Synergistic Combinations of a Pyrethroid Insecticide and an Emulsifiable Oil Formulation of Beauveria bassiana to Overcome Insecticide Resistance in Listronotus maculicollis (Coleoptera: Curculionidae).

PubMed

Wu, Shaohui; Kostromytska, Olga S; Koppenhöfer, Albrecht M

2017-08-01

The annual bluegrass weevil, Listronotus maculicollis (Kirby), is a major pest of golf course turf in eastern North America and has become particularly problematic owing to widespread development of insecticide resistance. As an alternative option to manage resistant adult L. maculicollis, we explored combinations of the pyrethroid insecticide bifenthrin with an emulsifiable oil formulation of the entomopathogenic fungus Beauveria bassiana strain GHA (Bb ES). Combinations synergistically enhanced mortality in both insecticide-susceptible and insecticide-resistant L. maculicollis adults in the laboratory when bifenthrin was used at LC50s for each population. To determine the component behind the synergism, technical spores of B. bassiana GHA and the emulsifiable oil carrier in the fungal formulation were tested separately or in combination with bifenthrin. In both separate and combined applications, the emulsifiable oil carrier was responsible for high mortality within 3 d after treatment and interacted synergistically with bifenthrin, whereas fungus-induced mortality started later. Strong synergism was also observed in three field experiments with a relatively resistant L. maculicollis population. Combinations of Bb ES and bifenthrin hold promise as an effective L. maculicollis management tool, particularly of pyrethroid-resistant populations. © The Authors 2017. Published by Oxford University Press on behalf of Entomological Society of America. All rights reserved. For Permissions, please email: journals.permissions@oup.com.

A novel surfactant-free lipid-based formulation for improving oral bioavailability of loratadine using colloidal silicon dioxide as emulsifier and solid carrier.

PubMed

Huang, Ri; Tan, Yonggang; Shen, Lao; Wang, Tao; Quan, Dongqin

2018-05-08

The purpose of this study was to develop an innovative surfactant-free lipid-based formulation (LF) for improving oral bioavailability of loratadine based on using solid particles colloidal silicon dioxide (CSD) as emulsifier and solid carrier. Loratadine was dissolved in oil solution with the aid of co-solvent and LF were prepared by a simple adsorption and milling technique. The LF Powder was evaluated in terms of angle of repose and X-ray powder diffraction. After dispersing and emulsifying in water, the particle size and morphology were also characterized. In vitro dissolution and pharmacokinetic behavior in vivo were also studied. Orthogonal design indicated that the amount of CSD in formulations had a major and significant influence on emulsification. The optimal formulation showed LF with good flowability and without crystallization or deposition of loratadine in it. After dispersing in water, an emulsion with mean droplet size of 1.2μm was obtained. Although the dissolution of drug from LF was slower in vitro in acidic aqueous solution, pharmacokinetic studies in vivo showed that the bioavailability of loratadine increased 2.49-fold by CF compared to commercial tablet. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Evaluation of emulsion emulsified by starch nanocrystal: A preliminary study

NASA Astrophysics Data System (ADS)

Ahmad, Azfar Al Ariff; Lazim, Azwan Mat

2018-04-01

The starch nanocrystals (SNC) used in this study were made of sago starch and prepared by using sulfuric acid hydrolysis of sago starch. The aim of this study is to look at the potential of SNC as and emulsifier. Previously, the SNC underwent analytical analysis in order to understand and evaluate the isolated SNC. The ability of SNC as emulsifier was further investigated in this study. Emulsions with low, medium and high oil content has been prepared in function of different wt% of SNC. The emulsion stability against coalescence for two weeks has also been studied. Results showed that the emulsions prepared are steadily stable after one weeks of storage without any separation and changes. From the observation, there are two major factor contributed to the formation of emulsion and its stability, the SNC concentration and oil content. Relatively, higher percentage of SNC resulting a higher emulsion index, whereas no emulsion was formed if oil content exceeding 50% of the systems. The most suitable formulation to prepare Pickering Emulsion is the oil content around 45% and SNC concentration around 2 - 4%.

Emulsified systems based on glyceryl monostearate and potassium cetyl phosphate: scale-up and characterization of physical properties.

PubMed

Baby, André Rolim; Santoro, Diego Monegatto; Velasco, Maria Valéria Robles; Dos Reis Serra, Cristina Helena

2008-09-01

Introducing a pharmaceutical product on the market involves several stages of research. The scale-up stage comprises the integration of previous phases of development and their integration. This phase is extremely important since many process limitations which do not appear on the small scale become significant on the transposition to a large one. Since scientific literature presents only a few reports about the characterization of emulsified systems involving their scaling-up, this research work aimed at evaluating physical properties of non-ionic and anionic emulsions during their manufacturing phases: laboratory stage and scale-up. Prototype non-ionic (glyceryl monostearate) and anionic (potassium cetyl phosphate) emulsified systems had the physical properties by the determination of the droplet size (D[4,3], mum) and rheology profile. Transposition occurred from a batch of 500-50,000g. Semi-industrial manufacturing involved distinct conditions: intensity of agitation and homogenization. Comparing the non-ionic and anionic systems, it was observed that anionic emulsifiers generated systems with smaller droplet size and higher viscosity in laboratory scale. Besides that, for the concentrations tested, augmentation of the glyceryl monostearate emulsifier content provided formulations with better physical characteristics. For systems with potassium cetyl phosphate, droplet size increased with the elevation of the emulsifier concentration, suggesting inadequate stability. The scale-up provoked more significant alterations on the rheological profile and droplet size on the anionic systems than the non-ionic.

Field evaluation of the biolarvicide, spinosad 20 per cent emulsifiable concentrate in comparison to its 12 per cent suspension concentrate formulation against Culex quinquefasciatus, the vector of bancroftian filariasis in India.

PubMed

Sadanandane, Candasamy; Gunasekaran, Kasinathan; Boopathi Doss, Ponnusamy Sivagnana; Jambulingam, Purushothaman

2018-01-01

Biolarvicides may offer alternatives to chemical larvicides as these are known to be safe to environment and selective against the target species. However, only a limited number of biolarvicides have been approved for mosquito larval control. In the current study, a new formulation of spinosad, 20 per cent emulsifiable concentrate (EC) was tested for its efficacy against Culex quinquefasciatus, in comparison to its 12 per cent suspension concentrate (SC). Spinosad 20 per cent EC was tested against Cx. quinquefasciatus immature at 25, 50, 100 and 150 mg active ingredient (ai)/m [2] in cesspits, drains and abandoned wells in comparison with spinosad 12 per cent SC at the optimum field application dosage of 50 mg ai/m [2] . The 20 per cent EC caused 90-100 per cent reduction of pupal density for 7-14 days in cesspits, 10-17 days in drains and 14-30 days in abandoned wells at all dosages tested. At lower dosages of 25 and 50 mg ai/m [2] , >90 per cent reduction of pupal density was observed for one week in cesspits and street drains and for two weeks in abandoned wells. The effective duration of control provided by the higher dosages, 100 and 150 mg ai/m [2] was 1.4 to 2 times greater than the lower dosages, 25 and 50 mg ai/m [2] . The findings showed that the spinosad 20 per cent EC can be used for larval control against Cx. quinquefasciatus, at the dosage of 25 mg ai/m [2] at weekly interval in cesspits and drains and at fortnightly interval in abandoned wells. Spinosad 20 per cent EC could be one of the options to be considered for larval control under integrated vector management.

Formulation and immunological evaluation of a trivalent vaccine comprising emulsified submicron particles and inactivated virions of H5N1/EV71/JEV

PubMed Central

Lin, Chih-Wei; Chang, Ching-Yun; Chen, Wei-Lin; Lin, Shih-Chang; Liao, Chien-Chun; Chang, Jui-Yuan; Liu, Chia-Chyi; Hu, Alan Yung-Chih; Lu, Tsung-Chun; Chou, Ai-Hsiang; Wu, Suh-Chin; Chong, Pele; Huang, Ming-Hsi

2013-01-01

Combination vaccines can reduce the number of injections and simplify the immunization schedule required to prevent different diseases. Here we assessed the immunogenicity in a mouse model of a vaccine composition comprising inactivated influenza viruses (H5N1/H1N1), enterovirus 71 (EV71), and/or Japanese encephalitis virus (JEV) and investigated whether the vaccine formulations can overcome the immunologic interference between the individual vaccine components. We demonstrated that the antigenic competition happens between H5N1/H1N1 or H5N1/EV71 inactivated virions when the vaccine combinations either formulated with Alum suspensions or without adjuvant. In the presence of PELC emulsified particles, EV71-specific immune responses before and after incorporating H5N1 virus into EV71 vaccine were detected of no significant difference; in addition, H5N1- and EV71-specific immune responses were found at the same level when H5N1/EV71/JEV consolidating into combination vaccine. Emulsified vaccine formulation was represented as a potential tool that is found to reduce the number of injections required to prevent multiple infectious strains causing the same disease (H5N1/H1N1) and/or that protect against different diseases (H5N1/EV71). Combination vaccines can also include a third component to protect against H5N1/EV71/JEV at the same time. PMID:23838466

Sterile Filtration of Highly Concentrated Protein Formulations: Impact of Protein Concentration, Formulation Composition, and Filter Material.

PubMed

Allmendinger, Andrea; Mueller, Robert; Huwyler, Joerg; Mahler, Hanns-Christian; Fischer, Stefan

2015-10-01

Differences in filtration behavior of concentrated protein formulations were observed during aseptic drug product manufacturing of biologics dependent on formulation composition. The present study investigates filtration forces of monoclonal antibody formulations in a small-scale set-up using polyvinylidene difluoride (PVDF) or polyethersulfone (PES) filters. Different factors like formulation composition and protein concentration related to differences in viscosity, as well as different filtration rates were evaluated. The present study showed that filtration behavior was influenced by the presence or absence of a surfactant in the formulation, which defines the interaction between filter membrane and surface active formulation components. This can lead to a change in filter resistance (PES filter) independent on the buffer system used. Filtration behavior was additionally defined by rheological non-Newtonian flow behavior. The data showed that high shear rates resulting from small pore sizes and filtration pressure up to 1.0 bar led to shear-thinning behavior for highly concentrated protein formulations. Differences in non-Newtonian behavior were attributed to ionic strength related to differences in repulsive and attractive interactions. The present study showed that the interplay of formulation composition, filter material, and filtration rate can explain differences in filtration behavior/filtration flux observed for highly concentrated protein formulations thus guiding filter selection. © 2015 Wiley Periodicals, Inc. and the American Pharmacists Association.

Foaming and emulsifying properties of pectin isolated from different plant materials

NASA Astrophysics Data System (ADS)

Yancheva, Nikoleta; Markova, Daniela; Murdzheva, Dilyana; Vasileva, Ivelina; Slavov, Anton

2016-03-01

The foaming and emulsifying properties of pectins obtained from waste rose petals, citrus pressings, grapefruit peels and celery were studied. It was found that the highest foaming capacity showed pectin derived from celery. The effect of pectin concentration on the foaming capacity of pectin solutions was investigated. For all the investigated pectins increasing the concentration led to increase of the foaming capacity. Emulsifying activity and emulsion stability of model emulsion systems (50 % oil phase) with 0.6 % pectic solutions were determined. The highest emulsifying activity and stability showed pectin isolated by dilute acid extraction from waste rose petals.

[Optimization of formulations for dietetic pastry products].

PubMed

Villarroel, M; Uquiche, E; Brito, G; Cancino, M

2000-03-01

Optimized formulations of dietetic pastry products such as cake and sponge cake premixes were formulated using the surface response methodology. % Emulsifier agent and baking time were the selected independent variables for cake, as well as % emulsifier agent % chlorinated flour the variables selected for sponge cake. Three different level of each variable summing up thirteen experimental formulae of each product were assessed to optimize the variables that could have some influence in the sensory characteristics of these dietetic products. The total sensory quality was determined for both dietetic products using the composite scoring test and a panel of 18 trained judges. Looking at the contour graphic and considering economic aspects the best combination of variables for cake formulation was 2% emulsifier agent and 48 minutes for baking time, With respect to sponge cake, the best combination was 6% emulsifier agent and 48% chlorinated flour. Shelf life studies showed that both dietetic formulations remained stable during storage conditions of 75 days at 30 degrees C. During this period, significant differences in sensory characteristics were not found (p < 0.05). Data of peroxide values were kept under the critical value reported for detection of organoleptic rancidity. Reported values of hedonic test showed that these dietetics pastry products had good acceptability, and open up marketing opportunities for new products with potential health benefits to consumers.

Influence of non-ionic emulsifier type on the stability of cinnamaldehyde nanoemulsions: A comparison of polysorbate 80 and hydrophobically modified inulin.

PubMed

Sedaghat Doost, Ali; Dewettinck, Koen; Devlieghere, Frank; Van der Meeren, Paul

2018-08-30

Cinnamaldehyde nanoemulsions were formulated to enable its application in an aqueous environment. The pure cinnamaldehyde nanoemulsions, stabilized by polysorbate 80 (at concentrations >0.5%), had both a higher stability and smaller droplet size, whereas the emulsions containing hydrophobically modified inulin (HMI) formed a colloidal dispersion with larger particle size. Incorporation of sunflower oil (SO) allowed postponement of Ostwald ripening for a sufficiently long period of time (at least 60 days). Cryo-SEM and droplet size analyses of the nanoemulsions emulsified by HMI revealed no significant changes during storage. Under these conditions, HMI as an emulsifier exhibited a powerful resistance to high salt contents (up to 2 M) and high thermal processing temperatures (90 °C). The surfactant type and SO content had no marked influence on the antimicrobial activity of the nanoemulsions. This study provides precious information for a commercial formulation of nanoemulsions with durable physical stability under severe stress conditions. Copyright © 2018 Elsevier Ltd. All rights reserved.

Selection of a discriminant and biorelevant in vitro dissolution test for the development of fenofibrate self-emulsifying lipid-based formulations.

PubMed

Pestieau, Aude; Krier, Fabrice; Brouwers, Adeline; Streel, Bruno; Evrard, Brigitte

2016-09-20

Fenofibrate, a BCS class II compound, has a low bioavailability especially when taken orally on an empty stomach. The challenge to find a new formulation for providing bioavailability, independent of food, is still ongoing. If the development of a suitable oral delivery formulation of BCS class II compounds is a frequent and great challenge to formulation scientists, the in vitro evaluation of these new formulations is also a great challenge. The purpose of this study was therefore to select an in vitro dissolution test that would be useful and as biorelevant as possible for the development of fenofibrate self-emulsifying lipid-based formulations. In this context, three different fenofibrate formulations, for which in vivo data are available in the literature, were tested using different dissolution tests until we found the one that was the most suitable. As part of this approach, we started with the simplest in vitro dissolution tests and progressed to tests that were increasingly more complex. The first tests were different single phase dissolution tests: a test under sink conditions based on the USP monograph, and different tests under non-sink conditions in non-biorelevant and biorelevant media. Given the inconclusive results obtained with these tests, biphasic dissolution systems were then tested: one with USP apparatus type II alone and another which combined USP apparatus types II and IV. This last combined test seemed the most suitable in vitro dissolution test for the development of the future fenofibrate lipid-based formulations we intend to develop in our own laboratory. Copyright © 2016 Elsevier B.V. All rights reserved.

A comparison of the stability of beverage cloud emulsions formulated with different gum acacia- and starch-based emulsifiers.

PubMed

Reiner, S J; Reineccius, G A; Peppard, T L

2010-06-01

The performance of several hydrocolloids (3 gum acacias, 1 modified gum acacia, and 3 modified starches) in stabilizing beverage emulsions and corresponding model beverages was investigated employing different core materials, emulsifier usage levels, and storage temperatures. Concentrated emulsions were prepared using orange terpenes or Miglyol 812 (comprising medium-chain triglycerides, MCT) weighted 1:1 with ester gum, stored at 25 or 35 degrees C, and analyzed on days 0, 1, and 3. On day 3, model beverages were made from each emulsion, stored at both temperatures, and analyzed weekly for 4 wk. Stability of concentrated emulsions was assessed by measuring mean particle size and by visual observations of ringing; beverage stability was judged similarly and also by loss of turbidity. Particle size measurements showed concentrated emulsions containing gum acacia or modified gum acacia with either core material were stable over 3 d storage at both temperatures whereas those made with modified starches were not, destabilization being faster at 35 degrees C. Beverages based on orange terpenes, in contrast to Miglyol, yielded smaller mean particle sizes, both on manufacture and during storage, regardless of hydrocolloid used. Visual observations of ringing generally supported this finding. Modified gum acacia was evaluated at both recommended and higher usage levels, stability increasing in the latter case. In general, all gum acacia and modified gum acacia emulsifiers were superior in stability to those based on modified starches, at either temperature, for orange terpene-based beverages. In Miglyol-based beverages, similar results were seen, except 1 modified starch performed as well as the gum acacia products.

Role of medium-chain fatty acids in the emulsification mechanistics of self-micro-emulsifying lipid formulations.

PubMed

Hasan, Naser M Y

2014-12-01

The objective of the present study was to design and develop stable o/w microemulsions comprising Miglyol 812, Imwitor 988 and Tagat TO as a non ionic surfactant. This was based on particle size measurements and phase behavior studies. The empirical role of incorporating medium-chain mono/di-glycerides in the lipid matrix in the mechanistic processes of emulsification was also established in various simulating physiological conditions. The efficiency of self-emulsification was evaluated under conditions of varying key compositions in the lipid mixtures; oil, cosurfactant and surfactant. Droplet diameter was measured using laser diffraction and light scattering techniques. Equilibrium phase studies were performed and phase boundaries were determined for the lipid-water systems. Microemulsion systems were produced from blends of Miglyol 812, Imwitor 988 and Tagat TO. An optimized formulation consisted of {Miglyol 812/Imwitor 988} and Tagat TO spontaneously self-emulsified in water producing dispersions with droplet diameters of ∼50 nm. Phase equilibrium diagrams have revealed significant enhancement in the water-solubilized region (L2) without any presence of liquid crystalline materials. Potential SMEDDS formulations for the bioavailability enhancement of poorly water-soluble compounds were developed by mixing blends of {Miglyol 812/Imwitor 988} and Tagat TO as a non-ionic surfactant. 'Diffusion and stranding' appears to be the dominant mechanism of emulsification.

Role of medium-chain fatty acids in the emulsification mechanistics of self-micro-emulsifying lipid formulations

PubMed Central

Hasan, Naser M.Y.

2014-01-01

Purpose The objective of the present study was to design and develop stable o/w microemulsions comprising Miglyol 812, Imwitor 988 and Tagat TO as a non ionic surfactant. This was based on particle size measurements and phase behavior studies. The empirical role of incorporating medium-chain mono/di-glycerides in the lipid matrix in the mechanistic processes of emulsification was also established in various simulating physiological conditions. Methods The efficiency of self-emulsification was evaluated under conditions of varying key compositions in the lipid mixtures; oil, cosurfactant and surfactant. Droplet diameter was measured using laser diffraction and light scattering techniques. Equilibrium phase studies were performed and phase boundaries were determined for the lipid–water systems. Results Microemulsion systems were produced from blends of Miglyol 812, Imwitor 988 and Tagat TO. An optimized formulation consisted of {Miglyol 812/Imwitor 988} and Tagat TO spontaneously self-emulsified in water producing dispersions with droplet diameters of ∼50 nm. Phase equilibrium diagrams have revealed significant enhancement in the water-solubilized region (L2) without any presence of liquid crystalline materials. Conclusions Potential SMEDDS formulations for the bioavailability enhancement of poorly water-soluble compounds were developed by mixing blends of {Miglyol 812/Imwitor 988} and Tagat TO as a non-ionic surfactant. ‘Diffusion and stranding’ appears to be the dominant mechanism of emulsification. PMID:25561872

The effects of emulsifying agents on disposition of lipid-soluble drugs included in fat emulsion.

PubMed

Suzuki, Yasuyuki; Masumitsu, Yasushi; Okudaira, Kazuho; Hayashi, Masahiro

2004-02-01

The uses for drug delivery systems of two soybean oil fat emulsions prepared with an emulsifying agent, phosphatidyl choline (PC) or Pluronic F-127 (PLU), were examined comparatively in vivo and in vitro. In the presence of lipoprotein lipase (LPL) in vitro, the mean particle size of the PLU emulsion changed less than that of the PC emulsion. The production of non-esterified fatty acid (NEFA) from the PLU emulsion in the presence of LPL was smaller than that from the PC emulsion. These in vitro results indicate that the PLU emulsion is more stable than the PC emulsion. Plasma NEFA concentration following intravenous administration of the emulsions decreased with time for the PC emulsion, but was kept lower and constant for the PLU emulsion, supporting the in vitro stability data. The order of plasma cyclosporine A (CsA) concentration following intravenous administration in the above two emulsions and the mixed solution of polyethylene glycol 400 (PEG) and dimethylamide (DMA) in rats was PLU emulsion>PC emulsion>PEG/DMA solution. The plasma concentration was maintained higher and tissue distribution lower for the PLU emulsion than for other formulations. The uptake of oil violet (OV) into the rat parenchymal cells from the PLU emulsion was approximately half that from the PC emulsion, but the uptake into the Kupffer cells was almost equal in both emulsions. In conclusion, these emulsifying agents can control plasma elimination and tissue distribution of lipophilic drugs included in the emulsion. The use of the emulsion formulation makes it possible to avoid side effects through the reduction of drug uptake into non-targeted tissues.

