), and plasma creatinine (Cr), as markers of liver and kidney toxicity in treated mice, were measured. Furthermore, the changes of tissue were assessed by histopathologic examination. Results: The findings showed that serum activity of ALP, SGOT, and SGPT and the levels of BUN and Cr in microemulsion base group was greater than normal saline group. However, this difference was not significant. Administration of LC and LCME in all doses resulted in a significant increase in the levels of BUN and serum activity of SGOT and SGPT in comparison to normal saline group (P < 0.05). Histopathological changes were observed in mice treated with LC or LCME. Conclusions: This study showed that subacute oral administration of different doses of LCME with severe toxicity in comparison to the same dose of LC. PMID:25866723

Pharmacokinetics and efficiency of brain targeting of ginsenosides Rg1 and Rb1 given as Nao-Qing microemulsion.

PubMed

Li, Tao; Shu, Ya-Jun; Cheng, Jia-Yin; Liang, Run-Cheng; Dian, Shao-Na; Lv, Xiao-Xun; Yang, Meng-Qi; Huang, Shu-Ling; Chen, Gang; Yang, Fan

2015-02-01

Nao-Qing solution has been shown to be clinically effective in the treatment of acute ischemic stroke (AIS). The purpose of this study was to improve the pharmacokinetics and brain uptake of Nao-Qing, administered as an oil-in-water microemulsion. Sprague-Dawley (SD) rats were given Nao-Qing microemulsion by intranasal or intragastric routes. Samples of blood, brain, heart, liver, lung and kidney were collected at pre-determined time intervals, and the contents of ginsenosides Rg1 and Rb1 (active ingredients of the Nao-Qing microemulsion) were analyzed by high-performance liquid chromatography (HPLC). The results showed that contents of ginsenosides Rg1 and Rb1 in Nao-Qing microemulsion was 8475.13 ± 54.61 μg/ml and 6633.42 ± 527.27 μg/ml, respectively, and that the particle size, pH and viscosity of the microemulsion were 19.9 ± 5.07 nm, 6.1 and 3.056 × 10(-3 )Pas, respectively. Absorption of ginsenoside Rg1 was higher than that of ginsenoside Rb1, which was barely detectable after intragastric administration; furthermore, the concentration of ginsenoside Rg1 in blood and other tissues at each time point was lower for intragastric than for intranasal administration. Compared with intragastric administration, intranasal administration resulted in a shorter tmax (0.08 versus 1 h), a higher Cmax (16.65 versus 11.29 μg/ml), and a higher area under the concentration-time curve (AUC) (592.91 versus 101.70 μgċh/ml) in the brain. The relative rates of uptake (Re) and the ratio of peak concentration (Ce) in the brain were 126.31% and 147.48% for ginsenoside Rg1, respectively. These data illustrate that intranasal administration can promote the absorption of drugs in Nao-Qing microemulsion and achieve fast effect.

Gel-like TPGS-Based Microemulsions for Imiquimod Dermal Delivery: Role of Mesostructure on the Uptake and Distribution into the Skin.

PubMed

Telò, Isabella; Favero, Elena Del; Cantù, Laura; Frattini, Noemi; Pescina, Silvia; Padula, Cristina; Santi, Patrizia; Sonvico, Fabio; Nicoli, Sara

2017-10-02

The aim of this work was to develop an innovative microemulsion with gel-like properties for the cutaneous delivery of imiquimod, an immunostimulant drug employed for the treatment of cutaneous infections and neoplastic conditions. A pseudoternary phase diagram was built using a 1/1 TPGS (d-α-tocopheryl polyethylene glycol 1000 succinate)/Transcutol mixture as surfactant system, and oleic acid as oil phase. Eight microemulsions-selected from the 1.25/8.75 oil/surfactants ratio, along the water dilution line (from 20 to 56% w/w)-were characterized in terms of rheological behavior, optical properties via polarized microscopy, and supramolecular structure using X-ray scattering. Then, these formulations were loaded with imiquimod and the uptake and distribution into the skin was evaluated on full-thickness porcine skin. X-ray scattering experiments revealed the presence of disconnected drops in the case of microemulsion with 20% water content. Diluting the system up to 48% water content, the structure turned into an interconnected lamellar microemulsion, reaching a proper disconnected lamellar structure for the highest water percentages (52-56%). Upon water addition, also the rheological properties changed from nearly Newtonian fluids to gel-like structures, displaying the maximum of viscosity for the 48% water content. Skin uptake experiments demonstrated that formulation viscosity, drug loading, and surfactant concentration did not play an important role on imiquimod uptake into the skin, while the skin penetration was related instead to the microemulsion mesostructure. In fact, drug uptake became enhanced by locally lamellar interconnected structures, while it was reduced in the presence of disconnected structures, either drops or proper lamellae. Finally, the data demonstrated that mesostructure also affects the drug distribution between the epidermis and dermis. In particular, a significantly higher dermal accumulation was found when disconnected lamellar structures are present, suggesting the possibility of tuning both drug delivery and localization into the skin by modifying microemulsions composition.

Surfactant induced stabilization of nano liquid crystalline (dodecane-phytantriol) droplet

NASA Astrophysics Data System (ADS)

Abbas, S.; Saha, Debasish; Kumar, Sugam; Aswal, V. K.; Kohlbrecher, J.

2018-04-01

The study of formation and stabilization of dodecane-phytantriol (DPT) microemulsions using ionic and nonionic surfactants are investigated. Small Angle Neutron Scattering (SANS) and Dynamic Light Scattering (DLS) techniques have been employed to study the resulting structures of the micro emulsion droplets. We show the formation of stable microemulsion droplets with absence of lyotropic liquid crystalline phase on addition of nonionic surfactant C12E10. The oil to surfactant ratio plays the crucial role in formation of stable droplet and its size. The dense presence of C12E10 molecules between microemulsion droplets protect them from coalescence while less number of C12E10 between the surface of droplets easily triggers the coalescence process. The interaction with both anionic (SDS) as well as cationic (DTAB) surfactants with DPT phase leads to formation of microemulsion droplets with lyotropic liquid crystalline phase.

Characterization of caprylocaproyl macrogolglycerides based microemulsion drug delivery vehicles for an amphiphilic drug.

PubMed

Djordjevic, Ljiljana; Primorac, Marija; Stupar, Mirjana; Krajisnik, Danina

2004-03-01

Microemulsion systems composed of water, isopropyl myristate, PEG-8 caprylic/capric glycerides (Labrasol), and polyglyceryl-6 dioleate (Plurol Oleique), were investigated as potential drug delivery vehicles for an amphiphilic model drug (diclofenac diethylamine). Pseudo-ternary phase diagram of the investigated system, at constant surfactant/cosurfactant mass ratio (Km 4:1) was constructed at room temperature by titration, and the oil-to-surfactant/cosurfactant mass ratios (O/SC) that exhibit the maximum in the solubilization of water were found. This allowed the investigation of the continuous structural inversion from water-in-oil to oil-in-water microemulsions on dilution with water phase. Furthermore, electrical conductivity (sigma) of the system at Km 1:4, and O/SC 0.250 was studied, and the percolation phenomenon was observed. Conductivity and apparent viscosity (eta') measurement results well described colloidal microstructure of the selected formulations, including gradual changes during their formation. Moreover, sigma, eta', and pH values of six selected microemulsion vehicles which differ in water phase volume fraction (phi(w)) at the selected Km and O/SC values, were measured. In order to investigate the influence of the amphiphilic drug on the vehicle microstructures, each system was formulated with 1.16% (w/w) diclofenac diethylamine. Electrical conductivity, and eta' of the investigated systems were strongly affected by drug incorporation. The obtained results suggest that diclofenac diethylamine interacts with the specific microstructure of the investigated vehicles, and that the different drug release kinetics from these microemulsions may be expected. The investigated microemulsions should be very interesting as new drug carrier systems for dermal application of diclofenac diethylamine.

Preparation, characterization and in vitro evaluation of microemulsion of raloxifene hydrochloride.

PubMed

Golmohammadzadeh, Shiva; Farhadian, Nafiseh; Biriaee, Amir; Dehghani, Faranak; Khameneh, Bahman

2017-10-01

Raloxifene hydrochloride (RLX) is a selective estrogen receptor modulator which is orally used for treatment of osteoporosis and prevention of breast cancer. The drug has low aqueous solubility and bioavailability. The aim of the present study is to formulate and characterize oil-in-water microemulsion systems for oral delivery of RLX. To enhance the drug aqueous solubility, microemulsion based on sesame oil was prepared. Sesame oil and Tween 80 were selected as the drug solvent oil and surfactant, respectively. In the first and second formulations, Edible glycerin and Span 80 were applied as co-surfactant, respectively. Pseudo-ternary phase diagrams showed that the best surfactant/co-surfactant ratios in the first and second formulations were 4:1 and 9:1, respectively. The particle size of all free drug-loaded and drug loaded samples were in the range of 31.25 ± 0.3 nm and 60.9 ± 0.1 nm, respectively. Electrical conductivity coefficient and refractive index of all microemulsion samples confirmed the formation of oil-in-water type of microemulsion. In vitro drug release profile showed that after 24 hours, 46% and 63% of the drug released through the first formulation in 0.1% (w/v) Tween 80 in distilled water as a release medium and phosphate buffer solution (PBS) at pH = 5.5, respectively. These values were changed to 57% and 98% for the second formulation. Results confirmed that the proposed microemulsion system containing RLX could improve and control the drug release profile in comparison to conventional dosage form.

Preparation of a solid self-microemulsifying drug delivery system by hot-melt extrusion.

PubMed

Silva, Luis Antonio D; Almeida, Susana L; Alonso, Ellen C P; Rocha, Priscila B R; Martins, Felipe T; Freitas, Luís A P; Taveira, Stephania F; Cunha-Filho, Marcilio S S; Marreto, Ricardo N

2018-04-25

Hot-melt extrusion (HME) has gained increasing attention in the pharmaceutical industry; however, its potential in the preparation of solid self-emulsifying drug delivery systems (S-SMEDDS) is still unexplored. This study sought to prepare enteric S-SMEDDS by HME and evaluate the effects of the process and formulation variables on S-SMEDDS properties via Box-Behnken design. Liquid SMEDDS were developed, and carvedilol was used as a class II model drug. Mean size, polydispersity index (PdI) and zeta potential of the resulting microemulsions were determined. The extrudates were then obtained by blending the lipid mixture and HPMCAS using a twin-screw hot-melt extruder. SEM, optical microscopy and PXRD were used to characterize the extrudates. In vitro microemulsion reconstitution and drug release were also studied. L-SMEDDS gave rise to microemulsions with low mean size, PdI and zeta potential (140.04 ± 7.22 nm, 0.219 ± 0.011 and -9.77 ± 0.86 mV). S-SMEDDS were successfully prepared by HME, and an HMPCAS matrix was able to avoid microemulsion reconstitution and retain drug release in pH 1.2 (12.97%-25.54%). Conversely, microemulsion reconstitution and drug release were gradual in pH 6.8 and complete for some formulations. Extrudates prepared at the lowest drug concentration and highest temperature and recirculation time promoted a complete and rapid drug release in pH 6.8 giving rise to small and uniform microemulsion droplets. Copyright © 2018 Elsevier B.V. All rights reserved.

Development of clinical dosage forms for a poorly water-soluble drug II: formulation and characterization of a novel solid microemulsion preconcentrate system for oral delivery of a poorly water-soluble drug.

PubMed

Li, Ping; Hynes, Sara R; Haefele, Thomas F; Pudipeddi, Madhu; Royce, Alan E; Serajuddin, Abu T M

2009-05-01

The solution of a poorly water-soluble drug in a liquid lipid-surfactant mixture, which served as a microemulsion preconcentrate, was converted into a solid form by incorporating it in a solid polyethylene glycol (PEG) matrix. The solid microemulsion preconcentrates thus formed consisted of Capmul PG8 (propylene glycol monocaprylate) as oil, Cremophor EL (polyoxyl 35 castor oil) as surfactant, and hydrophilic polymer PEG 3350 as solid matrix. The drug (aqueous solubility: 0.17 microg/mL at pH 1-8 and 25 degrees C) was dissolved in a melt of the mixture at 65-70 degrees C and then the hot solution was filled into hard gelatin capsules; the liquid gradually solidified upon cooling below 55 degrees C. The solid system was characterized by differential scanning calorimetry (DSC), scanning electron microscopy (SEM), confocal Raman microscopy (CRM), and the dispersion testing in water. It was confirmed that a solid microemulsion preconcentrate is a two-phase system, where clusters of crystalline PEG 3350 formed the solid structure (m.p. 55-60 degrees C) and the liquid microemulsion preconcentrate dispersed in between PEG 3350 crystals as a separate phase. The drug remained dissolved in the liquid phase. In vitro release testing showed that the preconcentrate dispersed readily in water forming a microemulsion with the drug dissolved in the oil particles (<150 nm) and the presence of PEG 3350 did not interfere with the process of self-microemulsification.

Design of Block Copolymer Costabilized Nonionic Microemulsions and Their In Vitro and In Vivo Assessment as Carriers for Sustained Regional Delivery of Ibuprofen via Topical Administration.

PubMed

Djekic, Ljiljana; Martinovic, Martina; Stepanović-Petrović, Radica; Tomić, Maja; Micov, Ana; Primorac, Marija

2015-08-01

Nonionic surfactants (caprylocaproyl macrogol-8 glycerides, octoxynol-12, polysorbate-20, and polyethylene glycol-40 hydrogenated castor oil) (47.03%, w/w), costabilizer (poloxamer 407) (12%-20%, w/w), oil (isopropyl myristate) (5.22%, w/w), water (q.s. ad 100%, w/w), and ibuprofen (5%, w/w) were used to develop oil-in-water microemulsions with Newtonian flow behavior, low viscosity (from 368 ± 38 to 916 ± 46 mPa s), and average droplet size from 14.79 ± 0.31 to 16.54 ± 0.75 nm. Ibuprofen in vitro release from the microemulsions was in accordance with zero-order kinetics (R0(2) > 0.99) for at least 12 h. The maximum drug release rate (3.55%h(-1) ) was from the microemulsion M3 comprising 16%, w/w of poloxamer 407. The release rate of ibuprofen from the reference hydrogel followed Higuchi kinetics (RH(2) > 0.99), and drug amount released after the 6th hour was negligible. In a rat model of inflammation, the microemulsion M3 was significantly more efficacious than the reference hydrogel in exerting antihyperalgesic effects in prophylactic topical treatment, whereas they were comparable in therapeutic treatment as well as in producing antiedematous effect in both protocols. No obvious skin irritation was observed in in vivo studies. The developed nonionic surfactants-based microemulsions containing the optimal concentration of poloxamer 407 could be promising carriers for sustained regional delivery of ibuprofen via topical administration. © 2015 Wiley Periodicals, Inc. and the American Pharmacists Association.

Facile synthesis of a silver nanoparticles/polypyrrole nanocomposite for non-enzymatic glucose determination.

PubMed

Poletti Papi, Maurício A; Caetano, Fabio R; Bergamini, Márcio F; Marcolino-Junior, Luiz H

2017-06-01

The present work describes the synthesis of a new conductive nanocomposite based on polypyrrole (PPy) and silver nanoparticles (PPy-AgNP) based on a facile reverse microemulsion method and its application as a non-enzymatic electrochemical sensor for glucose detection. Focusing on the best sensor performance, all experimental parameters used in the synthesis of nanocomposite were optimized based on its electrochemical response for glucose. Characterization of the optimized material by FT-IR, cyclic voltammetry, and DRX measurements and TEM images showed good monodispersion of semispherical Ag nanoparticles capped by PPy structure, with size average of 12±5nm. Under the best analytical conditions, the proposed sensor exhibited glucose response in linear dynamic range of 25 to 2500μmolL -1 , with limit of detection of 3.6μmolL -1 . Recovery studies with human saliva samples varying from 99 to 105% revealed the accuracy and feasibility of a non-enzymatic electrochemical sensor for glucose determination by easy construction and low-cost. Copyright © 2017 Elsevier B.V. All rights reserved.

Rapid detection of malachite green in fish based on CdTe quantum dots coated with molecularly imprinted silica.

PubMed

Wu, Le; Lin, Zheng-Zhong; Zhong, Hui-Ping; Peng, Ai-Hong; Chen, Xiao-Mei; Huang, Zhi-Yong

2017-08-15

A sensitive fluorescence sensor for the detection of malachite green (MG) was fabricated by grafting molecularly imprinted polymers (MIPs) onto the surface of CdTe quantum dots (QDs). The MIP-coated QDs were synthesized via a reverse microemulsion method using (3-aminopropyl)triethoxysilane (APTES) and tetraethyl orthosilicate (TEOS) as functional monomer and cross-linker, respectively. The optimum molar ratio of MG, functional monomer and cross-linker was 1:3:10. The MIP-coated QDs exhibited uniform spheres with diameter around 49nm and excellent fluorescence emission at λ ex 370nm. A linear relationship with two segments between the relative fluorescence intensities and the MG concentrations ranging from 0.08 to 20μmol·L -1 could be obtained with a detection limit of 12μg·kg -1 . The fluorescent probe was successfully applied to the determination of MG in fish samples with the spiked recoveries ranging from 94.3% to 109.5% which were in accordance with those of the measurement by HPLC-UV. Copyright © 2017 Elsevier Ltd. All rights reserved.

Synthesis of solution-processable poly(3,4 propylenedioxythiophene) nanobelts for electrochromic device applications

NASA Astrophysics Data System (ADS)

Raghavan, Siju Cherikkattil; Shivaprakash, N. Channegowda; Sindhu, Sukumaran Nair

2017-11-01

A new derivative of di-4-isopropyl benzyl substituted propylenedioxythiophene (ProDOT-IPBz2) monomer was synthesized and its resultant polymer was prepared by chemical and electrochemical methods. The chemical polymerization was carried out in a hexane/water reverse microemulsion system using sodium bis(2-ethylhexyl) sulfosuccinate (AOT) as self-assembling template. Chemically synthesized PProDOT-IPBz2 was formed as thin nanobelts with high aspect ratio (3:100), and it was found to be soluble in common organic solvents. The electrochemical and electrochromic (EC) properties of PProDOT-IPBz2 films were studied and it was found that PProDOT-IPBz2 films showed high transparency at oxidized state (+1.0 V) and dark purple color formed at reduced state (-1.0 V). The color contrast of solution cast film was calculated to be 37% T at 550 nm, however electropolymerized PProDOT-IPBz2 film exhibited a color contrast of 48% at 550 nm with switching speed of ∼1 s, and the coloration efficiency was calculated to be 305 cm2C-1.

Multiangular Rod-Shaped Na0.44MnO2 as Cathode Materials with High Rate and Long Life for Sodium-Ion Batteries.

PubMed

Liu, Qiannan; Hu, Zhe; Chen, Mingzhe; Gu, Qinfen; Dou, Yuhai; Sun, Ziqi; Chou, Shulei; Dou, Shi Xue

2017-02-01

The tunnel-structured Na 0.44 MnO 2 is considered as a promising cathode material for sodium-ion batteries because of its unique three-dimensional crystal structure. Multiangular rod-shaped Na 0.44 MnO 2 have been first synthesized via a reverse microemulsion method and investigated as high-rate and long-life cathode materials for Na-ion batteries. The microstructure and composition of prepared Na 0.44 MnO 2 is highly related to the sintering temperature. This structure with suitable size increases the contact area between the material and the electrolyte and guarantees fast sodium-ion diffusion. The rods prepared at 850 °C maintain specific capacity of 72.8 mA h g -1 and capacity retention of 99.6% after 2000 cycles at a high current density of 1000 mA g -1 . The as-designed multiangular Na 0.44 MnO 2 provides new insight into the development of tunnel-type electrode materials and their application in rechargeable sodium-ion batteries.

One-pot preparation of a mixed-mode organic-silica hybrid monolithic capillary column and its application in determination of endogenous gibberellins in plant tissues.

PubMed

Zhang, Zheng; Hao, Yan-Hong; Ding, Jun; Xu, Sheng-Nan; Yuan, Bi-Feng; Feng, Yu-Qi

2015-10-16

A newly improved one-pot method, based on "thiol-ene" click chemistry and sol-gel approach in microemulsion system, was developed for the preparation of C8/PO(OH)2-silica hybrid monolithic capillary column. The prepared monolith possesses large specific surface area, narrow mesopore size distribution and high column efficiency. The monolithic column was demonstrated to have cation exchange/reversed-phase (CX/RP) mixed-mode retention for analytes on nano-liquid chromatography (nano-LC). On the basis of the developed nano-LC system with MS detector coupled to pipette tip solid phase extraction (PT-SPE) and derivatization process, we then realized simultaneous determination of 10 gibberellins (GAs) with low limits of detection (LODs, 0.003-0.025 ng/mL). Furthermore, 6 endogenous GAs in only 5mg rice leaves (fresh weight) were successfully detected and quantified. The developed PT-SPE-nano-LC-MS strategy may offer promising applications in the determination of low abundant bioactive molecules from complex matrix. Copyright © 2015 Elsevier B.V. All rights reserved.

Crystal structure, magnetic properties and advances in hexaferrites: A brief review

NASA Astrophysics Data System (ADS)

Jotania, Rajshree

2014-10-01

Hexaferrites are hard magnetic materials and specifically ferri-magnetic oxides with hexagonal magnetoplumbite type crystallographic structure. Hexagonal ferrites are used as permanent magnets, high-density perpendicular and magneto-optical recording media, and microwave devices like resonance isolators, filters, circulators, phase shifters because of their high magnetic permeability, high electrical resistivity and moderable permittivity. In addition to these; hexagonal ferrites have excellent chemical stability, mechanical hardness and low eddy current loss at high frequencies. The preparation of hexaferrites is a complicated process. Various experimental techniques like standard ceramic techniques, solvent free synthesis route, co precipitation, salt-melt, ion exchange, sol-gel, citrate synthesis, hydrothermal synthesis, spray drying, water-in-oil microemulsion, reverse micelle etc are used to prepare hexaferrite materials. Structural, dielectric and magnetic properties, crystallite size of hexaferrites depend upon nature of substituted ions, method of preparation, sintering temperature and time. The recent interest is nanotechnology, the development of hexaferrite fibres and composites with carbon nano tubes (CNT). Magnetic properties of some doped and un-doped hexaferrites are discussed here. Recent advances in hexaferrites also highlighted in present paper.

Fabrication of hierarchically porous TiO2 nanofibers by microemulsion electrospinning and their application as anode material for lithium-ion batteries.

PubMed

Zhang, Jin; Cai, Yibing; Hou, Xuebin; Song, Xiaofei; Lv, Pengfei; Zhou, Huimin; Wei, Qufu

2017-01-01

Titanium dioxide (TiO 2 ) nanofibers have been widely applied in various fields including photocatalysis, energy storage and solar cells due to the advantages of low cost, high abundance and nontoxicity. However, the low conductivity of ions and bulk electrons hinder its rapid development in lithium-ion batteries (LIB). In order to improve the electrochemical performances of TiO 2 nanomaterials as anode for LIB, hierarchically porous TiO 2 nanofibers with different tetrabutyl titanate (TBT)/paraffin oil ratios were prepared as anode for LIB via a versatile single-nozzle microemulsion electrospinning (ME-ES) method followed by calcining. The experimental results indicated that TiO 2 nanofibers with the higher TBT/paraffin oil ratio demonstrated more axially aligned channels and a larger specific surface area. Furthermore, they presented superior lithium-ion storage properties in terms of specific capacity, rate capability and cycling performance compared with solid TiO 2 nanofibers for LIB. The initial discharge and charge capacity of porous TiO 2 nanofibers with a TBT/paraffin oil ratio of 2.25 reached up to 634.72 and 390.42 mAh·g -1 , thus resulting in a coulombic efficiency of 61.51%; and the discharge capacity maintained 264.56 mAh·g -1 after 100 cycles, which was much higher than that of solid TiO 2 nanofibers. TiO 2 nanofibers with TBT/paraffin oil ratio of 2.25 still obtained a high reversible capacity of 204.53 mAh·g -1 when current density returned back to 40 mA·g -1 after 60 cycles at increasing stepwise current density from 40 mA·g -1 to 800 mA·g -1 . Herein, hierarchically porous TiO 2 nanofibers have the potential to be applied as anode for lithium-ion batteries in practical applications.

Solubilization of water in water-in-oil microemulsions of kerosene

DOE Office of Scientific and Technical Information (OSTI.GOV)

Andheria, A.P.; Bhagwat, S.S.

1995-04-01

The incorporation of water into fuels formulated as microemulsions can offer several advantages such as fire resistance, increased flash point, and improved air-fuel contact. To this end, phase equilibria of kerosene microemulsions employing ionic and nonionic surfactants such as sodium di-(2-ethylhexyl) sulfosuccinate (AOT), lauryl diethanolamide (LDEA), nonylphenol EO-4.5 (NPEO-4.5), sorbitan monolaurate (Span-20), and cetyltrimethylammonium bromide (CTAB), as well as cosurfactants such as n-pentanol, n-hexanol, and n-heptanol, were studied. The effect of the aromaticity of the oil phase on the solubilization of water was also investigated.

Preparation of curcumin microemulsions with food-grade soybean oil/lecithin and their cytotoxicity on the HepG2 cell line.

PubMed

Lin, Chuan-Chuan; Lin, Hung-Yin; Chi, Ming-Hung; Shen, Chin-Min; Chen, Hwan-Wen; Yang, Wen-Jen; Lee, Mei-Hwa

2014-07-01

The choice of surfactants and cosurfactants for preparation of oral formulation in microemulsions is limited. In this report, a curcumin-encapsulated phospholipids-based microemulsion (ME) using food-grade ingredients soybean oil and soybean lecithin to replace ethyl oleate and purified lecithin from our previous study was established and compared. The results indicated soybean oil is superior to ethyl oleate as the oil phase in curcumin microemulsion, as proven by the broadened microemulsion region with increasing range of surfactant/soybean oil ratio (approx. 1:1-12:1). Further preparation of two formula with different particle sizes of formula A (30nm) and B (80nm) exhibited differential effects on the cytotoxicity of hepatocellular HepG2 cell lines. At 15μM of concentration, curcumin-ME in formula A with smaller particle size resulted in the lowest viability (approx. 5%), which might be explained by increasing intake of curcumin, as observed by fluorescence microscopy. In addition, the cytotoxic effect of curcumin-ME is exclusively prominent on HepG2, not on HEK293, which showed over 80% of viability at 15μM. The results from this study might provide an innovative applied technique in the area of nutraceuticals and functional foods. Copyright © 2014 Elsevier Ltd. All rights reserved.

Water-in-oil microemulsions for effective transdermal delivery of proteins.

PubMed

Russell-Jones, Gregory; Himes, Roy

2011-04-01

A water-in-oil microemulsion is a thermodynamically stable emulsion that has the capacity to 'hide' water-soluble molecules within a continuous oil phase. The very small size of the water droplets within the microemulsion means that these types of formulation can be applied topically to the skin, with the result that peptides and proteins can be delivered effectively into the dermal layer. This review discusses the general problems of peptide and protein delivery following topical application, and compares the possible routes of peptide and protein clearance and distribution within the body following topical administration. Several examples of successful peptide and protein delivery using microemulsions are discussed, in addition to the possible alterations in biological profiles following administration via this route. Water-in-oil microemulsions present themselves as an effective means of topical delivery of peptides and proteins of all sizes, and in high doses. These formulations are a cheap, stable, pain-free means of delivery of peptides and proteins to the skin. An exciting area of potential development is the area of weight control management. The results using insulin, IGF-I and GHRP-6 given topically are particularly intriguing. Whether these results can be replicated in humans and whether the use of these drugs for potential treatment of obesity will be commercially viable will be particularly interesting.

Novel extraction induced by microemulsion breaking: a model study for Hg extraction from Brazilian gasoline.

PubMed

Vicentino, Priscila O; Cassella, Ricardo J

2017-01-01

This paper proposes a novel approach for the extraction of Hg from Brazilian gasoline samples: extraction induced by microemulsion breaking (EIMB). In this approach, a microemulsion is formed by mixing the sample with n-propanol and HCl. Afterwards, the microemulsion is destabilized by the addition of water and the two phases are separated: (i) the top phase, containing the residual gasoline and (ii) the bottom phase, containing the extracted analyte in a medium containing water, n-propanol and the ethanol originally present in the gasoline sample. The bottom phase is then collected and the Hg is measured by cold vapor atomic absorption spectrometry (CV-AAS). This model study used Brazilian gasoline samples spiked with Hg (organometallic compound) to optimize the process. Under the optimum extraction conditions, the microemulsion was prepared by mixing 8.7mL of sample with 1.2mL of n-propanol and 0.1mL of a 10molL -1 HCl solution. Emulsion breaking was induced by adding 300µL of deionized water and the bottom phase was collected for the measurement of Hg. Six samples of Brazilian gasoline were spiked with Hg in the organometallic form and recovery percentages in the range of 88-109% were observed. Copyright © 2016 Elsevier B.V. All rights reserved.

Acute and sub-chronic toxicity studies of honokiol microemulsion.

PubMed

Zhang, Qianqian; Li, Jianguo; Zhang, Wei; An, Quan; Wen, Jianhua; Wang, Aiping; Jin, Hongtao; Chen, Shizhong

2015-04-01

The purpose of this study was to investigate the acute and sub-chronic toxicity of honokiol microemulsion. In the acute toxicity tests, the mice were intravenously injected graded doses of honokiol microemulsion and were observed for toxic symptoms and mortality daily for 14 days. In the sub-chronic toxicity study, rats were injected honokiol microemulsion at doses of 100, 500, 2500 μg/kg body weight (BW) for 30 days. After 30 days treatment and 14 days recovery, the rats were sacrificed for hematological, biochemical and histological examination. In the acute toxicity tests, the estimated median lethal dosage (LD50) was 50.5mg/kg body weight in mice. In the sub-chronic toxicity tests, the non-toxic reaction dose was 500 μg/kg body weight. In each treatment group, degeneration or/and necrosis in vascular endothelial cells and structure change of vessel wall can be observed in the injection site (cauda vein) of a few animals while there were no changes in the vessels of other organs. The overall findings of this study indicate that the honokiol microemulsion is non-toxic up to 500 μg/kg body weight, and it has irritation to the vascular of the injection site which should be paid attention to in clinical medication. Copyright © 2015. Published by Elsevier Inc.