Helix aspersa gelatin as an emulsifier and emulsion stabilizer: functional properties and effects on pancreatic lipolysis.

PubMed

Zarai, Zied; Balti, Rafik; Sila, Assaâd; Ben Ali, Yassine; Gargouri, Youssef

2016-01-01

Emulsions are widely used in food and pharmaceutical applications for the encapsulation, solubilization, entrapment, and controlled delivery of active ingredients. In order to fulfill the increasing demand for clean label excipients, natural polymers could be used to replace the potentially irritative synthetic surfactants used in emulsion formulation. In the present study, we have studied the properties of oil-in-water emulsions prepared with land snail gelatin (LSG) as the sole emulsifying agent, extracted and described for the first time. LSG was evaluated in terms of proximate composition, oil and water holding capacity, emulsifying and foaming properties, color and amino acid composition. Emulsions of trioctanoylglycerol (TC8) and olive oil were made at different gelatin/oil ratios and changes in droplet-size distribution were determined. The superior emulsifying properties of LSG, the susceptibility of gelatin protein emulsions increasing flocculation on storage, and the coalescence of gelatin emulsions following centrifugation were demonstrated. Furthermore, the effect of LSG on the activity of turkey pancreatic lipase (TPL) was evaluated through the pH-stat methodology with TC8 and olive oil emulsions. The LSG affected the TPL activity in a concentration-dependent way. Our results showed that LSG, comparably to gum arabic, increases the pancreatic lipase activity and improves its stability at the oil-water interface.

Formulation of wax oxybenzone microparticles using a factorial approach.

PubMed

Gomaa, Y A; Darwish, I A; Boraei, N A; El-Khordagui, L K

2010-01-01

Oxybenzone wax microparticles (MPs) were prepared by the hydrophobic congealable disperse phase method. The formulation of oxybenzone-loaded MPs was optimized using a 2⁴ experimental design. Factorial analysis indicated that the main MP characteristics were influenced by initial drug loading, emulsification speed, emulsifier concentration and hydrophilic-lipophilic balance. MPs were spherical with 50.5–88.1 μm size range, 17.8–38.9 drug content in mg/100 mg MPs and 33.1–87.2% oxybenzone release in 1 h. A wide range of sunscreen delivery systems suitable for different formulation purposes were generated which may contribute to the advanced formulation of sunscreen products with improved performance.

Development of rectal self-emulsifying suspension of a moisture-labile water-soluble drug.

PubMed

Kauss, Tina; Gaubert, Alexandra; Tabaran, Luc; Tonelli, Giovanni; Phoeung, Thida; Langlois, Marie-Hélène; White, Nick; Cartwright, Anthony; Gomes, Melba; Gaudin, Karen

2018-01-30

Self-emulsifying drug delivery systems, commonly used for oral delivery of poorly soluble compounds, were used to formulate water soluble but moisture labile compounds for rectal application. The objective was to use the oily phase of the system to formulate a liquid, non-aqueous product while obtaining the advantages of self-emulsification, rapid contact with the rectal mucosa and rapid absorption post-administration. Ceftriaxone was used as a model drug and the human bile salt sodium chenodeoxycholate was used as an absorption enhancer. After preliminary screening of 23 excipients, based on their emulsification ability and emulsion fineness in binary and ternary mixtures, a full factorial design was used to screen different formulations of three preselected excipients. The optimal formulation contained 60% of excipients, namely Capryol 90, Kolliphor EL and Kolliphor PS20 in 4 : 6 : 6 ratio and 40% of a powder blend that included 500 mg of ceftriaxone. Characterization of the system showed that it complied with the requirements for rectal administration, in particular rapid emulsification in a small quantity of liquid. Rabbit bioavailability showed rapid absorption of ceftriaxone, achieving 128% bioavailability compared to powder control formulation. These results demonstrated the potential of self-emulsifying formulations for rectal administration of Class 3 BCS drugs. Crown Copyright © 2017. Published by Elsevier B.V. All rights reserved.

The Ratios of Pre-emulsified Duck Skin for Optimized Processing of Restructured Ham.

PubMed

Shim, Jae-Yun; Kim, Tae-Kyung; Kim, Young-Boong; Jeon, Ki-Hong; Ahn, Kwang-Il; Paik, Hyun-Dong; Choi, Yun-Sang

2018-02-01

The purpose of this study was to investigate the quality of duck ham formulated with duck skin through the pre-emulsification process. The experiments to investigate the quality characteristics of duck ham were carried out to measure proximate composition, cooking loss, emulsion stability, pH, color, texture profile analysis, apparent viscosity, and sensory characteristics. Duck ham was prepared with various ratios of duck skin in pre-emulsion as follows: Control (duct skin 30%), T1 (duck skin 20% + pre-emulsified duck skin 10%), T2 (duck skin 15% + pre-emulsified duck skin 15%), T3 (duck skin 10% + pre-emulsified duck skin 20%), and T4 (pre-emulsified duck skin 30%). As the ratio of duck skin to pre-emulsified skin changed, the quality of duck ham in terms of moisture content, fat content, cooking loss, emulsion stability, lightness, textural analysis, apparent viscosity, and overall acceptability changed. The moisture content of T2 was the highest ( p <0.05) and that of the control and T4 was the lowest ( p <0.05). The fat content of control was higher than all treatments ( p <0.05). T2 had the lowest values in cooking loss, total expressible fluid, fat separation, hardness, springiness, and gumminess ( p <0.05). The score of overall acceptability of all treatments with pre-emulsified skin was higher than control ( p <0.05). Therefore, the pre-emulsification process can improve the quality characteristics of duck ham and 1:1 ratio of duck skin and pre-emulsified skin was the proper ratio to improve the quality characteristics of duck ham.

Self-double-emulsifying drug delivery system (SDEDDS): a new way for oral delivery of drugs with high solubility and low permeability.

PubMed

Qi, Xiaole; Wang, Lishuang; Zhu, Jiabi; Hu, Zhenyi; Zhang, Jie

2011-05-16

Water-in-oil-in-water (w/o/w) double emulsions are potential for enhancing oral bioavailability of drugs with high solubility and low permeability, but their industrial application is limited due to the instability. Herein, we developed a novel formulation, self-double-emulsifying drug delivery systems (SDEDDS) by formulating mixtures of hydrophilic surfactants and water-in-oil (w/o) emulsions, which were easier to be stable through formulations optimization. SDEDDS can spontaneously emulsify to water-in-oil-in-water (w/o/w) double emulsions in the mixed aqueous gastrointestinal environment, with drugs encapsulated in the internal water phase of the double emulsions. We employed SDEDDS to improve the oral absorption of pidotimod, a peptide-like drug with high solubility and low permeability. The optimized pidotimod-SDEDDS were found to be stable up to 6 months under 25°C. Plasma concentration-time profiles from pharmacokinetic studies in rats dosed with SDEDDS showed 2.56-fold (p<0.05) increased absorption of pidotimod, compared to the pidotimod solution. Histopathologic studies confirmed that SDEDDS exerted absorption promoting effect without serious local damages. These studies demonstrate that SDEDDS may be a promising strategy for peroral delivery of peptide and peptidomimetic drugs. Copyright © 2011 Elsevier B.V. All rights reserved.

Swirling cavitation improves the emulsifying properties of commercial soy protein isolate.

PubMed

Yang, Feng; Liu, Xue; Ren, Xian'e; Huang, Yongchun; Huang, Chengdu; Zhang, Kunming

2018-04-01

Since emulsifying properties are important functional properties of soy protein, many physical, chemical, and enzymatic methods have been applied to treat soy protein to improve emulsifying properties. In this study, we investigated the effects of swirling cavitation at different pressures and for different times on emulsifying and physicochemical properties of soy protein isolate (SPI). The SPI treated with swirling cavitation showed a significant decrease in particle size and increase in solubility. Emulsions formed from treated SPI had higher emulsifying activity and emulsifying stability indexes, smaller oil droplet sizes, lower flocculation indexes, higher adsorbed proteins, lower interfacial protein concentrations, and lower creaming indexes than those formed from untreated SPI, indicating that swirling cavitation improved the emulsifying properties of the SPI. Furthermore, swirling cavitation treatment significantly enhanced the surface hydrophobicity, altered the disulfide bond and exposed sulfhydryl group contents of the SPI. The secondary structure of the SPI was also influenced by swirling cavitation, with an increase in β-sheet content and a decrease in α-helix, β-turn, and random coil contents. In addition, several significant correlations between physicochemical and emulsifying properties were revealed by Pearson correlation analysis, suggesting that the physicochemical changes observed in treated SPI, including the decreased particle size, increased solubility and surface hydrophobicity, and enhanced β-sheet formation, may explain the improved emulsifying properties of the isolate. Thus, our findings implied that swirling cavitation treatment may be an effective technique to improve the emulsifying properties of SPI. Copyright © 2017 Elsevier B.V. All rights reserved.

Emulsifying conditions and processing parameters optimisation of kenaf seed oil-in-water nanoemulsions stabilised by ternary emulsifier mixtures.

PubMed

Cheong, Ai M; Tan, Chin P; Nyam, Kar L

2018-01-01

Kenaf ( Hibiscus cannabinus L.) seed oil has been proven for its multi-pharmacological benefits; however, its poor water solubility and stability have limited its industrial applications. This study was aimed to further improve the stability of pre-developed kenaf seed oil-in-water nanoemulsions by using food-grade ternary emulsifiers. The effects of emulsifier concentration (1, 5, 10, 15% w/w), homogenisation pressure (16,000, 22,000, 28,000 psi), and homogenisation cycles (three, four, five cycles) were studied to produce high stability of kenaf seed oil-in-water nanoemulsions using high pressure homogeniser. Generally, results showed that the emulsifier concentration and homogenisation conditions had great effect ( p < 0.05) on the particle sizes, polydispersity index and hence the physical stability of nanoemulsions. Homogenisation parameters at 28,000 psi for three cycles produced the most stable homogeneous nanoemulsions that were below 130 nm, below 0.16, and above -40 mV of particle size, polydispersity index, and zeta potential, respectively. Field emission scanning electron microscopy micrograph showed that the optimised nanoemulsions had a good distribution within nano-range. The optimised nanoemulsions were proved to be physically stable for up to six weeks of storage at room temperature. The results from this study also provided valuable information in producing stable kenaf seed oil nanoemulsions for the future application in food and nutraceutical industries.

The effect of emulsifying salts on the turbidity of a diluted milk system with varying pH and protein concentration.

PubMed

Culler, M D; Saricay, Y; Harte, F M

2017-06-01

Solutions of 10 commonly used emulsifying salts (ES) listed in the Code of Federal Regulations (21CFR133.179) for pasteurized process cheese were tested for their effect on the turbidity of a diluted milk system at different pH and protein concentrations to characterize the conditions that affect micellar structure. Emulsifying salt solutions were made by mixing the ES in a 1-in-20 dilution of water in skim milk ultrafiltrate (3 kDa molecular weight cut-off) to obtain ES concentrations from 0 to 248 mM. Skim milk was added to solutions containing nanopure water, skim milk ultrafiltrate, and a specific ES ranging in concentration from 0 to 248 mM and pH 5, 5.8, 6.8, 7.8, and 8.8. The turbidity of the samples was measured as the optical density at 400 nm immediately after mixing (time, t = 0), after 30 s (t = 30s), and after 30 min (t = 30min). Emulsifying salts were found to cause a decrease in the turbidity of the system, which was modeled using an exponential decay model, where C* represents a threshold salt concentration at which rapid dissociation occurs. At pH values 5.8 and 6.8, the ES caused the greatest decrease in turbidity of the diluted milk system. At pH 5, the ES had the least effect on the turbidity of the system. Sodium hexametaphosphate was found to have the strongest dissociative effect, with a C* value of 0.33 mM for t = 0 at pH 6.8. In contrast, the largest C* value calculated at pH 6.8 was monosodium phosphate at 278.22 mM. Increased time resulted in lower C* values. The model established for this study can be used to predict the dissociation of casein micelles in the presence of various types of ES. Copyright © 2017 American Dairy Science Association. Published by Elsevier Inc. All rights reserved.

Highly concentrated foam formulation for blast mitigation

DOEpatents

Tucker, Mark D.; Gao, Huizhen

2010-12-14

A highly concentrated foam formulation for blast suppression and dispersion mitigation for use in responding to a terrorism incident involving a radiological dispersion device. The foam formulation is more concentrated and more stable than the current blast suppression foam (AFC-380), which reduces the logistics burden on the user.

Effect of PLGA as a polymeric emulsifier on preparation of hydrophilic protein-loaded solid lipid nanoparticles.

PubMed

Xie, ShuYu; Wang, SiLiang; Zhao, BaoKai; Han, Chao; Wang, Ming; Zhou, WenZhong

2008-12-01

Most proteins are hydrophilic and poorly encapsulated into the hydrophobic matrix of solid lipid nanoparticles (SLN). To solve this problem, poly (lactic-co-glycolic acid) (PLGA) was utilized as a lipophilic polymeric emulsifier to prepare hydrophilic protein-loaded SLN by w/o/w double emulsion and solvent evaporation techniques. Hydrogenated castor oil (HCO) was used as a lipid matrix and bovine serum albumin (BSA), lysozyme and insulin were used as model proteins to investigate the effect of PLGA on the formulation of the SLN. The results showed that PLGA was essential for the primary w/o emulsification. In addition, the stability of the w/o emulsion, the encapsulation efficiency and loading capacity of the nanoparticles were enhanced with the increase of PLGA concentration. Furthermore, increasing PLGA concentration decreased zeta potential significantly but had no influence on particle size of the SLN. In vitro release study showed that PLGA significantly affected the initial burst release, i.e. the higher the content of PLGA, the lower the burst release. The released proteins maintained their integrity and bioactivity as confirmed by sodium dodecyl sulphate-polyacrylamide gel electrophoresis (SDS-PAGE) and biological assay. These results demonstrated that PLGA was an effective emulsifier for the preparation of hydrophilic protein-loaded SLN.

Effects of solid dispersion and self-emulsifying formulations on the solubility, dissolution, permeability and pharmacokinetics of isorhamnetin, quercetin and kaempferol in total flavones of Hippophae rhamnoides L.

PubMed

Zhao, Guoying; Duan, Jingze; Xie, Yan; Lin, Guobei; Luo, Huilin; Li, Guowen; Yuan, Xiurong

2013-07-01

The aim of this study was to investigate the effects of solid dispersions (SD) and self-emulsifying (SE) formulations on the solubility and absorption properties of active components in total flavones of Hippophae rhamnoides L. (TFH). The solubility, dissolution rate, permeability and pharmacokinetics of isorhamnetin, quercetin and kaempferol in TFH SD/SE formulations and TFH were compared. The results showed that the solubility and dissolution rate of isorhamnetin, quercetin and kaempferol in SD/SE formulations were significantly enhanced compared to those in TFH, however, their intestinal permeability was comparable. The bioavailability of isorhamnetin, quercetin and kaempferol in rats remarkably increased after oral administration of TFH SD formulations compared to TFH, but there was no significant increase after oral administration of TFH SE formulations. The results of this study indicated the SD formulations on the improvement of pharmacokinetic properties of isorhamnetin, quercetin and kaempferol in TFH were much better than those of SE formulations. The improvement of pharmacokinetic properties of isorhamnetin, quercetin and kaempferol in TFH by SD formulations was probably ascribed to the enhancement of the solubility and dissolution of the three components, but was not relevant to the intestinal permeability. Therefore, as for herb extracts containing multiple components, especially for their major components with poor water solubility, solid dispersion formulations might have the better potential to enhance their bioavailability.

Dropwise additive manufacturing of pharmaceutical products for amorphous and self emulsifying drug delivery systems.

PubMed

Içten, Elçin; Purohit, Hitesh S; Wallace, Chelsey; Giridhar, Arun; Taylor, Lynne S; Nagy, Zoltan K; Reklaitis, Gintaras V

2017-05-30

The improvements in healthcare systems and the advent of the precision medicine initiative have created the need to develop more innovative manufacturing methods for the delivery and production of individualized dosing and personalized treatments. In accordance with the changes observed in healthcare systems towards more innovative therapies, this paper presents dropwise additive manufacturing of pharmaceutical products (DAMPP) for small scale, distributed manufacturing of individualized dosing as an alternative to conventional manufacturing methods A dropwise additive manufacturing process for amorphous and self-emulsifying drug delivery systems is reported, which utilizes drop-on-demand printing technology for automated and controlled deposition of melt-based formulations onto inert tablets. The advantages of drop on demand technology include reproducible production of droplets with adjustable sizing and high placement accuracy, which enable production of individualized dosing even for low dose and high potency drugs. Flexible use of different formulations, such as lipid-based formulations, allows enhancement of the solubility of poorly water soluble and highly lipophilic drugs with DAMPP. Here, DAMPP is used to produce solid oral dosage forms from melts of an active pharmaceutical ingredient and a surfactant. The dosage forms are analyzed to show the amorphous nature, self-emulsifying drug delivery system characteristics and dissolution behavior of these formulations. Copyright © 2017 Elsevier B.V. All rights reserved.

7 CFR 58.631 - Emulsifiers.

Code of Federal Regulations, 2011 CFR

2011-01-01

... Specifications for Dairy Plants Approved for USDA Inspection and Grading Service 1 Quality Specifications for Raw Material § 58.631 Emulsifiers. Emulsifiers shall be clean and wholesome and consist of one or more of those...

7 CFR 58.631 - Emulsifiers.

Code of Federal Regulations, 2010 CFR

2010-01-01

... Specifications for Dairy Plants Approved for USDA Inspection and Grading Service 1 Quality Specifications for Raw Material § 58.631 Emulsifiers. Emulsifiers shall be clean and wholesome and consist of one or more of those...

Using oily wastewater emulsified fuel in boiler: energy saving and reduction of air pollutant emissions.

PubMed

Chen, Chun-Chi; Lee, Wen-Jhy

2008-01-01

The limited data for using emulsified oil have demonstrated its effectiveness in reducing flue gas pollutant emissions. The presence of a high concentration of toxic organic compounds in industrial wastewaters always presents significant problems. Therefore, this study was undertaken by using wastewater with COD of 9600 mg/L and total petroleum hydrocarbons-gasoline 440 mg/L for making an emulsified oil (wastewater content 20% with 0.1% surfactant) to evaluate the extent of reductions in both criteria pollutants and polycyclic aromatic hydrocarbons. For comparison, two other systems (heavy oil fuel and water-emulsified oil) were also conducted. The wastewater-emulsified oil fuel results in significant reductions in particulate matter (PM), NO(x), SO2, and CO as compared to heavy oil fuel and similar to those from water/oil emulsified fuel; for PM, it is better in wastewater-emulsified oil. The reductions of total PAH flue gas emissions are 38 and 30% for wastewater- and water-emulsified fuel, respectively; they are 63 and 44% for total BaP(eq), respectively. In addition to reducing flue gas pollutant emissions, the results also demonstrate that the use of wastewater-emulsified fuel in boiler operation provides several advantages: (1) safe disposal of industrial wastewater; and (2) energy savings of about 13%. Thus, wastewater/oil-emulsified fuel is highly suitable for use in boilers.

Thermal, emulsifying and rheological properties of polysaccharides sequentially extracted from Vaccinium bracteatum Thunb leaves.

PubMed

Xu, Qi-Xin; Shi, Jun-Jun; Zhang, Jian-Guo; Li, Ling; Jiang, Li; Wei, Zhao-Jun

2016-12-01

Plant polysaccharides are widely used in food industry as thickening and gelling agents and these attributes largely depend on their thermal, emulsifying and rheological properties. As known, the extraction methods always bring about the diversification of property and functions of polysaccharides. Thus, the Vaccinium bracteatum Thunb leaves polysaccharides (VBTLP) were sequentially extracted using hot buffer (HBSS), chelating agent (CHSS), dilute alkaline (DASS) and concentrated alkaline (CASS). The thermal, emulsifying and rheological properties of VBTLP were investigated in the present study. Within the range of 20-225°C, CHSS showed the highest peak temperature, whereas HBSS displayed the highest endothermic enthalpy and highest emulsifying activity, while, CASS showed the longest emulsifying stability. The VBTLP solutions exhibited non-Newtonian shear-thinning behavior within the concentrations of 0.6-2.5%. The apparent viscosity of VBTLP solution decreased under following conditions: acidic pH (4.0), alkaline pH (10.0), in the presence of Ca 2+ and at high temperature, while it increased in the presence of Na + and at freezing conditions. The modulus G' and G″ of VBTLP solutions were increased with increasing oscillation frequency, and the crossover frequency shifted to lower values when the polysaccharide content increased. The above results of thermal, emulsifying and rheological properties of VBTLPs supplied the basis for V. bracteatum leaves in potential industrial applications of foods. Copyright © 2016 Elsevier B.V. All rights reserved.

Self-emulsifying drug delivery systems: Design of a novel vaginal delivery system for curcumin.

PubMed

Köllner, S; Nardin, I; Markt, R; Griesser, J; Prüfert, F; Bernkop-Schnürch, A

2017-06-01

The aim of this study was to develop a vaginal self-emulsifying delivery system for curcumin being capable of spreading, of permeating the mucus gel layer and of protecting the drug being incorporated in oily nanodroplets towards mucus interactions and immobilization. The emulsifying properties of curcumin loaded SEDDS containing 30% Cremophor RH40, 20% Capmul PG-8, 30% Captex 300, 10% DMSO and 10% tetraglycol (SEDD formulation A) as well as 25% PEG 200, 35% Cremophor RH40, 20% Captex 355, 10% Caprylic acid and 10% Tween 80 (SEDD formulation B) after diluting 1+2 with artificial vaginal fluid were characterized regarding droplet size and zeta potential. Collagen swelling test was used to examine the irritation potential of SEDDS. Additionally to mucus binding studies, permeation studies in the mucus were performed. Furthermore, spreading potential of the novel developed formulations was compared with a commercial available o/w cream (non-ionic hydrophilic cream) on vaginal mucosa. SEDDS displayed a mean droplet size between 38 and 141nm and a zeta potential of -0.3 to -1.6mV. The collagen swelling test indicated no significant irritation potential of both formulations over 24h. An immediate interaction of unformulated curcumin with the mucus was determined, whereas both SEDDS facilitated drug permeation through the mucus layer. Formulation B showed a 2.2-fold improved transport ratio of curcumin compared to SEDD formulation A. In comparison to the vaginal cream, SEDD formulation A and B were able to spread over the vaginal mucosa and cover the tissue to a 17.8- and 14.8-fold higher extent, respectively. According to these results, SEDDS seems to be a promising tool for vaginal application. Copyright © 2017 Elsevier B.V. All rights reserved.

The effects of formulation on the immunostimulatory activity of dihydroheptaprenol.

PubMed

Roth, James A; Hibbard, Beth; Frank, Dagmar E; Kesl, Lyle; Robb, Edward J

2002-01-01

Holstein steer calves received a single injection of Miglyol (Sasol Chemical Industries, Ltd.) subcutaneously as a placebo, dihydroheptaprenol (DHP) (4 mg/kg) emulsified with lecithin subcutaneously, DHP in solution in Miglyol (4 mg/kg) subcutaneously, or DHP in solution in Miglyol (4 mg/kg) intranasally. The DHP emulsified in lecithin emulsion administered subcutaneously caused a substantial increase in body temperature, total leukocyte count, total neutrophil count, neutrophil cytochrome-c reduction, and neutrophil iodination 24 hours after administration and, for some of the parameters, at 48 hours. The DHP formulation in Miglyol did not have any of these effects when administered subcutaneously or intranasally. The carrier and formulation of DHP apparently have major effects on the biologic activity of DHP.

Effects of Vegetable Oil Type and Lipophilic Emulsifiers on the Induction Period of Fat Crystallization.

PubMed

Miyagawa, Yayoi; Ogawa, Takenobu; Nakagawa, Kyuya; Adachi, Shuji

2015-01-01

The induction period of crystallization, which is defined as the time required for oil to start to crystallize, is useful indicator of the freeze-thaw stability of food emulsions such as mayonnaise. We investigated the induction period of vegetable oils with low melting points, such as rapeseed and soybean oils, which are commonly employed for mayonnaise production. The induction period was measured by monitoring the temperature of a specimen during storage at low temperature. The induction period depended on the type of oil and lipophilic emulsifier, emulsifier concentration, and storage temperature. The effect of the oil type on the induction period depended on the composition of the oil. Differential scanning calorimetry (DSC) analyses of the lipophilic emulsifiers suggested that the melting trend of the emulsifier is strongly related to the induction period.

Effects of water-emulsified fuel on a diesel engine generator's thermal efficiency and exhaust.

PubMed

Syu, Jin-Yuan; Chang, Yuan-Yi; Tseng, Chao-Heng; Yan, Yeou-Lih; Chang, Yu-Min; Chen, Chih-Chieh; Lin, Wen-Yinn

2014-08-01

Water-emulsified diesel has proven itself as a technically sufficient improvement fuel to improve diesel engine fuel combustion emissions and engine performance. However, it has seldom been used in light-duty diesel engines. Therefore, this paper focuses on an investigation into the thermal efficiency and pollution emission analysis of a light-duty diesel engine generator fueled with different water content emulsified diesel fuels (WD, including WD-0, WD-5, WD-10, and WD-15). In this study, nitric oxide, carbon monoxide, hydrocarbons, and carbon dioxide were analyzed by a vehicle emission gas analyzer and the particle size and number concentration were measured by an electrical low-pressure impactor. In addition, engine loading and fuel consumption were also measured to calculate the thermal efficiency. Measurement results suggested that water-emulsified diesel was useful to improve the thermal efficiency and the exhaust emission of a diesel engine. Obviously, the thermal efficiency was increased about 1.2 to 19.9%. In addition, water-emulsified diesel leads to a significant reduction of nitric oxide emission (less by about 18.3 to 45.4%). However the particle number concentration emission might be increased if the loading of the generator becomes lower than or equal to 1800 W. In addition, exhaust particle size distributions were shifted toward larger particles at high loading. The consequence of this research proposed that the water-emulsified diesel was useful to improve the engine performance and some of exhaust emissions, especially the NO emission reduction. Implications: The accumulated test results provide a good basis to resolve the corresponding pollutants emitted from a light-duty diesel engine generator. By measuring and analyzing transforms of exhaust pollutant from this engine generator, the effects of water-emulsified diesel fuel and loading on emission characteristics might be more clear. Understanding reduction of pollutant emissions during the use

Enhancement of emulsifier production by Curvularia lunata in cadmium, zinc and lead presence.

PubMed

Paraszkiewicz, Katarzyna; Frycie, Aleksandra; Słaba, Mirosława; Długoński, Jerzy

2007-10-01

The influence of cadmium, zinc and lead on fungal emulsifier synthesis and on the growth of filamentous fungus Curvularia lunata has been studied. Tolerance to heavy metals established for C. lunata was additionally compared with the sensitivity exhibited by strains of Curvularia tuberculata and Paecilomyces marquandii-fungi which do not secrete compounds of emulsifying activity. Although C. lunata, as the only one out of all studied fungi, exhibited the lowest tolerance to heavy metals when grown on a solid medium (in conditions preventing emulsifier synthesis), it manifested the highest tolerance in liquid culture - in conditions allowing exopolymer production. Cadmium, zinc and lead presented in liquid medium up to a concentration of 15 mM had no negative effect on C. lunata growth and stimulated emulsifier synthesis. In the presence of 15 mM of heavy metals, both the emulsifier and 24-h-old growing mycelium exhibited maximum sorption capacities, which were determined as 18.2 +/- 2.67, 156.1 +/- 10.32 mg g(-1) for Cd2+, 22.2 +/- 3.40, 95.2 +/- 14.21 mg g(-1) for Zn2+ and 51.1 +/- 1.85, 230.0 +/- 28.47 mg g(-1) for Pb2+ respectively. The results obtained by us in this work indicate that the emulsifier acts as a protective compound increasing the ability of C. lunata to survive in heavy metal polluted environment. Enhancement of exopolymer synthesis in the presence of Cd2+, Zn2+ and Pb2+ may also suggest, at least to some extent, a metal-specific nature of emulsifier production in C. lunata. Due to accumulation capability and tolerance to heavy metals, C. lunata mycelium surrounded by the emulsifier could be applied for toxic metal removal.

Efficiency of emulsifier-free emulsions and emulsions containing rapeseed lecithin as delivery systems for vectorization and release of coenzyme Q10: physico-chemical properties and in vitro evaluation.

PubMed

Kaci, M; Arab-Tehrany, E; Dostert, G; Desjardins, I; Velot, E; Desobry, S

2016-11-01

To improve the encapsulation and release of coenzyme Q10 (CoQ10), emulsifier-free-emulsions were developed with a new emulsification process using high-frequency ultrasound (HFU) at 1.7MHz. Nano-emulsions containing CoQ10 were prepared with or without rapeseed lecithin as an emulsifier. The emulsions prepared with HFU were compared with an emulsion of CoQ10 containing emulsifier prepared with the same emulsification technique as well as with emulsions prepared with low-frequency ultrasound coupled with high-pressure homogenization (LFU+HPH). The physico-chemical properties of the emulsions were determined by average droplet size measurement with nano-droplet tracking analysis, droplet surface charge with ζ potential measurement, surface tension and rheological behaviour. Emulsions made by LFU+HPH with an emulsifier showed lower droplet sizes due to cavitation generated by the HFU process. Surface tension results showed that there was no significant difference between emulsions containing lecithin emulsifier regardless of the preparation process or the inclusion of CoQ10. In vitro biocompatibility tests were performed on human mesenchymal stem cells in order to show the cytotoxicity of various formulations and the efficiency of CoQ10-loaded emulsions. In vitro tests proved that the vectors were not toxic. Furthermore, CoQ10 facilitated a high rate of cell proliferation and metabolic activity especially when in an emulsifier-free formulation. Copyright © 2016 Elsevier B.V. All rights reserved.

Emulsifier of Arthrobacter RAG-1: specificity of hydrocarbon substrate.

PubMed Central

Rosenberg, E; Perry, A; Gibson, D T; Gutnick, D L

1979-01-01

The purified extracellular emulsifying factor produced by Arthrobacter RAG-1 (EF-RAG) emulsified light petroleum oil, diesel oil, and a variety of crude oils and gas oils. Although kerosine and gasoline were emulsified poorly by EF-RAG, they were converted into good substrates for emulsification by addition of aromatic compounds, such as 2-methylnaphthalene. Neither aromatic nor aliphatic fractions of crude oil were emulsified by EF-RAG; however, mixtures containing both fractions were emulsified. Pure aliphatic or aromatic hydrocarbons were emulsified poorly by EF-RAG. Binary mixtures containing an aliphatic and an aromatic hydrocarbon, however, were excellent substrates for EF-RAG-induced emulsification. Of a variety of alkylcyclohexane and alkylbenzene derivatives tested, only hexyl- or heptylbenzene and octyl- or decylcyclohexane were effectively emulsified by EF-RAG. These data indicate that for EF-RAG to induce emulsification of hydrocarbons in water, the hydrocarbon substrate must contain both aliphatic and cyclic components. With binary mixtures of methylnaphthalene and hexadecane, maximum emulsion was obtained with 25% hexadecane. PMID:453821

Effect of House Cricket (Acheta domesticus) Flour Addition on Physicochemical and Textural Properties of Meat Emulsion Under Various Formulations.

PubMed

Kim, Hyun-Wook; Setyabrata, Derico; Lee, YongJae; Jones, Owen G; Kim, Yuan H Brad

2017-12-01

The objective of this study was to determine the effect of house cricket (Acheta domesticus) flour addition on physicochemical and textural properties of meat emulsion under various formulations. As an initial marker of functionality, protein solubility, water absorption, emulsifying capacity, and gel formation ability of house cricket flour were determined at pH (2 to 10) and NaCl concentrations (0 to 2.10 M). Control emulsion was formulated with 60% lean pork, 20% back fat, and 20% ice. Six treatment emulsions were prepared with replacement of lean pork and/or back fat portions with spray-dried house cricket flour at 5% and 10% levels, based on a total sample weight. The protein solubility of house cricket flour (67 g protein/100 g) was significantly altered depending upon pH (P < 0.0001) and NaCl concentration (P = 0.0421). Similar water absorption capacity, emulsifying capacity, and gel formation ability of house cricket flour were found between 0 and 2.10 M NaCl concentration (P > 0.05). The replacement of lean meat/fat portion with house cricket flour within 10% level could fortify protein and some micronutrients (phosphorus, potassium, and magnesium) in meat emulsion, without negative impacts on cooking yield and textural properties. Our results suggest that house cricket flour can be used as an effective nonmeat functional ingredient to manufacture emulsified meat products. To better utilize house cricket flour as a food ingredient in wide application, understanding its technological properties in various pH, and ionic strength conditions is a pivotal step. Protein solubility of house cricket flour would be considerably affected by the varying pH and NaCl concentrations of applied conventional foods. In the case of meat emulsion, within 10% lean meat and/or fat portions could be successfully substituted with house cricket flour without detectable adverse impacts on technological properties associated with cooking yield and instrumental analysis of texture

Comparison of high-resolution ultrasonic resonator technology and Raman spectroscopy as novel process analytical tools for drug quantification in self-emulsifying drug delivery systems.

PubMed

Stillhart, Cordula; Kuentz, Martin

2012-02-05

Self-emulsifying drug delivery systems (SEDDS) are complex mixtures in which drug quantification can become a challenging task. Thus, a general need exists for novel analytical methods and a particular interest lies in techniques with the potential for process monitoring. This article compares Raman spectroscopy with high-resolution ultrasonic resonator technology (URT) for drug quantification in SEDDS. The model drugs fenofibrate, indomethacin, and probucol were quantitatively assayed in different self-emulsifying formulations. We measured ultrasound velocity and attenuation in the bulk formulation containing drug at different concentrations. The formulations were also studied by Raman spectroscopy. We used both, an in-line immersion probe for the bulk formulation and a multi-fiber sensor for measuring through hard-gelatin capsules that were filled with SEDDS. Each method was assessed by calculating the relative standard error of prediction (RSEP) as well as the limit of quantification (LOQ) and the mean recovery. Raman spectroscopy led to excellent calibration models for the bulk formulation as well as the capsules. The RSEP depended on the SEDDS type with values of 1.5-3.8%, while LOQ was between 0.04 and 0.35% (w/w) for drug quantification in the bulk. Similarly, the analysis of the capsules led to RSEP of 1.9-6.5% and LOQ of 0.01-0.41% (w/w). On the other hand, ultrasound attenuation resulted in RSEP of 2.3-4.4% and LOQ of 0.1-0.6% (w/w). Moreover, ultrasound velocity provided an interesting analytical response in cases where the drug strongly affected the density or compressibility of the SEDDS. We conclude that ultrasonic resonator technology and Raman spectroscopy constitute suitable methods for drug quantification in SEDDS, which is promising for their use as process analytical technologies. Copyright © 2011 Elsevier B.V. All rights reserved.

Effect of protein concentrates, emulsifiers on textural and sensory characteristics of gluten free cookies and its immunochemical validation.

PubMed

Sarabhai, Swati; Indrani, D; Vijaykrishnaraj, M; Milind; Arun Kumar, V; Prabhasankar, P

2015-06-01

The effect of 5, 7.5 and 10 % protein concentrates namely soya protein isolate (SPI), whey protein concentrate (WPC) and addition of 0.5 % emulsifiers such as glycerol monostearate (GMS), sodium stearoyl- 2- lactylate (SSL) and lecithin (LEC) on the rheological, sensory and textural characteristics of cookies with rice flour and its immunochemical validation was studied. The results showed that the use of 7.5 % SPI/WPC along with GMS significantly improved the quality characteristics of cookies with rice flour. Dot-Blot and Western-blot studies of cookies with 7.5 % of SPI or WPC confirmed that the anti-gliadin did not recognize these proteins. Carry- through process using ELISA kit confirmed that gluten was within the permissible limit in all the stages of processing and hence these cookies can be consumed by people suffering from celiac disease.

7 CFR 58.722 - Emulsifying agents.

Code of Federal Regulations, 2010 CFR

2010-01-01

... Specifications for Dairy Plants Approved for USDA Inspection and Grading Service 1 Quality Specifications for Raw Material § 58.722 Emulsifying agents. Emulsifying agents shall be those permitted by the Food and Drug Administration for the specific pasteurized process cheese product, and shall be free from extraneous material...

7 CFR 58.722 - Emulsifying agents.

Code of Federal Regulations, 2011 CFR

2011-01-01

... Specifications for Dairy Plants Approved for USDA Inspection and Grading Service 1 Quality Specifications for Raw Material § 58.722 Emulsifying agents. Emulsifying agents shall be those permitted by the Food and Drug Administration for the specific pasteurized process cheese product, and shall be free from extraneous material...

Grape seed and apple tannins: emulsifying and antioxidant properties.

PubMed

Figueroa-Espinoza, Maria Cruz; Zafimahova, Andrea; Alvarado, Pedro G Maldonado; Dubreucq, Eric; Poncet-Legrand, Céline

2015-07-01

Tannins are natural antioxidants found in plant-based foods and beverages, whose amphiphilic nature could be useful to both stabilize emulsions and protect unsaturated lipids from oxidation. In this paper, the use of tannins as antioxidant emulsifiers was studied. The main parameters influencing the stability of emulsions (i.e. tannins structure and concentration, aqueous phase pH, and ionic strength) were identified and optimized. Oil in water emulsions stabilized with tannins were compared with those stabilized with two commercial emulsifying agents, poly(vinyl alcohol) (PVA) and polyoxyethylene hydrogenated castor oil. In optimized conditions, the condensed tannins allowed to obtain a stability equivalent to that of PVA. Tannins presented good antioxidant activity in oil in water emulsion, as measured by the conjugated autoxidizable triene (CAT) assay. Copyright © 2015 Elsevier Ltd. All rights reserved.

Physical parameters of chlorphenamine maleate suppositories and its release as a function of particle size, concentration and nature of the base.

PubMed

el-Din, E N; Mursi, N M; Elbary, A A; Foda, N

1977-01-01

Suppositories of chlorphenamine maleate were formulated. The influence of particle size and percentage concentration of chlorphenamine maleate on the physical standards of its suppositories as well as the release of the drug from oily base (cacao butter), water-soluble base (carbowax) and emulsifying base (Witepsol) has been investigated.

Enhance the anti-microorganism activity of cinnamon oil by xanthan gum as emulsifying agent

NASA Astrophysics Data System (ADS)

Lieu, Dong M.; Dang, Thuy T. K.; Nguyen, Huong T.

2018-04-01

The aim of this study was to evaluate the effect of emulsifying agents (tween 20, DMSO (Dimethyl Sulfoxide) and xanthan gum) to inhibit Escherichia coli; Staphylococcus aureus; Saccharomyces cerevisiae and Aspergillus niger by cinnamon oil (Cinnamomum Cassia). Cinnamon oil was added in the emulsifying agents independently: tween 20 (0.3% v/v). DMSO (0.3% v/v) and xanthan gum (0.3% w/v) at different concentrations and evaluated their anti-microorganism activity by agar disk diffusion, mycelial growth inhibition and growth inhibition in liquid phase. The result indicated that, cinnamon oil diluted in different emulsifying agents showed the difference of the anti-microorganism activity, in which DMSO showed the lowest result. Xanthan gum and tween 20 show good stable emulsion. The anti-microorganism effect of cinnamon oil in tween 20 and xanthan gum was not significant difference. However, cinnamon oil in xanthan gum showed anti-microorganism activity better than tween 20 at low concentration in agar disk diffusion. This suggests that, cinnamon oil could be encapsulated by xanthan gum to enhance the anti-microorganism activity.

Application of D-optimal experimental design method to optimize the formulation of O/W cosmetic emulsions.

PubMed

Djuris, J; Vasiljevic, D; Jokic, S; Ibric, S

2014-02-01

This study investigates the application of D-optimal mixture experimental design in optimization of O/W cosmetic emulsions. Cetearyl glucoside was used as a natural, biodegradable non-ionic emulsifier in the relatively low concentration (1%), and the mixture of co-emulsifiers (stearic acid, cetyl alcohol, stearyl alcohol and glyceryl stearate) was used to stabilize the formulations. To determine the optimal composition of co-emulsifiers mixture, D-optimal mixture experimental design was used. Prepared emulsions were characterized with rheological measurements, centrifugation test, specific conductivity and pH value measurements. All prepared samples appeared as white and homogenous creams, except for one homogenous and viscous lotion co-stabilized by stearic acid alone. Centrifugation testing revealed some phase separation only in the case of sample co-stabilized using glyceryl stearate alone. The obtained pH values indicated that all samples expressed mild acid value acceptable for cosmetic preparations. Specific conductivity values are attributed to the multiple phases O/W emulsions with high percentages of fixed water. Results of the rheological measurements have shown that the investigated samples exhibited non-Newtonian thixotropic behaviour. To determine the influence of each of the co-emulsifiers on emulsions properties, the obtained results were evaluated by the means of statistical analysis (ANOVA test). On the basis of comparison of statistical parameters for each of the studied responses, mixture reduced quadratic model was selected over the linear model implying that interactions between co-emulsifiers play the significant role in overall influence of co-emulsifiers on emulsions properties. Glyceryl stearate was found to be the dominant co-emulsifier affecting emulsions properties. Interactions between the glyceryl stearate and other co-emulsifiers were also found to significantly influence emulsions properties. These findings are especially important

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.

Studies on gum of Moringa oleifera for its emulsifying properties.