Analgesic and anti-inflammatory controlled-released injectable microemulsion: Pseudo-ternary phase diagrams, in vitro, ex vivo and in vivo evaluation.

PubMed

Pineros, Isabel; Slowing, Karla; Serrano, Dolores R; de Pablo, Esther; Ballesteros, Maria Paloma

2017-04-01

Development of analgesic and anti-inflammatory controlled-released injectable microemulsions utilising lysine clonixinate (LC) as model drug and generally regarded as safe (GRAS) excipients. Different microemulsions were optimised through pseudo-ternary phase diagrams and characterised measuring droplet size, viscosity, ex vivo haemolytic activity and in vitro drug release. The anti-inflammatory and analgesic activity was tested in mice (Hot plate test) and rats (Carrageenan-induced paw edema test) respectively and their activity was compared to an aqueous solution of LC salt. The aqueous solution showed a faster and shorter response whereas the optimised microemulsion increased significantly (p<0.01) the potency and duration of the analgesic and anti-inflammatory activity after deep intramuscular injection. The droplet size and the viscosity were key factors to control the drug release from the systems and enhance the effect of the formulations. The microemulsion consisting of Labrafil®/Lauroglycol®/Polysorbate 80/water with LC (56.25/18.75/15/10, w/w) could be a promising formulation after buccal surgery due to its ability to control the drug release and significantly achieve greater analgesic and anti-inflammatory effect over 24h. Copyright © 2016. Published by Elsevier B.V.

Structure Study on Microemulsion System with an Ionic Liquid (IL) by Small-Angle Neutron Scattering

NASA Astrophysics Data System (ADS)

Kang, Tae Hui; Qian, Shuo; Smith, Gregory S.; Do, Changwoo; Heller, William T.

The self-assembly of IL with a long alkyl chains provides molecular level control on the structure enabling applications, including, creating microemulsion with dual functions of extractant and surfactant. The IL, C14MIMCl is not soluble in alkane solvents, even with the addition of octanol. However, with a small amount of water, a water-in-oil micromemulsion forms, that obeys the swelling law with water content. The mixed surfactant system, C14MIMCl/octanol, has different chemistry and molecular geometries depending on its composition. Through the use of SANS, it is possible to determine the impact of the surfactant system on the structure of the microemulsion, as well as to learn the composition of various regions in the structure. The microemulsion system was studied by dilution with octane from 10 to 70 wt%. A strong intensity peak was observed near 0.1 Å-1, and the stable phase shows a structural transition at 30 wt% octane. Contrast variation experiments were done with d-octane and h-octane to understand the structure of the microemulsion, as well as the structural transition. Further, systematic concentration studies of surfactant at constant water-to-oil molar ratio and of water at constant 30 wt% surfactant were performed.

Novel one-step route for synthesizing CdS/polystyrene nanocomposite hollow spheres.

PubMed

Wu, Dazhen; Ge, Xuewu; Zhang, Zhicheng; Wang, Mozhen; Zhang, Songlin

2004-06-22

CdS/polystyrene nanocomposite hollow spheres with diameters between 240 and 500 nm were synthesized under ambient conditions by a novel microemulsion method in which the polymerization of styrene and the formation of CdS nanoparticles were initiated by gamma-irradiation. The product was characterized by transmission electron microscopy (TEM), field-emission scanning electron microscopy (FESEM), X-ray powder diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy, and thermogravimetric analysis (TGA), which show the walls of the hollow spheres are porous and composed of polystyrene containing homogeneously dispersed CdS nanoparticles. The quantum-confined effect of the CdS/polystyrene nanocomposite hollow spheres is confirmed by the ultraviolet-visible (UV-vis) and photoluminescent (PL) spectra. We propose that the walls of these nanocomposite hollow spheres originate from the simultaneous synthesis of polystyrene and CdS nanoparticles at the interface of microemulsion droplets. This novel method is expected to produce various inorganic/polymer nanocomposite hollow spheres with potential applications in the fields of materials science and biotechnology.

Self-Assembly in Systems Containing Silicone Compounds

NASA Astrophysics Data System (ADS)

Ferreira, Maira Silva; Loh, Watson

2009-01-01

Chemical systems formed by silicone solvents and surfactants have potential applications in a variety of industrial products. In spite of their technological relevance, there are few reports on the scientific literature that focus on characterizing such ternary systems. In this work, we have aimed to develop a general, structural investigation on the phase diagram of one system that typically comprises silicone-based chemicals, by means of the SAXS (small-angle X-ray scattering) technique. Important features such as the presence of diverse aggregation states in the overall system, either on their own or in equilibrium with other structures, have been detected. As a result, optically isotropic chemical systems (direct and/or reversed microemulsions) and liquid crystals with lamellar or hexagonal packing have been identified and characterized.

Pharmacokinetics and pharmacodynamics of a new reformulated microemulsion and the long-chain triglyceride emulsion of propofol in beagle dogs

PubMed Central

Lee, S-H; Ghim, J-L; Song, M-H; Choi, H-G; Choi, B-M; Lee, H-M; Lee, E-K; Roh, Y-J; Noh, G-J

2009-01-01

Background and purpose: Microemulsion propofol was developed to eliminate lipid solvent-related adverse events of long-chain triglyceride emulsion (LCT) propofol. We compared dose proportionality, pharmacokinetic and pharmacodynamic characteristics of both formulations. Experimental approach: The study was a randomized, two-period and crossover design with 7-day wash-out period. Microemulsion and LCT propofol were administered by zero-order infusion (0.75, 1.00 and 1.25 mg·kg−1·min−1) for 20 min in 30 beagle dogs (male/female = 5/5 for each rate). Arterial samples were collected at preset intervals. The electroencephalographic approximate entropy (ApEn) was used as a measure of propofol effect. Dose proportionality, pharmacokinetic and pharmacodynamic bioequivalence were evaluated by non-compartmental analyses. Population analysis was performed using nonlinear mixed effects modelling. Key results: Both formulations showed dose proportionality at the applied dose range. The ratios of geometric means of AUClast and AUCinf between both formulations were acceptable for bioequivalence, whereas that of Cmax was not. The pharmacodynamic bioequivalence was indicated by the arithmetic means of AAC (areas above the ApEn time curves) and E0 (baseline ApEn)–Emax (maximally decreased ApEn) between both formulations. The pharmacokinetics of both formulations were best described by three compartment models. Body weight was a significant covariate for V1 of both formulations and sex for k21 of microemulsion propofol. The blood-brain equilibration rate constants (ke0, min−1) were 0.476 and 0.696 for microemulsion and LCT propofol respectively. Conclusions and implications: Microemulsion propofol was pharmacodynamically bioequivalent to LCT propofol although pharmacokinetic bioequivalence was incomplete, and demonstrated linear pharmacokinetics at the applied dose ranges. PMID:19925493

Structure of biodiesel based bicontinuous microemulsions for environmentally compatible decontamination: A small angle neutron scattering and freeze fracture electron microscopy study.

PubMed

Wellert, S; Karg, M; Imhof, H; Steppin, A; Altmann, H-J; Dolle, M; Richardt, A; Tiersch, B; Koetz, J; Lapp, A; Hellweg, T

2008-09-01

Most toxic industrial chemicals and chemical warfare agents are hydrophobic and can only be solubilized in organic solvents. However, most reagents employed for the degradation of these toxic compounds can only be dissolved in water. Hence, microemulsions are auspicious media for the decontamination of a variety of chemical warfare agents and pesticides. They allow for the solubilization of both the lipophilic toxics and the hydrophilic reagent. Alkyl oligoglucosides and plant derived solvents like rapeseed methyl ester enable the formulation of environmentally compatible bicontinuous microemulsions. In the present article the phase behavior of such a microemulsion is studied and the bicontinuous phase is identified. Small angle neutron scattering (SANS) and freeze fracture electron microscopy (FFEM) measurements are used to characterize the structure of the bicontinuous phase and allow for an estimation of the total internal interface. Moreover, also the influence of the co-surfactant (1-pentanol) on the structural parameters of the bicontinuous phase is studied with SANS.

Lecithin-based nanostructured gels for skin delivery: an update on state of art and recent applications.

PubMed

Elnaggar, Yosra S R; El-Refaie, Wessam M; El-Massik, Magda A; Abdallah, Ossama Y

2014-04-28

Conventional carriers for skin delivery encounter obstacles of drug leakage, scanty permeation and low entrapment efficiency. Phospholipid nanogels have recently been recognized as prominent delivery systems to circumvent such obstacles and impart easier application. The current review provides an overview on different types of lecithin nanostructured gels, with particular emphasis on liposomal versus microemulsion gelled systems. Liposomal gels investigated encompassed classic liposomal hydrogel, modified liposomal gels (e.g. Transferosomal, Ethosomal, Pro-liposomal and Phytosomal gels), Microgel in liposomes (M-i-L) and Vesicular phospholipid gel (VPG). Microemulsion gelled systems encompassed Lecithin microemulsion-based organogels (LMBGs), Pluronic lecithin organogels (PLOs) and Lecithin-stabilized microemulsion-based hydrogels. All systems were reviewed regarding matrix composition, state of art, characterization and updated applications. Different classes of lecithin nanogels exhibited crucial impact on transdermal delivery regarding drug permeation, drug loading and stability aspects. Future perspectives of this theme issue are discussed based on current laboratory studies. Copyright © 2014 Elsevier B.V. All rights reserved.

Drug nanocarriers for cancer chemotherapy based on microemulsions: The case of Vemurafenib analog PLX4720.

PubMed

Theochari, Ioanna; Goulielmaki, Maria; Danino, Dganit; Papadimitriou, Vassiliki; Pintzas, Alexandros; Xenakis, Aristotelis

2017-06-01

Oil-in-water (O/W) microemulsions based on Tween 80 as the emulsifier and triacetin as the dispersed oil phase were formulated to be used as delivery vehicles of Vemurafenib analog PLX4720. PLX4720 is a lipophilic antitumor drug against various cancer types correlated with the BRAF V600E mutation. The limits of the single-phase region corresponding to O/W microemulsions as described by ternary phase diagrams were examined. Droplet size measurements determined by dynamic light scattering (DLS) showed mean droplet diameters equal to 10±0.1nm both in the presence and in absence of the drug. Cryogenic-transmission electron microscopy (Cryo-TEM) images of the microemulsions showed the existence of small structures with uniform size distribution having also average diameters of approximately 10nm. Electron paramagnetic resonance (EPR) spectroscopy applying the spin probing technique confirmed PLX4720 location in the oil cores excluding its participation in the surfactants monolayer. Furthermore, cell viability assays on colon cancer cell lines Colo-205 and HT29 showed that microemulsions did not exhibit any cytotoxicity when added in ratios between 0.005% v/v and 0.2% v/v. When the cells were treated with encapsulated PLX4720 at two different concentrations (0.063 and 0.12μΜ) the same response as when dissolved in classic DMSO was observed. Copyright © 2017 Elsevier B.V. All rights reserved.

Microemulsion-enhanced remediation of soils contaminated with organochlorine pesticides.

PubMed

Zhang, Yanlin; Wong, Jonathan W C; Zhao, Zhenyong; Selvam, Ammaiyappan

2011-12-01

Soil contaminated by organic pollutants, especially chlorinated aromatic compounds such as DDT (1,1,1-trichloro-2,2-bis(4-chlorophenyl)ethane), is an environmental concern because of the strong sorption of organochlorine pesticide onto the soil matrix and persistence in the environment. The remediation of organochlorine pesticide contaminated soils through microemulsion is an innovative technology to expedite this process. The remediation efficiency was evaluated by batch experiments through studying the desorption of DDT and hexachlorocyclohexane (y-HCH) and sorption of microemulsion composed of Triton X-100, 1-pentanol and linseed oil in the soil-surfactant-water suspension system. The reduction of desorption efficiency caused by the sorption loss of microemulsion components onto the soil could be corrected by the appropriate adjustment of C/S (Cosurfactant/Surfactant) and O/S (Oil/Surfactant) ratio. The C/S and O/S ratios of 1:2 and 3:20 were suitable to desorb DDT and gamma-HCH from the studied soils because of the lower sorption of Triton X-100 onto the soil. Inorganic salts added in microemulsion increased the pesticides desorption efficiency of pesticides and calcium chloride has a stronger ability to enhance the desorption of DDT than sodium chloride. From the remediation perspective, the balance of surfactant or cosurfactant sorbed to soil and desorption efficiency should be taken into consideration to enhance the remediation of soils contaminated by organochlorine pesticides.

Bimetallic nanoparticles synthesized in microemulsions: A computer simulation study on relationship between kinetics and metal segregation.

PubMed

Tojo, Concha; Buceta, David; López-Quintela, M Arturo

2018-01-15

Computer simulations were carried out to study the origin of the different metal segregation showed by bimetallic nanoparticles synthesized in microemulsions. Our hypothesis is that the kinetics of nanoparticle formation in microemulsions has to be considered on terms of two potentially limiting factors, chemical reaction itself and the rate of reactants exchange between micelles. From the kinetic study it is deduced that chemical reduction in microemulsions is a pseudo first-order process, but not from the beginning. At the initial stage of the synthesis, redistribution of reactants between micelles is controlled by the intermicellar exchange rate, meanwhile the core and middle layers are being built. This exchange control has a different impact depending on the reduction rate of the particular metal in relation to the intermicellar exchange rate. For the case of Au/Pt nanoparticles, the kinetic constant of Au (fast reduction) is strongly dependent on intermicellar exchange rate and reactant concentration. On the contrary, the kinetic constant of Pt (slower reduction) remains constant. Therefore, the fact that the reaction takes place in a microemulsion affects more or less depending on the reduction rate of the metals. As a consequence, the final nanostructure not only depends on difference between the reduction rates of both metals, but also on the reduction rate of each metal in relation to the intermicellar exchange rate. Copyright © 2017 Elsevier Inc. All rights reserved.

Embryo-fetal development toxicity of honokiol microemulsion intravenously administered to pregnant rats.

PubMed

Zhang, Qianqian; Ye, Xiangfeng; Wang, Lingzhi; Peng, Bangjie; Zhang, Yingxue; Bao, Jie; Li, Wanfang; Wei, Jinfeng; Wang, Aiping; Jin, Hongtao; Chen, Shizhong

2016-02-01

The aim of this study was to evaluate the embryo-fetal development toxicity of honokiol microemulsion. The drug was intravenously injected to pregnant SD rats at dose levels of 0, 200, 600 and 2000 μg/kg/day from day 6-15 of gestation. All the pregnant animals were observed for body weights and any abnormal changes and subjected to caesarean-section on gestation day (GD) 20; all fetuses obtained from caesarean-section were assessed by external inspection, visceral and skeletal examinations. No treatment-related external alterations as well as visceral and skeletal malformations were observed in honokiol microemulsion groups. There was no significant difference in the body weight gain of the pregnant rats, average number of corpora lutea, and the gravid uterus weight in the honokiol microemulsion groups compared with the vehicle control group. However, at a dose level of 2000 μg/kg/day, there was embryo-fetal developmental toxicity observed, including a decrease in the body length and tail length of fetuses. In conclusion, the no-observed-adverse-effect level (NOAEL) of honokiol microemulsion is 600 μg/kg/day, 75 times above the therapeutic dosage and it has embryo-fetal toxicity at a dose level of 2000 μg/kg/day, which is approximately 250 times above the therapeutic dosage. Copyright © 2015 Elsevier Inc. All rights reserved.

Utilization of Microemulsions from Rhinacanthus nasutus (L.) Kurz to Improve Carotenoid Bioavailability

PubMed Central

Ho, Nai-Hsing; Inbaraj, Baskaran Stephen; Chen, Bing-Huei

2016-01-01

Carotenoids have been known to reduce the risk of several diseases including cancer and cardiovascular. However, carotenoids are unstable and susceptible to degradation. Rhinacanthus nasutus (L.) Kurz (R. nasutus), a Chinese medicinal herb rich in carotenoids, was reported to possess vital biological activities such as anti-cancer. This study intends to isolate carotenoids from R. nasutus by column chromatography, identify and quantify by HPLC-MS, and prepare carotenoid microemulsions for determination of absolute bioavailability in rats. Initially, carotenoid fraction was isolated using 250 mL ethyl acetate poured into an open-column packed with magnesium oxide-diatomaceous earth (1:3, w/w). Fourteen carotenoids including internal standard β-apo-8′-carotenal were resolved within 62 min by a YMC C30 column and gradient mobile phase of methanol-acetonitrile-water (82:14:4, v/v/v) and methylene chloride. Highly stable carotenoid microemulsions were prepared using a mixture of CapryolTM90, Transcutol®HP, Tween 80 and deionized water, with the mean particle being 10.4 nm for oral administration and 10.7 nm for intravenous injection. Pharmacokinetic study revealed that the absolute bioavailability of carotenoids in microemulsions and dispersion was 0.45% and 0.11%, respectively, while a much higher value of 6.25% and 1.57% were shown for lutein, demonstrating 4-fold enhancement in bioavailability upon incorporation of R. nasutus carotenoids into a microemulsion system. PMID:27150134

In Vivo Evaluation of Transdermal Iodide Microemulsion for Treating Iodine Deficiency Using Sprague Dawley Rats.

PubMed

Alayoubi, Alaadin; Sullivan, Ryan D; Lou, Hao; Patel, Hemlata; Mandrell, Timothy; Helms, Richard; Almoazen, Hassan

2016-06-01

The objective of this study was to evaluate the transdermal efficiency of iodide microemulsion in treating iodine deficiency using rats as an animal model. Animals were fed either iodine-deficient diet (20 μg/kg iodide) or control diet (200 μg/kg iodide) over a 17-month period. At month 14, iodide microemulsion was applied topically in iodine-deficient group and physiological evaluations of thyroid gland functions were characterized by monitoring the thyroid hormones (T3, T4), thyroid-stimulating hormone (TSH), iodide ion excretion in urine, and the overall rat body weights in both groups. Moreover, morphological evaluations of thyroid gland before and after treatment were performed by ultrasound imaging and through histological assessment. Prior to microemulsion treatment, the levels of T3, T4, and TSH in iodine-deficient group were statistically significant as compared to that in the control group. The levels of T3 and T4 increased while TSH level decreased significantly in iodine-deficient group within the first 4 weeks of treatment. After treatment, iodide concentration in urine increased significantly. There was no statistical difference in weight between the two groups. Ultrasound imaging and histological evaluations showed evidence of hyperplasia in iodine-deficient group. Topical iodide microemulsion has shown a promising potential as a novel delivery system to treat iodine deficiency.

Anti-Inflammatory Activity of Babassu Oil and Development of a Microemulsion System for Topical Delivery

PubMed Central

Reis, Mysrayn Y. F. A.; dos Santos, Simone M.; Silva, Danielle R.; Navarro, Daniela M. A. Ferraz; Santos, Geanne K. N.; Hallwass, Fernando; Bianchi, Otávio; Silva, Alexandre G.; Melo, Janaína V.; Machado, Giovanna; Saraiva, Karina L. A.

2017-01-01

Babassu oil extraction is the main income source in nut breakers communities in northeast of Brazil. Among these communities, babassu oil is used for cooking but also medically to treat skin wounds and inflammation, and vulvovaginitis. This study aimed to evaluate the anti-inflammatory activity of babassu oil and develop a microemulsion system with babassu oil for topical delivery. Topical anti-inflammatory activity was evaluated in mice ear edema using PMA, arachidonic acid, ethyl phenylpropiolate, phenol, and capsaicin as phlogistic agents. A microemulsion system was successfully developed using a Span® 80/Kolliphor® EL ratio of 6 : 4 as the surfactant system (S), propylene glycol and water (3 : 1) as the aqueous phase (A), and babassu oil as the oil phase (O), and analyzed through conductivity, SAXS, DSC, TEM, and rheological assays. Babassu oil and lauric acid showed anti-inflammatory activity in mice ear edema, through inhibition of eicosanoid pathway and bioactive amines. The developed formulation (39% A, 12.2% O, and 48.8% S) was classified as a bicontinuous to o/w transition microemulsion that showed a Newtonian profile. The topical anti-inflammatory activity of microemulsified babassu oil was markedly increased. A new delivery system of babassu microemulsion droplet clusters was designed to enhance the therapeutic efficacy of vegetable oil. PMID:29430254

A sensitive fluorescent nanosensor for chloramphenicol based on molecularly imprinted polymer-capped CdTe quantum dots.

PubMed

Amjadi, Mohammad; Jalili, Roghayeh; Manzoori, Jamshid L

2016-05-01

A novel fluorescent nanosensor using molecularly imprinted silica nanospheres embedded CdTe quantum dots (CdTe@SiO2 @MIP) was developed for detection and quantification of chloramphenicol (CAP). The imprinted sensor was prepared by synthesis of molecularly imprinting polymer (MIP) on the hydrophilic CdTe quantum dots via reverse microemulsion method using small amounts of solvents. The resulting CdTe@SiO2 @MIP nanoparticles were characterized by fluorescence, UV-vis absorption and FT-IR spectroscopy and transmission electron microscopy. They preserved 48% of fluorescence quantum yield of the parent quantum dots. CAP remarkably quenched the fluorescence of prepared CdTe@SiO2 @MIP, probably via electron transfer mechanism. Under the optimal conditions, the relative fluorescence intensity of CdTe@SiO2 @MIP decreased with increasing CAP by a Stern-Volmer type equation in the concentration range of 40-500 µg L(-1). The corresponding detection limit was 5.0 µg L(-1). The intra-day and inter-day values for the precision of the proposed method were all <4%. The developed sensor had a good selectivity and was applied to determine CAP in spiked human and bovine serum and milk samples with satisfactory results. Copyright © 2015 John Wiley & Sons, Ltd.

Preparation of CdS Nanoparticles by First-Year Undergraduates

ERIC Educational Resources Information Center

Winkelmann, Kurt; Noviello, Thomas; Brooks, Stephen

2007-01-01

The first year undergraduates use a simple method to synthesize 5-nm CdS nanoparticles in a water-in-oil microemulsion. The quantum size effect, the relationship between colors, optical absorbance, band-gap energy and the CdS particles affected by the formation of micelles are observed.

DOE Office of Scientific and Technical Information (OSTI.GOV)

Xu, Hang, E-mail: xhinbj@126.com; Li, Mei; Jun, Zhang

Graphical abstract: The micro morphological structure of the nano-TiO{sub 2} particles was also observed with TEM, as shown in figure. The TEM images clearly exhibited the homogeneous microstructure of particles with a size of around 10–15 nm. - Highlights: • Nano-TiO{sub 2} was prepared by complex techniques of sol–gel, micro-emulsion and solvent thermal. • The size of TiO{sub 2} was nano level and uniformity. • Nano-TiO{sub 2} exhibited high photo-catalytic activity at internal air lift circulating reactor. • The best nano-TiO{sub 2} dosage was obtained. - Abstract: Anatase nano-titania (TiO{sub 2}) powder was prepared by using a sol–gel process mediatedmore » in reverse microemulsion combined with a solvent thermal technique. The structures of the obtained TiO{sub 2} were characterized by TG-DSC, XRD, TEM. The photocatalytic decomposition of methylene blue (MB) on nano-TiO{sub 2} was studied by using an internal air lift circulating photocatalytic reactor. The results show that the anatase structure appears in the calcination temperature range of 400–510 °C, while the transformation of anatase into rutile takes place above 510 °C. The homogeneous microstructure of nano-TiO{sub 2} particles was obtained with a size of around 10–15 nm. In the photocatalytic performance, degradation process follows pseudo first order kinetics with different dosages of photocatalyst and initial MB concentrations and optimal TiO{sub 2} dosage is 0.1 g/L with neutral medium.« less

Antimicrobial edible coatings and films from micro-emulsions and their food applications

USDA-ARS?s Scientific Manuscript database

This study focused on the use of antimicrobial edible coatings and films from micro-emulsions to reduce populations of foodborne pathogens in foods. Corn-Bio-fiber gum (C-BFG) was used as an emulsifier with chitosan. Allyl isothiocyanate (AIT) and lauric arginate ester (LAE) served as antimicrobials...

Novel nanodispersed coal liquefaction catalysts: Molecular design via microemulsion-based synthesis. Final technical report, October 1990--December 1994

DOE Office of Scientific and Technical Information (OSTI.GOV)

Osseo-Asare, K.; Boakye, E.; Vittal, M.

1995-04-01

This report described the synthesis of Molybdenum Sulfides in microemulsions by acidification of ammonium tetrathiomolybdate. Molybdenum Sulfides have been shown to be potential coal liquefaction catalysts. The importance of particle size, temperature effects, and coal surface chemistry to impregnation are discussed.

A rapid and universal bacteria-counting approach using CdSe/ZnS/SiO2 composite nanoparticles as fluorescence probe.

PubMed

Fu, Xin; Huang, Kelong; Liu, Suqin

2010-02-01

In this paper, a rapid, simple, and sensitive method was described for detection of the total bacterial count using SiO(2)-coated CdSe/ZnS quantum dots (QDs) as a fluorescence marker that covalently coupled with bacteria using glutaraldehyde as the crosslinker. Highly luminescent CdSe/ZnS were prepared by applying cadmium oxide and zinc stearate as precursors instead of pyrophoric organometallic precursors. A reverse-microemulsion technique was used to synthesize CdSe/ZnS/SiO(2) composite nanoparticles with a SiO(2) surface coating. Our results showed that CdSe/ZnS/SiO(2) composite nanoparticles prepared with this method possessed highly luminescent, biologically functional, and monodispersive characteristics, and could successfully be covalently conjugated with the bacteria. As a demonstration, it was found that the method had higher sensitivity and could count bacteria in 3 x 10(2) CFU/mL, lower than the conventional plate counting and organic dye-based method. A linear relationship of the fluorescence peak intensity (Y) and the total bacterial count (X) was established in the range of 3 x 10(2)-10(7) CFU/mL using the equation Y = 374.82X-938.27 (R = 0.99574). The results of the determination for the total count of bacteria in seven real samples were identical with the conventional plate count method, and the standard deviation was satisfactory.

Slow relaxation mode in concentrated oil-in-water microemulsions consisting of repulsive droplets

NASA Astrophysics Data System (ADS)

Hattori, Y.; Ushiki, H.; Courbin, L.; Panizza, P.

2007-02-01

The present contribution reports on the observation of two diffusive relaxation modes in a concentrated microemulsion made of repulsive droplets. These two modes can be interpreted in the frame of Weissman’s and Pusey’s theoretical pioneering works. The fast mode is associated to the collective diffusion of droplets whereas the slow one corresponds to the relaxation of droplet concentration fluctuations associated with composition and/or size. We show that (i) repulsive interactions considerably slow down the latter and (ii) a generalized Stokes Einstein relationship between its coefficient of diffusion and the Newtonian viscosity of the solutions, similar to the Walden’s rule for electrolytes, holds for concentrated microemulsion systems made of repulsive droplets.

A Simple, Inexpensive Molecular Weight Measurement for Water-Soluble Polymers Using Microemulsions.

ERIC Educational Resources Information Center

Mathias, Lon J.; Moore, D. Roger

1985-01-01

Describes an experiment involving use of a microemulsion and its characteristic thermal phase change to determine molecular weights of polyoxyethylene samples. The experiment provides students with background information on polymers and organized media and with experience in evaluating polymer molecular weight by using a unique property of a…

Microemulsion flame pyrolysis for hopcalite nanoparticle synthesis: a new concept for catalyst preparation.

PubMed

Biemelt, T; Wegner, K; Teichert, J; Kaskel, S

2015-04-07

A new route to highly active hopcalite catalysts via flame spray pyrolysis of an inverse microemulsion precursor is reported. The nitrate derived nanoparticles are around 15 nm in diameter and show excellent conversion of CO under ambient conditions, outperforming commercial reference hopcalite materials produced by co-precipitation.

Water solubilization capacity of pharmaceutical microemulsions based on Peceol®, lecithin and ethanol.

PubMed

Mouri, Abdelkader; Diat, Olivier; Lerner, Dan Alain; El Ghzaoui, Abdeslam; Ajovalasit, Alessia; Dorandeu, Christophe; Maurel, Jean-Claude; Devoisselle, Jean-Marie; Legrand, Philippe

2014-11-20

Biocompatible microemulsions composed of Peceol(®), lecithin, ethanol and water developed for encapsulation of hydrophilic drugs were investigated. The binary mixture Peceol(®)/ethanol was studied first. It was shown that the addition of ethanol to pure Peceol(®) has a significant fluidifying and disordering effect on the Peceol(®) supramolecular structure with an enhancement in water solubilization. The water solubilization capacity was improved by adding lecithin as a third component. It was then demonstrated that the ethanol/lecithin weight ratio played an important role in determining the optimal composition in term of water solubilization efficiency, a necessary property for a nutraceutical or pharmaceutical application. The optimal ethanol/lecithin weight ratio in the Peceol(®) rich region was found to be 40/60. Combination different techniques such as SAXS, fluorimetry, rheology and conductivity, we analyzed the water uptake within the microemulsion taking into account the partitioning of ethanol between polar and apolar domains. This ethanol distribution quantified along a water dilution line has a major effect on microemulsion properties. Copyright © 2014 Elsevier B.V. All rights reserved.

Fourier transform infrared study on microemulsion system of potassium salt of bis(2-ethylhexyl) phosphinic acid (HA)

NASA Astrophysics Data System (ADS)

Zhou, Weijin; Shi, Nai; Wang, Yi; Chang, Zhiyuan; Wu, JinGuang

1994-01-01

To study microemulsion formation in a solvent extraction system is to probe into some basic principles of extraction chemistry in the light of combining extraction chemistry with surface chemistry. In our previous investigations, the microemulsions of the salts of HDEHP and PC88A have been studied systematically by FT-IR. In the experiment, we observed the change of peak positions and intensities of P equals O, P-O-C and P-O-H groups during saponification and hydration, and discovered that the peak of P-O-C splits apart into 1045 and 1075 cm-1. The vibration frequency of the P-O-C group in HDEHP and PC88A is quite close to the symmetric stretching frequency of the POO- group, and thus causes difficulties in the study of their peak position and absorbance variation. For this reason we synthesized bis(2-ethylhexyl) phosphinic acid without the P-O-C group. Infrared spectra in the range of 800 - 4000 cm-1 of this microemulsion system was studied.