PubMed

Panda, Dibya Sundar

2014-04-01

Emulsion has been a form of presenting water insoluble substances for a long period of time. Now a day, it has been a way of presenting various intravenous additives and diagnostic agents in X-ray examinations. Various substances can be used as emulsifying agent, which can be operationally defined as a stabilizer of the droplets formed of the internal phase. Gum from Moringa oleifera was evaluated for its emulsifying properties. Castor oil emulsions 30 percent (o/w), containing 2 to 4% Moringa oleifera gum was prepared. Emulsions containing equivalent concentration of acacia were also prepared for comparison. All the emulsions prepared were stored at room temperature and studied for stability at various time intervals for 8 weeks. The prepared emulsions were evaluated for creaming rate, globule size and rate of coalescence. 23 factorial design was chosen to investigate the effects of centrifugation, pH, temperature changes and electrolytes on the creaming rate and globule size. The results of the investigations show that the gum of Moringa oleifera possesses better emulsifying properties as compared to gum acacia. Gum of Moringa oleifera could be used in pharmaceutical and non-pharmaceutical preparation.

Effect of emulsifier type and concentration, aqueous phase volume and wax ratio on physical, material and mechanical properties of water in oil lipsticks.

PubMed

Beri, A; Norton, J E; Norton, I T

2013-12-01

Water-in-oil emulsions in lipsticks could have the potential to improve moisturizing properties and deliver hydrophilic molecules to the lips. The aims of this work were (i) to investigate the effect of emulsifier type (polymer vs. monomer, and saturated vs. unsaturated chain) and concentration on droplet size and (ii) to investigate the effect of wax ratio (carnauba wax, microcrystalline wax, paraffin wax and performalene) and aqueous phase volume on material properties (Young's modulus, point of fracture, elastic modulus and viscous modulus). Emulsion formation was achieved using a high shear mixer. Results showed that the saturated nature of the emulsifier had very little effect on droplet size, neither did the use of an emulsifier with a larger head group (droplet size ~18-25 μm). Polyglycerol polyricinoleate (PGPR) resulted in emulsions with the smallest droplets (~3-5 μm), as expected from previous studies that show that it produces a thick elastic interface. The results also showed that both Young's modulus and point of fracture increase with increasing percentage of carnauba wax (following a power law dependency of 3), but decrease with increasing percentage of microcrystalline wax, suggesting that the carnauba wax is included in the overall wax network formed by the saturated components, whereas the microcrystalline wax forms irregular crystals that disrupt the overall wax crystal network. Young's modulus, elastic modulus and viscous modulus all decrease with increasing aqueous phase volume in the emulsions, although the slope of the decrease in elastic and viscous moduli is dependent on the addition of solid wax, as a result of strengthening the network. This work suggests the potential use for emulsions in lipstick applications, particularly when PGPR is used as an emulsifier, and with the addition of solid wax, as it increases network strength. © 2013 Society of Cosmetic Scientists and the Société Française de Cosmétologie.

Understanding the effect of emulsifiers on bread aeration during breadmaking.

PubMed

Garzón, Raquel; Hernando, Isabel; Llorca, Empar; Rosell, Cristina M

2018-04-24

Much research has been done to explain the action of emulsifiers during breadmaking, but there is still plenty unknown to elucidate their functionality despite their diverse chemical structure. The aim of the present study was to provide some light on the role of emulsifiers on air incorporation into the dough and gas bubbles progress during baking and their relationship with bread features. Emulsifiers like diacetyl tartaric acid ester of monoglycerides (DATEM), sodium stearoyl lactylate (SSL), distilled monoglyceride (DMG-45 and DMG-75), lecithin and polyglycerol esters of fatty acids (PGEF) were tested in very hydrated doughs. Emulsifiers increase the maximum dough volume during proofing. Emulsifiers increase the number of bubbles incorporated during mixing, observing higher number of bubbles, particularly with PGEF. Major changes in dough occurred at 70 K when bubble size augmented, becoming more heterogeneous. DMG-75 produced the biggest bubbles. As a consequence, emulsifiers tend to increase the number of gas cells with lower size in the bread crumb, but led to greater crumb firmness, which suggested different interactions between emulsifiers and gluten, affecting protein polymerization during baking. The progress of the bubbles during baking allowed the differentiation of emulsifiers, which could explain their performance in breadmaking. © 2018 Society of Chemical Industry. © 2018 Society of Chemical Industry.

Measuring the emulsification dynamics and stability of self-emulsifying drug delivery systems.

PubMed

Vasconcelos, Teófilo; Marques, Sara; Sarmento, Bruno

2018-02-01

Self-emulsifying drug delivery systems (SEDDS) are one of the most promising technologies in the drug delivery field, particularly for addressing solubility and bioavailability issues of drugs. The development of these drug carriers excessively relies in visual observations and indirect determinations. The present manuscript intended to describe a method able to measure the emulsification of SEDDS, both micro and nano-emulsions, able to measure the droplet size and to evaluate the physical stability of these formulations. Additionally, a new process to evaluate the physical stability of SEDDS after emulsification was also proposed, based on a cycle of mechanical stress followed by a resting period. The use of a multiparameter continuous evaluation during the emulsification process and stability was of upmost value to understand SEDDS emulsification process. Based on this method, SEDDS were classified as fast and slow emulsifiers. Moreover, emulsification process and stabilization of emulsion was subject of several considerations regarding the composition of SEDDS as major factor that affects stability to physical stress and the use of multicomponent with different properties to develop a stable and robust SEDDS formulation. Drug loading level is herein suggested to impact droplets size of SEDDS after dispersion and SEDDS stability to stress conditions. The proposed protocol allows an online measurement of SEDDS droplet size during emulsification and a rationale selection of excipients based on its emulsification and stabilization performance. Copyright © 2017. Published by Elsevier B.V.

Acacia gum as modifier of thermal stability, solubility and emulsifying properties of α-lactalbumin.

PubMed

de Oliveira, Fabíola Cristina; Dos Reis Coimbra, Jane Sélia; de Oliveira, Eduardo Basílio; Rodrigues, Marina Quadrio Raposo Branco; Sabioni, Rachel Campos; de Souza, Bartolomeu Warlene Silva; Santos, Igor José Boggione

2015-03-30

Protein-polysaccharide conjugates often display improved techno-functional properties when compared to their individual involved biomolecules. α-Lactalbumin:acacia gum (α-la:AG) conjugates were prepared via Maillard reaction by the dry-heating method. Conjugate formation was confirmed using results of absorbance, o-phthalaldehyde test, sodium dodecyl sulfate-polyacrilamide gel electrophoresis (SDS-PAGE) and size exclusion chromatography. Techno-functional properties (emulsifying characteristics, solubility, and thermal stability) were evaluated for α-la, α-la/AG mixtures and α-la:AG conjugates. Conjugate thermal stability was improved compared to pure α-la treated at the same conditions of conjugate formation. Response surface methodology was used to establish models to predict solubility and emulsifying activity as functions of the salt concentration, pH and reaction time. α-la:AG conjugate solubility is affected in a complex manner by the three factors analyzed. Emulsifying activity index (EAI) of α-la is significantly affected by pH, while the α-la:AG EAI is affected by the three analyzed factors. Both solubility and EAI are maximized with pH 8.0, NaCl concentration of 0.3 mol L(-1) and two days of Maillard reaction. Copyright © 2014 Elsevier Ltd. All rights reserved.

Evaluation of new creosote formulations after extended exposures in fungal cellar tests and field plot tests

Treesearch

Douglas M. Crawford; Patricia K. Lebow; Rodney DeGroot

2000-01-01

This paper compares two new formulations of creosote and one pigment-emulsified creosote (PEC) with a formulation of creosote that met requirements of the AWPA standard P1/P13. Two softwood and two hardwood species were treated to four retention levels with each formulation. The evaluation of the four creosote formulations was done using (1) soil-block tests, (2)...

Filling of High-Concentration Monoclonal Antibody Formulations into Pre-filled Syringes: Investigating Formulation-Nozzle Interactions To Minimize Nozzle Clogging.

PubMed

Shieu, Wendy; Stauch, Oliver B; Maa, Yuh-Fun

2015-01-01

Syringe filling of high-concentration/viscosity monoclonal antibody formulations is a complex process that is not fully understood. This study, which builds on a previous investigation that used a bench-top syringe filling unit to examine formulation drying at the filling nozzle tip and subsequent nozzle clogging, further explores the impact of formulation-nozzle material interactions on formulation drying and nozzle clogging. Syringe-filling nozzles made of glass, stainless steel, or plastic (polypropylene, silicone, and Teflon®), which represent a full range of materials with hydrophilic and hydrophobic properties as quantified by contact angle measurements, were used to fill liquids of different viscosity, including a high-concentration monoclonal antibody formulation. Compared with hydrophilic nozzles, hydrophobic nozzles offered two unique features that discouraged formulation drying and nozzle clogging: (1) the liquid formulation is more likely to be withdrawn into the hydrophobic nozzle under the same suck-back conditions, and (2) the residual liquid film left on the nozzle wall when using high suck-back settings settles to form a liquid plug away from the hydrophobic nozzle tip. Making the tip of the nozzle hydrophobic (silicone-coating on glass and Teflon-coating stainless steel) could achieve the same suck-back performance as plastic nozzles. This study demonstrated that using hydrophobic nozzles are most effective in reducing the risk of nozzle clogging by drying of high-concentration monoclonal antibody formulation during extended nozzle idle time in a large-scale filling facility and environment. Syringe filling is a well-established manufacturing process and has been implemented by numerous contract manufacturing organizations and biopharmaceutical companies. However, its technical details and associated critical process parameters are rarely published. Information on high-concentration/viscosity formulation filling is particularly lacking. This

Impact of Lipid Components and Emulsifiers on Plant Sterols Bioaccessibility from Milk-Based Fruit Beverages.

PubMed

Alvarez-Sala, Andrea; Garcia-Llatas, Guadalupe; Cilla, Antonio; Barberá, Reyes; Sánchez-Siles, Luis Manuel; Lagarda, María Jesús

2016-07-20

Sterol bioaccessibility (BA) of three plant sterol (PS)-enriched milk-based fruit beverages (MFb) with different fat contents (1.1-2.4%), lipid sources (animal or vegetable), and without or with emulsifiers (whey proteins enriched with milk fat globule membrane (MFGM) or soy lecithin) was evaluated after simulated gastrointestinal digestion. The BA of total PS followed the order 31.4% (MFbM containing milk fat and whey proteins enriched with MFGM) = 28.2% (MFbO containing extra virgin olive oil and soy lecithin) > 8.7% (MFb without fat addition). Total and individual PS content in the bioaccessible fractions followed the order MFbM > MFbO > MFb. Consequently, formulation with MFGM is proposed in beverages of this kind to ensure optimum bioavailability of PS. Our results suggest that the BA of PS is influenced by the type and quantity of fat and the emulsifier type involved.

Potential of L-fucose isolated from Brown Seaweeds as Promising Natural Emulsifier compare to Carboxymethyl Cellulose (CMC)

NASA Astrophysics Data System (ADS)

Al-Baarri, A. N.; Legowo, A. M.; Widayat; Abduh, S. B. M.; Lestari, F. P.; Desnasari, D.; Santoso, I. P. M.

2018-02-01

L-fucose has been understood as sulfated polysaccharides and it could be extracted and fractionated from brown algae. These polysaccharides contains carbohydrate, sulfate, and protein that may be used as emulsifier. This research was aimed to study the emulsification properties of L-fucose through the determination of total dissolved solids (TDS), color CIE L*a*b* and stability of oil-in-water emulsion. As much as 0.5% of high concentrated L-fucose and 0.5% of carboxymethyl cellulose (CMC) were used as emulsifier in a 10% (v/v) oil-in-water (O/W) emulsion. The emulsifier was added to O/W emulsions and then heated at 72°C. Result of stability emulsion and TDS showed that L-fucose was comparable to the CMC but remarkable changed the color of O/W emulsion. Heating process significantly reduced the stability O/W emulsion when L-fucose was applied. As conclusion, L-fucose might be used as natural emulsifier in O/W emulsion but in the low heat treatment of food processing. This study may provide valuable information for utilizing natural emulsifier from abundant resources from nature.

Effect of type of emulsifiers and antioxidants on oxidative stability, colour and fatty acid profile of low-fat beef burgers enriched with unsaturated fatty acids and phytosterols.

PubMed

Pennisi Forell, S C; Ranalli, N; Zaritzky, N E; Andrés, S C; Califano, A N

2010-10-01

Low-fat beef burgers were formulated using fresh lean meat, 9.9% oleic sunflower oil and 0.1% deodorized fish oil to obtain a product enriched in unsaturated fatty acids. The effect of two emulsifiers (whey proteins or egg white) and natural antioxidants (tocopherols and/or oregano-rosemary), as well as the influence of frozen storage on the oxidative stability, colour, and fatty acid (FA) profile was determined on the cooked products. Whey proteins protected better against oxidation than egg white, and tocopherols demonstrated an adequate antioxidant effect in formulations with egg white. For all the formulations the unsaturated/saturated FA ratio was higher than 5.8, showing a good lipid balance in the products. The consumption of 100g of the cooked product would provide 6% of the recommended daily intake of phytosterols suggested to decrease cholesterol and the risk of heart disease. Formulated low-fat burgers with pre-emulsified oils and phytosterols could be considered to be potentially functional foodstuffs. Copyright (c) 2010 The American Meat Science Association. Published by Elsevier Ltd. All rights reserved.

Multi‐criteria manufacturability indices for ranking high‐concentration monoclonal antibody formulations

PubMed Central

Velayudhan, Ajoy; Thornhill, Nina F.

2017-01-01

ABSTRACT The need for high‐concentration formulations for subcutaneous delivery of therapeutic monoclonal antibodies (mAbs) can present manufacturability challenges for the final ultrafiltration/diafiltration (UF/DF) step. Viscosity levels and the propensity to aggregate are key considerations for high‐concentration formulations. This work presents novel frameworks for deriving a set of manufacturability indices related to viscosity and thermostability to rank high‐concentration mAb formulation conditions in terms of their ease of manufacture. This is illustrated by analyzing published high‐throughput biophysical screening data that explores the influence of different formulation conditions (pH, ions, and excipients) on the solution viscosity and product thermostability. A decision tree classification method, CART (Classification and Regression Tree) is used to identify the critical formulation conditions that influence the viscosity and thermostability. In this work, three different multi‐criteria data analysis frameworks were investigated to derive manufacturability indices from analysis of the stress maps and the process conditions experienced in the final UF/DF step. Polynomial regression techniques were used to transform the experimental data into a set of stress maps that show viscosity and thermostability as functions of the formulation conditions. A mathematical filtrate flux model was used to capture the time profiles of protein concentration and flux decay behavior during UF/DF. Multi‐criteria decision‐making analysis was used to identify the optimal formulation conditions that minimize the potential for both viscosity and aggregation issues during UF/DF. Biotechnol. Bioeng. 2017;114: 2043–2056. © 2017 The Authors. Biotechnology and Bioengineering Published by Wiley Perodicals, Inc. PMID:28464235

Residual determination and risk assessment of buprofezin in plum (Prunus domestica) grown in open-field conditions following the application of three different formulations.

PubMed

Kabir, Md Humayun; Abd El-Aty, A M; Kim, Sung-Woo; Lee, Han Sol; Rahman, Md Musfiqur; Lee, Young-Jun; Chung, Hyung Suk; Lieu, Truong; Choi, Jeong-Heui; Shin, Ho-Chul; Im, Geon-Jae; Hong, Su Myeong; Shim, Jae-Han

2016-11-01

This study was conducted to characterize the residual level and perform a risk assessment on buprofezin formulated as an emulsifiable concentrate, wettable powder, and suspension concentrate over various treatment schedules in plum (Prunus domestica). The samples were extracted with an AOAC quick, easy, cheap, effective, rugged, and safe, 'QuEChERS', method after major modifications. As intrinsic interferences were observed in blank plum samples following dispersive-solid phase extraction (consisting of primary secondary amine and C 18 sorbents), amino cartridges were used for solid-phase extraction. Analysis was carried out using liquid chromatography with diode array detection and confirmed by liquid chromatography-tandem mass spectrometry. The method showed excellent linearity with determination coefficient (R 2  = 1) and satisfactory recoveries (at two spiking levels, 0.5 and 2.5 mg/kg) between 90.98 and 94.74% with relative standard deviation (RSD) ≤8%. The limit of quantification (0.05 mg/kg) was considerably lower than the maximum residue limit (2 mg/kg) set by the Codex Alimentarius. Absolute residue levels for emulsifiable concentrates were highest, perhaps owing to the dilution rate and adjuvant. Notably, all formulation residues were lower than the maximum residue limit, and safety data proved that the fruits are safe for consumers. Copyright © 2016 John Wiley & Sons, Ltd. Copyright © 2016 John Wiley & Sons, Ltd.

Improving halva quality with dietary fibres of sesame seed coats and date pulp, enriched with emulsifier.

PubMed

Elleuch, Mohamed; Bedigian, Dorothea; Maazoun, Bouthaina; Besbes, Souhail; Blecker, Christophe; Attia, Hamadi

2014-02-15

Supplementation of halva with waste products of manufacturing, for example defatted sesame seed coats (testae) and date fibre concentrate, can improve its nutritional and organoleptic qualities. These constituents provide high fibre content and technological potential for retaining water and fat. Standard halva supplemented with date fibre concentrate, defatted sesame testae and emulsifier was evaluated for oil separation, texture and colour changes, sensory qualities and acceptability to a taste panel. Addition of both fibres with an emulsifier, improved emulsion stability and increased the hardness of halva significantly. The functional properties of sesame testae and date fibres promote nutrition and health, supplying polyphenol antioxidants and laxative benefits. Copyright © 2013 Elsevier Ltd. All rights reserved.

Field Evaluation of a Kudzu/Cottonseed Oil Formulation on the Persistence of the Beet Armyworm Nucleopolyhedrovirus

USDA-ARS?s Scientific Manuscript database

A plant extract (kudzu) was tested as a UV protectant for SeMNPV, with and without the addition of an oil/emulsifier (cottonseed oil/lecithin) formulation. Aqueous and oil emulsion formulations of the beet armyworm, Spodoptera exigua (Hübner), nucleopolyhedrovirus SeMNPV were applied to collards an...

Enhancement of oral bioavailability of atorvastatin calcium by self-emulsifying drug delivery systems (SEDDS).

PubMed

Kadu, Pawan J; Kushare, Sachin S; Thacker, Dhaval D; Gattani, Surendra G

2011-02-01

The aim of the present study was to formulate a self-emulsifying drug delivery system of atorvastatin calcium and its characterization including in vitro and in vivo potential. The solubility of atorvastatin calcium was determined in various vehicles such as Captex 355, Captex 355 EP/NF, Ethyl oleate, Capmul MCM, Capmul PG-8, Gelucire 44/14, Tween 80, Tween 20, and PEG 400. Pseudoternary phase diagrams were plotted on the basis of solubility data of drug in various components to evaluate the microemulsification region. Formulation development and screening was carried out based on results obtained from phase diagrams and characteristics of resultant microemulsion. Prepared formulations were tested for microemulsifying properties and evaluated for clarity, precipitation, viscosity determination, drug content and in vitro dissolution. The optimized formulation further evaluated for particle size distribution, zeta potential, stability studies and in vivo potential. In vivo performance of the optimized formulation was evaluated using a Triton-induced hypercholesterolemia model in male Albino Wistar rats. The formulation significantly reduced serum lipid levels as compared with atorvastatin calcium. Thus studies illustrated the potential use for the delivery of hydrophobic drug such as atorvastatin calcium by oral route.

Multi-criteria manufacturability indices for ranking high-concentration monoclonal antibody formulations.

PubMed

Yang, Yang; Velayudhan, Ajoy; Thornhill, Nina F; Farid, Suzanne S

2017-09-01

The need for high-concentration formulations for subcutaneous delivery of therapeutic monoclonal antibodies (mAbs) can present manufacturability challenges for the final ultrafiltration/diafiltration (UF/DF) step. Viscosity levels and the propensity to aggregate are key considerations for high-concentration formulations. This work presents novel frameworks for deriving a set of manufacturability indices related to viscosity and thermostability to rank high-concentration mAb formulation conditions in terms of their ease of manufacture. This is illustrated by analyzing published high-throughput biophysical screening data that explores the influence of different formulation conditions (pH, ions, and excipients) on the solution viscosity and product thermostability. A decision tree classification method, CART (Classification and Regression Tree) is used to identify the critical formulation conditions that influence the viscosity and thermostability. In this work, three different multi-criteria data analysis frameworks were investigated to derive manufacturability indices from analysis of the stress maps and the process conditions experienced in the final UF/DF step. Polynomial regression techniques were used to transform the experimental data into a set of stress maps that show viscosity and thermostability as functions of the formulation conditions. A mathematical filtrate flux model was used to capture the time profiles of protein concentration and flux decay behavior during UF/DF. Multi-criteria decision-making analysis was used to identify the optimal formulation conditions that minimize the potential for both viscosity and aggregation issues during UF/DF. Biotechnol. Bioeng. 2017;114: 2043-2056. © 2017 The Authors. Biotechnology and Bioengineering Published by Wiley Perodicals, Inc. © 2017 The Authors. Biotechnology and Bioengineering Published by Wiley Perodicals, Inc.

Competitive displacement of sodium caseinate by low-molecular-weight emulsifiers and the effects on emulsion texture and rheology.

PubMed

Munk, M B; Larsen, F H; van den Berg, F W J; Knudsen, J C; Andersen, M L

2014-07-29

Low-molecular-weight (LMW) emulsifiers are used to promote controlled destabilization in many dairy-type emulsions in order to obtain stable foams in whippable products. The relation between fat globule aggregation induced by three LMW emulsifiers, lactic acid ester of monoglyceride (LACTEM), saturated monoglyceride (GMS), and unsaturated monoglyceride (GMU) and their effect on interfacial protein displacement was investigated. It was found that protein displacement by LMW emulsifiers was not necessary for fat globule aggregation in emulsions, and conversely fat globule aggregation was not necessarily accompanied by protein displacement. The three LMW emulsifiers had very different effects on emulsions. LACTEM induced shear instability of emulsions, which was accompanied by protein displacement. High stability was characteristic for emulsions with GMS where protein was displaced from the interface. Emulsions containing GMU were semisolid, but only low concentrations of protein were detected in the separated serum phase. The effects of LACTEM, GMS, and GMU may be explained by three different mechanisms involving formation of interfacial α-gel, pickering stabilization and increased exposure of bound casein to the water phase. The latter may facilitate partial coalescence. Stabilizing hydrocolloids did not have any effect on the LMW emulsifiers' ability to induce protein displacement.

Antioxidant Properties of Astaxanthin in Oil-in-Water Emulsions with Differently-Charged Emulsifiers Under Chlorophyll Photosensitization.

PubMed

Yi, BoRa; Kim, Mi-Ja; Lee, JaeHwan

2018-03-01

The antioxidative or prooxidative properties of astaxanthin at the concentrations of 0, 10, and 100 μM were determined in oil-in-water (O/W) emulsions containing neutral, anionic, and cationic emulsifiers, which was Tween 20, sodium dodecyl sulfate, cetyltrimethylammonium bromide (CTAB), respectively, under chlorophyll photosensitization. The oxidative parameters and headspace volatiles were analyzed in O/W emulsions. In the 24 h period of visible light irradiation, 100 μM of astaxanthin acted as an antioxidant in O/W emulsions containing neutral and anionic emulsifiers. However, astaxanthin in O/W emulsions with a cationic emulsifier was neither an antioxidant nor a prooxidant. The profiles of volatile compounds showed that astaxanthin served as a singlet oxygen quencher in O/W emulsions containing neutral and anionic emulsifiers. However, in O/W emulsion with a cationic emulsifier, astaxanthin was neither a singlet oxygen quencher nor a free radical scavenger because prooxidant properties of CTAB overwhelmed the antioxidant effects of astaxanthin. Therefore, the antioxidant properties of astaxanthin were influenced by the emulsifier charges in O/W emulsions. Astaxanthin is a lipid-soluble pigment and has antioxidant, anticancer, and anti-inflammatory properties and beneficial effects on cardiovascular diseases. Many lipid-based foods are displayed on the shelves in the markets under fluorescent light. The addition of astaxanthin can extend the shelf life of O/W emulsion type foods such as beverage and dressing products under visible light irradiation. Also, oxidative stability in emulsion type foods containing astaxanthin rich natural ingredients can be predicted. © 2018 Institute of Food Technologists®.

Impact of carboxymethyl cellulose (CMC) and microcrystalline cellulose (MCC) on functional characteristics of emulsified sausages.

PubMed

Schuh, Valerie; Allard, Karin; Herrmann, Kurt; Gibis, Monika; Kohlus, Reinhard; Weiss, Jochen

2013-02-01

Inclusion of fibers, such as carboxymethyl cellulose (CMC) and microcrystalline cellulose (MCC), at the expense of fat or protein in meat batters could be used to produce healthier sausages while lowering production costs. To study the impact of CMC/MCC on structural/functional characteristics of emulsified sausages, standard-fat Lyoner-style sausages were formulated with CMC/MCC at concentrations of 0.3-2.0%. Methods of analysis included rheology, water binding capacity (WBC), texture measurements, and Confocal Laser Scanning Microscopy (CLSM). WBC, texture measurements, and rheology all indicated that addition of CMC (>0.7%) led to destabilization of the batter, which upon heating could no longer be converted into a coherent protein network, a fact that was also revealed in CLSM images. In contrast, MCC was highly compatible with the matrix and improved firmness (1405-1651N/100g) with increasing concentration compared to control (1381N/100g) while keeping WBC (4.6-5.9%) with <2% MCC at the level of the control (4.8%). Results were discussed in terms of molecular interactions of meat proteins with celluloses. Copyright © 2012 Elsevier Ltd. All rights reserved.

Novel cosmetic formulations containing a biosurfactant from Lactobacillus paracasei.

PubMed

Ferreira, A; Vecino, X; Ferreira, D; Cruz, J M; Moldes, A B; Rodrigues, L R

2017-07-01

Cosmetic and personal care products including toothpaste, shampoo, creams, makeup, among others, are usually formulated with petroleum-based surfactants, although in the last years the consume trend for "green" products is inducing the replacement of surface-active agents in these formulations by natural surfactants, so-called biosurfactants. In addition to their surfactant capacity, many biosurfactants can act as good emulsifiers, which is an extra advantage in the preparation of green cosmetic products. In this work, a biosurfactant obtained from Lactobacillus paracasei was used as a stabilizing agent in oil-in-water emulsions containing essential oils and natural antioxidant extract. In the presence of biosurfactant, maximum percentages of emulsion volumes (EV=100%) were observed, with droplets sizes about 199nm. These results were comparable with the ones obtained using sodium dodecyl sulfate (SDS), a synthetic well known surfactant with high emulsify capacity. Moreover, the biosurfactant and emulsions cytotoxicity was evaluated using a mouse fibroblast cell line. Solutions containing 5g/L of biosurfactant presented cell proliferation values of 97%, whereas 0.5g/L of SDS showed a strong inhibitory effect. Overall, the results herein gathered are very promising towards the development of new green cosmetic formulations. Copyright © 2017 Elsevier B.V. All rights reserved.

The role of endogenous lipids in the emulsifying properties of cocoa

NASA Astrophysics Data System (ADS)

Gould, Joanne; Furse, Samuel; Wolf, Bettina

2016-03-01

This paper describes a study in which the emulsifying properties of cocoa material with and without its lipid fraction were explored. This study was motivated by the commercial interest in naturally-occurring particulate emulsifiers as opposed to the chemically modified emulsifying particles presently available for commercial use. The hypothesis was that endogenous lipids from cocoa were responsible for driving the formation of stable oil-in-water (o/w) emulsions. The data presented includes relative quantification of phospholipids from different commercially available cocoa material using 31P NMR spectroscopy and analyses of the emulsifying power of delipidified cocoa material. The commercially available cocoa material comprised several phospholipids, with phosphatidylcholine being the most abundant in all samples. Dispersions of delipidified cocoa material were found to drive the formation of o/w emulsions despite the absence of lipids. We therefore concluded that the emulsifying behaviour of cocoa material is not entirely reliant upon the endogenous lipids. This suggests that cocoa material may have a new and potentially widespread use in industrial food preparation and may inform manufacturing strategies for novel food grade emulsifiers.

Destabilization and Treatment of Emulsified Oils in Wastewaters by Electrocoagulation.

PubMed

Genc, Ayten; Bakirci, Busra

2016-11-01

  In this study, the optimum operating conditions for the treatment of emulsified oils by electrocoagulation were determined depending on droplet stability analysis. Zeta potential measurements were used as the indication of oil droplet charges. In addition, the effects of pH and ionic conductivity on the droplet sizes and surface charges were investigated. The studied emulsified oil droplet sizes were more sensitive to changes in pH rather than salt concentration. The droplets became larger and unstable in alkaline conditions. As the initial pH of wastewaters increased, the oil removal efficiency increased during the electrocoagulation experiments as well. The use of iron or aluminum electrodes resulted in higher removal efficiencies in comparison to stainless steel electrodes. In addition, the energy consumption for aluminum electrodes was much lower than iron electrodes. To obtain 98% oil removal efficiency, distance between the electrodes was recommended to be less than or equal to 1 cm.

Development of formulations and processes to incorporate wax oleogels in ice cream.

PubMed

Zulim Botega, Daniele C; Marangoni, Alejandro G; Smith, Alexandra K; Goff, H Douglas

2013-12-01

The objective of this study was to investigate the influence of emulsifiers, waxes, fat concentration, and processing conditions on the application of wax oleogel to replace solid fat content and create optimal fat structure in ice cream. Ice creams with 10% or 15% fat were formulated with rice bran wax (RBW), candelilla wax (CDW), or carnauba wax (CBW) oleogels, containing 10% wax and 90% high-oleic sunflower oil. The ice creams were produced using batch or continuous freezing processes. Transmission electron microscopy (TEM) and cryo-scanning electron microscopy were used to evaluate the microstructure of ice cream and the ultrastructure of oleogel droplets in ice cream mixes. Among the wax oleogels, RBW oleogel had the ability to form and sustain structure in 15% fat ice creams when glycerol monooleate (GMO) was used as the emulsifier. TEM images revealed that the high degree of fat structuring observed in GMO samples was associated with the RBW crystal morphology within the fat droplet, which was characterized by the growth of crystals at the outer edge of the droplet. Continuous freezing improved fat structuring compared to batch freezing. RBW oleogels established better structure compared to CDW or CBW oleogels. These results demonstrate that RBW oleogel has the potential to develop fat structure in ice cream in the presence of GMO and sufficiently high concentrations of oleogel. © 2013 Institute of Food Technologists®

Study on adsorption properties of synthetic materials on marine emulsified oil

NASA Astrophysics Data System (ADS)

Zhang, Zhaoyang; Peng, Shitao; Wang, Xiaoli; Zhou, Ran; Luo, Lei

2018-02-01

As an effective measure for marine oil spill recovery, adsorption treatment can be adopted in areas where mechanical recovery is not applicable. This experiment is mainly aimed at studying the adsorption properties of synthetic materials on emulsified oil. The emulsified oil was prepared by simulating the emulsification process of marine oil spill via a wave-current flume, and the adsorption weights of synthetic materials on emulsified oil were obtained by performing a field adsorption experiment. Polypropylene, nano-polypropylene and hydrophobic melamine sponge were tested by adsorbing a variety of emulsified oils according to the Adsorption Property Test Method (Version F-726) defined by ASTM. Their adsorption weights on emulsified oil (with initial thickness of 5 mm and water content of 20.86%) are 5.42 g/g, 23.5 g/g and 82.15g/g, respectively, which, compared with that on gear oil in the initial state, are respective decreases of 46.39%, 19.88% and 11.84%, demonstrating obvious decreases in their adsorption performances.

Ravuconazole self-emulsifying delivery system: in vitro activity against Trypanosoma cruzi amastigotes and in vivo toxicity

PubMed Central

Spósito, Pollyanna Álvaro; Mazzeti, Ana Lia; de Oliveira Faria, Caroline; Urbina, Julio A; Pound-Lana, Gwenaelle; Bahia, Maria Terezinha; Mosqueira, Vanessa Furtado

2017-01-01

Self-emulsifying drug delivery systems (SEDDSs) are lipid-based anhydrous formulations composed of an isotropic mixture of oil, surfactant, and cosurfactants usually presented in gelatin capsules. Ravuconazole (Biopharmaceutics Classification System [BCS] Class II) is a poorly water-soluble drug, and a SEDDS type IIIA was designed to deliver it in a predissolved state, improving dissolution in gastrointestinal fluids. After emulsification, the droplets had mean hydrodynamic diameters <250 nm, zeta potential values in the range of −45 mV to −57 mV, and showed no signs of ravuconazole precipitation. Asymmetric flow field-flow fractionation with dynamic and multiangle laser light scattering was used to characterize these formulations in terms of size distribution and homogeneity. The fractograms obtained at 37°C showed a polydisperse profile for all blank and ravuconazole–SEDDS formulations but no large aggregates. SEDDS increased ravuconazole in vitro dissolution extent and rate (20%) compared to free drug (3%) in 6 h. The in vivo toxicity of blank SEDDS comprising Labrasol® surfactant in different concentrations and preliminary safety tests in repeated-dose oral administration (20 days) showed a dose-dependent Labrasol toxicity in healthy mice. Ravuconazole–SEDDS at low surfactant content (10%, v/v) in Trypanosoma cruzi-infected mice was safe during the 20-day treatment. The anti-T. cruzi activity of free ravuconazole, ravuconazole–SEDDS and each excipient were evaluated in vitro at equivalent ravuconazole concentrations needed to inhibit 50% or 90% (IC50 and IC90), respectively of the intracellular amastigote form of the parasite in a cardiomyocyte cell line. The results showed a clear improvement of the ravuconazole anti-T. cruzi activity when associated with SEDDS. Based on our results, the repurposing of ravuconazole in SEDDS dosage form is a strategy that deserves further in vivo investigation in preclinical studies for the treatment of human T

Effect of emulsifier and viscosity on oil separation in ready-to-use therapeutic food

USDA-ARS?s Scientific Manuscript database

Oil separation is a common food quality problem in ready-to-use therapeutic food (RUTF), the shelf-stable, peanut-based food used to treat severe acute malnutrition in home settings. Our objective was to evaluate the effect on oil separation of three emulsifiers at different concentrations in RUTF. ...

Self-emulsifying drug delivery systems as a tool to improve solubility and bioavailability of resveratrol

PubMed Central

Balata, Gehan F; Essa, Ebtessam A; Shamardl, Hanan A; Zaidan, Samira H; Abourehab, Mohammed AS

2016-01-01

Resveratrol is a nonflavonoid polyphenolic compound which has a broad range of desirable biological actions which include antioxidant, anti-inflammatory, antidiabetic, cardioprotective, and antitumor activities. However, there is concern that the bioavailability of resveratrol may limit some of its clinical utility. So, the aim of this study was to enhance the dissolution rate and oral hypoglycemic and hypolipidemic effect of resveratrol. This was achieved using self-emulsifying drug delivery system. The solubility of resveratrol was determined in various oils, surfactants, and cosurfactants. Phase diagram was plotted to identify the efficient self-emulsification regions using olive oil, Tween 80, and propylene glycol. The prepared self-emulsifying drug delivery system formulations were tested for thermodynamic stability, emulsification efficiency, droplet size, zeta potential, and in vitro drug release. Self-emulsification time averaged 17–99 seconds without precipitation and the mean droplet sizes ranged from 285 to 823 nm with overall zeta potential of −2.24 to −15.4 mv. All formulations improved drug dissolution in relation to unprocessed drug with a trend of decreased dissolution parameters with increasing oil content. The optimized formula, F19, with dissolution efficiency of 94% compared to only 42% of pure drug was used to study the in vivo hypoglycemic and hypolipidemic effects of resveratrol in diabetic-induced albino rats and comparing these effects with that of pure resveratrol in different doses. Treatment with the optimized formula, F19, at 10 mg/kg had significant hypoglycemic and hypolipidemic effects in diabetic-induced albino rats which were nearly similar to the high dose (20 mg/kg) of unprocessed resveratrol. From the study, it was concluded that formulation F19 has good emulsification property with uniform globule size, satisfactory in vitro drug release profile, and significant in vivo hypoglycemic effects which identify future

Self-emulsifying drug delivery systems as a tool to improve solubility and bioavailability of resveratrol.

PubMed

Balata, Gehan F; Essa, Ebtessam A; Shamardl, Hanan A; Zaidan, Samira H; Abourehab, Mohammed As

2016-01-01

Resveratrol is a nonflavonoid polyphenolic compound which has a broad range of desirable biological actions which include antioxidant, anti-inflammatory, antidiabetic, cardioprotective, and antitumor activities. However, there is concern that the bioavailability of resveratrol may limit some of its clinical utility. So, the aim of this study was to enhance the dissolution rate and oral hypoglycemic and hypolipidemic effect of resveratrol. This was achieved using self-emulsifying drug delivery system. The solubility of resveratrol was determined in various oils, surfactants, and cosurfactants. Phase diagram was plotted to identify the efficient self-emulsification regions using olive oil, Tween 80, and propylene glycol. The prepared self-emulsifying drug delivery system formulations were tested for thermodynamic stability, emulsification efficiency, droplet size, zeta potential, and in vitro drug release. Self-emulsification time averaged 17-99 seconds without precipitation and the mean droplet sizes ranged from 285 to 823 nm with overall zeta potential of -2.24 to -15.4 mv. All formulations improved drug dissolution in relation to unprocessed drug with a trend of decreased dissolution parameters with increasing oil content. The optimized formula, F19, with dissolution efficiency of 94% compared to only 42% of pure drug was used to study the in vivo hypoglycemic and hypolipidemic effects of resveratrol in diabetic-induced albino rats and comparing these effects with that of pure resveratrol in different doses. Treatment with the optimized formula, F19, at 10 mg/kg had significant hypoglycemic and hypolipidemic effects in diabetic-induced albino rats which were nearly similar to the high dose (20 mg/kg) of unprocessed resveratrol. From the study, it was concluded that formulation F19 has good emulsification property with uniform globule size, satisfactory in vitro drug release profile, and significant in vivo hypoglycemic effects which identify future opportunities

Effects of Emulsifier, Overrun and Dasher Speed on Ice Cream Microstructure and Melting Properties.

PubMed

Warren, Maya M; Hartel, Richard W

2018-03-01

Ice cream is a multiphase frozen food containing ice crystals, air cells, fat globules, and partially coalesced fat globule clusters dispersed in an unfrozen serum phase (sugars, proteins, and stabilizers). This microstructure is responsible for ice cream's melting characteristics. By varying both formulation (emulsifier content and overrun) and processing conditions (dasher speed), the effects of different microstructural elements, particularly air cells and fat globule clusters, on ice cream melt-down properties were studied. Factors that caused an increase in shear stress within the freezer, namely increasing dasher speed and overrun, caused a decrease in air cell size and an increase in extent of fat destabilization. Increasing emulsifier content, especially of polysorbate 80, caused an increase in extent of fat destabilization. Both overrun and fat destabilization influenced drip-through rates. Ice creams with a combination of low overrun and low fat destabilization had the highest drip-through rates. Further, the amount of remnant foam left on the screen increased with reduced drip-through rates. These results provide a better understanding of the effects of microstructure components and their interactions on drip-through rate. Manipulating operating and formulation parameters in ice cream manufacture influences the microstructure (air cells, ice crystals, and fat globule clusters). This work provides guidance on which parameters have most effect on air cell size and fat globule cluster formation. Further, the structural characteristics that reduce melt-down rate were determined. Ice cream manufacturers will use these results to tailor their products for the desired quality attributes. © 2018 Institute of Food Technologists®.

Concentration of Nicotine and Glycols in 27 Electronic Cigarette Formulations

PubMed Central

Peace, Michelle R.; Baird, Tyson R.; Smith, Nathaniel; Wolf, Carl E.; Poklis, Justin L.; Poklis, Alphonse

2016-01-01

Personal battery-powered vaporizers or electronic cigarettes were developed to deliver a nicotine vapor such that smokers could simulate smoking tobacco without the inherent pathology of inhaled tobacco smoke. Electronic cigarettes and their e-cigarette liquid formulations are virtually unregulated. These formulations are typically composed of propylene glycol and/or glycerin, flavoring components and an active drug, such as nicotine. Twenty-seven e-cigarette liquid formulations that contain nicotine between 6 and 22 mg/L were acquired within the USA and analyzed by various methods to determine their contents. They were screened by Direct Analysis in Real Time™ Mass Spectrometry (DART-MS). Nicotine was confirmed and quantitated by high-performance liquid chromatography–tandem mass spectrometry, and the glycol composition was confirmed and quantitated by gas chromatography–mass spectrometry. The DART-MS screening method was able to consistently identify the exact mass peaks resulting from the protonated molecular ion of nicotine, glycol and a number of flavor additives within 5 mmu. Nicotine concentrations were determined to range from 45 to 131% of the stated label concentration, with 18 of the 27 have >10% variance. Glycol composition was generally accurate to the product description, with only one exception where the propylene glycol to glycerin percentage ratio was stated as 50:50 and the determined concentration of propylene glycol to glycerin was 81:19 (% v/v). No unlabeled glycols were detected in these formulations. PMID:27165804

Self-micro emulsifying formulation improved intestinal absorption and oral bioavailability of bakuchiol.