Fluorinated microemulsions: A study of the phase behavior and structure

DOE Office of Scientific and Technical Information (OSTI.GOV)

LoNostro, P.; Choi, S.M.; Chen, S.H.

1999-06-24

Fluorinated surfactants have been studied for their peculiar property to form micellar aggregates in water and oils (hydrocarbons or fluorocarbons) and to produce stable microemulsions. Because of their capacity to dissolve large amounts of gases (such as oxygen and carbon dioxide) and for their characteristic physicochemical properties, fluorocarbons have been tested for specific medical purposes, and their microemulsions are among the most promising candidates for the production of suitable blood substitutes and other biocompatible fluids. The authors have synthesized a new partially fluorinated nonionic surfactant, namely, F(CF{sub 2}){sub 7}-CO-(OCH{sub 2}CH{sub 2}){sub 7.2}OCH{sub 3} (I), that forms stable microemulsions with watermore » and perfluorocarbons such as perfluorooctane (PFO). In this paper the authors describe for the first time the phase behaviors of perfluorooctanoic acid (PFOA) in water/PFH and in water/PFO, and that of ester I in water/PFO. Small-angle neutron-scattering (SANS) experiments provide a detailed description of the microstructure of the H{sub 2}O/PFO/PFOA ternary system.« less

Solubilization of Tea Seed Oil in a Food-Grade Water-Dilutable Microemulsion

PubMed Central

Deng, Lingli; Que, Fei; Wei, Hewen; Xu, Guangwei; Dong, Xiaowei; Zhang, Hui

2015-01-01

Food-grade microemulsions containing oleic acid, ethanol, Tween 20, and water were formulated as a carrier system for tea seed oil (Camellia oleifera Abel.). The effect of ethanol on the phase behavior of the microemulsion system was clearly reflected in pseudo-ternary diagrams. The solubilization capacity and solubilization efficiency of tea seed oil dispersions were measured along the dilution line at a 70/30 surfactant/oil mass ratio with Tween 20 as the surfactant and oleic acid and ethanol (1:3, w/w) as the oil phase. The dispersed phase of the microemulsion (1.5% weight ratio of tea seed oil to the total amount of oil, surfactant, and tea seed oil) could be fully diluted with water without phase separation. Differential scanning calorimetry and viscosity measurements indicated that both the carrier and solubilized systems underwent a similar microstructure transition upon dilution. The dispersion phases gradually inverted from the water-in-oil phase (< 35% water) to the bicontinuous phase (40–45% water) and finally to the oil-in-water phase (> 45% water) along the dilution line. PMID:25996147

Solubilization of tea seed oil in a food-grade water-dilutable microemulsion.

PubMed

Deng, Lingli; Que, Fei; Wei, Hewen; Xu, Guangwei; Dong, Xiaowei; Zhang, Hui

2015-01-01

Food-grade microemulsions containing oleic acid, ethanol, Tween 20, and water were formulated as a carrier system for tea seed oil (Camellia oleifera Abel.). The effect of ethanol on the phase behavior of the microemulsion system was clearly reflected in pseudo-ternary diagrams. The solubilization capacity and solubilization efficiency of tea seed oil dispersions were measured along the dilution line at a 70/30 surfactant/oil mass ratio with Tween 20 as the surfactant and oleic acid and ethanol (1:3, w/w) as the oil phase. The dispersed phase of the microemulsion (1.5% weight ratio of tea seed oil to the total amount of oil, surfactant, and tea seed oil) could be fully diluted with water without phase separation. Differential scanning calorimetry and viscosity measurements indicated that both the carrier and solubilized systems underwent a similar microstructure transition upon dilution. The dispersion phases gradually inverted from the water-in-oil phase (< 35% water) to the bicontinuous phase (40-45% water) and finally to the oil-in-water phase (> 45% water) along the dilution line.

Alkyl polyglucoside vs. ethoxylated surfactant-based microemulsions as vehicles for two poorly water-soluble drugs: physicochemical characterization and in vivo skin performance.

PubMed

Pajić, Nataša Z Bubić; Todosijević, Marija N; Vuleta, Gordana M; Cekić, Nebojša D; Dobričić, Vladimir D; Vučen, Sonja R; Čalija, Bojan R; Lukić, Milica Ž; Ilić, Tanja M; Savić, Snežana D

2017-12-20

Two types of biocompatible surfactants were evaluated for their capability to formulate skin-friendly/non-irritant microemulsions as vehicles for two poorly water-soluble model drugs differing in properties and concentrations: alkyl polyglucosides (decyl glucoside and caprylyl/capryl glucoside) and ethoxylated surfactants (glycereth-7-caprylate/ caprate and polysorbate 80). Phase behavior, structural inversion and microemulsion solubilization potential for sertaconazole nitrate and adapalene were found to be highly dependent on the surfactants structure and HLB value. Performed characterization (polarized light microscopy, pH, electrical conductivity, rheological, FTIR and DSC measurements) indicated a formulation containing glycereth- 7-caprylate/caprate as suitable for incorporation of both drugs, whereas alkyl polyglucoside-based systems did not exhibit satisfying solubilization capacity for sertaconazole nitrate. Further, monitored parameters were strongly affected by sertaconazole nitrate incorporation, while they remained almost unchanged in adapalene-loaded vehicles. In addition, results of the in vivo skin performance study supported acceptable tolerability for all investigated formulations, suggesting selected microemulsions as promising carriers worth exploring further for effective skin delivery of model drugs.

Delivery systems for biopharmaceuticals. Part II: Liposomes, Micelles, Microemulsions and Dendrimers.

PubMed

Silva, Ana C; Lopes, Carla M; Lobo, José M S; Amaral, Maria H

2015-01-01

Biopharmaceuticals are a generation of drugs that include peptides, proteins, nucleic acids and cell products. According to their particular molecular characteristics (e.g. high molecular size, susceptibility to enzymatic activity), these products present some limitations for administration and usually parenteral routes are the only option. To avoid these limitations, different colloidal carriers (e.g. liposomes, micelles, microemulsions and dendrimers) have been proposed to improve biopharmaceuticals delivery. Liposomes are promising drug delivery systems, despite some limitations have been reported (e.g. in vivo failure, poor long-term stability and low transfection efficiency), and only a limited number of formulations have reached the market. Micelles and microemulsions require more studies to exclude some of the observed drawbacks and guarantee their potential for use in clinic. According to their peculiar structures, dendrimers have been showing good results for nucleic acids delivery and a great development of these systems during next years is expected. This is the Part II of two review articles, which provides the state of the art of biopharmaceuticals delivery systems. Part II deals with liposomes, micelles, microemulsions and dendrimers.

Characterization of 1-ethyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide ([Emim][Tf2N])∕TX-100∕cyclohexane ternary microemulsion: investigation of photoinduced electron transfer in this RTIL containing microemulsion.

PubMed

Sarkar, Souravi; Pramanik, Rajib; Ghatak, Chiranjib; Rao, Vishal Govind; Sarkar, Nilmoni

2011-02-21

In this study we have characterized a ionic liquid 1-ethyl-3-methylimidazolium bis(trifluoromethyl- sulfonyl)imide containing ternary nonaqueous microemulsion ([Emim][Tf(2)N]∕∕TX-100∕cyclo- hexane). The phase behavior and dynamic light scattering study show that the [Emim][Tf(2)N]∕TX-100∕cyclohexane three component system can form microemulsion with [Emim][Tf(2)N] as polar core at suitable condition. We have investigated photoinduced electron transfer (PET) using dimethyl aniline as electron donor and several Coumarin dyes as electron acceptor molecules at two different R values (R = [ionic liquid]∕[surfactant]) to observe how the dynamics of the PET rate is affected in this type of confined microenvironment compared to that of the PET dynamics in neat ionic liquid and other pure solvent media. The plot of observed k(q) values with the free energy change (ΔG(0)) for electron transfer reaction shows an apparent inversion in the observed rate as predicted by the Marcus theory.

A novel micro-emulsion and micelle assembling method to prepare DEC205 monoclonal antibody coupled cationic nanoliposomes for simulating exosomes to target dendritic cells.

PubMed

Li, Kexin; Chang, Shasha; Wang, Zhongyan; Zhao, Xiuli; Chen, Dawei

2015-08-01

Cationic biomimetic exosomes were prepared using a novel micro-emulsion and micelle assembling method by introducing DEC205 monoclonal antibody as specific ligand to target dendritic cells (DCs). The Box-Behnken experimental design was applied for optimization of nanoliposomes (NLip) and DEC205 monoclonal antibody was then conjugated on the surface of NLip (DEC205-NLip). NLip and DEC205-NLip respectively had an average size of 62.7 ± 6.33 nm and 81.64 ± 4.25 nm, zeta potential of +30.5 ± 2.3 mV and +19.8 ± 1.8 mV and encapsulation efficiency of 91.02 ± 3.1% and 93.10 ± 2.2%. In addition, the toxicity studies confirmed DEC205 monoclonal antibody could significantly reduce the cytotoxicity of the cationic lipid against DCs. And the cellular uptake experiment evaluated the significant targeting effect of the DEC205 monoclonal antibody on DC cells. In conclusion, the novel method presented here to prepare biomimetic exosomes was an efficient approach to develop antigen carriers for specific DCs targeting. Copyright © 2015 Elsevier B.V. All rights reserved.

Physicochemical studies of mixed surfactant microemulsions with isopropyl myristate as oil.

PubMed

Bardhan, Soumik; Kundu, Kaushik; Saha, Swapan K; Paul, Bidyut K

2013-07-15

The present study is focused on evaluation of interfacial compositions and thermodynamic properties of w/o mixed surfactant [(sodium dodecylsulfate, SDS/polyoxyethylene (23) lauryl ether, Brij-35)/1-pentanol (Pn)/isopropyl myristate (IPM)] microemulsions under various physicochemical conditions by the dilution method. The number of moles of Pn at the interface (n(a)(i)) and bulk oil (n(a)(o)), and various thermodynamic parameters [viz. standard Gibbs free energy (ΔG(o→i)(0)), standard enthalpy (ΔH(o→i)(0)), and standard entropy (ΔS(o→i)(0)) of the transfer of Pn from bulk oil to the interface] have been found to be dependent on the molar ratio of water to surfactant (ω), concentration of Brij-35 (X(Brij-35)), and temperature. Temperature-insensitive microemulsions with zero specific heat capacity (ΔC(p)(0))(o→i) have been formed at specific compositions. The intrinsic enthalpy change of the transfer process (ΔH(0))(o→i)* has been evaluated from linear correlation between ΔH(o→i)(0) and ΔS(o→i)(0) at different experimental temperatures. The present report also aims at a precise characterization on the basis of molecular interactions between the constituents and provides insight into the nature of the oil/water interfaces of these systems by conductivity and dynamic light scattering studies as a function of ω and X(Brij-35). Conductivity studies reveal that incorporation of Brij-35 in non-percolating water/SDS/Pn/IPM systems makes them favorable for ω-induced percolation behavior up to X(Brij-35) ≤ 0.5. But further addition of Brij-35 causes a decrease in conductivity with increasing ω. Furthermore, the hydrodynamic diameters of the microemulsion droplets increase with increase in both X(Brij-35) and ω. Correlations of the results in terms of the evaluated physicochemical parameters have been attempted. Copyright © 2013 Elsevier Inc. All rights reserved.

Enhanced oral bioavailability of a sterol-loaded microemulsion formulation of Flammulina velutipes, a potential antitumor drug

PubMed Central

Yi, Chengxue; Zhong, Hui; Tong, Shanshan; Cao, Xia; Firempong, Caleb K; Liu, Hongfei; Fu, Min; Yang, Yan; Feng, Yingshu; Zhang, Huiyun; Xu, Ximing; Yu, Jiangnan

2012-01-01

Purpose To investigate the growth inhibition activity of Flammulina velutipes sterol (FVS) against certain human cancer cell lines (gastric SGC and colon LoVo) and to evaluate the optimum microemulsion prescription, as well as the pharmacokinetics of encapsulated FVS. Methods Molecules present in the FVS isolate were identified by gas chromatography/mass spectrometry analysis. The cell viability of FVS was assessed with methyl thiazolyl tetrazolium (MTT) bioassay. Based on the solubility study, phase diagram and stability tests, the optimum prescription of F. velutipes sterol microemulsions (FVSMs) were determined, followed by FVSMs characterization, and its in vivo pharmacokinetic study in rats. Results The chemical composition of FVS was mainly ergosterol (54.8%) and 22,23-dihydroergosterol (27.9%). After 72 hours of treatment, both the FVS (half-maximal inhibitory concentration [IC50] = 11.99 μg · mL−1) and the standard anticancer drug, 5-fluorouracil (IC50 = 0.88 μg · mL−1) exhibited strong in vitro antiproliferative activity against SGC cells, with IC50 > 30.0 μg · mL−1; but the FVS performed poorly against LoVo cells (IC50 > 40.0 μg · mL−1). The optimal FVSMs prescription consisted of 3.0% medium chain triglycerides, 5.0% ethanol, 21.0% Cremophor EL and 71.0% water (w/w) with associated solubility of FVS being 0.680 mg · mL−1 as compared to free FVS (0.67 μg · mL−1). The relative oral bioavailability (area-under-the-curve values of ergosterol and 22,23-dihydroergosterol showed a 2.56-fold and 4.50-fold increase, respectively) of FVSMs (mean diameter ~ 22.9 nm) as against free FVS were greatly enhanced. Conclusion These results indicate that the FVS could be a potential candidate for the development of an anticancer drug and it is readily bioavailable via microemulsion formulations. PMID:23049254

Low-dose oral microemulsion ciclosporin for severe, refractory ulcerative colitis.

PubMed

de Saussure, P; Soravia, C; Morel, P; Hadengue, A

2005-08-01

The optimal modalities of treatment with oral microemulsion ciclosporin in patients with severe, steroid-refractory ulcerative colitis are uncertain. To assess the applicability, in terms of efficacy and tolerability, of a standard oral microemulsion ciclosporin treatment protocol targeting relatively low blood ciclosporin concentrations, in patients with severe, steroid-resistant ulcerative colitis. Patients with a severe attack of ulcerative colitis and no satisfactory response to intravenous corticosteroids were started on oral microemulsion ciclosporin. Dosages were adapted according to a standard protocol, targeting a blood predose ciclosporin concentration (C0) of 100-200 ng/mL. Patients without a clinical response on day 8 were scheduled for colectomy. Sixteen patients were enrolled. A clinical response was observed in 14/16 (88%). The mean clinical activity index scores and concentrations of C-reactive protein on days 0, 4 and 8 were 11.8, 6.7 and 4.1, and 50.3, 19.3 and 9.7 mg/L respectively. The mean C0 (days 0-8) was 149 pg/mL. The mean creatinine clearance rates on days 0 and 8 were 88 and 96 mL/min. One patient had an acute elevation of transaminases that resulted in discontinuing ciclosporin. Even when dosed for a target C0 of 100-200 ng/mL, oral microemulsion ciclosporin for severe, steroid-refractory ulcerative colitis achieves an efficacy similar to that attained with higher, potentially more toxic levels. The oral route should replace intravenous treatment in this clinical setting.

Microemulsion Formulation of Carbendazim and Its In Vitro Antifungal Activities Evaluation

PubMed Central

Leng, Pengfei; Zhang, Zhiming; Li, Qian; Zhao, Maojun; Pan, Guangtang

2014-01-01

The fungus Rhizoctonia solani Kuhn is a widespread and destructive plant pathogen with a very broad host range. Although various pathogens, including R. solani, have been traditionally controlled using chemical pesticides, their use faces drawbacks such as environmental pollution, development of pesticide resistance, and other negative effects. Carbendazim is a well-known antifungal agent capable of controlling a broad range of plant diseases, but its use is hampered by its poor aqueous solubility. In this study, we describe an environmentally friendly pharmaceutical microemulsion system using carbendazim as the active ingredient, chloroform and acetic acid as solvents, and the surfactants HSH and 0204 as emulsifiers. This system increased the solubility of carbendazim to 30 g/L. The optimal microemulsion formulation was determined based on a pseudo-ternary phase diagram; its physicochemical characteristics were also tested. The cloud point was greater than 90°C and it was resistant to freezing down to −18°C, both of which are improvements over the temperature range in which pure carbendazim can be used. This microemulsion meets the standard for pesticide microemulsions and demonstrated better activity against R. solani AG1-IA, relative to an aqueous solution of pure carbendazim (0.2 g/L). The mechanism of activity was reflected in the inhibition of against R. solani AG1-IA including mycelium growth, and sclerotia formation and germination were significantly better than that of 0.2 g/L carbendazim water solution according to the results of t-test done by SPSS 19. PMID:25310219

In vivo evaluation of anticonvulsant and antioxidant effects of phenobarbital microemulsion for transdermal administration in pilocarpine seizure rat model.

PubMed

Figueiredo, Kayo Alves; Medeiros, Shirlene Cesário; Neves, Jamilly Kelly Oliveira; da Silva, José Alexsandro; da Rocha Tomé, Adriana; Carvalho, André Luis Menezes; de Freitas, Rivelilson Mendes

2015-04-01

This study aimed to evaluate a microemulsion system (ME) containing phenobarbital in epilepsy model induced by pilocarpine in rats and to oxidative stress and histologic lesions in hippocampus. The microemulsion was applied to the shaved back of Wistar rats. The animals were divided into the following groups: control group (P400); ME50 40mg/kg, topically-t.p.; ME100, 40mg/kg, t.p.; EM50, 40mg/kg, t.p.; phenobarbital solution 40mg/kg (PS), oral. After 60min, behavioral changes were evaluated for 1h in the model of epileptical crisis induced by pilocarpine. Phenobarbital in microemulsion was able to increase the latency for status epilepticus (SE) (p<0.05), decrease the number of epileptical crisis (ME50: p<0.001; ME100: p<0.01) and decrease mortality rate by 80% compared to P400. In EM50 and PS groups, deaths were decreased by 53.3% and 100% respectively. The ME50 and ME100 groups were able to reduce oxidative stress in experimental animals when compared to the P400. The microemulsion was still capable of reducing neuronal damage in the hippocampal areas. The results of this study come in an innovative way, demonstrating the ability of transdermal ME50 and ME100 to reduce pilocarpine-induced epileptical crisis, oxidative stress, besides neuronal damages. Copyright © 2015 Elsevier Inc. All rights reserved.

Transdermal agomelatine microemulsion gel: pyramidal screening, statistical optimization and in vivo bioavailability.

PubMed

Said, Mayada; Elsayed, Ibrahim; Aboelwafa, Ahmed A; Elshafeey, Ahmed H

2017-11-01

Agomelatine is a new antidepressant having very low oral drug bioavailability less than 5% due to being liable to extensive hepatic 1st pass effect. This study aimed to deliver agomelatine by transdermal route through formulation and optimization of microemulsion gel. Pyramidal screening was performed to select the most suitable ingredients combinations and then, the design expert software was utilized to optimize the microemulsion formulations. The independent variables of the employed mixture design were the percentages of capryol 90 as an oily phase (X 1 ), Cremophor RH40 and Transcutol HP in a ratio of (1:2) as surfactant/cosurfactant mixture 'S mix ' (X 2 ) and water (X 3 ). The dependent variables were globule size, optical clarity, cumulative amount permeated after 1 and 24 h, respectively (Q1 and Q 24 ) and enhancement ratio (ER). The optimized formula was composed of 5% oil, 45% S mix and 50% water. The optimized microemulsion formula was converted into carbopol-based gel to improve its retention on the skin. It enhanced the drug permeation through rat skin with an enhancement ratio of 37.30 when compared to the drug hydrogel. The optimum ME gel formula was found to have significantly higher C max , AUC 0-24 h and AUC 0-∞ than that of the reference agomelatine hydrogel and oral solution. This could reveal the prosperity of the optimized microemulsion gel formula to augment the transdermal bioavailability of agomelatine.

Microemulsion formulation of Carbendazim and its in vitro antifungal activities evaluation.

PubMed

Leng, Pengfei; Zhang, Zhiming; Li, Qian; Zhao, Maojun; Pan, Guangtang

2014-01-01

The fungus Rhizoctonia solani Kuhn is a widespread and destructive plant pathogen with a very broad host range. Although various pathogens, including R. solani, have been traditionally controlled using chemical pesticides, their use faces drawbacks such as environmental pollution, development of pesticide resistance, and other negative effects. Carbendazim is a well-known antifungal agent capable of controlling a broad range of plant diseases, but its use is hampered by its poor aqueous solubility. In this study, we describe an environmentally friendly pharmaceutical microemulsion system using carbendazim as the active ingredient, chloroform and acetic acid as solvents, and the surfactants HSH and 0204 as emulsifiers. This system increased the solubility of carbendazim to 30 g/L. The optimal microemulsion formulation was determined based on a pseudo-ternary phase diagram; its physicochemical characteristics were also tested. The cloud point was greater than 90°C and it was resistant to freezing down to -18°C, both of which are improvements over the temperature range in which pure carbendazim can be used. This microemulsion meets the standard for pesticide microemulsions and demonstrated better activity against R. solani AG1-IA, relative to an aqueous solution of pure carbendazim (0.2 g/L). The mechanism of activity was reflected in the inhibition of against R. solani AG1-IA including mycelium growth, and sclerotia formation and germination were significantly better than that of 0.2 g/L carbendazim water solution according to the results of t-test done by SPSS 19.

"Micro to macro (M2M)"--A novel approach for intravenous delivery of propofol.

PubMed

Damitz, Robert; Chauhan, Anuj

2015-10-15

Propofol emulsions have limited shelf life and safety concerns for injection. Microemulsions of propofol are thermodynamically stable and simpler to manufacture, but cause additional pain on injection. We propose a novel micro to macro (M2M) approach of destabilizing a microemulsion immediately prior to injection. Microemulsions of propofol were prepared at two to three times the drug loadings of commercial formulations. We determined suitable microemulsion compositions which destabilize into macroemulsions after two or three fold dilutions with water. Droplet growth after dilution was measured with dynamic light scattering. Increasing solution turbidity after dilution was also measured optically with millisecond resolution. Experimental data was analyzed in the context of a coalescence model. Microemulsions rapidly coalesce into larger droplet size macroemulsions after dilution according to the phase diagram shift. The resulting macroemulsions are metastable retaining their droplet size for several hours. Droplet growth occurs on the order of seconds and a metastable size of about 1 micron is reached in minutes. Rates of droplet growth and metastable droplet sizes depend on the surfactant composition. The coalescence model predicts droplet growth with good agreement but only after accounting for the finite probability of coalescence from each collision. The M2M concept has been demonstrated for the anesthetic drug propofol which may improve stability and manufacturability in addition to reducing pain on injection. This approach could be adapted to other hydrophobic vesicant drugs as well. Copyright © 2015 Elsevier B.V. All rights reserved.

Syntheses of crosslinked latex nanoparticles using differential microemulsion polymerization

NASA Astrophysics Data System (ADS)

Hassmoro, N. F.; Rusop, M.; Abdullah, S.

2013-06-01

The differential microemulsion polymerization was used to synthesize latex nanoparticles. In this paper, 1, 3-butylene glycol dimethacrylate (1, 3-BGDMA) was used as a crosslinker respectively 1-5 weight% of monomer total. Butyl acrylate (BA), butyl methacrylate (BMA), and methacrylic acid (MAA) was used as the monomer. The thin film of latex nanoparticles were prepared by using spin coating method and have been dried at 100°C for 5 minutes. The amount of the crosslinker added in the polymerization was optimized and we found that the particle sizes fall in the range of 30-60 nm. The structural morphology of the uncrosslinked latex represented the most homogeneous image compared to the crosslinked latex. The effect of the amount of crosslinker on the particle sizes investigated by the Zeta-sizer Nano series while Atomic Force microscopy (AFM) was used to study the structural properties of latex nanoparticles.

Spontaneous and Flow-Driven Interfacial Phase Change: Dynamics of Microemulsion Formation at the Pore Scale.

PubMed

Tagavifar, Mohsen; Xu, Ke; Jang, Sung Hyun; Balhoff, Matthew T; Pope, Gary A

2017-11-14

The dynamic behavior of microemulsion-forming water-oil-amphiphiles mixtures is investigated in a 2.5D micromodel. The equilibrium phase behavior of such mixtures is well-understood in terms of macroscopic phase transitions. However, what is less understood and where experimental data are lacking is the coupling between the phase change and the bulk flow. Herein, we study the flow of an aqueous surfactant solution-oil mixture in porous media and analyze the dependence of phase formation and spatial phase configurations on the bulk flow rate. We find that a microemulsion forms instantaneously as a boundary layer at the initial surface of contact between the surfactant solution and oil. The boundary layer is temporally continuous because of the imposed convection. In addition to the imposed flow, we observe spontaneous pulsed Marangoni flows that drag the microemulsion and surfactant solution into the oil stream, forming large (macro)emulsion droplets. The formation of the microemulsion phase at the interface distinguishes the situation from that of the more common Marangoni flow with only two phases present. Additionally, an emulsion forms via liquid-liquid nucleation or the Ouzo effect (i.e., spontaneous emulsification) at low flow rates and via mechanical mixing at high flow rates. With regard to multiphase flow, contrary to the common belief that the microemulsion is the wetting liquid, we observe that the minor oil phase wets the solid surface. We show that a layered flow pattern is formed because of the out-of-equilibrium phase behavior at high volumetric flow rates (order of 2 m/day) where advection is much faster than the diffusive interfacial mass transfer and transverse mixing, which promote equilibrium behavior. At lower flow rates (order of 30 cm/day), however, the dynamic and equilibrium phase behaviors are well-correlated. These results clearly show that the phase change influences the macroscale flow behavior.

Fluorescence resonance energy transfer in microemulsions composed of tripled-chain surface active ionic liquids, RTILs, and biological solvent: an excitation wavelength dependence study.

PubMed

Banerjee, Chiranjib; Kundu, Niloy; Ghosh, Surajit; Mandal, Sarthak; Kuchlyan, Jagannath; Sarkar, Nilmoni

2013-08-15

In this article we have reported the fluorescence resonance energy transfer (FRET) study in our earlier characterized surface active ionic liquids (SAILs)-containing microemulsion, i.e., N-methyl-N-propylpyrrolidinium bis(trifluoromethanesulfonyl)imide ([P13][Tf2N])/[CTA][AOT]/isopropyl myristate ([IPM]) and N,N,N-trimethyl-N-propylammonium bis(trifluoromethanesulfonyl)imide ([N3111][Tf2N])/[CTA][AOT]/[IPM] microemulsions (Banerjee, C.; Mandal, S.; Ghosh, S.; Kuchlyan, J.; Kundu, N.; Sarkar, N. J. Phys. Chem. B 2013, 117, 3927-3934). The occurrence of effective FRET from the donor, coumarin-153 (C-153) to the acceptor rhodamine 6G (R6G) is evident from the decrease in the steady state fluorescence intensity of the donor with addition of acceptor and subsequent increase in the fluorescence intensity of the acceptor in the presence of donor. The excitation wavelength dependent FRET from C-153 to R6G has also been performed to assess the dynamic heterogeneity of these confined systems. In time-resolved experiments, the significant rise time of the acceptor in the presence of the donor further confirms the occurrence of FRET. The multiple donor-acceptor (D-A) distances, for various microemulsions, obtained from the rise times of the acceptor emission in the presence of a donor can be rationalized from the varying distribution of the donor, C-153, in the different regions of the microemulsion. Time-resolved measurement reveals that with increasing excitation wavelength from 408 to 440 nm, the contribution of the faster rise component of FRET increases significantly due to the close proximity of the C-153 and R6G in the polar region of the microemulsion where occurrence of FRET is very high. Moreover, we have also studied the FRET with variation of R (R = [room temperature ionic liquids (RTILs)]/[surfactant]) and shown that the effect of excitation wavelength on FRET is similar irrespective of R values.

Goat anti-rabbit IgG conjugated fluorescent dye-doped silica nanoparticles for human breast carcinoma cell recognition.

PubMed

Chen, Min-Yan; Chen, Ze-Zhong; Wu, Ling-Ling; Tang, Hong-Wu; Pang, Dai-Wen

2013-11-12

We report an indirect method for cancer cell recognition using photostable fluorescent silica nanoprobes as biological labels. The dye-doped fluorescent silica nanoparticles were synthesized using the water-in-oil (W/O) reverse microemulsion method. The silica matrix was produced by the controlled hydrolysis of tetraethylorthosilicate (TEOS) in water nanodroplets with the initiation of ammonia (NH3·H2O). Fluorescein isothiocyanate (FITC) or rhodamine B isothiocyanate conjugated with dextran (RBITC-Dextran) was doped in silica nanoparticles (NPs) with a size of 60 ± 5 nm as a fluorescent signal element by covalent bonding and steric hindrance, respectively. The secondary antibody, goat anti-rabbit IgG, was conjugated on the surface of the PEG-terminated modified FITC-doped or RBITC-Dextran-doped silica nanoparticles (PFSiNPs or PBSiNPs) by covalent binding to the PEG linkers using the cyanogen bromide method. The concentrations of goat anti-rabbit IgG covering the nanoprobes were quantified via the Bradford method. In the proof-of-concept experiment, an epithelial cell adhesion molecule (EpCAM) on the human breast cancer SK-Br-3 cell surface was used as the tumor marker, and the nanoparticle functionalized with rabbit anti-EpCAM antibody was employed as the nanoprobe for cancer cell recognition. Compared with fluorescent dye labeled IgG (FITC-IgG and RBITC-IgG), the designed nanoprobes display dramatically increased stability of fluorescence as well as photostability under continuous irradiation.