PubMed

Pi, Jiaxin; Gao, Xu; Yu, Yue; Zheng, Yin; Zhu, Zhuangzhi; Wang, Yajing

2014-10-18

Bakuchiol (BAK), isolated from the seeds of Psoralea corylifolia L., recently presents a variety of pharmacologic activities. However, the poor oral bioavailability limits its further development and clinical use. The purpose of this study was to establish a self-microemulsifying (SME) formulation for oral delivery improvement of BAK. The optimized liquid SME formulation was comprised of BAK (40 %), Cremophor RH 40 (30 %) and Labrasol (30 %). The emulsion droplets were spherical in shape, and particle size and zeta potential were determined. The in vitro dissolution test of BAK-SME formulation illustrated faster dissolution rate than the bulk drug. The permeabilities of 40 μg mL -1 BAK-SME formulation in rat intestinal segments of duodenum, jejunum, ileum and colon were 30.91 × 10 -3 , 23.61 × 10 -3 , 29.43 × 10 -3 and 23.62 × 10 -3 cm min -1 , respectively, exhibiting 3.99 times in duodenum, 2.59 times in ileum and 2.31 times in colon greater than BAK perfusate. The oral bioavailability of BAK-SME formulation at a dose of 150 mg kg -1 was determined in rats. The C max and the AUC (0-24h) were 515.4 ng mL -1 and 4,327.2 h ng mL -1 , respectively, which were 1.90 fold and 1.73 fold greater than the value of BAK suspension. All these results clearly stated that BAK-SME formulation performed well-improvement on oral bioavailability of BAK.

Formulation and in vitro and in vivo characterization of a phenytoin self-emulsifying drug delivery system (SEDDS).

PubMed

Atef, Eman; Belmonte, Albert A

2008-11-15

The aim of this study is to develop and characterize a self-emulsifying drug delivery system (SEDDS) of phenytoin, and to compare its relative bioavailability to a commercially available suspension. Four phenytoin SEDDS were prepared and evaluated. Following emulsification, the optimized formula was selected to have the smallest mean particle size and the highest absolute zeta potential, which should yield the formation of a stable emulsion. Its dissolution characteristics were superior to the other SEDDS formulas. In vivo and in vitro tests were run to compare the optimized formula, SEDDS II, to a commercially available Dilantin suspension. The in vitro dissolution indicated a significant improvement in phenytoin release characteristics. The in vivo study using male rats showed a clear enhancement in phenytoin oral absorption from SEDDS compared to Dilantin suspension. The area under the curve AUC((-10min-->10h)) of phenytoin after SEDDS administration increased by 2.3 times compared to Dilantin (p<0.05), and the rate of absorption of phenytoin was significantly faster from the SEDDS. The concentration after 30min (C(30min)) of SEDDS administration was 4.9 times higher than C(30min) after Dilantin administration (p<0.05). A sustained effect of phenytoin in plasma was also observed. After 12 weeks storage, SEDDS II was found to be chemically and physically stable under stressed conditions.

Fabrication of Concentrated Fish Oil Emulsions Using Dual-Channel Microfluidization: Impact of Droplet Concentration on Physical Properties and Lipid Oxidation.

PubMed

Liu, Fuguo; Zhu, Zhenbao; Ma, Cuicui; Luo, Xiang; Bai, Long; Decker, Eric Andrew; Gao, Yanxiang; McClements, David Julian

2016-12-21

Chemically unstable lipophilic bioactives, such as polyunsaturated lipids, often have to be encapsulated in emulsion-based delivery systems before they can be incorporated into foods, supplements, and pharmaceuticals. The objective of this study was to develop highly concentrated emulsion-based fish oil delivery systems using natural emulsifiers. Fish oil-in-water emulsions were fabricated using a highly efficient dual-channel high-pressure microfluidizer. The impact of oil concentration on the formation, physical properties, and oxidative stability of fish oil emulsions prepared using two natural emulsifiers (quillaja saponins and rhamnolipids) and one synthetic emulsifier (Tween-80) was examined. The mean droplet size, polydispersity, and apparent viscosity of the fish oil emulsions increased with increasing oil content. However, physically stable emulsions with high fish oil levels (30 or 40 wt %) could be produced using all three emulsifiers, with rhamnolipids giving the smallest droplet size (d < 160 nm). The stability of the emulsions to lipid oxidation increased as the oil content increased. The oxidative stability of the emulsions also depended on the nature of the emulsifier coating the lipid droplets, with the oxidative stability decreasing in the following order: rhamnolipids > saponins ≈ Tween-80. These results suggest that rhamnolipids may be particularly effective at producing emulsions containing high concentrations of ω-3 polyunsaturated fatty acids-rich fish oil.

A novel method to prepare concentrated conidial biomass formulation of Trichoderma harzianum for seed application.

PubMed

Singh, P C; Nautiyal, C S

2012-12-01

To prepare concentrated formulation of Trichoderma harzianum MTCC-3841 (NBRI-1055) with high colony forming units (CFU), long shelf life and efficient in root colonization by a simple scrapping method. NBRI-1055 spores scrapped from potato dextrose agar plates were used to prepare a concentrated formulation after optimizing carrier material, moisture content and spore harvest time. The process provides an advantage of maintaining optimum moisture level by the addition of water rather than dehydration. The formulation had an initial 11-12 log(10) CFU g(-1). Its concentrated form reduces its application amount by 100 times (10 g 100 kg(-1) seed) and provides 3-4 log(10) CFU seed(-1). Shelf life of the product was experimentally determined at 30 and 40 °C and predicted at other temperatures following Arrhenius equation. The concentrated formulation as compared to similar products provides an extra advantage of smaller packaging for storage and transportation, cutting down product cost. Seed application of the formulation recorded significant increase in plant growth promotion. Stable and effective formulation of Trichoderma harzianum NBRI-1055 was obtained by a simple scrapping method. A new method for the production of concentrated, stable, effective and cost efficient formulation of T. harzianum has been validated for seed application. © 2012 The Society for Applied Microbiology.

Ultrasound Assisted Synthesis of Hydroxylated Soybean Lecithin from Crude Soybean Lecithin as an Emulsifier.

PubMed

Chiplunkar, Pranali P; Pratap, Amit P

2017-10-01

Soybean lecithin is a by-product obtained during degumming step of crude soybean oil refining. Crude soybean lecithin (CSL) contains major amount of phospholipids (PLs) along with minor amount of acylglycerols, bioactive components, etc. Due to presence of PLs, CSL can be used as an emulsifier. Crude soybean lecithin (CSL) was utilized to synthesize hydroxylated soybean lecithin (HSL) by hydroxylation using hydrogen peroxide and catalytic amount of lactic acid to enhance the hydrophilicity and emulsifying properties of CSL. To reduce the reaction time and to increase rate of reaction, HSL was synthesized under ultrasound irradiation. The effect of different operating parameters such as lactic acid, hydrogen peroxide, temperature, ultrasonic power and duty cycle in synthesis of HSL were studied and optimized. The surface tension (SFT), interfacial tension (IFT) and the critical micelle concentration (CMC) of the HSL (26.11 mN/m, 2.67 mN/m, 112 mg/L) were compared to CSL (37.53 mN/m, 6.22 mN/m, 291 mg/L) respectively. The HSL has better emulsion stability and low foaming characteristics as compared to CSL. Therefore, the product as an effective emulsifier can be used in food, pharmacy, lubricant, cosmetics, etc.

An alkyl polyglucoside-mixed emulsifier as stabilizer of emulsion systems: the influence of colloidal structure on emulsions skin hydration potential.

PubMed

Savic, Snezana; Lukic, Milica; Jaksic, Ivana; Reichl, Stephan; Tamburic, Slobodanka; Müller-Goymann, Christel

2011-06-01

To be considered as a suitable vehicle for drugs/cosmetic actives, an emulsion system should have a number of desirable properties mainly dependent on surfactant used for its stabilization. In the current study, C(12-14) alkyl polyglucoside (APG)-mixed emulsifier of natural origin has been investigated in a series of binary (emulsifier concentration 10-25% (w/w)) and ternary systems with fixed emulsifier content (15% (w/w)) with or without glycerol. To elucidate the systems' colloidal structure the following physicochemical techniques were employed: polarization and transmission electron microscopy, X-ray diffraction (WAXD and SAXD), thermal analysis (DSC and TGA), complex rheological, pH, and conductivity measurements. Additionally, the emulsion vehicles' skin hydration potential was tested in vivo, on human skin under occlusion. In a series of binary systems with fixed emulsifier/water ratios ranging from 10/90 to 25/75 the predominance of a lamellar mesophase was found, changing its character from a liquid crystalline to a gel crystalline type. The same was observed in gel emulsions containing equal amounts of emulsifier and oil (15% (w/w)), but varying in glycerol content (0-25%). Different emulsion samples exhibited different water distribution modes in the structure, reflecting their rheological behavior and also their skin hydration capacity. Copyright © 2011 Elsevier Inc. All rights reserved.

Concentration of Nicotine and Glycols in 27 Electronic Cigarette Formulations.

PubMed

Peace, Michelle R; Baird, Tyson R; Smith, Nathaniel; Wolf, Carl E; Poklis, Justin L; Poklis, Alphonse

2016-07-01

Personal battery-powered vaporizers or electronic cigarettes were developed to deliver a nicotine vapor such that smokers could simulate smoking tobacco without the inherent pathology of inhaled tobacco smoke. Electronic cigarettes and their e-cigarette liquid formulations are virtually unregulated. These formulations are typically composed of propylene glycol and/or glycerin, flavoring components and an active drug, such as nicotine. Twenty-seven e-cigarette liquid formulations that contain nicotine between 6 and 22 mg/L were acquired within the USA and analyzed by various methods to determine their contents. They were screened by Direct Analysis in Real Time™ Mass Spectrometry (DART-MS). Nicotine was confirmed and quantitated by high-performance liquid chromatography-tandem mass spectrometry, and the glycol composition was confirmed and quantitated by gas chromatography-mass spectrometry. The DART-MS screening method was able to consistently identify the exact mass peaks resulting from the protonated molecular ion of nicotine, glycol and a number of flavor additives within 5 mmu. Nicotine concentrations were determined to range from 45 to 131% of the stated label concentration, with 18 of the 27 have >10% variance. Glycol composition was generally accurate to the product description, with only one exception where the propylene glycol to glycerin percentage ratio was stated as 50:50 and the determined concentration of propylene glycol to glycerin was 81:19 (% v/v). No unlabeled glycols were detected in these formulations. © The Author 2016. Published by Oxford University Press. All rights reserved. For Permissions, please email: journals.permissions@oup.com.

Dietary emulsifiers impact the mouse gut microbiota promoting colitis and metabolic syndrome.

PubMed

Chassaing, Benoit; Koren, Omry; Goodrich, Julia K; Poole, Angela C; Srinivasan, Shanthi; Ley, Ruth E; Gewirtz, Andrew T

2015-03-05

The intestinal tract is inhabited by a large and diverse community of microbes collectively referred to as the gut microbiota. While the gut microbiota provides important benefits to its host, especially in metabolism and immune development, disturbance of the microbiota-host relationship is associated with numerous chronic inflammatory diseases, including inflammatory bowel disease and the group of obesity-associated diseases collectively referred to as metabolic syndrome. A primary means by which the intestine is protected from its microbiota is via multi-layered mucus structures that cover the intestinal surface, thereby allowing the vast majority of gut bacteria to be kept at a safe distance from epithelial cells that line the intestine. Thus, agents that disrupt mucus-bacterial interactions might have the potential to promote diseases associated with gut inflammation. Consequently, it has been hypothesized that emulsifiers, detergent-like molecules that are a ubiquitous component of processed foods and that can increase bacterial translocation across epithelia in vitro, might be promoting the increase in inflammatory bowel disease observed since the mid-twentieth century. Here we report that, in mice, relatively low concentrations of two commonly used emulsifiers, namely carboxymethylcellulose and polysorbate-80, induced low-grade inflammation and obesity/metabolic syndrome in wild-type hosts and promoted robust colitis in mice predisposed to this disorder. Emulsifier-induced metabolic syndrome was associated with microbiota encroachment, altered species composition and increased pro-inflammatory potential. Use of germ-free mice and faecal transplants indicated that such changes in microbiota were necessary and sufficient for both low-grade inflammation and metabolic syndrome. These results support the emerging concept that perturbed host-microbiota interactions resulting in low-grade inflammation can promote adiposity and its associated metabolic effects

Dietary emulsifiers impact the mouse gut microbiota promoting colitis and metabolic syndrome

PubMed Central

Chassaing, Benoit; Koren, Omry; Goodrich, Julia; Poole, Angela; Srinivasan, Shanthi; Ley, Ruth E.; Gewirtz, Andrew T.

2015-01-01

Summary The intestinal tract is inhabited by a large diverse community of microbes collectively referred to as gut microbiota. While gut microbiota provide important benefits to its host, especially in metabolism and immune development, disturbance of the microbiota-host relationship is associated with numerous chronic inflammatory diseases, including inflammatory bowel disease (IBD) and the group of obesity-associated diseases collectively referred to as metabolic syndrome. A primary means by which the intestine is protected from its microbiota is via multilayered mucus structures that cover the intestinal surface thus allowing the vast majority of gut bacteria to be kept at a safe distance from epithelial cells that line the intestine 1. Thus, agents that disrupt mucus-bacterial interactions might have the potential to promote diseases associated with gut inflammation. Consequently, it has been hypothesized that emulsifiers, detergent-like molecules that are a ubiquitous component of processed foods and that can increase bacterial translocation across epithelia in vitro 2, might be promoting the post-mid 20th century increase in IBD 3. Herein, we observed that, in mice, relatively low concentrations of two commonly used emulsifiers, namely carboxymethylcellulose and polysorbate-80, induced low-grade inflammation and obesity/metabolic syndrome in WT hosts and promoted robust colitis in mice predisposed to this disorder. Emulsifier-induced metabolic syndrome was associated with microbiota encroachment, altered species composition, and increased pro-inflammatory potential. Use of germ-free mice and fecal transplants indicated that such changes in microbiota were necessary and sufficient for both low-grade inflammation and metabolic syndrome. These results support the emerging concept that perturbed host-microbiota interactions resulting in low-grade inflammation can promote adiposity and its associated metabolic effects. Moreover, they suggest that broad use of

Novel Approaches in Formulation of Entomopathogenic Fungi for Control of Insects in Soil, Foliar, and Structural Habitats: Thinking Outside the Box and Expecting the Unexpected

USDA-ARS?s Scientific Manuscript database

By and large, mycoinsecticide formulations have involved sprayable products, typically oil flowables, emulsifiable suspensions, wettable powders, and water dispersable granules. Various nutritive or inert carriers have been used to create granular formulations for use against soil pests. Sometime...

Salbutamol sulfate suppositories: influence of formulation on physical parameters and stability.

PubMed

Taha, Ehab I; Zaghloul, Abdel-Azim A; Kassem, Alaa A; Khan, Mansoor A

2003-01-01

To prepare and evaluate a suppository dosage form of salbutamol sulfate. The prepared formulae with and without different concentrations of gels were tested for hardness, melting time, content uniformity, and drug release. The stability of some of the selected formulae was assessed. Salbutamol sulfate was formulated as a rectal suppository with emulsifying fatty bases (suppocire and witepsol) and water-soluble bases (PEG) adopting the molding from a melt technique. Physical characteristics and dissolution profiles of the prepared formulations were determined as the responses. The effects of adding gels, methyl cellulose (MC), and Eudispert (Eud) and their concentrations (1, 3, and 6%) on these responses were also investigated. Formulations showing high rank order were scaled up for shelf-life stability study for one year. The results showed that all the investigated formulae have acceptable physical characteristics with respect to hardness, melting time (except F7), and uniformity of drug content. The amount of drug dissolved in 100 min of dissolution time was inversely affected by the melting point of the fatty base. The release from PEG bases was found to be molecular weight dependent. Addition of 1% MC or Eud gel increased the release from all the investigated formulae. Increasing gel concentration to 3% then to 6% showed different effects on the release. The degradation of salbutamol sulfate in the investigated formulae was found to be a first-order reaction. Rectal suppository of salbutamol sulfate could be prepared as an alternative to the oral dosage form to circumvent the first-pass metabolism.

Development of Pales Weevil Larvae on an Emulsified Synthetic Diet

Treesearch

H.A. Thomas

1971-01-01

The effect of adding an emulsifier to an artificial diet for pales weevil larvae was studied. The hypothesis was that fat-soluble ingredients would be better dispersed in the aqueous media, possibly leading to improved larval growth. The results suggest some Improvement occurred when the emulsifier was incorporated.

Effects of a sphingolipid-enriched dairy formulation on postprandial lipid concentrations.

PubMed

Ohlsson, L; Burling, H; Duan, R-D; Nilsson, A

2010-11-01

The digestion of sphingolipids (SL) is slow and is catalyzed by mucosal enzymes. Dietary SL was shown to inhibit cholesterol absorption and to lower plasma cholesterol, triglycerides (TG) and hepatic fat accumulation in animal models. A dairy formulation based on fractionation of buttermilk, which is enriched in milk polar lipids of which SL account for a large part is now available. In this study, we examined whether this formulation, when ingested with a standard breakfast, exerted a different influence on postprandial lipids than an equivalent control formulation lacking the polar milk lipids. A total of 18 healthy male volunteers aged 22-65 years ingested a high-fat (40 g) standard breakfast together with a milk-like formulation containing 975 mg of milk SL (A) or the control formulation (B). Postprandial levels of TG, total, low-density lipoprotein (LDL) and high-density lipoprotein (HDL) cholesterol, apolipoprotein AI (ApoAI), ApoB, glucose and insulin were measured 1 to 7 h after the meal. No difference was seen between experimental and control groups in postprandial levels of TG, insulin, ApoA1 or ApoB. After 1 hour there was a trend of lower cholesterol concentrations in large TG-rich lipoproteins after formulation A. The SL-rich buttermilk drink may affect cholesterol concentrations in TG-rich lipoproteins, but has no effect on postprandial TG after a breakfast with butter fat as the major lipid.

SNEDDS curcumin formulation leads to enhanced protection from pain and functional deficits associated with diabetic neuropathy: an insight into its mechanism for neuroprotection.

PubMed

Joshi, Rayanta P; Negi, Geeta; Kumar, Ashutosh; Pawar, Yogesh B; Munjal, Bhushan; Bansal, Arvind K; Sharma, Shyam S

2013-08-01

Curcumin has shown to be effective against various diabetes related complications. However major limitation with curcumin is its low bioavailability. In this study we formulated and characterized self nano emulsifying drug delivery system (SNEDDS) curcumin formulation to enhance its bioavailability and then evaluated its efficacy in experimental diabetic neuropathy. Bioavailability studies were performed in male Sprague Dawley rats. Further to evaluate the efficacy of formulation in diabetic neuropathy various parameters like nerve function and sensorimotor perception were assessed along with study of inflammatory proteins (NF-κB, IKK-β, COX-2, iNOS, TNF-α and IL-6). Nanotechnology based formulation resulted in prolonged plasma exposure and bioavailability. SNEDDS curcumin provided better results against functional, behavioural and biochemical deficits in experimental diabetic neuropathy, when compared with naive curcumin. Further western blot analysis confirmed the greater neuroprotective action of SNEDDS curcumin. SNEDDS curcumin formulation due to higher bioavailability was found to afford enhanced protection in diabetic neuropathy. In this study the authors formulated and characterized a self-emulsifying drug delivery system for formulation to enhance curcumin bioavailability in experimental diabetic neuropathy. Enhanced efficacy was demonstrated in a rat model. Copyright © 2013 Elsevier Inc. All rights reserved.

Emulsifying properties of succinylated arabinoxylan-protein gum produced from corn ethanol residuals

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

Xiang, Zhouyang; Runge, Troy

This study investigated the possibilities of making valuable products from corn ethanol byproducts and providing the beverage industries more variety of high quality emulsifiers other than gum arabic. An arabinoxylan-protein gum (APG) was extracted from distillers' grains (DG), a low-value corn ethanol byproduct, and modified through acylation with succinic anhydride. The effects of pH and degree of substitution (DS) on the emulsifying properties of succinylated APG, referred to as SAPG, were investigated. Emulsion particle size and stability of APG and gum arabic were comparable at pH 3.5–6.5. Succinylation could enhance the emulsifying properties of APG. Compared to gum arabic, atmore » pH < 5, SAPG emulsions had larger particle size but comparable stability, whereas at pH > 5, SAPG had much smaller particle size and better stability than gum arabic. The results suggested that SAPG, compared to gum arabic, could be a comparable emulsifier at low pH values and a better emulsifier at neutral pH values.« less

Emulsifying properties of succinylated arabinoxylan-protein gum produced from corn ethanol residuals

DOE PAGES

Xiang, Zhouyang; Runge, Troy

2015-07-21

This study investigated the possibilities of making valuable products from corn ethanol byproducts and providing the beverage industries more variety of high quality emulsifiers other than gum arabic. An arabinoxylan-protein gum (APG) was extracted from distillers' grains (DG), a low-value corn ethanol byproduct, and modified through acylation with succinic anhydride. The effects of pH and degree of substitution (DS) on the emulsifying properties of succinylated APG, referred to as SAPG, were investigated. Emulsion particle size and stability of APG and gum arabic were comparable at pH 3.5–6.5. Succinylation could enhance the emulsifying properties of APG. Compared to gum arabic, atmore » pH < 5, SAPG emulsions had larger particle size but comparable stability, whereas at pH > 5, SAPG had much smaller particle size and better stability than gum arabic. The results suggested that SAPG, compared to gum arabic, could be a comparable emulsifier at low pH values and a better emulsifier at neutral pH values.« less

Comparison of subarachnoid anesthetic effect of emulsified volatile anesthetics in rats.

PubMed

Guo, Jiao; Zhou, Cheng; Liang, Peng; Huang, Han; Li, Fengshan; Chen, Xiangdong; Liu, Jin

2014-01-01

Spinal cord is an important target of volatile anesthetics in particular for the effect of immobility. Intrathecal injection of volatile anesthetics has been found to produce subarachnoid anesthesia. The present study was designed to compare spinal anesthetic effects of emulsified volatile anesthetics, and to investigate the correlation between their spinal effects and general effect of immobility. In this study, halothane, isoflurane, enflurane and sevoflurane were emulsified by 30% Intralipid. These emulsified volatile anesthetics were intravenously and intrathecally injected, respectively. ED50 of general anesthesia and EC50 of spinal anesthesia were determined. The durations of general and spinal anesthesia were recorded. Correlation analysis was applied to evaluate the anesthetic potency of volatile anesthetics between their spinal and general effects. ED50 of general anesthesia induced by emulsified halothane, isoflurane, enflurane and sevoflurane were 0.41 ± 0.07, 0.54 ± 0.07, 0.74 ± 0.11 and 0.78 ± 0.08 mmol/kg, respectively, with significant correlation to their inhaled MAC (R(2) = 0.8620, P = 0.047). For intrathecal injection, EC50 of spinal anesthesia induced by emulsified halothane, isoflurane, enflurane and sevoflurane were 0.35, 0.27, 0.33 and 0.26 mol/L, respectively, which could be predicted by the product of inhaled MAC and olive oil/gas partition coefficients (R(2) = 0.9627, P = 0.013). In conclusion, potency and efficacy of the four emulsified volatile anesthetics in spinal anesthesia were similar and could be predicted by the product of inhaled MAC and olive oil/gas partition coefficients (MAC × olive oil/gas partition coefficients).

Disintegration and cancer immunotherapy efficacy of a squalane-in-water delivery system emulsified by bioresorbable poly(ethylene glycol)-block-polylactide.

PubMed

Chen, Wei-Lin; Liu, Shih-Jen; Leng, Chih-Hsiang; Chen, Hsin-Wei; Chong, Pele; Huang, Ming-Hsi

2014-02-01

Vaccine adjuvant is conferred on the substance that helps to enhance antigen-specific immune response. Here we investigated the disintegration characteristics and immunotherapy potency of an emulsified delivery system comprising bioresorbable polymer poly(ethylene glycol)-polylactide (PEG-PLA), phosphate buffer saline (PBS), and metabolizable oil squalane. PEG-PLA-stabilized oil-in-water emulsions show good stability at 4 °C and at room temperature. At 37 °C, squalane/PEG-PLA/PBS emulsion with oil/aqueous weight ratio of 7/3 (denominated PELA73) was stable for 6 weeks without phase separation. As PEG-PLA being degraded, 30% of free oil at the surface layer and 10% of water at the bottom disassociated from the PELA73 emulsion were found after 3 months. A MALDI-TOF MS study directly on the DIOS plate enables us to identify low molecular weight components released during degradation. Our results confirm the loss of PLA moiety of the emulsifier PEG-PLA directly affected the stability of PEG-PLA-stabilized emulsion, leading to emulsion disintegration and squalane/water phase separation. As adjuvant for cancer immunotherapeutic use, an HPV16 E7 peptide antigen formulated with PELA73 plus immunostimulatory CpG molecules could strongly enhance antigen-specific T-cell responses as well as anti-tumor ability with respected to non-formulated or Alum-formulated peptide. Accordingly, these advances may be a potential immunoregulatory strategy in manipulating the immune responses induced by tumor-associated antigens. Copyright © 2013 The Authors. Published by Elsevier Ltd.. All rights reserved.

Effect of binary organic solvents together with emulsifier on particle size and in vitro behavior of paclitaxel-encapsulated polymeric lipid nanoparticles.

PubMed

Qin, Shuzhi; Sun, Xiangshi; Li, Feng; Yu, Kongtong; Zhou, Yulin; Liu, Na; Zhao, Chengguo; Teng, Lesheng; Li, Youxin

2017-12-21

Biodegradable nanoparticles with diameters between 100 nm and 500 nm are of great interest in the contexts of targeted delivery. The present work provides a review concerning the effect of binary organic solvents together with emulsifier on particle size as well as the influence of particle size on the in vitro drug release and uptake behavior. The polymeric lipid nanoparticles (PLNs) with different particle sizes were prepared by using binary solvent dispersion method. Various formulation parameters such as binary organic solvent composition and emulsifier types were evaluated on the basis of their effects on particle size and size distribution. PLNs had a strong dependency on the surface tension, intrinsic viscosity and volatilization rate of binary organic solvents and the hydrophilicity/hydrophobicity of emulsifiers. Acetone-methanol system together with pluronic F68 as emulsifier was proved to obtain the smallest particle size. Then the PLNs with different particle sizes were used to investigate how particle size at nanoscale affects interacted with tumor cells. As particle size got smaller, cellular uptake increased in tumor cells and PLNs with particle size of ~120 nm had the highest cellular uptake and fastest release rate. The paclitaxel (PTX)-loaded PLNs showed a size-dependent inhibition of tumor cell growth, which was commonly influenced by cellular uptake and PTX release. The PLNs would provide a useful means to further elucidate roles of particle size on delivery system of hydrophobic drugs. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Anti-cancer evaluation of quercetin embedded PLA nanoparticles synthesized by emulsified nanoprecipitation.

PubMed

Pandey, Sanjeev K; Patel, Dinesh K; Thakur, Ravi; Mishra, Durga P; Maiti, Pralay; Haldar, Chandana

2015-04-01

This study was carried out to synthesize quercetin (Qt) embedded poly(lactic acid) (PLA) nanoparticles (PLA-Qt) and to evaluate anti-cancer efficacy of PLA-Qt by using human breast cancer cells. PLA-Qt were synthesized by using novel emulsified nanoprecipitation technique with varying dimension of 32 ± 8 to 152 ± 9 nm of PLA-Qt with 62 ± 3% (w/w) entrapment efficiency by varying the concentration of polymer, emulsifier, drug and preparation temperature. The dimension of PLA-Qt was measured through transmission electron microscopy indicating larger particle size at higher concentration of PLA. The release rate of Qt from PLA-Qt was found to be more sustained for larger particle dimension (152 ± 9 nm) as compared to smaller particle dimension (32 ± 8 nm). Interaction between Qt and PLA was verified through spectroscopic and calorimetric methods. Delayed diffusion and stronger interaction in PLA-Qt caused the sustained delivery of Qt from the polymer matrix. In vitro cytotoxicity study indicate the killing of ∼ 50% breast cancer cells in two days at 100 μg/ml of drug concentration while the ∼ 40% destruction of cells require 5 days for PLA-Qt (46 ± 6 nm; 20mg/ml of PLA). Thus our results propose anticancer efficacy of PLA-Qt nanoparticles in terms of its sustained release kinetics revealing novel vehicle for the treatment of cancer. Copyright © 2015 Elsevier B.V. All rights reserved.

Adsorption at the biocompatible α-pinene-water interface and emulsifying properties of two eco-friendly surfactants.

PubMed

Trujillo-Cayado, Luis Alfonso; Ramírez, Pablo; Alfaro, María Carmen; Ruíz, Manuela; Muñoz, José

2014-10-01

In this contribution, we provide an accurate characterization at the α-pinene/water interface of two commercial polyoxytheylene glycerol ester surfactants which differ in the number of ethylene oxide (EO) groups, comprising a systematic analysis of interfacial pressure isotherms, dynamic curves, interfacial rheology and emulsifying properties. Polyoxyethylene glycerol esters derived from cocoa oil are non-ionic surfactants obtained from a renewable source which fulfill the environmental and toxicological requirements to be used as eco-friendly emulsifying agents. α-Pinene is a renewable biosolvent completely insoluble in water, which could find numerous applications. Interfacial rheology and equilibrium interfacial pressure data fitted a rigorous reorientation model that assumes that the surfactant molecules, when adsorbed at the interface, can acquire two orientations. The surfactant with the highest number of EO groups (Levenol C201) turned out to be more surface active at the α-pinene/water interface. In addition, the surfactant with the lowest number of EO groups (Levenol H&B) is solubilized into the adjacent oil phase. Slightly concentrated α-pinene emulsions were obtained using both surfactants. Nevertheless, more stable α-pinene emulsions with smaller droplet sizes and lower polidispersity were obtained when Levenol C201 was used as emulsifier instead of Levenol H&B. The systematic characterization presented in this work provides important new findings on the interfacial and emulsifying properties of polyoxytheylene glycerol ester surfactants, which can be applied in the rational development of new biocompatible products. Copyright © 2014 Elsevier B.V. All rights reserved.

Topical nanoparticulate formulation of drugs for ocular keratitis

NASA Astrophysics Data System (ADS)

Yang, Xiaoyan

bacterial corneal keratitis. Experimental designs were employed in order to investigate specific effects of independent variables during preparation of HB-loaded PLGA NP and corresponding responses in optimizing the formulation. NP containing HB were prepared by an oil-in-water (O/W) emulsion evaporation technique with different surfactants including polyvinyl alcohol (PVA), pluronic F-108 and chitosan. NP were characterized with respect to particle size, entrapment efficiency, polydispersity, drug loading, surface morphology, zeta potential and crystallinity. In vitro release of HB from NP showed a biphasic release pattern with an initial burst phase followed by a sustained phase. Such burst effect was completely eliminated when NP were suspended in thermosensitive gels and zero-order release kinetics was observed. Percentage of uptake in HCEC after 4 h was 59.09+/-6.21% for PVA-emulsified NP relative to 55.74+/-6.26% for pluronic-emulsified NP, and 62.54+/-3.30% for chitosan-emulsified NP, respectively. In HCEC cell line, chitosan-emulsified NP with chitosan showed highest cellular uptake efficiency over PVA- and pluronic-emulsified NP. However, NP with chitosan indicated significant cytotoxicity under 200 and 500 ?g/mL after 48 h, while NP with PVA and pluronic showed no significant cytotoxicity. PLGA NP dispersed in thermosensitive gels can be considered as a promising drug delivery system for the treatment of anterior eye diseases.

Development of optimized self-nano-emulsifying drug delivery systems (SNEDDS) of carvedilol with enhanced bioavailability potential.

PubMed

Singh, Bhupinder; Khurana, Lalit; Bandyopadhyay, Shantanu; Kapil, Rishi; Katare, O O P

2011-11-01

Carvedilol, a widely prescribed cardiovascular drug for hypertension and congestive heart failure, exhibits low and variable bioavailability owing to poor absorption and extensive hepatic first-pass metabolism. The current research work, therefore, entails formulation development of liquid self-nano-emulsifying drug delivery systems (SNEDDS) to enhance the bioavailability of carvedilol by facilitating its transport via lymphatic circulation. The formulation constituents, i.e. lipids, surfactants, and co-surfactants, were selected on the basis of solubility studies. Pseudo-ternary phase diagrams were constructed to embark upon the selection of blend of lipidic (i.e. Capmul PG8) and hydrophilic components (i.e. Cremophor EL as surfactant and Transcutol HP as co-surfactant) for efficient and robust formulation of SNEDDS. The SNEDDS, systematically optimized employing a central composite design (CCD), were evaluated for various response variables viz drug release parameters, emulsification time, emulsion droplet size, and mean dissolution time. In vitro drug release studies depicted that the release from SNEDDS systems followed a non-Fickian kinetic behavior. The TEM imaging of the optimized formulation affirmed the uniform shape and nano size of the system. Accelerated studies of the optimized formulation indicated high stability of the formulation for 6 months. The in situ perfusion studies carried out in wistar rats construed several fold augmentation in the permeability and absorption potential of the optimized formulation vis-à-vis marketed formulation. Thus, the present studies ratified the potential of SNEDDS in augmenting the oral bioavailability of BCS class II drugs.

Cyclosporine a loaded solid lipid nanoparticles: optimization of formulation, process variable and characterization.

PubMed

Varia, Jigisha K; Dodiya, Shamsunder S; Sawant, Krutika K

2008-01-01

Solid lipid nanoparticles (SLNs) loaded with Cyclosporine A using glyceryl monostearate (GMS) and glyceryl palmitostearate (GPS) as lipid matrices were prepared by melt-homogenization using high-pressure homogenizer. Various process parameters such as homogenization pressure, homogenization cycles and formulation parameters such as ratio of drug: lipid, emulsifier: lipid and emulsifier: co-emulsifier were optimized using particle size and entrapment efficiencies as the dependent variables. The mean particle size of optimized batches of the GMS SLN and GPS SLN were found to be 131 nm and 158 nm and their entrapment efficiencies were 83 +/- 3.08% and 97 +/- 2.59% respectively. To improve the handling processing and stability of the prepared SLNs, the SLN dispersions were spray dried and its effect on size and reconstitution parameters were evaluated. The spray drying of SLNs did not significantly alter the size of SLNs and they exhibited good redispersibility. Solid state studies such as Infra Red Spectroscopy and Differential Scanning Calorimetry indicated absence of any chemical interaction between Cyclosporine A and the lipids. Scanning Electron Microscopy of optimized formulations showed spherical shape with smooth and non porous surface. In vitro release studies revealed that GMS based SLNs released the drug faster (41.12% in 20 hours) than GPS SLNs (7.958% in 20 hours). Release of Cyclosporine A from GMS SLN followed Higuchi equation better than first order while release from GPS SLN followed first order better than Higuchi model.

Stability of buffer-free freeze-dried formulations: A feasibility study of a monoclonal antibody at high protein concentrations.

PubMed

Garidel, Patrick; Pevestorf, Benjamin; Bahrenburg, Sven

2015-11-01

We studied the stability of freeze-dried therapeutic protein formulations over a range of initial concentrations (from 40 to 160 mg/mL) and employed a variety of formulation strategies (including buffer-free freeze dried formulations, or BF-FDF). Highly concentrated, buffer-free liquid formulations of therapeutic monoclonal antibodies (mAbs) have been shown to be a viable alternative to conventionally buffered preparations. We considered whether it is feasible to use the buffer-free strategy in freeze-dried formulations, as an answer to some of the known drawbacks of conventional buffers. We therefore conducted an accelerated stability study (24 weeks at 40 °C) to assess the feasibility of stabilizing freeze-dried formulations without "classical" buffer components. Factors monitored included pH stability, protein integrity, and protein aggregation. Because the protein solutions are inherently self-buffering, and the system's buffer capacity scales with protein concentration, we included highly concentrated buffer-free freeze-dried formulations in the study. The tested formulations ranged from "fully formulated" (containing both conventional buffer and disaccharide stabilizers) to "buffer-free" (including formulations with only disaccharide lyoprotectant stabilizers) to "excipient-free" (with neither added buffers nor stabilizers). We evaluated the impacts of varying concentrations, buffering schemes, pHs, and lyoprotectant additives. At the end of 24 weeks, no change in pH was observed in any of the buffer-free formulations. Unbuffered formulations were found to have shorter reconstitution times and lower opalescence than buffered formulations. Protein stability was assessed by visual inspection, sub-visible particle analysis, protein monomer content, charge variants analysis, and hydrophobic interaction chromatography. All of these measures found the stability of buffer-free formulations that included a disaccharide stabilizer comparable to buffer

Comparison of subarachnoid anesthetic effect of emulsified volatile anesthetics in rats

PubMed Central

Guo, Jiao; Zhou, Cheng; Liang, Peng; Huang, Han; Li, Fengshan; Chen, Xiangdong; Liu, Jin

2014-01-01

Spinal cord is an important target of volatile anesthetics in particular for the effect of immobility. Intrathecal injection of volatile anesthetics has been found to produce subarachnoid anesthesia. The present study was designed to compare spinal anesthetic effects of emulsified volatile anesthetics, and to investigate the correlation between their spinal effects and general effect of immobility. In this study, halothane, isoflurane, enflurane and sevoflurane were emulsified by 30% Intralipid. These emulsified volatile anesthetics were intravenously and intrathecally injected, respectively. ED50 of general anesthesia and EC50 of spinal anesthesia were determined. The durations of general and spinal anesthesia were recorded. Correlation analysis was applied to evaluate the anesthetic potency of volatile anesthetics between their spinal and general effects. ED50 of general anesthesia induced by emulsified halothane, isoflurane, enflurane and sevoflurane were 0.41 ± 0.07, 0.54 ± 0.07, 0.74 ± 0.11 and 0.78 ± 0.08 mmol/kg, respectively, with significant correlation to their inhaled MAC (R2 = 0.8620, P = 0.047). For intrathecal injection, EC50 of spinal anesthesia induced by emulsified halothane, isoflurane, enflurane and sevoflurane were 0.35, 0.27, 0.33 and 0.26 mol/L, respectively, which could be predicted by the product of inhaled MAC and olive oil/gas partition coefficients (R2 = 0.9627, P = 0.013). In conclusion, potency and efficacy of the four emulsified volatile anesthetics in spinal anesthesia were similar and could be predicted by the product of inhaled MAC and olive oil/gas partition coefficients (MAC × olive oil/gas partition coefficients). PMID:25674241

Enhanced effectiveness of tocotrienol-based nano-emulsified system for topical delivery against skin carcinomas.

PubMed

Pham, Jimmy; Nayel, Amy; Hoang, Christina; Elbayoumi, Tamer

2016-06-01

The potent anti-proliferative and pro-apoptotic actions of tocotrienols (T3) against cancer, but not normal tissues, have been hampered by their limited systemic bioavailabilty. Recent expansive development of diverse nanoemulsion (NE) vehicles emphasized their vast potential to improve the effective dosing of different clinical and experimental drugs of lipophilic nature, such as T3. The emphasis of the present work is to develop a pharmaceutically scalable, low-energy nano-emulsification approach for optimized incorporation of T3-rich palm oil (Tocomin®), possessing anticancer activity as a potential cutaneous delivery platform for adjunctive therapy of skin carcinomas, either alone or in combination with other chemotherapeutic agents. Different Tocomin®-NEs, obtained with different homogenization strategies, were screened based on physicochemical uniformity (droplet size, charge and polydispersity) and subjected to stress physical stability testing, along with chemical content analysis (≥90% Tocomin® - incorporation efficiency). Adopted hybrid nano-emulsification of Tocomin®, correlated with highest preservation of DPPH-radical scavenging capacity of active T3 in prototype formulation, Tocomin®-NE, which effectively permeated diffusion cell membranes 4-folds higher than propyleneglycol (PG)-admixed Tocomin® control. Against two different cell models of human cutaneous carcinoma, Tocomin®-hybrid NE demonstrated significantly stronger cytotoxic profiles (p ≤ 0.01), visible in both concentration- and time- dependent manners, with at least 5-folds lower IC50 values, compared to those estimated for the closest Tocomin®-control. The proposed hybrid nano-emulsified formulation of Tocomin® provides simple and stable delivery platform, for effective topical application against keratinocyte tumors.

Nanoparticle-Based Topical Ophthalmic Gel Formulation for Sustained Release of Hydrocortisone Butyrate.

PubMed

Yang, Xiaoyan; Trinh, Hoang M; Agrahari, Vibhuti; Sheng, Ye; Pal, Dhananjay; Mitra, Ashim K

2016-04-01

This study was conducted to develop formulations of hydrocortisone butyrate (HB)-loaded poly(D,L-lactic-co-glycolic acid) nanoparticles (PLGA NP) suspended in thermosensitive gel to improve ocular bioavailability of HB for the treatment of bacterial corneal keratitis. PLGA NP with different surfactants such as polyvinyl alcohol (PVA), pluronic F-108, and chitosan were prepared using oil-in-water (O/W) emulsion evaporation technique. NP were characterized with respect to particle size, entrapment efficiency, polydispersity, drug loading, surface morphology, zeta potential, and crystallinity. In vitro release of HB from NP showed a biphasic release pattern with an initial burst phase followed by a sustained phase. Such burst effect was completely eliminated when nanoparticles were suspended in thermosensitive gels and zero-order release kinetics was observed. In HCEC cell line, chitosan-emulsified NP showed the highest cellular uptake efficiency over PVA- and pluronic-emulsified NP (59.09 ± 6.21%, 55.74 ± 6.26%, and 62.54 ± 3.30%, respectively) after 4 h. However, chitosan-emulsified NP indicated significant cytotoxicity of 200 and 500 μg/mL after 48 h, while PVA- and pluronic-emulsified NP exhibited no significant cytotoxicity. PLGA NP dispersed in thermosensitive gels can be considered as a promising drug delivery system for the treatment of anterior eye diseases.

Implications of interfacial characteristics of food foaming agents in foam formulations.