Cd-free Cu-Zn-In-S/ZnS quantum dots@SiO2 multiple cores nanostructure: preparation and application for white LEDs

NASA Astrophysics Data System (ADS)

Jiang, Tongtong; Shen, Mohan; Dai, Peng; Wu, Mingzai; Yu, Xinxin; Li, Guang; Xu, Xiaoliang; Zeng, Haibo

2017-10-01

The work reports the fabrication of Cu doped Zn-In-S (CZIS) alloy quantum dots (QDs) using dodecanethiol and oleic acid as stabilizing ligands. With the increase of doped Cu element, the photoluminescence (PL) peak is monotonically red shifted. After coating ZnS shell, the PL quantum yield of CZIS QDs can reach 78%. Using reverse micelle microemulsion method, CZIS/ZnS QDs@SiO2 multi-core nanospheres were synthesized to improve the colloidal stability and avoid the aggregation of QDs. The obtained multi-core nanospheres were dispersed in curing adhesive, and applied as a color conversion layer in down converted light-emitting diodes. After encapsulation in curing adhesive, the newly designed LEDs show artifically regulated color coordinates with varying the weight ratio of green QDs and red QDs, and the concentrations of these two types of QDs. Moreover, natural white and warm white LEDs with correlated color temperature of 5287, 6732, 2731, and 3309 K can be achieved, which indicates that CZIS/ZnS QDs@SiO2 nanostructures are promising color conversion layer material for solid-state lighting application.

Effect of AOT Microemulsion Composition on the Hydrodynamic Diameter and Electrophoretic Mobility of Titanium Oxide Nanoparticles

NASA Astrophysics Data System (ADS)

Shaparenko, N. O.; Beketova, D. I.; Demidova, M. G.; Bulavchenko, A. I.

2018-05-01

The hydrodynamic diameter and electrophoretic mobility of titania nanoparticles in AOT microemulsions are studied depending on their water content (from 0 to 1.5 vol %), chloroform content in n-decane-chloroform mixture (from 0 to 30 vol %) and temperature (from 0 to 60°C). Considerable changes in diameter (from 20 to 400 nm) are detected upon adding water to the microemulsion. The electrophoretic mobility grows by 2-3 times upon adding chloroform, or as the temperature falls. The observed features allow us to halve the time of electrophoretic concentration for 140 nm TiO2 nanoparticles, and to concentrate 14 nm nanoparticles that do not exhibit electrophoretic mobility in the absence of chloroform.

Simultaneous determination of kolliphor HS15 and miglyol 812 in microemulsion formulation by ultra-high performance liquid chromatography coupled with nano quantity analyte detector.

PubMed

Zhang, Honggen; Wang, Zhenyu; Liu, Oscar

2016-02-01

A novel method for simultaneous determination of kolliphor HS15 and miglyol 812 in microemulsion formulation was developed using ultra-high performance liquid chromatography coupled with a nano quantitation analytical detector (UHPLC-NQAD). All components in kolliphor HS15 and miglyol 812 were well separated on an Acquity BEH C 18 column. Mobile phase A was 0.1% trifluoroacetic acid (TFA) in water and mobile phase B was acetonitrile. A gradient elution sequence was programed initially with 60% organic solvent, slowly increased to 100% within 8 min. The flow rate was 0.7 mL/min. Good linearity ( r >0.95) was obtained in the range of 27.6-1381.1 μg/mL for polyoxyl 15 hydroxystearate in kolliphor HS15, 0.8-202.0 μg/mL for caprylic acid triglyceride and 2.7-221.9 μg/mL for capric acid triglyceride in miglyol 812. The relative standard deviations (RSD) ranged from 0.6% to 1.7% for intra-day precision and from 0.4% to 2.7% for inter-day precision. The overall recoveries (accuracy) were 99.7%-101.4% for polyoxyl 15 hydroxystearate in kolliphor HS15, 96.7%-99.6% for caprylic acid triglyceride, and 94.1%-103.3% for capric acid triglyceride in miglyol 812. Quantification limits (QL) were determined as 27.6 μg/mL for polyoxyl 15 hydroxystearate in kolliphor HS15, 0.8 μg/mL for caprylic acid triglyceride, and 2.7 μg/mL for capric acid triglyceride in miglyol 812. No interferences were observed in the retention time ranges of kolliphor HS15 and miglyol 812. The method was validated in terms of specificity, linearity, precision, accuracy, QL, and robustness. The proposed method has been applied to microemulsion formulation analyses with good recoveries (82.2%-103.4%).

Lecithin-linker formulations for self-emulsifying delivery of nutraceuticals.

PubMed

Chu, Jacquelene; Cheng, Yu-Ling; Rao, A Venketeshwer; Nouraei, Mehdi; Zarate-Muñoz, Silvia; Acosta, Edgar J

2014-08-25

Lecithin-linker microemulsions are formulations produced with soybean lecithin in combination with a highly lipophilic (lipophilic linker) and highly hydrophilic (hydrophilic linkers) surfactant-like additives. In this work, lecithin-linker systems were formulated to produce self-emulsifying delivery systems for β-carotene and β-sitosterol. The concentration of the lipophilic linker, sorbitan monooleate, was adjusted to minimize the formation of liquid crystals. The concentration of hydrophilic linkers, decaglyceryl caprylate/caprate and PEG-6-caprylic/capric glycerides, was gradually increased (scanned) until single phase clear microemulsions were obtained. For these scans, the oil (ethyl caprate) to water ratio was set to 1. The single phase, clear microemulsions were diluted with fed-state simulated intestinal fluid (FeSSIF) and produced stable emulsions, with drop sizes close to 200 nm. Using pseudo-ternary phase diagrams to evaluate the process of dilution of microemulsion preconcentrates (mixtures of oil, lecithin and linkers with little or no water) with FeSSIF, it was determined that self-emulsifying systems are obtained when the early stages of the dilution produce single phase microemulsions. If liquid crystals or multiple phase systems are obtained during those early stages, then the emulsification yields unstable emulsions with large drop sizes. An in vitro permeability study conducted using a Flow-Thru Dialyzer revealed that stable emulsions with drop sizes of 150-300 nm produce large and irreversible permeation of β-carotene to sheep intestine. On the other hand, unstable emulsions produced without the linker combination separated in the dialyzer chamber. Copyright © 2014 Elsevier B.V. All rights reserved.

Microemulsion Transdermal Formulation for Simultaneous Delivery of Valsartan and Nifedipine: Formulation by Design.

PubMed

Sood, Jatin; Sapra, Bharti; Tiwary, Ashok K

2017-08-01

The objective of the study was to optimize the proportion of different components for formulating oil in water microemulsion formulation meant for simultaneous transdermal delivery of two poorly soluble antihypertensive drugs. Surface response methodology of Box-Behnken design was utilized to evaluate the effect of two oils (Captex 500 - x1 and Capmul MCM - x2) and surfactant (Acrysol EL135 - x3) on response y1 (particle size), y2 (solubility of valsartan), and y3 (solubility of nifedipine). The important factors which significantly affected the responses were identified and validated using ANOVA. The model was diagnosed using normal plot of residuals and Box-Cox plot. The design revealed an inverse correlation between particle size and concentration of Capmul MCM and Acrysol EL 135. However, an increase in concentration of Captex 500 led to an increase in particle size of microemulsion. Solubility of valsartan decreased while that of nifedipine increased with increase in concentration of Captex 500. Capmul MCM played a significant role in increasing the solubility of valsartan. The effect of Acrysol EL 135 on solubility of both drugs, although significant, was only marginal as compared to that of Captex 500 and Capmul MCM. The optimized microemulsion was able to provide an enhancement ratio of 27.21 and 63.57-fold for valsartan and nifedipine, respectively, with respect to drug dispersion in aqueous surfactant system when evaluated for permeation studies. The current studies candidly suggest the scope of microemulsion systems for solubilizing as well as promoting the transport of both drugs across rat skin at an enhanced permeation rate.

FIELD IMPLEMENTATION OF A WINSOR TYPE I SURFACTANT/ALCOHOL MIXTURE FOR IN SITU SOLUBILIZATION OF A COMPLEX LNAPL AS A SINGLE-PHASE MICROEMULSION

EPA Science Inventory

A Winsor Type I surfactant/alcohol mixture was used as an in situ flushing agent to solubilize a muticomponent nonaqueous phase liquid (NAPL) as a single-phase microemulsion (SPME) in a hydraulically isolated test cell at Hill Air Force Base (AFB), Utah. The surfactant (polyoxye...

Fuel Microemulsions for Jet Engine Smoke Reduction

DTIC Science & Technology

1980-05-01

ESL-TR-80-25 FUEL MICROEMULSIONS FOR JET ENGINE SMOKE REDUCTION LEVEL$: 0• D.W. NAEGELI , G.E. FODOR, C.A. MOSES MOBILE ENERGY DIVISION 1N•j SOUTHWEST...Moses, C.A, and D.W. Naegeli , "Fuel Property Effects on Combustor Per- formance," AS!E Paper 79-GT-178, San Diego, CA, January 1979. 17. Naegeli , D.W

Reactivity, chemoselectivity, and diastereoselectivity of the oxyfunctionalization of chiral allylic alcohols and derivatives in microemulsions: comparison of the chemical oxidation by the hydrogen peroxide/sodium molybdate system with the photooxygenation.

PubMed

Nardello, Véronique; Caron, Laurent; Aubry, Jean-Marie; Bouttemy, Sabine; Wirth, Thomas; Saha-Möller Chantu, R; Adam, Waldemar

2004-09-01

The chiral allylic alcohols 1a-d and their acetate (1e) and silyl ether (1f) derivatives have been oxidized by the H2O2/MoO4(2)- system, a convenient and efficient chemical source of singlet oxygen. This chemical peroxidation (formation of the allylic hydroperoxides 2) has been conducted in various media, which include aqueous solutions, organic solvents, and microemulsions. The reactivity, chemoselectivity, and diastereoselectivity of this chemical oxidation are compared to those of the sensitized photooxygenation, with the emphasis on preparative applications in microemulsion media. While a similar threo diastereoselectivity is observed for both modes of peroxidation, the chemoselectivity differs significantly, since in the chemical oxidation with the H2O2/MoO4(2)- system the undesirable epoxidation by the intermediary peroxomolybdate competes efficiently with the desirable peroxidation by the in situ generated singlet oxygen. A proper choice of the type of microemulsion and the reaction conditions furnishes a high chemoselectivity (up to 97%) in favor of threo-diastereoselective (up to 92%) peroxidation. Copyright 2004 American Chemical Society

Continuous process for singlet oxygenation of hydrophobic substrates in microemulsion using a pervaporation membrane.

PubMed

Caron, Laurent; Nardello, Véronique; Mugge, José; Hoving, Erik; Alsters, Paul L; Aubry, Jean-Marie

2005-02-15

Chemically generated singlet oxygen (1O2, 1Deltag) is able to oxidize a great deal of hydrophobic substrates from molybdate-catalyzed hydrogen peroxide decomposition, provided a suitable reaction medium such as a microemulsion system is used. However, high substrate concentrations or poorly reactive organics require large amounts of H2O2 that generate high amounts of water and thus destabilize the system. We report results obtained on combining dark singlet oxygenation of hydrophobic substrates in microemulsions with a pervaporation membrane process. To avoid composition alterations after addition of H2O2 during the peroxidation, the reaction mixture circulates through a ceramic membrane module that enables a partial and selective dewatering of the microemulsion. Optimization phase diagrams of sodium molybdate/water/alcohol/anionic surfactant/organic solvent have been elaborated to maximize the catalyst concentration and therefore the reaction rate. The membrane selectivity towards the mixture constituents has been investigated showing that a high retention is observed for the catalyst, for organic solvents and hydrophobic substrates, but not for n-propanol (cosurfactant) and water. The efficiency of such a process is illustrated with the peroxidation of a poorly reactive substrate, viz., beta-pinene.

Process spectroscopy in microemulsions—Raman spectroscopy for online monitoring of a homogeneous hydroformylation process

NASA Astrophysics Data System (ADS)

Paul, Andrea; Meyer, Klas; Ruiken, Jan-Paul; Illner, Markus; Müller, David-Nicolas; Esche, Erik; Wozny, Günther; Westad, Frank; Maiwald, Michael

2017-03-01

A major industrial reaction based on homogeneous catalysis is hydroformylation for the production of aldehydes from alkenes and syngas. Hydroformylation in microemulsions, which is currently under investigation at Technische Universität Berlin on a mini-plant scale, was identified as a cost efficient approach which also enhances product selectivity. Herein, we present the application of online Raman spectroscopy on the reaction of 1-dodecene to 1-tridecanal within a microemulsion. To achieve a good representation of the operation range in the mini-plant with regard to concentrations of the reactants a design of experiments was used. Based on initial Raman spectra partial least squares regression (PLSR) models were calibrated for the prediction of 1-dodecene and 1-tridecanal. Limits of predictions arise from nonlinear correlations between Raman intensity and mass fractions of compounds in the microemulsion system. Furthermore, the prediction power of PLSR models becomes limited due to unexpected by-product formation. Application of the lab-scale derived calibration spectra and PLSR models on online spectra from a mini-plant operation yielded promising estimations of 1-tridecanal and acceptable predictions of 1-dodecene mass fractions suggesting Raman spectroscopy as a suitable technique for process analytics in microemulsions.

Antimicrobial property and microstructure of micro-emulsion edible composite films against Listeria.

PubMed

Guo, Mingming; Jin, Tony Z; Yadav, Madhav P; Yang, Ruijin

2015-09-02

Edible antimicrobial composite films from micro-emulsions containing all natural compounds were developed and their antimicrobial properties and microstructures were investigated. Chitosan, allyl isothiocyanate (AIT), barley straw arabinoxylan (BSAX), and organic acids (acetic, lactic and levulinic acids) were used as film-forming agent, antimicrobial agent, emulsifier, and solvent, respectively. Micro-emulsions were obtained using high pressure homogenization (HPH) processing at 138MPa for 3cycles. The composite films made from the micro-emulsions significantly (p<0.05) inactivated Listeria innocua in tryptic soy broth (TSB) and on the surface of ready-to-eat (RTE) meat samples, achieving microbial reductions of over 4logCFU/ml in TSB after 2days at 22°C and on meat samples after 35days at 10°C. AIT was a major contributor to the antimicrobial property of the films and HPH processing further enhanced its antimicrobial efficacy, while the increase of chitosan from 1.5% to 3%, or addition of acetic acid to the formulations didn't result in additional antimicrobial effects. This study demonstrated an effective approach to developing new edible antimicrobial films and coatings used for food applications. Published by Elsevier B.V.

Nanometric Surface Oscillation Spectroscopy of Water-Poor Microemulsions.

PubMed

Corti, Mario; Raudino, Antonio; Cantù, Laura; Theisen, Johannes; Pleines, Maximilian; Zemb, Thomas N

2018-06-18

Selectively exchanging metal complexes between emulsified water-poor microemulsions and concentrated solutions of mixed electrolytes is the core technology for strategic metal recycling. Nanostructuration triggered by solutes present in the organic phase is understood, but little is known about fluctuations of the microemulsion-water interface. We use here a modified version of an opto-electric device initially designed for air bubbles, in order to evidence resonant electrically induced surface waves of an oily droplet suspended in an aqueous phase. Resonant waves of nanometer amplitude of a millimeter-sized microemulsion droplet containing a common ion-specific extractant diluted by dodecane and suspended in a solution of rare earth nitrate are evidenced for the first time with low excitation fields (5 V/cm). From variation of the surface wave spectrum with rare earth concentration, we evidence up-take of rare-earth ions at the interface and at higher concentration the formation of a thin "crust" of liquid crystal forming at unusually low concentration, indicative of a surface induced phase transition. The effect of the liquid crystal structure on the resonance spectrum is backed up by a model, which is used to estimate crust thickness.

Preparation and evaluation of a multimodal minoxidil microemulsion versus minoxidil alone in the treatment of androgenic alopecia of mixed etiology: a pilot study

PubMed Central

Sakr, Farouk M; Gado, Ali MI; Mohammed, Haseebur R; Adam, Abdel Nasser Ismail

2013-01-01

Background: The variable success of topical minoxidil in the treatment of androgenic alopecia has led to the hypothesis that other pathways could mediate this form of hair loss, including infection and/or microinflammation of the hair follicles. In this study, we prepared a multimodal microemulsion comprising minoxidil (a dihydrotestosterone antagonist), diclofenac (a nonsteroidal anti-inflammatory agent), and tea tree oil (an anti-infective agent). We investigated the stability and physicochemical properties of this formulation, and its therapeutic efficacy compared with a formulation containing minoxidil alone in the treatment of androgenic alopecia. Methods: We developed a multimodal oil/water (o/w) microemulsion, a formulation containing minoxidil alone, and another containing vehicle. A three-phase diagram was constructed to obtain the optimal concentrations of the selected oil, surfactant, and cosurfactant. Thirty-two men aged 18–30 years were randomized to apply 1 mL of microemulsion containing the multimodal formulation (formulation A, n = 11), minoxidil alone (formulation B, n = 11) or placebo (formulation C, n = 10) twice daily to the affected area for 32 weeks. Efficacy was evaluated by mean hair count, thickness, and weight on the targeted area of the scalp. Global photographs were taken, changes in the area of scalp coverage were assessed by patients and external investigators, and the benefits and safety of the study medications were evaluated. The physical stability of formula A was examined after a shelf storage period of 24 months. Results: Formulation A achieved a significantly superior response than formulations B and C in terms of mean hair count (P < 0.001), mean hair weight (P < 0.001), and mean hair thickness (P < 0.05). A patient self-assessment questionnaire demonstrated that the multimodal minoxidil formulation significantly (P < 0.001) slowed hair loss, increased hair growth, and improved appearance, and showed no appreciable side effects, such as itching and/or inflammation of the scalp compared with the minoxidil alone and placebo formulations. These improvements were in agreement with the photographic assessments made by the investigators. Formula A was shown to be an o/w formulation with consistent pH, viscosity, specific gravity, and homogeneity, and was physically stable after 24 months of normal storage. Conclusion: A multimodal microemulsion comprising minoxidil, diclofenac, and tea tree oil was significantly superior to minoxidil alone and placebo in terms of stability, safety, and efficacy, and achieved an earlier response in the treatment of androgenic alopecia compared with minoxidil alone in this 32-week pilot study. PMID:23807837

Thromboelastographic and Pharmacokinetic Profiles of Micro- and Macro-emulsions of Propofol in the Swine

PubMed Central

Morey, Timothy E.; Modell, Jerome H.; Garcia, Jorge E.; Bewernitz, Michael; Derendorf, Hartmut; Varshney, Manoj; Gravenstein, Nikolaus; Shah, Dinesh O.; Dennis, Donn M.

2010-01-01

Purpose Compared to traditional macroemulsion propofol formulations currently in clinical use, microemulsion formulations of this common intravenous anesthetic may offer advantages. We characterized the pharmacokinetics and coagulation effects as assessed by thromboelastography of these formulations in swine. Methods Yorkshire swine (20-30 kg, either sex, n=15) were sedated, anesthetized with isoflurane, and instrumented to obtain a tracheostomy, internal jugular access, and carotid artery catheterization. Propofol (2 mg/kg, 30 s) was administered as macroemulsion (10 mg/mL; Diprivan®; n=7) or a custom (2 mg/kg, 30 s) microemulsion (10 mg/mL; n=8). Arterial blood specimens acquired pre- and post-injection (1 and 45 min) were used for thromboelastography. Arterial blood specimens (n=12 samples / subject, 60 min) were serially collected, centrifuged, and analyzed with solid-phase extraction with UPLC to determine propofol plasma concentrations. Non-compartmental pharmacokinetic analysis was applied to plasma concentrations. Results No changes were noted in thromboelastographic R time (P=0.74), K time (P=0.41), α angle (P=0.97), or maximal amplitude (P=0.71) for either propofol preparation. Pharmacokinetic parameters k (P=0.45), t1/2 (P=0.26), Co (P=0.89), AUC0-∞ (P=0.23), Cl (P=0.14), MRT (P=0.47), Vss (P=0.11) of the two formulations were not significantly different. Conclusion The microemulsion and macroemulsion propofol formulations had similar pharmacokinetics and did not modify thromboelastographic parameters in swine. PMID:20578214

FT-IR Spectroscopic Evidence Of Phase Transition For NaA-ROH-Kerosine-H2O Microemulsion System Containing Nd3+ Ions

NASA Astrophysics Data System (ADS)

Liao, Hua; Xu, Zhen-Hua; Shi, Nai; Wu, Jin-Guang; Xu, Guang-Xian

1989-12-01

In the previous investigation, the saponification of naphthenic acid extractant system has been proved to be a process of the formation of a microemulsion of 14/0 type, and its full extraction of rare earths is a process of destruction of the W/O microemulsion[1]. When NdCl3 is partially extracted with NaA (sodium naphthenate) secoctylalcohol-- kerosine-- water microemulsion system (ME), both the NdA3 and the NaA co-exist in the same organic phase. However,the formation mechanism of microemulsion containing neodymium has not been much studied. In this paper, 10 aliquots of fully saponificated extractants were equilibrated with various amounts of NdC13 solutions respectively, then ten organic phases with different extraction efficiencies of neodymium from 094 to 9094 were obtained. After extraction,the volume of neodymium containing organic phase increased by 5 to 4594, because of the transfer of water molecules. The appearance of these organic phase still remained clear and transparent. The average hydrodynamic radius of the drops were found to be 100-300 Angstrom by using light scattering techniques. The results give a direct evidence of the microemulsion formation in the organic phase. Their FT-IR spectra were measured with CaFa liquid cells utilizing a Nicolet 7199B FT-IR spectrometer. The presence of various amounts of water in the organic phases was clearly detected from the relative intensity changes of 1644 cm-I, which is assigned to the bending mode of 1110 molecules. Fig.1 shows the change of water contents to the percent extraction of neodymium. Comparsion with the FT-IR spectra, it is seen that the 1560 cm-1 peak of the full saponificated extractant is attributed to the asym. stretching vibration of COO''' group, it shifted to 1536 for 100% extration of Nd ions, indicating the formation of neodymium naphthenate (NdA ) from ionic sodium naphthenate. The sym. strethching vibration of COO''' located at 1406 cm-1, it shifted to 1408 cm in 45% Nd extration. and disappeared when the percentage extration of Nd3+ was larger than 50%, at the same time, the water content dropped sharply (Fig.1).These results suggested that a series of microemulsion containing Nd ions formed in these organic phases, at the transition region ( more than 50 percentage extration of neodymium), a morphological change of the W/0 dispersion system might occur.

Microemulsion characterization by the use of a noninvasive backscatter fiber optic probe

NASA Technical Reports Server (NTRS)

Ansari, Rafat R.; Dhadwal, Harbans S.; Cheung, H. M.; Meyer, William V.

1993-01-01

This paper demonstrates the utility of a noninvasive backscatter fiber optic probe for dynamic light-scattering characterization of a microemulsion comprising sodium dodecyl sulfate/1-butanol/ brine/heptane. The fiber probe, comprising two optical fibers precisely positioned in a stainless steel body, is a miniaturized and efficient self-beating dynamic light-scattering system. Accuracy of particle size estimation is better than +/- 2 percent.

Nucleation of an oil phase in a nonionic microemulsion-containing chlorinated oil upon systematic temperature quench.

PubMed

Deen, G Roshan; Pedersen, Jan Skov

2010-06-17

A clear and stable nonionic model microemulsion consisting of pentaoxyethylene glycol dodecyl ether (C(12)E(5)), water, and 1-chlorotetradecane (CLTD) was prepared. This system was subjected to a systematic temperature quench (perturbation out of equilibrium) in steps of 1.0 degrees C from 20.4 to 15.3 degrees C in the unstable region of its phase diagram. The change in turbidity (for droplet volume fractions of 0.02 and 0.08) and hydrodynamic radius (R(h)) (for a droplet volume fraction of 0.02) of the system on its way to its new equilibrium was measured at each quench temperature. For small systematic temperature quenches just below the emulsification failure boundary (EFB) the turbidity decreases and remains constant indicating quick changes in the microstructures. Further lowering of temperature brings the system to the unstable region where the turbidity and light scattering increase sharply as function of time because of expulsion of excess oil from the microemulsion droplets. The newly formed oil-rich droplets grow in size as a function of time. These observations indicate the existence of a narrow but observable metastable region en route to the new equilibrium where both microemulsion droplets and larger oil-rich droplets coexist. The region in which microemulsion droplets are metastable is very narrow and is concentration-dependent. The presence of a metastable region is as for other similar systems attributed to the presence of a free energy barrier for the formation of the larger oil-rich droplets associated with curvature free energy of the surfactant film. The turbidity-time curves were converted to the radius-time curves using a model assuming monodisperse spherical droplets. The obtained results are in good agreement with the results for the hydrodynamic radius. The observed average radius from both type of measurements decreases in the metastable region. By performing calculation of the influence of eccentricity and size polydispersity on the observed radius, we have shown that the distribution of the microemulsion droplets becomes more homogeneous in the metastable region.

Dispersion of ceria nanoparticles on γ-alumina surface functionalized using long chain carboxylic acids

NASA Astrophysics Data System (ADS)

Ledwa, Karolina Anna; Kępiński, Leszek

2017-04-01

Dispersion and stability of nanoparticles on a support is determined by the interaction between these phases. In case of hydrophobic nanoparticles (e.g. synthesized by reverse microemulsion method) the interaction with hydrophilic support (e.g. γ-Al2O3) is weak and agglomeration as well as poor resistance to sintering may cause problems. The bonding of the particles to the support may be effectively strengthened by proper modification of the support, e.g. by adsorption of hydrophobic compounds on its surface. In this work decanoic, myristic, stearic and oleic acid were used for the first time to cover γ-Al2O3 surface in order to enhance the dispersion of ceria nanoparticles deposited afterward by impregnation on such support. TGA and FTIR methods revealed that at monolayer coverage (1.1-2.5 molecules per nm2) the acid molecules are firmly bounded to the alumina surface. Morphology, textural properties, phase composition and reducibility of the CeO2/γ-Al2O3 samples were investigated using TEM, SEM, BET, XRD and H2-TPR methods. It has been shown that deposition of CeO2 nanoparticles on γ-Al2O3 surface covered with all studied acids enhances its dispersion, stability and reducibility. The most effective modification of the γ-Al2O3 surface was obtained at loading of 2.3 molecules of decanoic acid per nm2 of the support.

Effect of different polysorbates on development of self-microemulsifying drug delivery systems using medium chain lipids.

PubMed

Shah, Ankita; Thool, Prajwal; Sorathiya, Komal; Prajapati, Hetal; Dalrymple, Damon; Serajuddin, Abu T M

2018-02-01

The primary objective of this study was to develop lipid-based self-microemulsifying drug delivery systems (SMEDDS) without using any organic cosolvents that would spontaneously form microemulsions upon dilution with water. Cosolvents were avoided to prevent possible precipitation of drug upon dilution and other stability issues. Different polysorbates, namely, Tween 20, Tween 40, Tween 60, and Tween 80, were used as surfactants, and Captex 355 EP/NF (glycerol tricaprylate/caprate) or its 1:1 mixture with Capmul MCM NF (glycerol monocaprylocaprate) were used as lipids. Captex 355-Tween-water ternary phase diagrams showed that oil-in-water microemulsions were formed only when the surfactant content was high (80-90%) and the lipid content low (10-20%). Thus, mixtures of Tweens with Captex 355 alone were not suitable to prepare SMEDDS with substantial lipid contents. However, when Captex 355 was replaced with the 1:1 mixture of Captex 355 and Capmul MCM, clear isotropic microemulsion regions in phase diagrams with sizes in the increasing order of Tween 20 < Tween 40 < Tween 60 < Tween 80 were obtained. Tween 80 had the most profound effect among all surfactants as microemulsions were formed with lipid to surfactant ratios as high as 7:3, which may be attributed to the presence of double bond in its side chain that increased the curvature of surfactant layer. Thus, lipid-surfactant mixtures containing 1:1 mixture of medium chain triglyceride (Captex 355) and monoglyceride (Capmul MCM) and as low as 30% Tween 80 were identified as organic cosolvent-free systems for the preparation of SMEDDS. Formulations with a model drug, probucol, dispersed spontaneously and rapidly upon dilution with water to form microemulsions without any drug precipitation.

The effect of microemulsion composition on the morphology of Pd nanoparticles deposited at the surface of TiO2 and photoactivity of Pd-TiO2

NASA Astrophysics Data System (ADS)

Długokęcka, Marta; Łuczak, Justyna; Polkowska, Żaneta; Zaleska-Medynska, Adriana

2017-05-01

A series of microemulsion (ME) system, constituted by different water to surfactant molar ratios (Wo) and oil to surfactant mass ratios (S), have been applied for Pd-TiO2 preparation. The effect of ME properties on the morphology of Pd nanoparticles formed at TiO2 surface and an effect of Pd size and distribution on the surface and photocatalytic properties of Pd-TiO2 were investigated. Microemulsion systems were characterized by means of viscosity, density, dynamic light scattering as well as surface tension measurements to find a correlation between the conditions of Pd nanoparticles formation, their morphology and photocatalyst features. The photocatalysts were characterized by transmission electron microscopy (TEM), X-ray diffraction analysis (XRD), UV-vis diffuse-reflectance spectroscopy (DRS), BET surface area and elemental analysis. The photocatalytic properties of Pd-modified TiO2 particles were studied in a model reaction of phenol photodegradation under Vis irradiation, as well as active species involved in the photocatalytic reaction were determined. Microemulsion composition was found to be a crucial parameter in determining the features of the TiO2-based photocatalysts covered by metallic nanoparticles. The highest photocatalytic activity under Vis radiation was observed for the Pd-TiO2 sample (average diameter 2.4 nm) obtained using 0.1 mol% Pd in the ME system containing 1.5 wt% of water and 82.8 wt% of cyclohexane with average droplet size of 2.83 ± 0.18 nm. In this regard, synthesis of such metal-semiconductor composites through the microemulsion route should always be preceded by investigation of ME properties in order to the eliminate the inhibitory effect of ME internal structure.

Quality by Design approach for an in situ gelling microemulsion of Lorazepam via intranasal route.

PubMed

Shah, Vidhi; Sharma, Mukesh; Pandya, Radhika; Parikh, Rajesh K; Bharatiya, Bhavesh; Shukla, Atindra; Tsai, Hsieh-Chih

2017-06-01

The present study illustrates the application of the concept of Quality by Design for development, optimization and evaluation of Lorazepam loaded microemulsion containing ion responsive In situ gelator gellan gum and carbopol 934. A novel approach involving interactions between surfactant and polymer was employed to achieve controlled drug release and reduced mucociliary clearance. Microemulsion formulated using preliminary solubility study and pseudo ternary phase diagrams showed significantly improved solubilization capacity of Lorazepam with 54.31±6.07nm droplets size. The effect of oil to surfactant/cosurfactant ratio and concentration of gelling agent on the drug release and viscosity of microemulsion gel (MEG) was evaluated using a 3 2 full factorial design. The gel of optimized formulation (MEG 1 ) showed a drug release up to 6h of 97.32±1.35% of total drug loaded. The change in shear-dependent viscosity for different formulations on interaction with Simulated Nasal Fluid depicts the crucial role of surfactant-polymer interactions on the gelation properties along with calcium ions binding on the polymer chains. It is proposed that the surfactant-polymer interactions in the form of a stoichiometric hydrogen bonding between oxyethylene and carboxylic groups of the polymers used, provides exceptional ME stability and adhesion properties. Compared with the marketed formulation, optimized MEG showed improved pharmacodynamic activity. Ex vivo diffusion studies revealed significantly higher release for MEG compared to microemulsion and drug solution. MEG showed higher flux and permeation across goat nasal mucosa. According to the study, it could be concluded that formulation would successfully provide the rapid onset of action, and decrease the mucociliary clearance due to formation of in situ gelling mucoadhesive system. Copyright © 2017 Elsevier B.V. All rights reserved.

Evaluation of local tolerance of the antiretroviral spermicide (WHI-07)-loaded gel-microemulsion in the porcine female reproductive tract.

PubMed

D'Cruz, Osmond J; Uckun, Fatih M

2008-04-01

The local tolerance of the antiretroviral spermicide, WHI-07 (5-bromo-6-methoxy-5,6-dihydro-3'-azidothymidine-5'-(p-bromophenyl)-methoxyalaninyl phosphate)-loaded gel-microemulsion was evaluated in a physiologically relevant and sensitive porcine model. Gilts (Duroc) in nonestrus stages of the reproductive cycle received either a single or a daily intravaginal application of 2.0% WHI-07 via a gel-microemulsion for 6 days. Cervicovaginal lavage (CVL) fluid was obtained for up to 72 h after a single exposure and the cellular profile and levels of inflammatory cytokines (IL-1beta, IL-8, IFN-gamma and TNF-alpha) were quantitated by flow cytometry and chemiluminescence-based multiplex immunoassay, respectively. The reproductive tract (vagina, cervix, uteri and Fallopian tubes) harvested on day 7 was scored histologically for evidence of mucosal irritation using a new scoring criterion for ten histological endpoints that reflect pathological changes in the epithelial/ subepithelial and vascular/perivascular compartments. When compared with irritant reactions caused by the detergent-type spermicide, benzalkonium chloride (BZK), the scatter profile of CVL immune cells and basal levels of proinflammatory cytokines (IL-1beta, IL-8, IFN-gamma and TNF-alpha) in CVL fluid were unaffected by intravaginal exposure to 2% WHI-07. Unlike BZK, endpoint histology of the proximal and distal regions of the reproductive tract from gilts treated with 2.0% WHI-07 via gel-microemulsion for 6 days did not result in mucosal irritation or alteration in the epithelium, subepithelium/lamina propria, vessels/perivascular tissues and underlying/surrounding muscles. Based on surrogate markers for inflammation, leukocyte profile and histologic data for local tolerance, repeated intravaginal administration of WHI-07 via gel-microemulsion as a prophylactic contraceptive is unlikely to cause vaginal irritation.

Quality by design approach for understanding the critical quality attributes of cyclosporine ophthalmic emulsion.

PubMed

Rahman, Ziyaur; Xu, Xiaoming; Katragadda, Usha; Krishnaiah, Yellela S R; Yu, Lawrence; Khan, Mansoor A

2014-03-03

Restasis is an ophthalmic cyclosporine emulsion used for the treatment of dry eye syndrome. There are no generic products for this product, probably because of the limitations on establishing in vivo bioequivalence methods and lack of alternative in vitro bioequivalence testing methods. The present investigation was carried out to understand and identify the appropriate in vitro methods that can discriminate the effect of formulation and process variables on critical quality attributes (CQA) of cyclosporine microemulsion formulations having the same qualitative (Q1) and quantitative (Q2) composition as that of Restasis. Quality by design (QbD) approach was used to understand the effect of formulation and process variables on critical quality attributes (CQA) of cyclosporine microemulsion. The formulation variables chosen were mixing order method, phase volume ratio, and pH adjustment method, while the process variables were temperature of primary and raw emulsion formation, microfluidizer pressure, and number of pressure cycles. The responses selected were particle size, turbidity, zeta potential, viscosity, osmolality, surface tension, contact angle, pH, and drug diffusion. The selected independent variables showed statistically significant (p < 0.05) effect on droplet size, zeta potential, viscosity, turbidity, and osmolality. However, the surface tension, contact angle, pH, and drug diffusion were not significantly affected by independent variables. In summary, in vitro methods can detect formulation and manufacturing changes and would thus be important for quality control or sameness of cyclosporine ophthalmic products.

Synthesis and toxicity test of magnetic nanoparticle via biocompatible microemulsion system as template for application in targeted drug delivery

NASA Astrophysics Data System (ADS)

Kader, Razinah Abdul; Rose, Laili Che; Suhaimi, Hamdan; Manickam, Mariessa Soosai

2017-09-01

This work reports the preparation of magnetic nanoparticles (FeNPs) using biocompatible W/O microemulsion for biomedical applications. W/O microemulsion was formed using decane as oil phase, water, tween 80 as non-ionic surfactant and hexanol as organic solvent. The synthesized FeNPs were characterised by using Fourier Transform Infrared Resonance Spectroscopy (FTIR), Scanning Electron Microscopy (SEM) and X-Ray Diffraction (XRD). The FTIR showed that Fe-O bond exist on 581cm-1 having strong magnetic strength whereas SEM showed the morphology surface of magnetic nanoparticles (FeNPs). Furthermore, analysis of XRD pattern magnetic nanoparticles (FeNPs) reveals a cubic iron oxide phase with good crystallize structure. Furthermore, toxicity test on human liver cells proved that it is 70% safe on human and proved to be a safety nanomedicine.

Analytical applications of emulsions and microemulsions.

PubMed

Burguera, José Luis; Burguera, Marcela

2012-07-15

Dispersion systems like emulsions and microemulsions are able to solubilize both polar and non-polar substances due to the special arrangement of the oil and aqueous phases. The main advantages of using emulsions or microemulsions in analytical chemistry are that they do not require the previous destruction of the sample matrix or the use of organic solvents as diluents, and behave similarly to aqueous solutions, frequently allowing the use of aqueous standard solutions for calibration. However, it appears that there are many contradictory concepts and misunderstandings often related to terms definition when referring to such systems. The main aim of this review is to outline the differences between these two aggregates and to give an overview of the most recent advances on their analytical applications with emphasis on the potentiality of the on-line emulsification processes. Copyright © 2012 Elsevier B.V. All rights reserved.

[Color-tunable nano-material alpha-NaYF4 : Yb, Er, Tm prepared by microemulsion-hydrothermal method].

PubMed

Long, Dan-Dan; Zhang, Qing-Xia; Wang, Yu; Zhang, Fan; Wang, Yan-Fei; Zhou, Xin; Qi, Xiao-Hua; Zhang, Heng; Yan, Jing-Hui; Zou, Ming-Qiang

2013-08-01

NaYF4 : Yb3+, Er3+, Tm3+ nanoparticles were prepared by microemulsion-hydrothermal method. Crystal phase, morphology and structure of the samples were characterized by X-ray diffraction (XRD) and scanning electron microscopy (SEM). The luminescence properties were studied by up-conversional fluorescence spectroscopy. The XRD patterns of as-prepared samples were in agreement with the PDF # 77-2042 of cubic NaYF4. SEM images of the particles showed that the samples were cotton-like spherical in shape and which were assembled by smaller nano-particles. The average size was 120 nm, while the shape was regular and the particle size was homogeneous. Under the excitation of 980 nm, the as-prepared particles could emit blue (438 and 486 nm), green (523 and 539 nm) and red (650 nm) light simultaneously. It can be seen from the color coordinates figure (CIE) that when doping concentration ratio of Tm3+ and E3+ increased from 0 to 2, the whole emitting light color of samples movedto green region. While the ratio was 1 : 1, pseudo white light was obtained. As the ratio changed from 2 to 7, the luminous color was moved to red region.

Simultaneous microemulsion liquid chromatographic analysis of fat-soluble vitamins in pharmaceutical formulations: optimization using genetic algorithm.

PubMed

Momenbeik, Fariborz; Roosta, Mostafa; Nikoukar, Ali Akbar

2010-06-11

An environmentally benign and simple method has been proposed for separation and determination of fat-soluble vitamins using isocratic microemulsion liquid chromatography. Optimization of parameters affecting the separation selectivity and efficiency including surfactant concentration, percent of cosurfactant (1-butanol), and percent of organic oily solvent (diethyl ether), temperature and pH were performed simultaneously using genetic algorithm method. A new software package, MLR-GA, was developed for this purpose. The results indicated that 73.6mM sodium dodecyl sulfate, 13.64% (v/v) 1-butanol, 0.48% (v/v) diethyl ether, column temperature of 32.5 degrees C and 0.02M phosphate buffer of pH 6.99 are the best conditions for separation of fat-soluble vitamins. At the optimized conditions, the calibration plots for the vitamins were obtained and detection limits (1.06-3.69microgmL(-1)), accuracy (recoveries>94.3), precision (RSD<3.96) and linearity (0.01-10mgmL(-1)) were estimated. Finally, the amount of vitamins in multivitamin syrup and a sample of fish oil capsule were determined. The results showed a good agreement with those reported by manufactures. Copyright 2010 Elsevier B.V. All rights reserved.

Enhanced Oxidation and Solvolysis Reactions in Chemically Inert Microheterogeneous Systems.

DTIC Science & Technology

1986-01-15

has been found in a O/W microemulsion containing sodium lauryl sulfate , cyclohexane, n-butanol and water. SHORT TERM PROJECTS New O/W and W/O...microemulsion containing lauryl acid sodium salt, cyclohexane, n-butanol and water towards hydrogen peroxide has been tested. Kinetic measurements...using hydrogen peroxide The system lauryl acid sodium salt, cyclohexane, n-butanol, water has been selected as one of those potentially compatible

Efficacy of mometasone furoate microemulsion in the treatment of erosive-ulcerative oral lichen planus: pilot study.

PubMed

Aguirre, J M; Bagán, J V; Rodriguez, C; Jimenez, Y; Martínez-Conde, R; Díaz de Rojas, F; Ponte, A

2004-08-01

Oral lichen planus (OLP) is a frequent immunological chronic disease, having different clinical forms: asymptomatic and symptomatic. Symptomatic OLP has been palliated with topical corticosteroids with different levels of efficacy and safety. The purpose of this pilot phase II clinical trial was to determine the efficacy of mometasone furoate microemulsion upon the symptoms and signs of erosive-ulcerative OLP. Forty-nine patients with clinical and histologically confirmed erosive-ulcerative OLP were enrolled in this study (36 women and 13 men). Their average age was 56.4 years (from 28 to 78). The treatment consisted of 0.1% mometasone furoate microemulsion mouthwash three times a day over 30 days. Pain, erythema and ulceration were assessed after 15 and 30 days of treatment. The data was processed and statistically analysed by student's t-test for paired samples. Mometasone caused a statistically significant reduction in pain (3.58 vs. 0.65, P = 0.0000). Treatment significantly reduced the surface area of erythema (155.2 vs. 21.9 mm(2), P = 0.0001) and ulceration (30.7 vs. 7.3 mm(2), P = 0.0000). None of these patients suffered severe adverse effects. Mometasone furoate microemulsion is a safe and effective therapy in the treatment of symptomatic erosive-ulcerative OLP.

Combined effects of the drug distribution and mucus diffusion properties of self-microemulsifying drug delivery systems on the oral absorption of fenofibrate.

PubMed

Sunazuka, Yushi; Ueda, Keisuke; Higashi, Kenjirou; Tanaka, Yusuke; Moribe, Kunikazu

2018-05-24

We present the absorption improvement mechanism of fenofibrate (FFB), a Biopharmaceutics Classification System (BCS) class II drug, from self-microemulsifying drug delivery systems (SMEDDS), centered on improving the diffusion of FFB through the unstirred water layer (UWL). Four SMEDDS formulations containing Labrafac™ lipophile WL 1349 (WL1349) or Labrafil ® M 1944CS (M1944) oils and NIKKOL HCO-40 (HCO40) or NIKKOL HCO-60 (HCO60) surfactants were prepared. Every SMEDDS formulation formed microemulsion droplets of approximately 30 nm. In vitro tests showed that the microemulsion droplets containing M1944 had relatively small FFB solubilization capacities, causing larger amounts of FFB to be dissolved in the bulk water phase, compared to the droplets containing WL1349. The diffusivity of the microemulsion droplets through the mucin solution layer was enhanced when using HCO40 compared to HCO60. The oral absorption in rats was the highest when using the SMEDDS formulation containing M1944 and HCO40. High FFB distribution in the bulk water phase and fast diffusion of microemulsion droplets through the mucus layer contributed to the efficient delivery of FFB molecules through the UWL to the epithelial cells, leading to enhanced FFB absorption. Copyright © 2018 Elsevier B.V. All rights reserved.

Jojoba Oil Soft Colloidal Nanocarrier of a Synthetic Retinoid: Preparation, Characterization and Clinical Efficacy in Psoriatic Patients.

PubMed

Nasr, Maha; Abdel-Hamid, Sameh; Moftah, Noha H; Fadel, Maha; Alyoussef, Abdullah A

2017-01-01

Nanotechnology has provided substantial benefits in drug delivery, especially in the treatment of dermatological diseases. Psoriasis is a chronic inflammatory skin disease in which topical delivery of antipsoriatic agents is considered the first line treatment. To investigate whether the encapsulation of the synthetic retinoid tazarotene in a nanocarrier based on jojoba oil would decrease its irritation potential and clinically improve its therapeutic outcome in psoriatic patients. A microemulsion system based on jojoba wax and labrasol/plurol isostearique was prepared and characterized. The selected formula displayed spherical morphology, particle size of 15.49±2.41 nm, polydispersity index of 0.20 ±0.08, negative charge and low viscosity. The microemulsion provided two folds increase in skin deposition of tazarotene, correlating with higher reduction in psoriatic patients PASI scores after treatment (68% reduction in PASI scores versus 8.96% reduction with the marketed gel). No irritation was encountered in patients using microemulsion, with redness and inflammation reported with the marketed gel-treated patients. Jojoba oil microemulsion proved to be advantageous in reducing the irritancy of tazarotene, enhancing its skin deposition and achieving better therapeutic outcome in psoriatic patients. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Kinetic model for reactivity in quaternary water-in-oil microemulsions.

PubMed

García-Río, Luis; Hervella, Pablo

2006-11-06

A study was carried out on the nitrosation of piperazine (PIP) and N-methylbenzylamine (MeBzAm) by N-methyl-N-nitroso-p-toluenesulfonamide (MNTS) in quaternary microemulsions of tetradecyltrimethylammonium bromide (TTABr)/isooctane/alcohol/water, varying the nature and the concentration of the following alcohols: 1-pentanol, 1-hexanol, 1-heptanol, 1-octanol and 1-decanol keeping the [1-alcohol]/[TTABr] = 4 relationship constant. In addition a study was carried out on the influence of the alcohol concentration, working with molar relationships [1-hexanol]/[TTABr]=3, 4 and 5. On the basis of the molar volumes of the alcohol and surfactant and the concentration of alcohol at the interface it was possible to calculate the change in its volume with as varying compositions of the microemulsion. In order to interpret the experimental results a kinetic model was devised which takes into account the distribution of the reactants between the different pseudophases and the change in the volume of the interface. The rate constants at the interface of the microemulsion are lower than in pure water and are independent of the nature of the alcohol used as a cosurfactant and the molar relationship [alcohol]/[TTABr]. This independence indicates that the main role of the cosurfactant is to increase the volume of the interface with the consequent dilution of the reactants.

Efficacy of nano- and microemulsion-based topical gels in delivery of ibuprofen: an in vivo study.

PubMed

Azizi, Mosayeb; Esmaeili, Fariba; Partoazar, Alireza; Ejtemaei Mehr, Shahram; Amani, Amir

2017-03-01

Nanoemulsion has shown many advantages in drug delivery systems. In this study, for the first time, analgesic and anti-inflammatory properties of a nanomelusion of almond oil with and without ibuprofen was compared with corresponding microemulsion and commercial topical gel of the drug using formalin and carrageenan tests, respectively. Almond oil (oil phase) was mixed with Tween 80 and Span 80 (surfactants), and ethanol (co-surfactant) and them distilled water (aqueous phase) was then added to the mixture at once. Prepared nanoemulsions were pre-emulsified into a 100 ml beaker using magnet/stirrer (1000 rpm). Then, using a probe ultrasonicator (Hielscher UP400s, Hielscher, Ringwood, NJ) the nanoemulsions were formed. The optimised nanoemulsion formulation containing 2.5% ibuprofen, showed improved analgesic and anti-inflammatory effects compared with commercial product and corresponding microemulsion product containing 5% ibuprofen (i.e. twice the content of ibuprofen in the nanoemulsion) in vivo. The nanoemulsion preparation showed superior analgesic activities during chronic phase. Also, it decreased the inflammation from the first hour, while the microemulsion and the commercial product started to show their anti-inflammatory effects after 2 and 3 h, respectively. Our finding suggests that the size of the emulsion particles must be considered as an important factor in topical drug delivery systems.

Solubility and transdermal permeation properties of a dehydroepiandrosterone cyclodextrin complex from hydrophilic and lipophilic vehicles.

PubMed

Ceschel, GianCarlo; Bergamante, Valentina; Maffei, Paola; Lombardi Borgia, Simone; Calabrese, Valeria; Biserni, Stefano; Ronchi, Celestino

2005-01-01

The permeation ability of a compound is due principally to its concentration in the vehicle and to its aptitude to cross the stratum corneum of the skin. In this work ex-vivo permeation studies on newly developed formulations containing dehydroepiandrosterone (DHEA) were carried out to investigate vehicles that increase drug permeation through the skin. To enhance the solubility of DHEA, its complex form with alpha-cyclodextrin was used. In addition, the two forms (pure drug and complex form) were introduced in hydrophilic (water), lipophilic (paraffin oil), and microemulsion vehicles to evaluate the synergic effect of cyclodextrins and microemulsion vehicles on solubility and permeation. From the results, DHEA solubility is notably conditioned by the type of the vehicle used: the highest solubilities (both for pure and complex drug forms) were obtained with microemulsion, followed by paraffin oil and water. Moreover, in all the studied vehicles, the c-DHEA was more soluble than DHEA. Permeation profile fluxes showed very interesting differences. That reflect the varying drug forms (pure drug and complex form), vehicles used, and drug concentrations in the vehicles. The major flux was obtained in complex of DHEA with alpha-cyclodextrins in the microemulsion vehicle. Therefore, this type of vehicle and drug form would be very useful in the development of a topical formulation containing DHEA.

Temperature-sensitive microemulsion gel: an effective topical delivery system for simultaneous delivery of vitamins C and E.

PubMed

Rozman, Branka; Zvonar, Alenka; Falson, Francoise; Gasperlin, Mirjana

2009-01-01

Microemulsions (ME)--nanostructured systems composed of water, oil, and surfactants--have frequently been used in attempts to increase cutaneous drug delivery. The primary objective addressed in this work has been the development of temperature-sensitive microemulsion gel (called gel-like ME), as an effective and safe delivery system suitable for simultaneous topical application of a hydrophilic vitamin C and a lipophilic vitamin E. By changing water content of liquid o/w ME (o/w ME), a gel-like ME with temperature-sensitive rheological properties was formed. The temperature-driven changes in its microstructure were confirmed by rotational rheometry, viscosity measurements, and droplet size determination. The release studies have shown that the vitamins' release at skin temperature from gel-like ME were comparable to those from o/w ME and were much faster and more complete than from o/w ME conventionally thickened with polymer (o/w ME carbomer). According to effectiveness in skin delivery of both vitamins, o/w ME was found the most appropriate, followed by gel-like ME and by o/w ME carbomer, indicating that no simple correlation between vitamins release and skin absorption could be found. The cytotoxicity studies revealed good cell viability after exposure to ME and confirmed all tested microemulsions as nonirritant.

A Novel Equation-of-State to Model Microemulsion Phase Behavior for Enhanced Oil Recovery Application

NASA Astrophysics Data System (ADS)

Ghosh, Soumyadeep

Surfactant-polymer (SP) floods have significant potential to recover waterflood residual oil in shallow oil reservoirs. A thorough understanding of surfactant-oil-brine phase behavior is critical to the design of chemical EOR floods. While considerable progress has been made in developing surfactants and polymers that increase the potential of a chemical enhanced oil recovery (EOR) project, very little progress has been made to predict phase behavior as a function of formulation variables such as pressure, temperature, and oil equivalent alkane carbon number (EACN). The empirical Hand's plot is still used today to model the microemulsion phase behavior with little predictive capability as these and other formulation variables change. Such models could lead to incorrect recovery predictions and improper flood designs. Reservoir crudes also contain acidic components (primarily naphthenic acids), which undergo neutralization to form soaps in the presence of alkali. The generated soaps perform synergistically with injected synthetic surfactants to mobilize waterflood residual oil in what is termed alkali-surfactant-polymer (ASP) flooding. The addition of alkali, however, complicates the measurement and prediction of the microemulsion phase behavior that forms with acidic crudes. In this dissertation, we account for pressure changes in the hydrophilic-lipophilic difference (HLD) equation. This new HLD equation is coupled with the net-average curvature (NAC) model to predict phase volumes, solubilization ratios, and microemulsion phase transitions (Winsor II-, III, and II+). This dissertation presents the first modified HLD-NAC model to predict microemulsion phase behavior for live crudes, including optimal solubilization ratio and the salinity width of the three-phase Winsor III region at different temperatures and pressures. This new equation-of-state-like model could significantly aid the design and forecast of chemical floods where key variables change dynamically, and in screening of potential candidate reservoirs for chemical EOR. The modified HLD-NAC model is also extended here for ASP flooding. We use an empirical equation to calculate the acid distribution coefficient from the molecular structure of the soap. Key HLD-NAC parameters like optimum salinities and optimum solubilization ratios are calculated from soap mole fraction weighted equations. The model is tuned to data from phase behavior experiments with real crudes to demonstrate the procedure. We also examine the ability of the new model to predict fish plots and activity charts that show the evolution of the three-phase region. The modified HLD-NAC equations are then made dimensionless to develop important microemulsion phase behavior relationships and for use in tuning the new model to measured data. Key dimensionless groups that govern phase behavior and their effects are identified and analyzed. A new correlation was developed to predict optimum solubilization ratios at different temperatures, pressures and oil EACN with an average relative error of 10.55%. The prediction of optimum salinities with the modified HLD approach resulted in average relative errors of 2.35%. We also present a robust method to precisely determine optimum salinities and optimum solubilization ratios from salinity scan data with average relative errors of 1.17% and 2.44% for the published data examined.

Intranasal mucoadhesive microemulsions of clonazepam: preliminary studies on brain targeting.

PubMed

Vyas, Tushar K; Babbar, A K; Sharma, R K; Singh, Shashi; Misra, Ambikanandan

2006-03-01

The aim of this investigation was to prepare clonazepam microemulsions (CME) for rapid drug delivery to the brain to treat acute status epileptic patients and to characterize and evaluate the performance of CME in vitro and in vivo in rats. The CME were prepared by the titration method and were characterized for globule size and size distribution, zeta potential, and drug content. CME was radiolabeled with (99m)Tc (technetium) and biodistribution of drug in the brain was studied in Swiss albino rats after intranasal and intravenous administrations. Brain scintigraphy imaging in rabbits was also performed to ascertain the uptake of the drug into the brain. Pre and postCME formulation treated human nasal mucosa was subjected to transmission electron microscopy to investigate the mechanism of drug uptake across the nasal mucosa. CME were transparent and stable with mean globule size of 15 +/- 10 nm and zeta potential of -30 mV to -40 mV. (99m)Tc-labeled clonazepam solution ((99m)Tc CS)/ clonazepam microemulsion (CME)/clonazepam mucoadhesive microemulsion (CMME) were found to be stable and suitable for in vivo studies. Brain/blood uptake ratios at 0.50 hour (h) following intranasal CMME, CME, clonazepam solution (CS), and intravenous CME administrations were found to be 0.67, 0.50, 0.48, and 0.13, respectively indicating more effective targeting with intranasal administration and best targeting of the brain with intranasal CMME. Brain/blood ratio at all sampling points up to 8 h following intranasal administration of CMME compared to intravenous was found to be twofold higher indicating larger extent of distribution of the drug in brain. Rabbit brain scintigraphy also showed higher intranasal uptake of the drug into the brain. Transmission electron microscopy revealed significant accretion of CMME within interstitial spaces and paracellular mode of transport due to stretching of the tight junctions present in the nasal mucosa. This investigation demonstrates a more rapid and larger extent of transport of clonazepam into the rat brain with intranasal CMME, which may prove useful in treating acute status epileptics. Copyright 2006 Wiley-Liss, Inc. and the American Pharmacists Association.

Progress in the use of microemulsions for transdermal and dermal drug delivery.

PubMed

Ita, Kevin

2017-06-01

Transdermal drug delivery continues to attract considerable interest in the scientific community. However, due to the hindrance provided by the stratum corneum, it is not possible to deliver most medications in therapeutically significant amounts. One of the ways of increasing the penetration of drugs across the skin is through the use of microemulsions (MEs). This review focuses on the role of MEs in enhancing topical and transdermal drug delivery.

Kinetic Study on the Formation of Bimetallic Core-Shell Nanoparticles via Microemulsions

PubMed Central

Tojo, Concha; Vila-Romeu, Nuria

2014-01-01

Computer calculations were carried out to determine the reaction rates and the mean structure of bimetallic nanoparticles prepared via a microemulsion route. The rates of reaction of each metal were calculated for a particular microemulsion composition (fixed intermicellar exchange rate) and varying reduction rate ratios between both metal and metal salt concentration inside the micelles. Model predictions show that, even in the case of a very small difference in reduction potential of both metals, the formation of an external shell in a bimetallic nanoparticle is possible if a large reactant concentration is used. The modification of metal arrangement with concentration was analyzed from a mechanistic point of view, and proved to be due to the different impact of confinement on each metal: the reaction rate of the faster metal is only controlled by the intermicellar exchange rate but the slower metal is also affected by a cage-like effect. PMID:28788260

Sign Switch of Gaussian Bending Modulus for Microemulsions: A Self-Consistent Field Analysis Exploring Scale Invariant Curvature Energies

NASA Astrophysics Data System (ADS)

Varadharajan, Ramanathan; Leermakers, Frans A. M.

2018-01-01

Bending rigidities of tensionless balanced liquid-liquid interfaces as occurring in microemulsions are predicted using self-consistent field theory for molecularly inhomogeneous systems. Considering geometries with scale invariant curvature energies gives unambiguous bending rigidities for systems with fixed chemical potentials: the minimal surface I m 3 m cubic phase is used to find the Gaussian bending rigidity κ ¯, and a torus with Willmore energy W =2 π2 allows for direct evaluation of the mean bending modulus κ . Consistent with this, the spherical droplet gives access to 2 κ +κ ¯. We observe that κ ¯ tends to be negative for strong segregation and positive for weak segregation, a finding which is instrumental for understanding phase transitions from a lamellar to a spongelike microemulsion. Invariably, κ remains positive and increases with increasing strength of segregation.

Synthesis and applications of crack-free SiO2 monolith containing CdSe/ZnS quantum dots as passive lighting sources.

PubMed

Yi, Dong Kee

2008-09-01

A reverse microemulsion technique has been used to synthesize quantum dot nanocomposites within a SiO2 surface coating. With this approach, the unique optical properties of the CdSe/ZnS quantum dots were preserved. CdSe/ZnS/SiO2 nanoparticles were homogeneously distributed in a tetramethyl orthosilicate ethanol solution and gelation process was initiated within a 10 min, and was left over night at room temperature and dried fully to achieve a solid SiO, monolith. The resulting monolith was transparent and fluorescent under ultraviolet (UV) lamp. Moreover the monolith produced was crack-free. Further studies on the photo stability of the monolith were performed using a high power UV LED device. Remarkably, quantum dots in the SiO, monolith showed better photo stability compared with those dispersed in a polymer matrix.

Biodegradable chitosan nanogels crosslinked with genipin.

PubMed

Arteche Pujana, Maite; Pérez-Álvarez, Leyre; Cesteros Iturbe, Luis Carlos; Katime, Issa

2013-05-15

Chitosan nanoparticles crosslinked with genipin were prepared by reverse microemulsion that allowed to obtain highly monodisperse (3-20 nm by TEM) nanogels. The incorporation of genipin into chitosan was confirmed and quantitatively evaluated by UV-vis and (1)H NMR. Loosely crosslinked chitosan networks showed higher water solubility at neutral pHs than pure chitosan. The hydrodynamic diameter of the genipin-chitosan nanogels ranged from 270 to 390 nm and no remarkable differences were found when the crosslinking degree was varied. The hydrodynamic diameters of the nanoparticles increased slightly at acidic pH and the protonation of ionizable amino groups with the pH was confirmed by the zeta potential measurements. The biocompatible and biodegradable nature, as well as the colloidal and monodisperse particle size of the prepared nanogels, make them attractive candidates for a large variety of biomedical applications. Copyright © 2013 Elsevier Ltd. All rights reserved.

Tuning sputtered gold thickness to enhance absorption and emission in core-shell type erbium doped upconversion nanoparticles

NASA Astrophysics Data System (ADS)

Manurung, R. V.; Wu, C. T.; Chattopadhyay, S.

2018-03-01

Upconversion nanoparticles (UCNPs) converts near-infrared excitation to visible emission with advantages e.g. photostable, non-blinking, and background-free probes for bioimaging and biosensor. However, low quantum yield and low efficiency (∼1%) as drawback need to be enhanced. A plasmonic gold nano-structured surface was designed and fabricated to couple with the 980 nm radiation and produce plasmonic enhancement of the upconversion luminescence. The synthesis of the UCNPs was done by thermal decomposition and SiO2 coating prepared by the reverse microemulsion process. Here, we report a novel tunable plasmon-enhanced fluorescence by modulating the thickness and surface roughness of gold island film on Si. The localized surface plasmon resonance (LSPR) at 980 nm was obtained, matched with the native excitation of UCNPs resulting in maximum enhancement of 10-fold of green emission band at 540 nm for the Er-doped UCNPs.

Detection of trace tetracycline in fish via synchronous fluorescence quenching with carbon quantum dots coated with molecularly imprinted silica

NASA Astrophysics Data System (ADS)

Yang, Ji; Lin, Zheng-Zhong; Nur, A.-Zha; Lu, Yan; Wu, Ming-Hui; Zeng, Jun; Chen, Xiao-Mei; Huang, Zhi-Yong

2018-02-01

A novel fluorescence-based sensor combining synchronous fluorescence spectroscopy (SFS) with molecularly imprinted polymers (MIPs) was fabricated with reverse microemulsion method. Tetracycline (TC), (3-aminopropyl) triethoxysilane (APTES), tetraethyl orthosilicate (TEOS) and carbon quantum dots (CDs) were used as template, functional monomer, cross-linker and signal sources respectively in the probe preparation. A synchronous fluorescence emission (λem) at 355 nm was observed for the prepared MIP-coated CDs (MIP@CDs) particles when the wavelength interval (Δλ) was set as 70 nm, and the synchronous fluorescence intensity could be rapidly and efficiently quenched by TC based on inner filter effect (IFE). The quenching efficiencies of synchronous fluorescence intensity was linearly fitted with tetracycline (TC) concentrations ranging from 0.1 to 50 μmol L- 1 with a detection limit (DL) of 9 nmol L- 1 (3σ, n = 9). The MIP@CDs was used as a probe to detect TC in fish samples with the recoveries ranging from 98.4% to 103.1% and the relative standard deviation less than 6.0%. The results illustrated that the as-prepared MIP@CDs could be applied to the detection of trace TC in fish samples with rapidity, high sensitivity and accuracy.

Activated microporous materials through polymerization of microemulsion precursors

NASA Astrophysics Data System (ADS)

Venkatesan, Arunkumar

Microemulsions have been well studied for their unique characteristics. They are isotropic, thermodynamically stable and microstructured mixtures of oil and water stabilized by one or more surfactant species. They are formed spontaneously and are thermodynamically stable. Microemulsion precursors can be polymerized to make microporous solids with controlled pore structure and sizes. These polymeric solids have been studied extensively in the past. Although the fundamental properties of the microporous solids have been studied in depth, the development of specific applications that will utilize the unique properties of these solids has not been exhaustively researched. The current work establishes the feasibility of making activated microporous solids from microemulsion precursors, by the use of a ligand that chelates metals and also attaches itself to the polymer monolith. It also uses a novel 'in-situ' incorporation by combining the formulation and incorporation steps into one. The research objectives are, to formulate a microemulsion system that can yield useful microporous solids upon polymerization and activation, to characterize these solids using existing techniques available for analysis of similar microporous solids, to identify and understand the effect of the variables in the system and to study the influence of these variables on the performance characteristics of this material. Characterization techniques like Differential Scanning Calorimetry, Thermogravimetric Analysis and Scanning Electron Microscopy were used. A hydroxyethylmethylmethacrylate/methylmethacrylate/aqueous phase containing 10% SDS' system was chosen as the precursor microemulsion and the corresponding microporous solids were made. A metal chelating ligand, Congo Red, was incorporated onto the microporous polymer using NaOH as a binding agent. The ability of the resultant 'activated' microporous solid to remove metal ions from solution, was evaluated. The metal ion chosen was chromium and the influence of variables such as NaOH loading, Congo Red loading, Cross linker content etc. were studied. It was found that the microporous solids were effective in removing chromium from solution. They outperformed similar polymeric solids with ligands (reported in literature) in chromium removal. A removal of about 1500 micro moles of chromium ions per gram of dry polymer from a solution of 5 mMol/L initial concentration of chromium was observed. This is much more than the removal of 340 micro moles/gram of dry polymer reported in literature for comparable non-microporous systems.

Relaxation phenomena in AOT-water-decane critical and dense microemulsions

NASA Astrophysics Data System (ADS)

Letamendia, L.; Pru-Lestret, E.; Panizza, P.; Rouch, J.; Sciortino, F.; Tartaglia, P.; Hashimoto, C.; Ushiki, H.; Risso, D.

2001-11-01

We report on extensive measurements of the low and high frequencies sound velocity and sound absorption in AOT-water-decane microemulsions deduced from ultrasonic and, for the first time as far as the absorption is concerned, from Brillouin scattering experiments. New experimental results on dielectric relaxation are also reported. Our results, which include data taken for critical as well as dense microemulsions, show new interesting relaxation phenomena. The relaxation frequencies deduced from very high frequency acoustical measurements are in good agreement with new high frequency dielectric relaxation measurements. We show that along the critical isochore, sound dispersion, relaxation frequency, and static dielectric permittivity can be accurately fitted to power laws. The absolute values of the new exponents we derived from experimental data are nearly equal, and they are very close to β=0.33 characterising the shape of the coexistence curve. The exponent characterising the infinite frequency permittivity is very close to 0.04 relevant to the diverging shear viscosity. For dense microemulsions, two well defined relaxation domains have been identified and the temperature variations of the sound absorption and the zero frequency dielectric permittivity bear striking similarities. We also show that the relaxation frequency of the slow relaxation process is almost independent of temperature and volume fraction and so cannot be attributed to percolation phenomena, whereas it can more likely be attributed to an intrinsic relaxation process probably connected to membrane fluctuations.

Ophthalmic delivery of Cyclosporine A from Brij-97 microemulsion and surfactant-laden p-HEMA hydrogels.

PubMed

Kapoor, Yash; Chauhan, Anuj

2008-09-01

Cyclosporine A (CyA) is an immunosuppressant drug that is used for treating a variety of ocular diseases and disorders. CyA is commonly delivered via eye drops, which is highly inefficient due to a low bioavailability of less than 5%. The bioavailability of ophthalmic drugs can be substantially improved to about 50% by delivering them via contact lenses. This paper focuses on the development of nanostructured poly (2-hydroxyethyl methacrylate) (p-HEMA) hydrogels containing microemulsions or micelles of Brij 97 (C(18)H(35)(OCH(2)CH(2))(10)) for extended delivery of CyA. Release of CyA from these nanostructured hydrogels was performed in vitro to explore the mechanisms of release and the effects of surfactant concentration, processing conditions and storage on the release kinetics. Results show that the surfactant and microemulsion-laden gels can deliver CyA at therapeutic dosages for a period of about 20 days. Release of the drug is diffusion controlled with effective diffusivities decreasing with increasing surfactant loading. The release kinetics are relatively similar for both surfactant and microemulsion-laden gels with comparable surfactant loading. The results also show that these hydrogels retain their effectiveness even after exposure to all the relevant processing conditions including unreacted monomer extraction, autoclaving and packaging, and so these materials seem to be very promising for ophthalmic delivery of CyA and perhaps other drugs.

One-pot synthesis of BiOCl half-shells using microemulsion droplets as templates with highly photocatalytic performance for the degradation of ciprofloxacin

NASA Astrophysics Data System (ADS)

Mao, Danjun; Yu, Anqing; Ding, Shanshan; Wang, Fei; Yang, Shaogui; Sun, Cheng; He, Huan; Liu, Yazi; Yu, Kai

2016-12-01

Ultrathin BiOCl half-shells have been synthesized via an ionic liquid-in-water (IL/W) microemulsion, applying the liquid-liquid boundary of the emulsion system as a template. Surfactant TX-100 acted as the stabilizer of the IL-microemulsion, which is of critical importance for the formation of BiOCl half-shells. The hollow structures were characterized using X-ray diffraction, scanning and transmission electron microscopy, diffuse reflectance spectroscopy and specific surface area, respectively. Possible formation mechanisms for the BiOCl half-shells were discussed. Moreover, the ultrathin BiOCl half-shells exhibited distinctly enhanced photocatalytic efficiency toward the degradation of colourless ciprofloxacin (CIP, a representative broad-spectrum antibiotic agent) under solar light irradiation as compared to BiOCl nanosheets. The photogenerated reactive species are verified by scavenger experiments, which reveals that rad O2- and h+ were the two major photoactive species toward the photodegradation of CIP over ultrathin BiOCl half-shells under solar-light. The enhanced activities of ultrathin BiOCl half-shells were mainly ascribed to the synergistic effect of the increased light-harvesting, larger BET surface area, faster separation and transfer of electron-hole pairs. It is hoped that the ionic liquid microemulsion-mediated route can be extended to the purposive design and fabrication of other halogen-containing inorganic hollow materials.

Antimicrobial edible coatings and films from micro-emulsions and their food applications.

PubMed

Guo, Mingming; Yadav, Madhav P; Jin, Tony Z

2017-12-18

This study focused on the use of antimicrobial edible coatings and films from micro-emulsions to reduce populations of foodborne pathogens in foods. Corn-Bio-fiber gum (C-BFG) was used as an emulsifier with chitosan. Allyl isothiocyanate (AIT) and lauric arginate ester (LAE) served as antimicrobials. Micro-emulsions were obtained from a solution consisting of 1% chitosan, 0.5% C-BFG, and 1-4% AIT or LAE which was subject to high pressure homogenization (HPH) processing at 138MPa for 3cycles. Coatings and films produced from the micro-emulsions had micro-pores with sizes ranging from 100 to 300nm and micro-channels that hold antimicrobials effectively and facilitate the release of antimicrobials from the center to the surface of the films or coatings, thus enhancing their antimicrobial efficacy. The coatings and films with 1% AIT reduced populations of Listeria innocua by over 5, 2, and 3 log CFU in culture medium (Tryptic soy broth, TSB), ready-to-eat meat, and strawberries, respectively. The coatings and films with 1% LAE reduced populations of Escherichia coli O157:H7 and Salmonella spp. by over 5 and 2 log CFU in TSB and strawberries, respectively. This study provides an innovative approach for the development of effective antimicrobial materials to reduce food borne pathogenic contaminants on ready-to-eat meat, strawberries, or other food. Published by Elsevier B.V.

Development of liposomal and microemulsion formulations for transdermal delivery of clonazepam: effect of randomly methylated β-cyclodextrin.

PubMed

Mura, Paola; Bragagni, Marco; Mennini, Natascia; Cirri, Marzia; Maestrelli, Francesca

2014-11-20

Transdermal administration of clonazepam, a poorly water-soluble benzodiazepine, is an interesting strategy for overcoming the drawbacks of its oral administration. With this aim, two nano-carrier formulations, based on ultra-deformable liposomes and microemulsions, have been developed to favour clonazepam transdermal delivery. Considering the solubilizing power of methyl-βcyclodextrin (Me-βCD) toward clonazepam and its potential positive influence on transdermal drug delivery, the effect of its addition to these formulations was investigated. Artificial lipophilic membranes simulating the skin allowed a rapid evaluation of the drug permeation properties from the systems, compared with those from an aqueous drug suspension, with or without Me-βCD. The best formulations were further characterized by permeation through excised rabbit ear skin. All the formulations increased drug permeability, ranging from 2-fold (liposomes without Me-βCD), up to over 4-fold (microemulsions containing Me-βCD). The different formulations allowed for pointing out different possible permeation enhancing mechanisms of Me-βCD: increase in drug solubility and thermodynamic activity in the vehicle, when added to the drug aqueous suspension; interactions with the vesicle bilayer, in case of liposomal formulations; interactions with the skin membrane lipids, as evidenced in experiments with excised rabbit ear for microemulsions containing Me-βCD, that were then selected for further in vivo studies. Copyright © 2014. Published by Elsevier B.V.

D-optimal experimental approach for designing topical microemulsion of itraconazole: Characterization and evaluation of antifungal efficacy against a standardized Tinea pedis infection model in Wistar rats.

PubMed

Kumar, Neeraj; Shishu

2015-01-25

The study aims to statistically develop a microemulsion system of an antifungal agent, itraconazole for overcoming the shortcomings and adverse effects of currently used therapies. Following preformulation studies like solubility determination, component selection and pseudoternary phase diagram construction, a 3-factor D-optimal mixture design was used for optimizing a microemulsion having desirable formulation characteristics. The factors studied for sixteen experimental trials were percent contents (w/w) of water, oil and surfactant, whereas the responses investigated were globule size, transmittance, drug skin retention and drug skin permeation in 6h. Optimized microemulsion (OPT-ME) was incorporated in Carbopol based hydrogel to improve topical applicability. Physical characterization of the formulations was performed using particle size analysis, transmission electron microscopy, texture analysis and rheology behavior. Ex vivo studies carried out in Wistar rat skin depicted that the optimized formulation enhanced drug skin retention and permeation in 6h in comparison to conventional cream and Capmul 908P oil solution of itraconazole. The in vivo evaluation of optimized formulation was performed using a standardized Tinea pedis model in Wistar rats and the results of the pharmacodynamic study, obtained in terms of physical manifestations, fungal-burden score, histopathological profiles and oxidative stress. Rapid remission of Tinea pedis from rats treated with OPT-ME formulation was observed in comparison to commercially available therapies (ketoconazole cream and oral itraconazole solution), thereby indicating the superiority of microemulsion hydrogel formulation over conventional approaches for treating superficial fungal infections. The formulation was stable for a period of twelve months under refrigeration and ambient temperature conditions. All results, therefore, suggest that the OPT-ME can prove to be a promising and rapid alternative to conventional antifungal therapies against superficial fungal infections. Copyright © 2014 Elsevier B.V. All rights reserved.

New Class of Amphiphiles Designed for Use in Water-in-Supercritical CO2 Microemulsions.

PubMed

Sagisaka, Masanobu; Ogiwara, Shunsuke; Ono, Shinji; James, Craig; Yoshizawa, Atsushi; Mohamed, Azmi; Rogers, Sarah E; Heenan, Richard K; Yan, Ci; Peach, Jocelyn Alice; Eastoe, Julian

2016-11-29

Water-in-supercritical CO 2 microemulsions formed using the hybrid F-H surfactant sodium 1-oxo-1-[4-(perfluorohexyl)phenyl]hexane-2-sulfonate, FC6-HC4, have recently been shown to have the highest water-solubilizing power ever reported. FC6-HC4 demonstrated the ability to outperform not only other surfactants but also other FCm-HCn analogues containing different fluorocarbon and hydrocarbon chain lengths (Sagisaka, M. et al. Langmuir 2015, 31, 7479-7487). With the aim of clarifying the key structural features of this surfactant, this study examined the phase behavior and water/supercritical CO 2 aggregate formation of 1-oxo-1-[4-(perfluorohexyl)phenyl]hexane (Nohead FC6-HC4), which is an FC6-HC4 analogue but now, interestingly, without the sulfonate headgroup. Surprisingly, Nohead FC6-HC4, which would not normally be identified as a classic surfactant, yielded transparent single-phase W/CO 2 microemulsions with polar cores able to solubilize a water-soluble dye, even at pressures and temperatures so low as to approach the critical point of CO 2 (e.g., ∼100 bar at 35 °C). High-pressure small-angle scattering (SANS) measurements revealed the transparent phases to consist of ellipsoidal nanodroplets of water. The morphology of these droplets was shown to be dependent on the pressure, Nohead FC6-HC4 concentration, and water-to-surfactant molar ratio. Despite having almost the same structure as Nohead FC6-HC4, analogues containing both shorter and longer hydrocarbons were unable to form W/CO 2 microemulsion droplets. This shows the importance of the role of the hydrocarbon chain in the stabilization of W/CO 2 microemulsions. A detailed examination of the mechanism of Nohead FC6-HC4 adsorption onto the water surface suggests that the hexanoyl group protrudes into the aqueous core, allowing for association between the carbonyl group and water.

Microemulsion-based synergistic dual-drug codelivery system for enhanced apoptosis of tumor cells.

PubMed

Qu, Ding; Ma, Yihua; Sun, Wenjie; Chen, Yan; Zhou, Jing; Liu, Congyan; Huang, Mengmeng

2015-01-01

A microemulsion-based synergistic dual-drug codelivery system was developed for enhanced cell apoptosis by transporting coix seed oil and etoposide into A549 (human lung carcinoma) cells simultaneously. Results obtained by dynamic light scattering showed that an etoposide (VP16)-loaded coix seed oil microemulsion (EC-ME) delivery system had a small size around 35 nm, a narrow polydispersity index, and a slightly negative surface charge. The encapsulating efficiency and total drug loading rate were 97.01% and 45.48%, respectively, by high-performance liquid chromatography. The release profiles at various pH values showed an obvious pH-responsive difference, with the accumulated amount of VP16 released at pH 4.5 (and pH 5.5) being 2.7-fold higher relative to that at pH 7.4. Morphologic alteration (particle swelling) associated with a mildly acidic pH environment was found on transmission electron microscopy. In the cell study, the EC-ME system showed a significantly greater antiproliferative effect toward A549 cells in comparison with free VP16 and the mixture of VP16 and coix seed oil. The half-maximal inhibitory concentration of the EC-ME system was 3.9-fold and 10.4-fold lower relative to that of free VP16 and a mixture of VP16 and coix seed oil, respectively. Moreover, fluorescein isothiocyanate and VP16 (the green fluorescent probe and entrapped drug, respectively) were efficiently internalized into the cells by means of coix seed oil microemulsion through intuitive observation and quantitative measurement. Importantly, an EC-ME system containing 20 μg/mL of VP16 showed a 3.3-fold and 3.5-fold improvement in induction of cell apoptosis compared with the VP-16-loaded microemulsion and free VP16, respectively. The EC-ME combination strategy holds promise as an efficient drug delivery system for induction of apoptosis and treatment of lung cancer.

Microemulsions and Aggregation Formation in Extraction Processes for Used Nuclear Fuel: Thermodynamic and Structural Studies

DOE Office of Scientific and Technical Information (OSTI.GOV)

Nilsson, Mikael

Advanced nuclear fuel cycles rely on successful chemical separation of various elements in the used fuel. Numerous solvent extraction (SX) processes have been developed for the recovery and purification of metal ions from this used material. However, the predictability of process operations has been challenged by the lack of a fundamental understanding of the chemical interactions in several of these separation systems. For example, gaps in the thermodynamic description of the mechanism and the complexes formed will make predictions very challenging. Recent studies of certain extraction systems under development and a number of more established SX processes have suggested thatmore » aggregate formation in the organic phase results in a transformation of its selectivity and efficiency. Aggregation phenomena have consistently been interfering in SX process development, and have, over the years, become synonymous with an undesirable effect that must be prevented. This multiyear, multicollaborative research effort was carried out to study solvation and self-organization in non-aqueous solutions at conditions promoting aggregation phenomena. Our approach to this challenging topic was to investigate extraction systems comprising more than one extraction reagent where synergy of the metal ion could be observed. These systems were probed for the existence of stable microemulsions in the organic phase, and a number of high-end characterization tools were employed to elucidate the role of the aggregates in metal ion extraction. The ultimate goal was to find connections between synergy of metal ion extraction and reverse micellar formation. Our main accomplishment for this project was the expansion of the understanding of metal ion complexation in the extraction system combining tributyl phosphate (TBP) and dibutyl phosphoric acid (HDBP). We have found that for this system no direct correlation exists for the metal ion extraction and the formation of aggregates, meaning that the metal ion is not solubilized in a reverse micelle core. Rather we have found solid evidence that the metal ions are extracted and coordinated by the organic ligands as suggested by classic SX theories. However, we have challenged the existence of mixed complexes that have been suggested to exist in this particular extraction system. Most importantly we have generated a wealth of information and trained students on important lab techniques and strengthened the collaboration between the DOE national laboratories and US educational institution involved in this work.« less

Electrical percolation in the presence of attractive interactions: An effective medium lattice approach applied to microemulsion systems

NASA Astrophysics Data System (ADS)

Hattori, Y.; Ushiki, H.; Engl, W.; Courbin, L.; Panizza, P.

2005-08-01

Within the framework of an effective medium approach and a mean-field approximation, we present a simple lattice model to treat electrical percolation in the presence of attractive interactions. We show that the percolation line depends on the magnitude of interactions. In 2 dimensions, the percolation line meets the binodal line at the critical point. A good qualitative agreement is observed with experimental results on a ternary AOT-based water-in-oil microemulsion system.

Poly(n-hexyl methacrylate) polymerization in three-component microemulsion stabilized by a cationic surfactant.

PubMed

Katime, Issa; Arellano, Jesús; Schulz, Pablo

2006-04-15

The polymerization of n-hexyl methacrylate (n-HMA) in three-component microemulsion stabilized with dodecyltrimethylammonium bromide (DTAB) is reported as a function of monomer and initiator concentrations and temperature. The obtained latices were bluish, transparent, and translucent. Particle sizes and molar masses were on the order of 20 nm and 3 x 10(6) g/mol, respectively. In all cases, high reaction rates and final conversions of 98% were obtained. Polymerization temperature has a strong effect on reaction rate and conversion.

Simultaneous Determination of Hydrochlorothiazide and Losartan Potassium in Osmotic Pump Tablets by Microemulsion Liquid Chromatography.

PubMed

Li, Liangxing; Lai, Caiyun; Xuan, Xueyi; Gao, Chongkai; Li, Ning

2016-09-01

A rapid and efficient oil-in-water microemulsion liquid chromatographic (MELC) method has been optimized and validated for the determination of hydrochlorothiazide (HCT) and losartan potassium (LOP) in osmotic pump tablets. Samples were injected into a C18 (150 mm × 4.6 mm ID, 5 µm particle size) analytical column, which was maintained at 30°C. The most effective MELC system had a mobile phase consisting of 95% (v/v) of 3.0% (w/w) SDS, 6.0% (w/w) n-butanol, 0.8% (w/w) n-octane, 90.2% (w/w) water and 5% (v/v) acetonitrile (pH 5). The flow rate was 1.0 mL min(-1) and UV detection was performed at 265 nm. Linearity ranged from 2.5 to 12.5 µg mL(-1) for HCT and 10.0-60.0 µg mL(-1) for LOP (r > 0.999 for both drugs). The proposed method was rapid, precise (RSDs < 1.4%) and accurate (98.9% recovery for HCT and 101% recovery for LOP). It is applicable to simultaneous determination of HCT and LOP in osmotic pump tablets. © The Author 2016. Published by Oxford University Press. All rights reserved. For Permissions, please email: journals.permissions@oup.com.

Novel gadopentetic acid-doped silica nanoparticles conjugated with YPSMA-1 targeting prostate cancer for MR imaging: an in vitro study.

PubMed

Jiang, Wei; He, Xiaojing; Fang, Huiying; Zhou, Xue; Ran, Haitao; Guo, Dajing

2018-05-05

The early diagnosis of prostate cancer (PCa) is particularly important for reducing its high mortality rate. With the development of molecular magnetic resonance imaging (MRI), early diagnosis via non-invasive imaging has become possible. In this study, gadopentetic acid (GA)-doped silica (Gd@SiO 2 ) was first synthesized by a reverse microemulsion method, and amino and carboxyl groups were then successively introduced onto the surface of this Gd@SiO 2 . After these steps, a monoclonal antibody (YPSMA-1) to prostate-specific membrane antigen (PSMA) was conjugated with carboxyl-modified Gd@SiO 2 (Gd@SiO 2 -COOH) nanoparticles (NPs) by the carbodiimide method. Gd@SiO 2 -Ab NPs were thus obtained as specific MR contrast agents for PCa-targeted imaging. Transmission electron microscopy showed that the Gd@SiO 2 -Ab NPs exhibited a dispersed spherical morphology with a relatively uniform size distribution. The Gd@SiO 2 -Ab NPs showed high stability and high the longitudinal relaxation rate (r 1 ). Cell-targeting experiments in vitro demonstrated the high potential of the synthesized NPs to target PSMA receptor-positive PCa cells. In vitro cytotoxicity assays showed that the Gd@SiO 2 -Ab NPs exhibited good biological safety. These results suggest that the synthesized Gd@SiO 2 -Ab NPs have great potential as specific MR contrast agents for PSMA receptor-positive PCa cells. Copyright © 2018 Elsevier Inc. All rights reserved.

Phosphatidylcholine embedded micellar systems: enhanced permeability through rat skin.

PubMed

Spernath, Aviram; Aserin, Abraham; Sintov, Amnon C; Garti, Nissim

2008-02-15

Micellar and microemulsion systems are excellent potential vehicles for delivery of drugs because of their high solubilization capacity and improved transmembrane bioavailability. Mixtures of propylene glycol (PG) and nonionic surfactants with sodium diclofenac (DFC) were prepared in the presence of phosphatidylcholine (PC) as transmembrane transport enhancers. Fully dilutable systems with maximum DFC solubilization capacity (SC) at pH 7 are presented. It was demonstrated that the concentrates underwent phase transitions from reverse micelles to swollen reverse micelles and, via the bicontinuous transitional mesophase, into inverted O/W microstructures. The SC decreases as a function of dilution. DFC transdermal penetration using rat skin in vitro correlated with SC, water content, effect of phospholipid content, presence of an oil phase, and ethanol. Skin penetration from the inverted bicontinuous mesophase and the skin penetration from the O/W-like microstructure were higher than that measured from the W/O-like droplets, especially when the micellar system containing the nonionic surfactant, sugar ester L-1695, and hexaglycerol laurate. PC embedded within the micelle interface significantly increased the penetration flux across the skin compared to micellar systems without the embedded PC at their interface. Moreover, the combination of PC with HECO40 improved the permeation rate (P) and shortened the lag-time (T(L)).

Evaluation of a multiarray system for pharmaceutical analysis by microemulsion electrokinetic chromatography.

PubMed

Lynen, Frederic; Saavedra, Luis; Saveedra, Luis; Nickerson, Beverly; Sandra, Pat

2011-05-15

A multiplexed capillary electrophoresis (CE) system equipped with 96 channels was evaluated for high-throughput screening in drug discovery by microemulsion electrokinetic chromatography (MEEKC). Method transfer from a single channel to a multichannel CE system is described. Loss of efficiency and reduced migration times could be elucidated to the poor efficacy in Joule heat dissipation by forced air cooling in the multiarray system compared to liquid cooling in the single channel instrument. On the other hand, only 48 channels could actually be used because of the maximum total current of 3 mA. Precision data remained below 8% and 9% for migration times and peak areas, respectively. Some UV-detector cross-talk interference between neighboring capillary channels was noted. Impurities at 0.5% compared to the main peak (100%) could be detected with the multiplexed system which is 10 times lower compared to the single capillary system. Higher efficiency and improved figures of merit (absolute sensitivity and no cross-talk interferences) were obtained by using an array of only 24 capillaries. Copyright © 2011 Elsevier B.V. All rights reserved.

Determination of food colorants in a wide variety of food matrices by microemulsion electrokinetic capillary chromatography. Considerations on the found concentrations and regulated consumption limits.

PubMed

Bordagaray, Ane; Garcia-Arrona, Rosa; Vidal, Maider; Ostra, Miren

2018-10-01

Color additives are used widely by the food industry to confer a desirable appearance. Some of the most used colorants (Tartrazine (E102), Sunset Yellow (E110), Red Allure (E129) and Blue Brilliant (E133)) were determined in this study using microemulsion electrokinetic capillary chromatography (MEEKC). Regression coefficients were greater than 0.9981; intra- and inter-day precisions, in terms of percentage RSD, were less than 7.01% and 8.55%, respectively; recoveries were between 90 and 100% in most cases. LODs and LOQs ranged from 0.24 to 1.21 mg L -1 and from 0.80 to 4.03 mg L -1 , respectively. Moreover, MEEKC consumed less solvent than HPLC, making the analysis more environmentally friendly. The proposed method is suitable for the determination of colorants in a wide variety of foods. Results showed that consumers should be aware of colorants to avoid consumption exceeding recommended amounts. Copyright © 2018 Elsevier Ltd. All rights reserved.

Structural characterization and antimicrobial properties of silver nanoparticles prepared by inverse microemulsion method.

PubMed

Wani, Irshad A; Khatoon, Sarvari; Ganguly, Aparna; Ahmed, Jahangeer; Ahmad, Tokeer; Manzoor, Nikhat

2013-01-01

Silver nanoparticles have been synthesized in the inverse microemulsions formed using three different surfactants viz., cetyl-trimethyl ammonium bromide (CTAB), Tergitol and Triton X-100. We have done a systematic study of the effect of the surfactants on the particle size and properties of the silver nanoparticles. Microscopic studies show the formation of spheres, cubes and discs shaped silver nanostructures with the size in the range from 8 to 40 nm. Surface plasmon resonance (SPR) peak was observed around 400 nm and 500 nm. In addition to SPR some extra peaks have also been observed due to the formation of silver metal clusters. The surface area increases from 3.45 to 15.06 m(2)/g with decreasing the size of silver nanoparticles (40-8 nm). To investigate the antimicrobial activity of silver nanoparticles, the nanoparticles were tested against the yeast, Candida albicans and the bacterium, E. coli. The results suggest very good antimicrobial activity of the silver nanoparticles against the test microbes. The mode of action of the antimicrobial activity was also proposed. Copyright © 2012 Elsevier B.V. All rights reserved.

Preservation of anthocyanins in solid lipid nanoparticles: Optimization of a microemulsion dilution method using the Placket-Burman and Box-Behnken designs.

PubMed

Ravanfar, Raheleh; Tamaddon, Ali Mohammad; Niakousari, Mehrdad; Moein, Mahmoud Reza

2016-05-15

Anthocyanins are the main polyphenol components from red cabbage (Brassica oleracea L. Var. Capitata f. Rubra) extracts that have inherent antioxidant activities. Anthocyanins are effectively stable in acidic gastric digestion conditions, with nearly 100% phenol content recovery. However, the total phenol content recovery after simulated pancreatic digestion was approximately 25%. To protect anthocyanins against harsh environmental conditions (e.g., pH and temperature), solid lipid nanoparticles were prepared by the dilution of water in oil (w/o) microemulsions containing anthocyanins in aqueous media. The formulations were characterized for particle size and encapsulation efficiency. The formulation parameters (e.g., volume of the internal aqueous phase, homogenization time and the percentages of total lipid, total surfactant or stabilizer) were optimized using the Placket-Burman and Box-Behnken experimental designs. Entrapment efficiency (89.2 ± 0.3%) was calculated when the mean particle size was 455 ± 2 nm. A scanning electron microscopy study revealed the spherical morphology of the particles. Copyright © 2015 Elsevier Ltd. All rights reserved.

Comparison and functionalization study of microemulsion-prepared magnetic iron oxide nanoparticles.

PubMed

Okoli, Chuka; Sanchez-Dominguez, Margarita; Boutonnet, Magali; Järås, Sven; Civera, Concepción; Solans, Conxita; Kuttuva, Gunaratna Rajarao

2012-06-05

Magnetic iron oxide nanoparticles (MION) for protein binding and separation were obtained from water-in-oil (w/o) and oil-in-water (o/w) microemulsions. Characterization of the prepared nanoparticles have been performed by TEM, XRD, SQUID magnetometry, and BET. Microemulsion-prepared magnetic iron oxide nanoparticles (ME-MION) with sizes ranging from 2 to 10 nm were obtained. Study on the magnetic properties at 300 K shows a large increase of the magnetization ~35 emu/g for w/o-ME-MION with superparamagnetic behavior and nanoscale dimensions in comparison with o/w-ME-MION (10 emu/g) due to larger particle size and anisotropic property. Moringa oleifera coagulation protein (MOCP) bound w/o- and o/w-ME-MION showed an enhanced performance in terms of coagulation activity. A significant interaction between the magnetic nanoparticles and the protein can be described by changes in fluorescence emission spectra. Adsorbed protein from MOCP is still retaining its functionality even after binding to the nanoparticles, thus implying the extension of this technique for various applications.

Structured fluids as microreactors for flavor formation by the Maillard reaction.

PubMed

Vauthey, S; Milo, C; Frossard, P; Garti, N; Leser, M E; Watzke, H J

2000-10-01

Thermal reactions of cysteine/furfural and cysteine/ribose mixtures were studied in model systems to gain more insight into the influence of structured fluids such as L(2) microemulsions and cubic phases on the generation of aroma compounds. Formation of 2-furfurylthiol from cysteine/furfural was particularly efficient in L(2) microemulsions and cubic phases compared to aqueous systems. The reaction led to the formation of two new sulfur compounds, which were identified as 2-(2-furyl)thiazolidine and, tentatively, N-(2-mercaptovinyl)-2-(2-furyl)thiazolidine. Similarly, generation of 2-furfurylthiol and 2-methyl-3-furanthiol from cysteine/ribose mixtures was strongly enhanced in structured fluids. The cubic phase was shown to be even more efficient in flavor generation than the L(2) microemulsion. It was denoted "cubic catalyst" or "cubic selective microreactor". The obtained results are interpreted in terms of a surface and curvature control of the reactions defined by the structural properties of the formed surfactant associates.

The Effect of AOT and Octanoic Acid on the Formation of Stable Water-in-diesel Microemulsion

NASA Astrophysics Data System (ADS)

Zhang, Yue; Misran, Misni Bin; Wang, Zhicheng; Zhang, Yu

2017-05-01

Sodium bis(2-ethylhexyl)sulfosuccinate (AOT) and octanoic acid (OA) were used as surfactants to prepare water-in-diesel microemulsion. The effect of mixed surfactants ratio on the phase behavior of water-in-diesel microemulsion was investigated. The R0-T plot phase diagrams for the diesel/AOT and OA/water system with different surfactant ratios were constructed at 30-80 °C. The results indicate that the largest single phase region could be obtained when OA to AOT molar ratio was 1. The temperature had a significant influence on phase transformation behavior. The single phase separated into two immiscible phases with the increase of temperature when R0 value was above 10. Compared with applying AOT alone, mixing AOT with appropriate amount of OA is benefit to form smaller nanosized W/O droplets. The determination of particle size was performed to verify the phase transformation behavior, and the results were consistent with the phase diagrams.

The effect of amphiphilic polymers with a continuous amphiphilicity profile on the membrane properties in a bicontinuous microemulsions studied by neutron scattering

NASA Astrophysics Data System (ADS)

Klemmer, Helge F. M.; Frielinghaus, Henrich; Allgaier, Jürgen; Ohl, Michael; Holderer, Olaf

2017-06-01

Microemulsion systems consisting of oil, water and surfactant have been studied with neutron scattering techniques. The amount of surfactant needed to form a microemulsion can be dramatically reduced by the addition of small amounts of amphiphilic block copolymers (boosting effect). Here, we studied the influence of block copolymers with gradually changing amphiphilicity from hydrophilic to hydrophobic. Small angle neutron scattering (SANS), neutron spin echo spectroscopy (NSE) and phase diagram measurements in combination give access to the elastic properties of the membrane. The underlying NSE experiments for this interpretation rely on smallest changes of the relaxation curves (of ca. 1% steps) for still small changes of the bending rigidity (of ca. 10% steps). This high reliability of the experiments conducted at the SNS-NSE displays the accuracy of the instrument itself and the latest developments of the evaluation software, which were necessary to interpret such tiny changes of the bending rigidity reliably.

The CdCl2 effects on synthetic DNAs encaged in the nanodomains of a cationic water-in-oil microemulsion.

PubMed

Airoldi, Marta; Gennaro, Giuseppe; Giomini, Marcello; Giuliani, Anna Maria; Giustini, Mauro; Palazzo, Gerardo

2011-07-14

The present work is dedicated to the study of the interactions of CdCl(2) with the synthetic polynucleotides polyAT and polyGC confined in the nanoscopic aqueous compartment of the water-in-oil microemulsion CTAB/pentanol/hexane/water, with the goal to mimic in vitro the situation met by the nucleic acids in vivo. In biological structures, in fact, very long strings of nucleic acids are segregated into very small compartments having a radius exceedingly smaller than the length of the encapsulated macromolecule. For comparison, the behaviour of polyGC was also studied in aqueous solutions of matched composition. The conformational and thermal stabilities of both polynucleotides enclosed in the inner compartment of the microemulsion are scarcely affected by the presence of CdCl(2), whereas in solution immediate and large effects were observed also at room temperature. The lack of effects of CdCl(2) on the properties of the biopolymers entrapped in the aqueous core of the microemulsion has been attributed to the peculiar characteristics of the medium (low dielectric constant, in particular) which cause a total repression of the CdCl(2) dissociation that is not complete even in water. In fact, several of the numerous effects of CdCl(2) observed on the conformational stability of polyGC in aqueous solutions have also been ascribed to the limited dissociation of the cadmium salt.

Optimization of minoxidil microemulsions using fractional factorial design approach.

PubMed

Jaipakdee, Napaphak; Limpongsa, Ekapol; Pongjanyakul, Thaned

2016-01-01

The objective of this study was to apply fractional factorial and multi-response optimization designs using desirability function approach for developing topical microemulsions. Minoxidil (MX) was used as a model drug. Limonene was used as an oil phase. Based on solubility, Tween 20 and caprylocaproyl polyoxyl-8 glycerides were selected as surfactants, propylene glycol and ethanol were selected as co-solvent in aqueous phase. Experiments were performed according to a two-level fractional factorial design to evaluate the effects of independent variables: Tween 20 concentration in surfactant system (X1), surfactant concentration (X2), ethanol concentration in co-solvent system (X3), limonene concentration (X4) on MX solubility (Y1), permeation flux (Y2), lag time (Y3), deposition (Y4) of MX microemulsions. It was found that Y1 increased with increasing X3 and decreasing X2, X4; whereas Y2 increased with decreasing X1, X2 and increasing X3. While Y3 was not affected by these variables, Y4 increased with decreasing X1, X2. Three regression equations were obtained and calculated for predicted values of responses Y1, Y2 and Y4. The predicted values matched experimental values reasonably well with high determination coefficient. By using optimal desirability function, optimized microemulsion demonstrating the highest MX solubility, permeation flux and skin deposition was confirmed as low level of X1, X2 and X4 but high level of X3.

Design, Development, and Optimization of Dexibuprofen Microemulsion Based Transdermal Reservoir Patches for Controlled Drug Delivery

PubMed Central

Ali, Fatima Ramzan; Yousuf, Rabia Ismail; Ali, Syed Abid; Imtiaz, Muhammad Suleman; Bashir, Lubna; Naz, Shazia

2017-01-01

The aim of the study was to develop a reservoir-type transdermal patch for a controlled delivery of dexibuprofen and to evaluate its in vivo anti-inflammatory activity in Albino Wistar rats. In order to develop these patches, six formulations of dexibuprofen microemulsion comprising ethyl oleate, Tween 80: PG (2 : 1), and water were prepared by simplex lattice design and characterized. The reservoir compartment was filled with these microemulsions and in vitro release and skin permeation were assessed. The optimized patch was obtained on the basis of the responses: Q24 and flux. The impact of drug loading, surface area, membrane thickness, adhesive, and agitation speed on drug release and permeation was also studied. The skin sensitivity reaction and in vivo anti-inflammatory activity of optimized patch were evaluated. Stability study at three different temperatures for three months was carried out. The result suggests that a membrane based patch with zero-order release rate, Q24 of 79.13 ± 3.08%, and maximum flux of 331.17 µg/cm2h can be obtained exhibiting suitable anti-inflammatory activity with no visible skin sensitivity reaction. The outcomes of stability study recommend storage of patches at 4°C having shelf-life of 6.14 months. The study demonstrates that the reservoir-type transdermal patch of dexibuprofen microemulsion has a potential of delivering drug across skin in controlled manner with required anti-inflammatory activity. PMID:29090219

Hydrolysis of triolein in phospholipid vesicles and microemulsions by a purified rat liver acid lipase.

PubMed

Burrier, R E; Brecher, P

1983-10-10

An acid lipase was purified from rat liver lysosomes. Lipase purification involved affinity chromatography, gel filtration, and stabilization of the purified preparation using ethylene glycol and Triton X-100. A molecular weight of 67,000-69,000 was determined independently using density gradient centrifugation, sodium dodecyl sulfate-polyacrylamide gel electrophoresis, and gel filtration. To study enzyme action, model substrates were prepared by incorporating radiolabeled triolein into either unilamellar vesicles or microemulsions. Substrates were prepared by cosonicating aqueous dispersions of lecithin and triolein. Formation of vesicles or emulsions depended on the relative amount of each lipid and on sonication conditions. Vesicles were prepared at molar ratios between 70:1 and 26:1 (lecithin:triolein) and the microemulsion preparation at a molar ratio of 1:1. The substrate particles were of similar size (220-250 A) as determined by Bio-Gel A-15m chromatography. Hydrolysis of triolein contained in vesicles or emulsions was similar with respect to pH, temperature, and reaction products. Kinetic studies on vesicles with increasing triolein content showed progressively greater Vmax values (0-0.6 mumol/min/mg), and Vmax for the emulsion was 3.1 mumol/min/mg. Addition of human very low or low density lipoprotein produced a dose-dependent inhibition with both substrates. The results show that synthetically prepared microemulsions are stable and effective substrates for the acid lipase and indicate that surface-oriented triolein is hydrolyzed in both preparations.

Preparation, optimization, and evaluation of Zaltoprofen-loaded microemulsion and microemulsion-based gel for transdermal delivery.

PubMed

Mishra, Ratnesh; Prabhavalkar, Kedar S; Bhatt, Lokesh Kumar

2016-12-01

Zaltoprofen, a non-steroidal anti-inflammatory drug, has potent inhibitory action against nociceptive responses. However, gastrointestinal ulcer accompanied with anemia due to the bleeding are most cited side effects associated with it. Due to this, administration of Zaltoprofen is not suitable for individuals with gastric ulcer. Thus, there is unmet need to develop an alternative delivery system that will be easy to administer and can avoid ulcerogenic side effects associated with it. Present study was aimed to prepare and evaluate microemulsion (ME) and microemulsion-based gel formulation of Zaltoprofen for transdermal delivery. Pseudo-ternary phase diagrams were utilized to prepare ME formulations. Effect of surfactant and co-surfactant mass ratio on the ME formation and permeation of ME were evaluated and formulation was optimized. Permeation studies were performed using excised pigskin was studied. Efficacy of optimized formulations was evaluated in rat model of inflammation and pain. Composition of optimized formulation was 1% (w/w) Zaltoprofen, 20% (w/w) Capryol 90, 50% (w/w) Smix (2:1, Cremophor RH 40 and Transcutol P). Optimized formulation showed globule size of 22.11 nm, polydispersity index of 0.251 and zeta potential of -11.4 mV. ME gel was found safe in skin irritation study. Significant analgesic activity and anti-inflammatory activity of ME gel was observed in hot plate test and rat paw edema test, respectively. In conclusion, results of present study suggest that ME could be a promising formulation for transdermal administration of Zaltoprofen.

Controlled Synthesis and Utilization of Metal and Oxide Hybrid Nanoparticles

NASA Astrophysics Data System (ADS)

Crane, Cameron

This dissertation reports the development of synthetic methods concerning rationally-designed, hybrid, and multifunctional nanomaterials. These methods are based on a wet chemical, solution phase approach that utilizes the knowledge of synthetic organic and inorganic chemistry to generate building blocks in solution for the growth of nanocrystals and hybrid nanostructures. This work builds on the prior knowledge of shape-controlled synthesis of noble metal nanocrystals and expands into the challenging realm of the more reactive first row transition metals. Specifically, a microemulsion sol-gel method was developed to synthesize Au-SiO2 dimers as precursors for the synthesis of segmented heterostructures of noble metals that can be used for catalysis. This microemulsion sol-gel method was modified to synthesize an aqueous suspension of oxidation-resistant Cu-SiO2 core-shell nanoparticles that can be used for sensing and catalysis. A thermal decomposition approach was developed, wherein zero-valence metal precursor complexes in the presence of seed nanoparticles produced metal-metal oxide core-shell structures with well-controlled shell thickness. This method was demonstrated on AuCu 3-Fe3O4, AuCu3-NiO, and AuCu3 -MnO core-shell systems. Switching the core from AuCu3 alloy to pure Cu, this method could extend to Cu-Fe3O4 and Cu-MnO systems. Further etching the Cu core in these core-shell structures led to the formation of the hollow metal oxides which provides a versatile route to hollow nanostructures of metal oxides. This work develops the synthetic library of tools for the production of hybrid nanostructures with multiple functionalities.

Interdroplet attractive forces in AOT water-in-oil microemulsions formed in subcritical and supercritical solvents

DOE Office of Scientific and Technical Information (OSTI.GOV)

Tingey, J.M.; Fulton, J.L.; Smith, R.D.

1990-03-08

The van der Waals attractive interactions between aqueous droplets in water-in-oil type microemulsions have been investigated for a range of continuous-phase solvents including the alkanes from methane to isooctane and the noble gases, krypton and xenon. Hamaker constants for water droplets with surfactant shells of the sodium bis(2-ethylhexyl) sulfosuccinate (AOT) in subcritical and supercritical solvents were calculated by using Lifshitz theory and the resulting interaction potential calculations qualitatively account for many features of the phase behavior of these systems.

Enhanced percutaneous permeability of diclofenac using a new U-type dilutable microemulsion.

PubMed

Shevachman, Marina; Garti, Nissim; Shani, Arnon; Sintov, Amnon C

2008-04-01

Enhanced systemic absorption in vivo and percutaneous penetration in vitro was demonstrated after transdermal administration of diclofenac sodium formulated in U-type microemulsion. Diclofenac sodium was solubilized in a typical four-component system consisting of an oil, polyoxyethylene-10EO-oleyl alcohol (Brij 96V) as the surfactant, and 1-hexanol along water dilution line W46 (40 wt % surfactant and 60 wt % oil phase before water titration). Viscosity and small angle X-ray scattering measurements have evidenced bicontinuous structures within water fractions of 0.25 and 0.5 along the dilution line. Self-diffusion NMR studies showed that drug molecules accumulated in the interfacial film and, to some extent, dissolved in the oil. Relative to a commercial macro-emulsion cream (Voltaren Emulgel), microemulsions containing paraffin oil or isopropyl myristate increased the in vivo transdermal penetration rate of diclofenac by two order of magnitude, whereas the rat plasma levels were increased by one order of magnitude. The in vitro data obtained from excised rat skin were comparable to the in vivo results, but suffered from discrepancies from the ideal in vivo-in vitro correlation, which might be explained by optimal in vitro conditions of perfusion and hydration. It has also been found that when jojoba oil is formulated as the oil phase in the microemulsion, the penetration rate of the drug decreases significantly. Based on the three-dimensional structure of jojoba oil, the wax is presumed to prevent the drug from being freely diffused into the skin while migrating from the interfacial film into the continuous oil phase.

Dispersion of microemulsion drops in HEMA hydrogel: a potential ophthalmic drug delivery vehicle.

PubMed

Gulsen, Derya; Chauhan, Anuj

2005-03-23

Approximately 90% of all ophthalmic drug formulations are now applied as eye-drops. While eye-drops are convenient and well accepted by patients, about 95% of the drug contained in the drops is lost due to absorption through the conjunctiva or through the tear drainage. A major fraction of the drug eventually enters the blood stream and may cause side effects. The drug loss and the side effects can be minimized by using disposable soft contact lenses for ophthalmic drug delivery. The essential idea is to encapsulate the ophthalmic drug formulations in nanoparticles, and disperse these drug-laden particles in the lens material. Upon insertion into the eye, the lens will slowly release the drug into the pre lens (the film between the air and the lens) and the post-lens (the film between the cornea and the lens) tear films, and thus provide drug delivery for extended periods of time. This paper focuses on dispersing stabilized microemulsion drops in poly-2-hydroxyethyl methacrylate (p-HEMA) hydrogels. The results of this study show that the p-HEMA gels loaded with a microemulsion that is stabilized with a silica shell are transparent and that these gels release drugs for a period of over 8 days. Contact lenses made of microemulsion-laden gels are expected to deliver drugs at therapeutic levels for a few days. The delivery rates can be tailored by controlling the particle and the drug loading. It may be possible to use this system for both therapeutic drug delivery to eyes and the provision of lubricants to alleviate eye problems prevalent in extended lens wear.

Tissue compatibility and pharmacokinetics of three potential subcutaneous injectables for low-pH drug solutions.

PubMed

Wu, Zimei; Tucker, Ian G; Razzak, Majid; McSporran, Keith; Medlicott, Natalie J

2010-07-01

The aim of the study was to investigate the tissue tolerance and bioavailability of four formulations containing 5% ricobendazole solubilised at low pH, following subcutaneous injection in sheep. Formulations were: a water-in-oil emulsion, a microemulsion, a hydroxypropyl-beta-cyclodextrin (HP-beta-CD, 20%) drug solution, and a low-pH drug solution (reference). In-vitro cytotoxicity of the formulations was investigated in L929 fibroblasts using MTS viability and lactate dehydrogenase leakage assays. Each formulation and respective vehicle was injected into either side of the back of a sheep to investigate the tissue tolerance and pharmacokinetics. In-vitro studies suggested that both the emulsion and the microemulsion are unlikely to give a burst release of the low-pH drug solution in aqueous media. The microemulsion showed the greatest in-vitro cytotoxic effect but no significant difference was observed between the other formulations. In sheep, the three new formulations and vehicles caused little or no injection-site reactions compared with a marked response to the reference formulation. Bioavailabilities of HP-beta-CD formulation, emulsion and microemulsion formulations, relative to the reference formulation, were 194, 155 and 115%, respectively. The three new subcutaneous injectables showed promise for reducing irritation of low-pH solubilised ricobendazole. HP-beta-CD significantly enhanced the drug absorption. Controlling the burst release of the low-pH drug solution may improve tissue tolerance and minimise post-injection precipitation, and hence increase drug bioavailability. The in-vitro cytotoxicity studies did not predict the in-vivo irritation effects.

Influence of a multiple emulsion, liposomes and a microemulsion gel on sebum, skin hydration and TEWL.

PubMed

Mahrhauser, D; Nagelreiter, C; Baierl, A; Skipiol, J; Valenta, C

2015-04-01

In this study, the influence of three cosmetically relevant, priorly characterized vehicles on skin hydration, sebum content and transepidermal water loss was investigated. The chosen vehicles included a liposomal pre-formulation, a multiple W/O/W emulsion and a microemulsion gel. The in vivo effects of these vehicles were demonstrated and compared among them. The stability of the prepared vehicles was determined visually, microscopically, rheologically by pH measurements and particle size. Interactions with skin were assessed by non-invasive biophysical techniques using the Corneometer(®), Aqua Flux(®) and Sebumeter, measuring skin hydration, TEWL and skin sebum content, respectively. All vehicles remained stable over an observation period of 6 weeks. The multiple emulsion increased sebum content and skin hydration. In case of the liposomes, each monitored parameter remained almost constant. In contrast, the microemulsion gel lowered skin hydration and increased TEWL values, but even 1 week after termination of the treatment TEWL decreased almost close to control levels. All produced vehicles were proven to remain physically stable over the duration of this study. The used multiple emulsion showed very skin-friendly properties by increasing sebum and skin hydration. Likewise, the liposomal pre-formulation exhibited no negative effects. On the contrary, the investigated microemulsion gel seemed to have skin dehydrating and TEWL increasing features. However, the multiple emulsion as well as liposomes was identified to be well-tolerated vehicles for skin which might qualify them for the use in cosmetic formulations. © 2014 Society of Cosmetic Scientists and the Société Française de Cosmétologie.

Formulation development and in vitro evaluation of solidified self-microemulsion in the form of tablet containing atorvastatin calcium.

PubMed

Ali, Kazi Asraf; Mukherjee, Biswajit; Bandyopadhyay, Amal Kumar

2013-11-01

The objective of our present study was to prepare solid self-microemulsion in the form of tablet of a poorly water soluble drug, Atorvastatin calcium (ATNC) to increase the solubility, dissolution rate, and minimize the hazards experienced from liquid emulsions. Self-microemulsifying ATNC tablet was formulated mainly by using self-emulsifying base, solidifying agent silicon dioxide and sodium starch glycolate as tablet disintegrant. Self-emulsifying base containing Transcutol P, Gelucire 44/14, and Lutrol F68 with their ratios in the formulation, were best selected by solubility study and ternary phase diagram in different vehicles. Particle size of microemulsion from tablet, physical parameters of the tablet and drug content has been checked. In vitro drug release rate has been carried out in phosphate buffer medium (pH 6.8). Physicochemical characterization of the drug in the optimized formulation has been performed to check drug-excipient incompatibility, if any. Average particle diameter of the emulsions formed from the tablet was found to be below 100 nm in case of formulation F4 and F5, which indicated microemulsions has been formed. In vitro drug release from the formulations F3, F4, and F5 was found to be >90%, indicated the enhancement of solubility of ATNC compared to parent drug. Differential thermal analysis (DTA), Powder X-ray Diffraction (X-RD) and Fourier transform infra red (FTIR) study proved the identity of the drug in the optimized formulation. The tablet form of self-microemulsifying (SME) drug delivery is good for solubility enhancement.

Synthesis of fluorescent dye-doped silica nanoparticles for target-cell-specific delivery and intracellular microRNA imaging.

PubMed

Li, Henan; Mu, Yawen; Qian, Shanshan; Lu, Jusheng; Wan, Yakun; Fu, Guodong; Liu, Songqin

2015-01-21

MicroRNA (miRNA) is found to be up-regulated in many kinds of cancer and therefore is classified as an oncomiR. Herein, we design a multifunctional fluorescent nanoprobe (FSiNP-AS/MB) with the AS1411 aptamer and a molecular beacon (MB) co-immobilized on the surface of the fluorescent dye-doped silica nanoparticles (FSiNPs) for target-cell-specific delivery and intracellular miRNA imaging. The FSiNPs were prepared by a facile reverse microemulsion method from tetraethoxysilane and silane derivatized coumarin that was previously synthesized by click chemistry. The as-prepared FSiNPs possess uniform size distribution, good optical stability and biocompatibility. In addition, there is a remarkable affinity interaction between the AS1411 aptamer and the nucleolin protein on the cancer cell surface. Thus, a target-cell-specific delivery system by the FSiNP-AS/MB is proposed for effectively transferring a MB into the cancer cells to recognize the target miRNA. Using miRNA-21 in MCF-7 cells (a human breast cancer cell line) as a model, the proposed multifunctional nanosystems not only allow target-cell-specific delivery with the binding affinity of AS1411, but also can track simultaneously the transfected cells and detect intracellular miRNA in situ. The proposed multifunctional nanosystems are a promising platform for a highly sensitive luminescent nonviral vector in biomedical and clinical research.

Optimized microemulsions and solid microemulsion systems of simvastatin: characterization and in vivo evaluation.

PubMed

Dixit, Rahul P; Nagarsenker, Mangal S

2010-12-01

The study describes development of solid microemulsions (SME) for improved delivery of simvastatin (SMV). Pseudo-ternary phase diagrams were constructed and MEs were optimized for oil and drug content. SMEs were prepared using colloidal silicon dioxide to adsorb the liquid ME. MEs were characterized for mean globule size in aqueous medium and the SMEs were evaluated for powder characteristics, mean globule size after dilution with water, dissolution profile and for in vivo efficacy in rats. X-ray diffraction studies indicated complete amorphization and/or solubilization of SMV in the SMEs. It was supported by scanning electronic microscopic studies, which did not show evidence of precipitation of the drug on the surface of the carrier. Dissolution studies revealed remarkable increase in dissolution of the drug as compared to plain drug. All the formulations provided significant reduction in the total cholesterol levels in hyperlipidemic rats with reference to rats of control group (p < 0.05). The proposed SMEs have potential to deliver water insoluble drugs like SMV by oral route for better efficacy. © 2010 Wiley-Liss, Inc. and the American Pharmacists Association

To Model Chemical Reactivity in Heterogeneous Emulsions, Think Homogeneous Microemulsions.

PubMed

Bravo-Díaz, Carlos; Romsted, Laurence Stuart; Liu, Changyao; Losada-Barreiro, Sonia; Pastoriza-Gallego, Maria José; Gao, Xiang; Gu, Qing; Krishnan, Gunaseelan; Sánchez-Paz, Verónica; Zhang, Yongliang; Dar, Aijaz Ahmad

2015-08-25

Two important and unsolved problems in the food industry and also fundamental questions in colloid chemistry are how to measure molecular distributions, especially antioxidants (AOs), and how to model chemical reactivity, including AO efficiency in opaque emulsions. The key to understanding reactivity in organized surfactant media is that reaction mechanisms are consistent with a discrete structures-separate continuous regions duality. Aggregate structures in emulsions are determined by highly cooperative but weak organizing forces that allow reactants to diffuse at rates approaching their diffusion-controlled limit. Reactant distributions for slow thermal bimolecular reactions are in dynamic equilibrium, and their distributions are proportional to their relative solubilities in the oil, interfacial, and aqueous regions. Our chemical kinetic method is grounded in thermodynamics and combines a pseudophase model with methods for monitoring the reactions of AOs with a hydrophobic arenediazonium ion probe in opaque emulsions. We introduce (a) the logic and basic assumptions of the pseudophase model used to define the distributions of AOs among the oil, interfacial, and aqueous regions in microemulsions and emulsions and (b) the dye derivatization and linear sweep voltammetry methods for monitoring the rates of reaction in opaque emulsions. Our results show that this approach provides a unique, versatile, and robust method for obtaining quantitative estimates of AO partition coefficients or partition constants and distributions and interfacial rate constants in emulsions. The examples provided illustrate the effects of various emulsion properties on AO distributions such as oil hydrophobicity, emulsifier structure and HLB, temperature, droplet size, surfactant charge, and acidity on reactant distributions. Finally, we show that the chemical kinetic method provides a natural explanation for the cut-off effect, a maximum followed by a sharp reduction in AO efficiency with increasing alkyl chain length of a particular AO. We conclude with perspectives and prospects.

Water soluble folate-chitosan nanogels crosslinked by genipin.

PubMed

Pujana, Maite Arteche; Pérez-Álvarez, Leyre; Iturbe, L Carlos Cesteros; Katime, Issa

2014-01-30

Folate-chitosan conjugates were prepared by a concurrent functionalization and crosslinking reaction with the natural crosslinker genipin. Genipin molecule was employed simultaneously as crosslinker agent and spacer molecule in order to allow the functionalization with folic acid for active tumor targeting. The reaction was carried out in reverse microemulsion which provided colloidal size and monodisperse particle size distribution. The water solubility of the obtained folate-genipin-chitosan nanogels was studied as function of the pH of the medium and all nanoparticles were totally dispersible at physiological pH. The enzymatic degradability of the nanogels in a lysozyme solution was evaluated at acidic and physiological pH. QELS analyses of the swelling behavior of the nanogels with the pH did not show a clear pH-sensitivity. However, the study on the loading and release capacity of 5-fluorouracil revealed an interesting pH-responsive behavior of the nanogels that makes them promising as nanodevices for targeted anticancer drug delivery. Copyright © 2013 Elsevier Ltd. All rights reserved.

Modeling micelle formation and interfacial properties with iSAFT classical density functional theory

NASA Astrophysics Data System (ADS)

Wang, Le; Haghmoradi, Amin; Liu, Jinlu; Xi, Shun; Hirasaki, George J.; Miller, Clarence A.; Chapman, Walter G.

2017-03-01

Surfactants reduce the interfacial tension between phases, making them an important additive in a number of industrial and commercial applications from enhanced oil recovery to personal care products (e.g., shampoo and detergents). To help obtain a better understanding of the dependence of surfactant properties on molecular structure, a classical density functional theory, also known as interfacial statistical associating fluid theory, has been applied to study the effects of surfactant architecture on micelle formation and interfacial properties for model nonionic surfactant/water/oil systems. In this approach, hydrogen bonding is explicitly included. To minimize the free energy, the system minimizes interactions between hydrophobic components and hydrophilic components with water molecules hydrating the surfactant head group. The theory predicts micellar structure, effects of surfactant architecture on critical micelle concentration, aggregation number, and interfacial tension isotherm of surfactant/water systems in qualitative agreement with experimental data. Furthermore, this model is applied to study swollen micelles and reverse swollen micelles that are necessary to understand the formation of a middle-phase microemulsion.

Preparation of highly fluorescent magnetic nanoparticles for analytes-enrichment and subsequent biodetection.

PubMed

Zhang, Bingbo; Chen, Bingdi; Wang, Yilong; Guo, Fangfang; Li, Zhuoquan; Shi, Donglu

2011-01-15

Bifunctional nanoparticles with highly fluorescence and decent magnetic properties have been widely used in biomedical application. In this study, highly fluorescent magnetic nanoparticles (FMNPs) with uniform size of ca. 40 nm are prepared by encapsulation of both magnetic nanoparticles (MNPs) and shell/core quantum dots (QDs) with well-designed shell structure/compositions into silica matrix via a one-pot reverse microemulsion approach. The spectral analysis shows that the FMNPs hold high fluorescent quantum yield (QY). The QYs and saturation magnetization of the FMNPs can be regulated by varying the ratio of the encapsulated QDs to MNPs. Moreover, the surface of the FMNPs can be modified to offer chemical groups for antibody conjugation for following use in target-enrichment and subsequent fluorescent detection. The in vitro immunofluorescence assay and flow cytometric analysis indicate that the bifunctional FMNPs-antibody bioconjugates are capable of target-enrichment, magnetic separation and can also be used as alternative fluorescent probes on flow cytometry for biodetection. Copyright © 2010 Elsevier Inc. All rights reserved.

Influence of Scaffold Size on Bactericidal Activity of Nitric Oxide Releasing Silica Nanoparticles

PubMed Central

Carpenter, Alexis W.; Slomberg, Danielle L.; Rao, Kavitha S.; Schoenfisch, Mark H.

2011-01-01

A reverse microemulsion synthesis was used to prepare amine functionalized silica nanoparticles of three distinct sizes (i.e., 50, 100, and 200 nm) with identical amine concentrations. The resulting hybrid nanoparticles, consisting of N-(6 aminohexyl) aminopropyltrimethoxysilane and tetraethoxysilane, were highly monodisperse in size. N-diazeniumdiolate nitric oxide (NO) donors were subsequently formed on secondary amines while controlling reaction conditions to keep the total amount of nitric oxide (NO) released constant for each particle size. The bactericidal efficacy of the NO releasing nanoparticles against Pseudomonas aeruginosa increased with decreasing particle size. Additionally, smaller diameter nanoparticles were found to associate with the bacteria at a faster rate and to a greater extent than larger particles. Neither control (non-NO-releasing) nor NO releasing particles exhibited toxicity towards L929 mouse fibroblasts at concentrations above their respective minimum bactericidal concentrations. This study represents the first investigation of the bactericidal efficacy of NO-releasing silica nanoparticles as a function of particle size. PMID:21842899

Development and critical evaluation of fluorescent chloride nanosensors.

PubMed

Graefe, Anja; Stanca, Sarmiza E; Nietzsche, Sandor; Kubicova, Lenka; Beckert, Rainer; Biskup, Christoph; Mohr, Gerhard J

2008-09-01

In this study, we describe the preparation and evaluation of new fluorescent sensor nanoparticles for the ratiometric measurement of chloride concentrations. Both a chloride-sensitive dye (lucigenin) and a reference dye (sulforhodamine derivative) were incorporated into polyacrylamide nanoparticles via inverse microemulsion polymerization and investigated for their response to chloride ions in buffered suspension as well as in living cells. The fluorescence intensity of lucigenin reversibly decreased in the presence of chloride ions due to a collisional quenching process, which can be described with the Stern-Volmer equation. The determined Stern-Volmer constant K SV for the quenching of lucigenin incorporated into particles was found to be 53 M (-1) and is considerably smaller than the Stern-Volmer constant for quenching of free lucigenin ( K SV = 250 M (-1)) under the same conditions. To test the nanosensors in living cells, we incorporated them into Chinese hamster ovary cells and mouse fibroblasts by using the conventional lipofectamin technique and monitored the response to changing chloride concentrations in the cell.

Synthesis of strontium hexaferrite nanoparticles prepared using co-precipitation method and microemulsion processing

NASA Astrophysics Data System (ADS)

Drmota, A.; Žnidaršič, A.; Košak, A.

2010-01-01

Strontium hexaferrite (SrFe12O19) nanoparticles have been prepared with co-precipitation in aqueous solutions and precipitation in microemulsion system water/SDS/n-butanol/cyclohexane, using iron and strontium nitrates in different molar rations as a starting materials. The mixed Sr2+, Fe3+ hydroxide precursors obtained during the reaction between corresponding metal nitrates and tetramethylammonium hydroxide (TMAH), which served as a precipitating reagent, were calcined in a wide temperature range, from 350 °C to 1000 °C in a static air atmosphere. The influence of the Sr2+/Fe3+ molar ratio and the calcination temperature to the chemistry of the product formation, its crystallite size, morphology and magnetic properties were investigated. It was found that the formation of single phase SrFe12O19 with relatively high specific magnetization (54 Am2/kg) was achieved at the Sr2+/Fe3+ molar ration of 6.4 and calcination at 800 °C for 3h with heating/cooling rate 5 °C/min. The prepared powders were characterized using X-ray diffractometry (XRD) and specific surface area measurements (BET). The specific magnetization (DSM-10, magneto-susceptometer) of the prepared samples was measured.

Determination of quantitative retention-activity relationships between pharmacokinetic parameters and biological effectiveness fingerprints of Salvia miltiorrhiza constituents using biopartitioning and microemulsion high-performance liquid chromatography.

PubMed

Gao, Haoshi; Huang, Hongzhang; Zheng, Aini; Yu, Nuojun; Li, Ning

2017-11-01

In this study, we analyzed danshen (Salvia miltiorrhiza) constituents using biopartitioning and microemulsion high-performance liquid chromatography (MELC). The quantitative retention-activity relationships (QRARs) of the constituents were established to model their pharmacokinetic (PK) parameters and chromatographic retention data, and generate their biological effectiveness fingerprints. A high-performance liquid chromatography (HPLC) method was established to determine the abundance of the extracted danshen constituents, such as sodium danshensu, rosmarinic acid, salvianolic acid B, protocatechuic aldehyde, cryptotanshinone, and tanshinone IIA. And another HPLC protocol was established to determine the abundance of those constituents in rat plasma samples. An experimental model was built in Sprague Dawley (SD) rats, and calculated the corresponding PK parameterst with 3P97 software package. Thirty-five model drugs were selected to test the PK parameter prediction capacities of the various MELC systems and to optimize the chromatographic protocols. QRARs and generated PK fingerprints were established. The test included water/oil-soluble danshen constituents and the prediction capacity of the regression model was validated. The results showed that the model had good predictability. Copyright © 2017. Published by Elsevier B.V.

A microemulsion of puerarin-phospholipid complex for improving bioavailability: preparation, in vitro and in vivo evaluations.

PubMed

Wu, Jun-Yong; Li, Yong-Jiang; Han, Meng; Hu, Xiong-Bin; Yang, Le; Wang, Jie-Min; Xiang, Da-Xiong

2018-08-01

Puerarin is a phytochemical with various pharmacological effects, but poor water solubility and low oral bioavailability limited usage of puerarin. The purpose of this study was to develop a new microemulsion (ME) based on phospholipid complex technique to improve the oral bioavailability of puerarin. Puerarin phospholipid complex (PPC) was prepared by a solvent evaporation method and was characterized by X-ray diffraction and infrared spectroscopy. Pseudo-ternary phase diagrams were constructed to investigate the effects of different oil on the emulsifying performance of the blank ME. Intestinal mucosal injury test was conducted to evaluate safety of PPC-ME, and no sign of damage on duodenum, jejunum and ileum of rats was observed using hematoxylin-eosin staining. In pharmacokinetic study of PPC-ME, a significantly greater C max (1.33 µg/mL) was observed when compared to puerarin (C max 0.55 µg/mL) or PPC (C max 0.70 µg/mL); the relative oral bioavailability of PPC-ME was 3.16-fold higher than puerarin. In conclusion, the ME combined with the phospholipid complex technique was a promising strategy to enhance the oral bioavailability of puerarin.

Search for extraterrestrial life using chiral molecules: mandelate racemase as a test case.

PubMed

Thaler, Tracey L; Gibbs, Phillip R; Trebino, Rick P; Bommarius, Andreas S

2006-12-01

We have investigated an enzymatic racemization reaction as a marker for extraterrestrial life, which resulted in a change in optical rotation of a mandelic acid over time, as measured by polarimetry. Mandelate racemase was active in aqueous buffer in a temperature range between 0 degrees C and 70 degrees C and also in concentrated ammonium salt solutions and water-in-oil microemulsions in a temperature range between -30 degrees C and 60-70 degrees C; however, the enzyme was not active in several organic cryosolvents. Thus, we have demonstrated that concentrated ammonium salt solutions and water-in-oil microemulsions, both of which are able to form on extraterrestrial planets and moons in the presence of liquid water, are suitable media for enzyme reactions at subzero temperatures. Kinetic data for the mandelate racemase reaction obtained by polarimetry, while reproducible and internally consistent, differed significantly from several sets of data obtained previously by other methods such as chromatography and hydrogen-deuterium exchange. However, we conclude that reactions yielding a polarimetric signal, such as the racemizations employed in this work, are suitable mechanisms by which to utilize a change in chirality over time as a tool to detect signs of life.

Formulation and evaluation of lecithin organogel for topical delivery of fluconazole.

PubMed

Jadhav, Kisan R; Kadam, Vilasrao J; Pisal, Sambhaji S

2009-04-01

The purpose of the present study was to develop and investigate the suitability of microemulsion based lecithin organogel formulations for topical delivery of fluconazole in order to bypass its gastrointestinal adverse effects. The ternary phase diagrams were developed and various organogel formulations were prepared using pharmaceutically acceptable surfactant (lecithin) and ethyl oleate (EO). Solubility of fluconazole in EO and EO-lecithin reverse micellar system was determined. The transdermal permeability of fluconazole from different concentrations of lecithin organogels containing EO as oil phase was analyzed using Keshary-Chien diffusion cell through excised rat skin. Solubility of fluconazole in EO-lecithin reverse micellar system was almost 3 folds higher than that in EO. Gelation and immobilization of oil require critical solubility-insolubility balance of gelator. The occurrence of gel phase was lecithin concentration dependent and was observed in 10-60% w/v of system. Organogel containing 300 mM of lecithin showed the higher drug release and better relative consistency. Hence, it was selected for antifungal activity. The increase in antifungal activity of fluconazole in lecithin organogel may be because of the surfactant action of the lecithin and EO that may help in the diffusion of drug. The histopathological data showed that EO-lecithin organogels were safe enough for the topical purpose. Hence, the present lecithin based organogel appears beneficial for topical delivery of fluconazole in terms of easy preparation, safety, stability and low cost.

Zinc Oxide—From Synthesis to Application: A Review

PubMed Central

Kołodziejczak-Radzimska, Agnieszka; Jesionowski, Teofil

2014-01-01

Zinc oxide can be called a multifunctional material thanks to its unique physical and chemical properties. The first part of this paper presents the most important methods of preparation of ZnO divided into metallurgical and chemical methods. The mechanochemical process, controlled precipitation, sol-gel method, solvothermal and hydrothermal method, method using emulsion and microemulsion enviroment and other methods of obtaining zinc oxide were classified as chemical methods. In the next part of this review, the modification methods of ZnO were characterized. The modification with organic (carboxylic acid, silanes) and inroganic (metal oxides) compounds, and polymer matrices were mainly described. Finally, we present possible applications in various branches of industry: rubber, pharmaceutical, cosmetics, textile, electronic and electrotechnology, photocatalysis were introduced. This review provides useful information for specialist dealings with zinc oxide. PMID:28788596

Locus-specific microemulsion catalysts for sulfur mustard (HD) chemical warfare agent decontamination.

PubMed

Fallis, Ian A; Griffiths, Peter C; Cosgrove, Terence; Dreiss, Cecile A; Govan, Norman; Heenan, Richard K; Holden, Ian; Jenkins, Robert L; Mitchell, Stephen J; Notman, Stuart; Platts, Jamie A; Riches, James; Tatchell, Thomas

2009-07-22

The rates of catalytic oxidative decontamination of the chemical warfare agent (CWA) sulfur mustard (HD, bis(2-chlororethyl) sulfide) and a range (chloroethyl) sulfide simulants of variable lipophilicity have been examined using a hydrogen peroxide-based microemulsion system. SANS (small-angle neutron scattering), SAXS (small-angle X-ray scattering), PGSE-NMR (pulsed-gradient spin-echo NMR), fluorescence quenching, and electrospray mass spectroscopy (ESI-MS) were implemented to examine the distribution of HD, its simulants, and their oxidation/hydrolysis products in a model oil-in-water microemulsion. These measurements not only present a means of interpreting decontamination rates but also a rationale for the design of oxidation catalysts for these toxic materials. Here we show that by localizing manganese-Schiff base catalysts at the oil droplet-water interface or within the droplet core, a range of (chloroethyl) sulfides, including HD, spanning some 7 orders of octanol-water partition coefficient (K(ow)), may be oxidized with equal efficacy using dilute (5 wt. % of aqueous phase) hydrogen peroxide as a noncorrosive, environmentally benign oxidant (e.g., t(1/2) (HD) approximately 18 s, (2-chloroethyl phenyl sulfide, C(6)H(5)SCH(2)CH(2)Cl) approximately 15 s, (thiodiglycol, S(CH(2)CH(2)OH)(2)) approximately 19 s {20 degrees C}). Our observations demonstrate that by programming catalyst lipophilicity to colocalize catalyst and substrate, the inherent compartmentalization of the microemulsion can be exploited to achieve enhanced rates of reaction or to exert control over product selectivity. A combination of SANS, ESI-MS and fluorescence quenching measurements indicate that the enhanced catalytic activity is due to the locus of the catalyst and not a result of partial hydrolysis of the substrate.

Photolysis study of octyl p-methoxycinnamate loaded microemulsion by molecular fluorescence and chemometric approach

NASA Astrophysics Data System (ADS)

Nascimento, Danielle Silva; Insausti, Matías; Band, Beatriz Susana Fernández; Grünhut, Marcos

2018-02-01

Octyl p-methoxycinnamate (OMC) is one of the most widely used sunscreen agents. However, the efficiency of OMC as UV filter over time is affected due to the formation of the cis-isomer which presents a markedly lower extinction coefficient (εcis = 12,600 L mol- 1 cm- 1 at 291 nm) than the original trans-isomer (εtrans = 24,000 L mol- 1 cm- 1 at 310 nm). In this work, a novel carrier for OMC based on an oil-in-water microemulsion is proposed in order to improve the photostability of this sunscreen. The formulation was composed of 29.2% (w/w) of a 3:1 mixture of ethanol (co-surfactant) and decaethylene glycol mono-dodecyl ether (surfactant), 1.5% (w/w) of oleic acid (oil phase) and 69.2% (w/w) of water. This microemulsion was prepared in a simple way, under moderate stirring at 25 °C and using acceptable, biocompatible and accessible materials for topical use. OMC was incorporated in the vehicle at a final concentration of 5.0% (w/w), taking into account the maximum permitted levels established by international norms. Then, a photolysis study of the loaded formulation was performed using a continuous flow system. The direct photolysis was monitored over time by molecular fluorescence. The recorded spectra data between 370 y 490 nm were analyzed by multivariate curve resolution-alternating least squares algorithm. The kinetic rate constants corresponding to the photolysis of the trans-OMC were calculated from the concentration profiles, resulting in 0.0049 s- 1 for the trans-OMC loaded microemulsion and 0.0131 s- 1 for the trans-OMC in aqueous media. These results demonstrate a higher photostability of the trans-OMC when loaded in the proposed vehicle with respect to the free trans-OMC in aqueous media.

Laundry Detergency of Solid Non-Particulate Soil Using Microemulsion-Based Formulation.

PubMed

Chanwattanakit, Jarussri; Chavadej, Sumaeth

2018-02-01

Laundry detergency of solid non-particulate soil on polyester and cotton was investigated using a microemulsion-based formulation, consisting of an anionic extended surfactant (C 12,13 -4PO-SO 4 Na) and sodium mono-and di-methyl naphthalene sulfonate (SMDNS) as the hydrophilic linker, to provide a Winsor Type III microemulsion with an ultralow interfacial tension (IFT). In this work, methyl palmitate (palmitic acid methyl ester) having a melting point around 30°C, was used as a model solid non-particulate (waxy) soil. A total surfactant concentration of 0.35 wt% of the selected formulation (4:0.65 weight ratio of C 12,13 -4PO-SO 4 Na:SMDNS) with 5.3 wt% NaCl was able to form a middle phase microemulsion at a high temperature (40°C),which provided the highest oil removal level with the lowest oil redeposition and the lowest IFT, and was much higher than that with a commercial detergent or de-ionized water. Most of the detached oil, whether in liquid or solid state, was in an unsolubilized form. Hence, the dispersion stability of the detached oil droplets or solidified oil particles that resulted from the surfactant adsorption played an important role in the oil redeposition. For an oily detergency, the lower the system IFT, the higher the oil removal whereas for a waxy (non-particulate) soil detergency, the lower the contact angle, the higher the solidified oil removal. For a liquefied oil, the detergency mechanism was roll up and emulsification with dispersion stability, while that for the waxy soil (solid oil) was the detachment by wettability with dispersion stability.

Preparation and evaluation of microemulsion-based transdermal delivery of Cistanche tubulosa phenylethanoid glycosides

PubMed Central

Yang, Jianhua; Xu, Huanhuan; Wu, Shanshan; Ju, Bowei; Zhu, Dandan; Yan, Yao; Wang, Mei; Hu, Junping

2017-01-01

The primary aim of the present study was to develop a novel microemulsion (ME) formulation to deliver phenylethanoid glycoside (PG) for use in skin lighteners and sunscreens. The oil phase was selected on the basis of drug solubility, while the surfactant and cosurfactant were screened and selected on the basis of their solubilizing capacity and the efficiency with which they formed MEs. Pseudoternary phase diagrams were constructed to evaluate ME regions and five formulations of oil-in-water MEs were selected as vehicles. In vitro skin permeation experiments were performed to optimize the ME formulation and to evaluate its permeability in comparison to that of saline solution. The physicochemical properties of the optimized ME and the permeating ability of PG delivered by this ME were also investigated. The optimized ME formulation was composed of isopropyl myristate (7%, w/w), Cremorphor EL (21%, w/w), propylene glycol (7%, w/w) and water (65%, w/w). The cumulative amount of PG that permeated through excised mouse skin when carried by ME was ~1.68 times that when PG was carried by saline solution only. The cumulative amount of PG in the microemulsion (4149.650±37.3 µg·cm−2) was significantly greater than that of PG in the saline solution (2288.63±20.9 µg·cm−2). Furthermore, the permeability coefficient indicated that optimized microemulsion was a more efficient carrier for transdermal delivery of PG than the control solution (8.87±0.49 cm/hx10−3 vs. 5.41±0.12 cm/hx10−3). Taken together, the permeating ability of ME-carried PG was significantly increased compared with saline solution. PMID:28138704

Interaction of human low density lipoprotein and apolipoprotein B with ternary lipid microemulsion. Physical and functional properties.

PubMed

Chun, P W; Brumbaugh, E E; Shiremann, R B

1986-12-31

Based on data from sedimentation velocity experiments, electrophoresis, electron microscopy, cellular uptake studies, scanning molecular sieve chromatography using a quasi-three-dimensional data display and flow performance liquid chromatography (FPLC), models for the interaction of human serum low density lipoprotein (LDL) and of apolipoprotein B (apo B) with a ternary lipid microemulsion (ME) are proposed. The initial step in the interaction of LDL (Stokes radius 110 A) with the ternary microemulsion (Stokes radius 270 A) appears to be attachment of the LDL to emulsion particles. This attachment is followed by a very slow fusion into particles having a radius of approx. 280 A. Sonication of this mixture yields large aggregates. Electron micrographs of deoxycholate-solubilized apo B indicate an arrangement of apo B resembling strings of beads. During incubation, these particles also attach to the ternary microemulsion particles and, upon sonication, spherical particles result which resemble native LDL particles in size. Scanning chromatography corroborates the electron microscopy results. By appropriate choice of display angles in a quasi-three-dimensional display of the scanning data (corrected for gel apparent absorbance) taken at equal time intervals during passage of a sample through the column, changes in molecular radius of less than 10 A can be detected visually. Such a display gives a quantitative estimate of 101 +/- 2 A for these particles (compared to 110 A for native LDL). The LDL-ME particles and apo B-ME particles compete efficiently with native LDL for cellular binding and uptake. Cellular association studies indicate that both LDL- and apo B-ME particles are effective vehicles for lipid delivery into cells.

DOE Office of Scientific and Technical Information (OSTI.GOV)

Piepel, Gregory F.; Pasquini, Benedetta; Cooley, Scott K.

In recent years, multivariate optimization has played an increasing role in analytical method development. ICH guidelines recommend using statistical design of experiments to identify the design space, in which multivariate combinations of composition variables and process variables have been demonstrated to provide quality results. Considering a microemulsion electrokinetic chromatography method (MEEKC), the performance of the electrophoretic run depends on the proportions of mixture components (MCs) of the microemulsion and on the values of process variables (PVs). In the present work, for the first time in the literature, a mixture-process variable (MPV) approach was applied to optimize a MEEKC method formore » the analysis of coenzyme Q10 (Q10), ascorbic acid (AA), and folic acid (FA) contained in nutraceuticals. The MCs (buffer, surfactant-cosurfactant, oil) and the PVs (voltage, buffer concentration, buffer pH) were simultaneously changed according to a MPV experimental design. A 62-run MPV design was generated using the I-optimality criterion, assuming a 46-term MPV model allowing for special-cubic blending of the MCs, quadratic effects of the PVs, and some MC-PV interactions. The obtained data were used to develop MPV models that express the performance of an electrophoretic run (measured as peak efficiencies of Q10, AA, and FA) in terms of the MCs and PVs. Contour and perturbation plots were drawn for each of the responses. Finally, the MPV models and criteria for the peak efficiencies were used to develop the design space and an optimal subregion (i.e., the settings of the mixture MCs and PVs that satisfy the respective criteria), as well as a unique optimal combination of MCs and PVs.« less

Simultaneous determination of ingredients in a cold medicine by cyclodextrin-modified microemulsion electrokinetic chromatography.

PubMed

Okamoto, Hitoshi; Nakajima, Toshiaki; Ito, Yuji; Aketo, Takao; Shimada, Kenji; Yamato, Susumu

2005-03-09

Cyclodextrin-modified microemulsion electrokinetic chromatography (CD-MEEKC) was used to simultaneously determine 14 active ingredients (thiamine nitrate, anhydrous caffeine, acetaminophen, riboflavin, guaifenesin, pseudoephedrine hydrochloride, ascorbic acid, ethenzamide, DL-methylephedrine hydrochloride, dihydrocodeine phosphate, ibuprofen, noscapine, carbinoxamine maleate, and bromhexine hydrochloride) in a cold medicine. Separation of the ingredients was optimized by changing the SDS concentration and oil type and the addition of 2-propanol and cyclodextrin (CD) to the separation solution. The separation selectivity was improved dramatically by changing CD type. All of the active ingredients and formulation excipients were successfully separated with the use of a separation solution consisting of 0.81% (w/w) pentane, 6.61% (w/w) 1-butanol, 2% (w/w) 2-propanol, 4.47% (w/w) SDS, and 86.11% (w/w) 10 mM sodium tetraborate solution with 3 mM 2,6-di-O-methyl-beta-CD. The established method was then validated and demonstrated to be applicable to the determination of the active ingredients in a model cold medicine. No interference from the formulation excipients was observed. Good linearities were obtained with correlation coefficients above 0.999. Recovery and precision ranged from 99.1 to 100.7% and from 0.5 to 2.8% R.S.D., respectively. The detection limit for ingredients ranged from 0.6 to 4.2 microg ml(-1). Good agreement was obtained between the established method and the traditional HPLC method. These results suggest that CD-MEEKC can be used for the determination of multiple ingredients in cold medicine.

Accurate determination of sulfur in gasoline and related fuel samples using isotope dilution ICP-MS with direct sample injection and microwave-assisted digestion.

PubMed

Heilmann, Jens; Boulyga, Sergei F; Heumann, Klaus G

2004-09-01

Inductively coupled plasma isotope-dilution mass spectrometry (ICP-IDMS) with direct injection of isotope-diluted samples into the plasma, using a direct injection high-efficiency nebulizer (DIHEN), was applied for accurate sulfur determinations in sulfur-free premium gasoline, gas oil, diesel fuel, and heating oil. For direct injection a micro-emulsion consisting of the corresponding organic sample and an aqueous 34S-enriched spike solution with additions of tetrahydronaphthalene and Triton X-100, was prepared. The ICP-MS parameters were optimized with respect to high sulfur ion intensities, low mass-bias values, and high precision of 32S/34S ratio measurements. For validation of the DIHEN-ICP-IDMS method two certified gas oil reference materials (BCR 107 and BCR 672) were analyzed. For comparison a wet-chemical ICP-IDMS method was applied with microwave-assisted digestion using decomposition of samples in a closed quartz vessel inserted into a normal microwave system. The results from both ICP-IDMS methods agree well with the certified values of the reference materials and also with each other for analyses of other samples. However, the standard deviation of DIHEN-ICP-IDMS was about a factor of two higher (5-6% RSD at concentration levels above 100 mircog g(-1)) compared with those of wet-chemical ICP-IDMS, mainly due to inhomogeneities of the micro-emulsion, which causes additional plasma instabilities. Detection limits of 4 and 18 microg g(-1) were obtained for ICP-IDMS in connection with microwave-assisted digestion and DIHEN-ICP-IDMS, respectively, with a sulfur background of the used Milli-Q water as the main limiting factor for both methods.

Synthesis of visible light driven cobalt tailored Ag{sub 2}O/TiON nanophotocatalyst by reverse micelle processing for degradation of Eriochrome Black T

DOE Office of Scientific and Technical Information (OSTI.GOV)

Hussain, Syed Tajammul, E-mail: dr_tajammul@yahoo.ca; Rashid; Department of Chemistry, Quaid-i-Azam University, Islamabad

2013-02-15

Graphical abstract: Cobalt tailored Ag{sub 2}O/TiON nanophotocatalyst is synthesized using reverse micelle technique and it showed extraordinary photocatalytic activity. Display Omitted Highlights: ► TiON/Ag{sub 2}O/Co nanophotocatalyst is synthesized using microemulsion technique. ► Low temperature anatase phase and outstanding photocatlytic activity is observed. ► Effect of temperature and inert atmosphere on materials phase is investigated. ► Homogeneous dopants distribution and oxygen vacancies are examined. ► Enhancement in surface area, quantum efficiency and optical properties is observed. -- Abstract: An ultra efficient cobalt tailored silver and nitrogen co-doped titania (TiON/Ag{sub 2}O/Co) visible nanophotocatalyst is successfully synthesized using modified reverse micelle processing. Composition,more » phase, distribution of dopants, functional group analysis, optical properties and morphology of synthesized materials are investigated by means of X-ray diffraction (XRD), transmission electron microscopy (TEM) based techniques and others. Charge states of titanium (Ti) and silver are explored through core-loss electron energy loss spectroscopy (EELS) analysis and X ray photoelectron spectroscopy (XPS). Our characterization results showed that the synthesized nanophotocatalyst consisted of anatase phased qausispherical nanoparticles that exhibited homogeneous distribution of dopants, large surface area, high quantum efficiency and enhanced optical properties. At lower content of doped Co ions, the TiON/Ag{sub 2}O responded with extraordinary photocatalytic properties. The cobalt tailored nanophotocatalyst showed remarkable activity against Eriochrome Black T (EBT). Moreover, comparative degradation behavior of EBT with TiON, Ag{sub 2}O/TiON and Co/Ag{sub 2}O/TiON is also investigated.« less

Investigation of atmospheric oxidation of propyl gallate in an anionic surfactant system in the absence and presence of ascorbic acid.

PubMed

Szymula, M

2004-01-01

The antioxidant efficiency of two hydrophilic species, ascorbic acid (AA) and propyl gallate (PG), in an anionic surfactant system are studied. Ascorbic acid and propyl gallate are dissolved/solubilized in a microemulsion formed by water, pentanol, and sodium dodecyl sulfate. The determination of propyl gallate decomposition/oxidation kinetics shows enhanced oxidation of PG with increasing pentanol concentration in the system. When ascorbic acid and propyl gallate are both present in water, in surfactant aqueous solution, and in the studied microemulsion systems, the molecular complex AAPG is formed. After some time the complex decomposes.

Effective charges and zeta potentials of oil in water microemulsions in the presence of Hofmeister salts.

PubMed

Dos Santos, Alexandre P; Levin, Yan

2018-06-14

We present a theory which allows us to calculate the effective charge and zeta potential of oil droplets in microemulsions containing Hofmeister salts. A modified Poisson-Boltzmann equation is used to account for the surface and ion polarizations and hydrophobic and dispersion interactions. The ions are classified as kosmotropes and chaotropes according to their Jones-Dole viscosity B coefficient. Kosmotropes stay hydrated and do not enter into the oil phase, while chaotropes can adsorb to the oil-water interface. The effective interaction potentials between ions and oil-water interface are parametrized so as to accurately account for the excess interfacial tension.