PubMed

Rodríguez Patino, Juan M; Carrera Sánchez, Cecilio; Rodríguez Niño, Ma Rosario

2008-08-05

The manufacture of food dispersions (emulsions and foams) with specific quality attributes depends on the selection of the most appropriate raw materials and processing conditions. These dispersions being thermodynamically unstable require the use of emulsifiers (proteins, lipids, phospholipids, surfactants etc.). Emulsifiers typically coexist in the interfacial layer with specific functions in the processing and properties of the final product. The optimum use of emulsifiers depends on our knowledge of their interfacial physico-chemical characteristics - such as surface activity, amount adsorbed, structure, thickness, topography, ability to desorb (stability), lateral mobility, interactions between adsorbed molecules, ability to change conformation, interfacial rheological properties, etc. -, the kinetics of film formation and other associated physico-chemical properties at fluid interfaces. These monolayers constitute well defined systems for the analysis of food colloids at the micro- and nano-scale level, with several advantages for fundamental studies. In the present review we are concerned with the analysis of physico-chemical properties of emulsifier films at fluid interfaces in relation to foaming. Information about the above properties would be very helpful in the prediction of optimised formulations for food foams. We concluded that at surface pressures lower than that of monolayer saturation the foaming capacity is low, or even zero. A close relationship was observed between foaming capacity and the rate of diffusion of the foaming agent to the air-water interface. However, the foam stability correlates with the properties of the film at long-term adsorption.

Self-emulsifying excipient platform for improving technological properties of alginate-hydroxypropylcellulose pellets.

PubMed

Mannina, Paolo; Segale, Lorena; Giovannelli, Lorella; Bonda, Andrea Foglio; Pattarino, Franco

2016-02-29

In this work, alginate, alginate-pectin and alginate-hydroxypropylcellulose pellets were produced by ionotropic gelation and characterized. Ibuprofen was selected as model drug; it was suspended in the polymeric solution in crystalline form or dissolved in a self-emulsifying phase and then dispersed into the polymeric solution. The self-emulsifying excipient platform composed of Labrasol (PEG-8 caprylic/capric glycerides) and d-α-tocopherol polyethylene glycol 1000 succinate (TPGS), able to solubilize the drug was used to improve the technological and biopharmaceutical properties of the alginate pellets. The pellets had diameters between 1317 and 2026 μm and a high drug content (>51%). DSC analysis showed the amorphous state of drug in the pellets containing the self-emulsifying phase. All the systems restricted drug release in conditions simulating the gastric environment and made the drug completely available at a pH value typical for the intestine. Only alginate-HPC systems containing the drug solubilized into the self-emulsifying phase showed the ability to partially control the release of ibuprofen at neutral pH. The self-emulsifying excipient platform is a useful tool to improve technological and biopharmaceutical properties of alginate-HPC pellets. Copyright © 2015 Elsevier B.V. All rights reserved.

Enhanced absorption of indomethacin after oral or rectal administration of a self-emulsifying system containing indomethacin to rats.

PubMed

Kim, J Y; Ku, Y S

2000-01-20

A self-emulsifying system (SES), a mixture of an oil and a surfactant which forms an oil-in-water emulsion, is expected to improve the in vitro drug dissolution and enhance the in vivo drug absorption. In this study, a poorly water-soluble drug, indomethacin (IDM) was incorporated into the SES to increase bioavailability. The SES with 30% of Tween 85 and 70% of ethyl oleate, EO (w/w) was selected as an optimized formulation (high drug loading, low surfactant concentration, and small particle size). After an oral administration of the SES containing IDM and IDM suspension, (IDM was suspended in methyl cellulose), 22.5 mg/kg as IDM, to rats, the area under the plasma concentration-time curve from time zero to the last measured time in plasma, 12 h (AUC(0-12 h)) was significantly greater (57% increase) in the SES, suggesting that oral absorption of IDM increased significantly by the SES. After a rectal administration of gelatin hollow type suppositories, filled with the SES containing IDM and IDM powder physically mixed with the SES, 22. 5 mg/kg, to rats, the AUC(0-12 h) also increased significantly (41% increase) by the SES, suggesting that rectal absorption of IDM also increased significantly by the SES.

Mayonnaise contributes to increasing postprandial serum β-carotene concentration through the emulsifying property of egg yolk in rats and humans.

PubMed

Takeda, Sayaka; Kimura, Mamoru; Marushima, Ranko; Takeuchi, Ayako; Takizawa, Kazue; Ogino, Yuji; Masuda, Yasunobu; Kunou, Masaaki; Hasegawa, Mineo; Maruyama, Chizuko

2011-01-01

We performed in vitro, animal, and human studies to clarify the effect of mayonnaise on β-carotene intake and its mechanism. In an artificial gastric juice model, we examined the transfer of β-carotene from grated carrot to mayonnaise or vegetable oil. Mayonnaise was more easily dispersed in artificial gastric juice than vegetable oil. The β-carotene concentration was greater in mayonnaise than vegetable oil. In rats, the postprandial serum β-carotene concentration in the mayonnaise group (β-carotene with mayonnaise) was higher than that in the control (β-carotene only) and vegetable oil (β-carotene with vegetable oil) groups. Continuous feeding of dietary β-carotene (14 d), employing mayonnaise or egg yolk, resulted in an increased accumulation of β-carotene in the liver. In a human study, diets were provided in the form of (1) carrot as a control (CON), (2) carrot juice (JU), (3) carrot with oil (OIL) and (4) carrot with mayonnaise (MS). Following collection of fasting blood samples, nine adult males consumed one of the four diets in random order. Fasting and postprandial changes in serum β-carotene were assessed at 2, 3, 4, 6 and 8 h following ingestion of each diet. The incremental areas under the curves of serum β-carotene concentration were higher following MS than following both CON and JU. In conclusion, we suggest that mayonnaise contributes to raising the serum β-carotene concentration when consumed with carrots rich in β-carotene, and that its mechanism is related to the emulsifying property of the egg yolk contained in mayonnaise.

Preparation and evaluation of a self-emulsifying drug delivery system of etoposide-phospholipid complex.

PubMed

Wu, Zhongbin; Guo, Dan; Deng, Li; Zhang, Yue; Yang, Qiuxia; Chen, Jianming

2011-01-01

The aim of this study was to develop a new phospholipid complex self-emulsifying drug delivery system (PC-SEDDS) to enhance bioavailability of oral etoposide, a drug with poor water solubility. Etoposide-phospholipid complex (EPC) was prepared by reacting etoposide and phospholipid in tetrahydrofuran and confirmed as a phospholipid compound by differential scanning calorimetry (DSC). Solubility of EPC and etoposide was determined in various vehicles. Pseudoternary phase diagrams were constructed to identify the efficient self-emulsification region of EPC-SEDDS, and the effects of oil concentration, drug loading, and aqueous media on droplet size were investigated. The optimal formulation of EPC-SEDDS was EPC:octyl and decyl monoglyceride (ODO):Cremopher EL:PEG-400 (1:20:48:32) (w/w/w/w). Compared with etoposide-phospholipid complex suspension (EPCS) and etoposide suspension (ES), cumulative release of etoposide from EPC-SEDDS increased by 1.31 and 2.65 fold at 24 hours, respectively. Compared with ES, relative bioavailability of EPC-SEDDS, E-SEDDS, and EPCS after oral administration in rats was enhanced by 60.21-, 44.9-, and 8.44- fold, respectively. The synergistic effect between PC and SEDDS contributed to the enhanced bioavailability of etoposide. It was concluded that PC-SEDDS proved to be a potential system for delivering orally administered hydrophobic compounds including etoposide.

Enhanced colonic delivery of ciclosporin A self-emulsifying drug delivery system encapsulated in coated minispheres.

PubMed

Keohane, Kieran; Rosa, Mónica; Coulter, Ivan S; Griffin, Brendan T

2016-01-01

Investigate the potential of coated minispheres (SmPill®) to enhance localized Ciclosporin A (CsA) delivery to the colon. CsA self-emulsifying drug delivery systems (SEDDS) were encapsulated into SmPill® minispheres. Varying degrees of coating thickness (low, medium and high) were applied using ethylcellulose and pectin (E:P) polymers. In vitro CsA release was evaluated in simulated gastric and intestinal media. Bioavailability of CsA in vivo following oral administration to pigs of SmPill® minispheres was compared to Neoral® po and Sandimmun® iv in a pig model. CsA concentrations in blood and intestinal tissue were determined by HPLC-UV. In vitro CsA release from coated minispheres decreased with increasing coating thickness. A linear relationship was observed between in vitro CsA release and in vivo bioavailability (r(2) = 0.98). CsA concentrations in the proximal, transverse and distal colon were significantly higher following administration of SmPill®, compared to Neoral® po and Sandimmun® iv (p < 0.05). Analysis of transverse colon tissue subsections also revealed significantly higher CsA concentrations in the mucosa and submucosa using SmPill® minispheres (p < 0.05). Modulating E:P coating thickness controls release of CsA from SmPill® minispheres. Coated minispheres limited CsA release in the small intestine and enhanced delivery and uptake in the colon. These findings demonstrate clinical advantages of an oral coated minisphere-enabled CsA formulation in the treatment of inflammatory conditions of the large intestine.

Surface phase behavior and microstructure of lipid/PEG-emulsifier monolayer-coated microbubbles.

PubMed

Borden, Mark A; Pu, Gang; Runner, Gabriel J; Longo, Marjorie L

2004-06-01

Langmuir trough methods and fluorescence microscopy were combined to investigate the phase behavior and microstructure of monolayer shells coating micron-scale bubbles (microbubbles) typically used in biomedical applications. The monolayer shell consisted of a homologous series of saturated acyl chain phospholipids and an emulsifier containing a single hydrophobic stearate chain and polyethylene glycol (PEG) head group. PEG-emulsifier was fully miscible with expanded phase lipids and phase separated from condensed phase lipids. Phase coexistence was observed in the form of dark condensed phase lipid domains surrounded by a sea of bright, emulsifier-rich expanded phase. A rich assortment of condensed phase area fractions and domain morphologies, including networks and other novel structures, were observed in each batch of microbubbles. Network domains were reproduced in Langmuir monolayers under conditions of heating-cooling followed by compression-expansion, as well as in microbubble shells that underwent surface flow with slight compression. Domain size decreased with increased cooling rate through the phase transition temperature, and domain branching increased with lipid acyl chain length at high cooling rates. Squeeze-out of the emulsifier at a surface pressure near 35 mN/m was indicated by a plateau in Langmuir isotherms and directly visualized with fluorescence microscopy, although collapse of the solid lipid domains occurred at much higher surface pressures. Compression of the monolayer past the PEG-emulsifier squeeze-out surface pressure resulted in a dark shell composed entirely of lipid. Under certain conditions, the PEG-emulsifier was reincorporated upon subsequent expansion. Factors that affect shell formation and evolution, as well as implications for the rational design of microbubbles in medical applications, are discussed.

Larvicidal activity of neem oil (Azadirachta indica) formulation against mosquitoes

PubMed Central

Dua, Virendra K; Pandey, Akhilesh C; Raghavendra, Kamaraju; Gupta, Ashish; Sharma, Trilochan; Dash, Aditya P

2009-01-01

Background Mosquitoes transmit serious human diseases, causing millions of deaths every year. Use of synthetic insecticides to control vector mosquitoes has caused physiological resistance and adverse environmental effects in addition to high operational cost. Insecticides of botanical origin have been reported as useful for control of mosquitoes. Azadirachta indica (Meliaceae) and its derived products have shown a variety of insecticidal properties. The present paper discusses the larvicidal activity of neem-based biopesticide for the control of mosquitoes. Methods Larvicidal efficacy of an emulsified concentrate of neem oil formulation (neem oil with polyoxyethylene ether, sorbitan dioleate and epichlorohydrin) developed by BMR & Company, Pune, India, was evaluated against late 3rd and early 4th instar larvae of different genera of mosquitoes. The larvae were exposed to different concentrations (0.5–5.0 ppm) of the formulation along with untreated control. Larvicidal activity of the formulation was also evaluated in field against Anopheles, Culex, and Aedes mosquitoes. The formulation was diluted with equal volumes of water and applied @ 140 mg a.i./m2 to different mosquito breeding sites with the help of pre calibrated knapsack sprayer. Larval density was determined at pre and post application of the formulation using a standard dipper. Results Median lethal concentration (LC50) of the formulation against Anopheles stephensi, Culex quinquefasciatus and Aedes aegypti was found to be 1.6, 1.8 and 1.7 ppm respectively. LC50 values of the formulation stored at 26°C, 40°C and 45°C for 48 hours against Ae. aegypti were 1.7, 1.7, 1.8 ppm while LC90 values were 3.7, 3.7 and 3.8 ppm respectively. Further no significant difference in LC50 and LC90 values of the formulation was observed against Ae. aegypti during 18 months storage period at room temperature. An application of the formulation at the rate of 140 mg a.i./m2 in different breeding sites under natural field

Larvicidal activity of neem oil (Azadirachta indica) formulation against mosquitoes.

PubMed

Dua, Virendra K; Pandey, Akhilesh C; Raghavendra, Kamaraju; Gupta, Ashish; Sharma, Trilochan; Dash, Aditya P

2009-06-08

Mosquitoes transmit serious human diseases, causing millions of deaths every year. Use of synthetic insecticides to control vector mosquitoes has caused physiological resistance and adverse environmental effects in addition to high operational cost. Insecticides of botanical origin have been reported as useful for control of mosquitoes. Azadirachta indica (Meliaceae) and its derived products have shown a variety of insecticidal properties. The present paper discusses the larvicidal activity of neem-based biopesticide for the control of mosquitoes. Larvicidal efficacy of an emulsified concentrate of neem oil formulation (neem oil with polyoxyethylene ether, sorbitan dioleate and epichlorohydrin) developed by BMR & Company, Pune, India, was evaluated against late 3rd and early 4th instar larvae of different genera of mosquitoes. The larvae were exposed to different concentrations (0.5-5.0 ppm) of the formulation along with untreated control. Larvicidal activity of the formulation was also evaluated in field against Anopheles, Culex, and Aedes mosquitoes. The formulation was diluted with equal volumes of water and applied @ 140 mg a.i./m(2) to different mosquito breeding sites with the help of pre calibrated knapsack sprayer. Larval density was determined at pre and post application of the formulation using a standard dipper. Median lethal concentration (LC(50)) of the formulation against Anopheles stephensi, Culex quinquefasciatus and Aedes aegypti was found to be 1.6, 1.8 and 1.7 ppm respectively. LC(50) values of the formulation stored at 26 degrees C, 40 degrees C and 45 degrees C for 48 hours against Ae. aegypti were 1.7, 1.7, 1.8 ppm while LC(90) values were 3.7, 3.7 and 3.8 ppm respectively. Further no significant difference in LC(50) and LC(90) values of the formulation was observed against Ae. aegypti during 18 months storage period at room temperature. An application of the formulation at the rate of 140 mg a.i./m(2) in different breeding sites under natural

Design of lipid-based formulations for oral administration of poorly water-soluble drug fenofibrate: effects of digestion.

PubMed

Mohsin, Kazi

2012-06-01

Lipid-based drug carriers are likely to have influence on bioavailability through enhanced solubilization of the drug in the gastrointestinal tract. The study was designed to investigate the lipid formulation digestibility in the simulated gastro intestinal media. Fenofibrate was formulated in representative Type II, IIIA, IIIB and IV self-emulsifying/microemulsifying lipid delivery systems (SEDDS and SMEDDS designed for oral administration) using various medium-chain glyceride components, non-ionic surfactants and cosolvents as excipients. Soybean oil was used only as an example of long-chain triglycerides to compare the effects of formulation with their counterparts. The formulations were subjected to in vitro digestion specifically to predict the fate of the drug in the gastro intestinal tract after exposure of the formulation to pancreatic enzymes and bile. In vitro digestion experiments were carried out using a pH-stat maintained at pH 7.5 for 30 min using intestinal fluids simulating the fed and fasted states. The digestion rate was faster and almost completed in Type II and IIIA systems. Most of the surfactants used in the studies are digestible. However, the high concentration of surfactant and/or cosolvent used in Type IIIB or IV systems lowered the rate of digestion. The digestion of medium-chain triglycerides was faster than long-chain triglycerides, but kept comparatively less drug in the post digestion products. Medium-chain mixed glycerides are good solvents for fenofibrate as rapidly digested but to improve fenofibrate concentration in post digestion products the use of long-chain mixed glycerides are suggested for further investigations.

Design and evaluation of self-emulsifying drug delivery systems of Rhizoma corydalis decumbentis extracts.

PubMed

Ma, Hongda; Zhao, Qingchun; Wang, Yongjun; Guo, Tao; An, Ye; Shi, Guobing

2012-10-01

To improve the dissolution and oral absorption of Rhizoma corydalis decumbentis extracts (RCDE), a famous traditional Chinese herbal medicine which contains poorly water-soluble active components, self-emulsifying drug-delivery systems (SEDDS) were designed and evaluated in vitro and in vivo for the first time. Six formulations were prepared, and pseudoternary phase diagrams were constructed to identify the efficient self-emulsication region through the modified visual test. The optimized formulation consisted of 45% Solutol, 40% ethyl oleate, and 15% Transcutol P. The mean droplet size distribution of the optimized SEDDS was less than 100 nm. The release of the active components (protopine and tetrahydropalmatine) in RCDE from SEDDS hard gelatin capsules showed a faster rate in comparison with the commercial tablets. After oral administration of RCDE SEDDS capsules or the commercial tablets to fasted rats, the relative bioavailability of SEDDS capsules for protopine and tetrahydropalmatine was 209.7% and 133.2% compared with commercial tablets, respectively. Our study indicated that SEDDS has the potential to improve the bioavailability of traditional Chinese medicines, in which many active components are hydrophobic, such as RCDE.

Stabilization of a non-aqueous self-double-emulsifying delivery system of rutin by fat crystals and nonionic surfactants: preparation and bioavailability study.

PubMed

Wang, Qiang; Huang, Juan; Hu, Caibiao; Xia, Nan; Li, Tong; Xia, Qiang

2017-07-19

Literature examples of non-aqueous Pickering emulsions stabilized by fat crystals are very rare. Moreover, the applications of rutin are limited due to its low solubility in both water and oils (less than 0.10 mg g -1 and 0.25 mg g -1 , respectively). Thus, herein, we developed an optimum formulation of a non-aqueous self-double-emulsifying delivery system (SDEDS) containing rutin and evaluated its oral bioavailability. The new formulation stabilized by fat crystals (glycerol monostearate, GMS) and nonionic surfactants was prepared via a two-step emulsification process. The presence of a mixture of GMS crystals and nonionic surfactants effectively improves the stability of the emulsions. The non-aqueous SDEDS spontaneously forms oil-in-oil-in-water (O/O/W) double emulsions in the gastrointestinal environment with the inner oil phase mainly containing the active ingredients. It is stable at both 4 °C and 25 °C for 30 days and could enhance the dissolution properties of the active ingredients. Furthermore, the protection of rutin against digestion-mediated precipitation was observed when the formulation contained a high concentration of GMS crystals. The oral absolute bioavailability of rutin obtained from SDEDS (8.62%) is 1.76-fold higher than that of the actives suspension (4.90%). Thus, the non-aqueous SDEDS is an attractive candidate for the encapsulation of water-insoluble and simultaneously oil-insoluble nutrients (such as rutin) and for use in oral delivery applications.

Resveratrol self-emulsifying system increases the uptake by endothelial cells and improves protection against oxidative stress-mediated death.

PubMed

Amri, Ahmed; Le Clanche, Solenn; Thérond, Patrice; Bonnefont-Rousselot, Dominique; Borderie, Didier; Lai-Kuen, René; Chaumeil, Jean-Claude; Sfar, Souad; Charrueau, Christine

2014-04-01

The aim of the present study was to develop and characterize a resveratrol self-emulsifying drug delivery system (Res-SEDDS), and to compare the uptake of resveratrol by bovine aortic endothelial cells (BAECs), and the protection of these cells against hydrogen peroxide-mediated cell death, versus a control resveratrol ethanolic solution. Three Res-SEDDSs were prepared and evaluated. The in vitro self-emulsification properties of these formulations, the droplet size and the zeta potential of the nanoemulsions formed on adding them to water under mild agitation conditions were studied, together with their toxicity on BAECs. An optimal atoxic formulation (20% Miglyol® 812, 70% Montanox® 80, 10% ethanol 96% v/v) was selected and further studied. Pre-incubation of BAECs for 180 min with 25 μM resveratrol in the nanoemulsion obtained from the selected SEDDS significantly increased the membrane and intracellular concentrations of resveratrol (for example, 0.076±0.015 vs. ethanolic solution 0.041±0.016 nmol/mg of protein after 60 min incubation, p<0.05). Resveratrol intracellular localization was confirmed by fluorescence confocal microscopy. Resveratrol nanoemulsion significantly improved the endothelial cell protection from H2O2-induced injury (750, 1000 and 1500 μM H2O2) in comparison with incubation with the control resveratrol ethanolic solution (for example, 55±6% vs. 38±5% viability after 1500 μM H2O2 challenge, p<0.05). In conclusion, formulation of resveratrol as a SEDDS significantly improved its cellular uptake and potentiated its antioxidant properties on BAECs. Copyright © 2013 Elsevier B.V. All rights reserved.

Physical properties of ice cream containing milk protein concentrates.

PubMed

Alvarez, V B; Wolters, C L; Vodovotz, Y; Ji, T

2005-03-01

Two milk protein concentrates (MPC, 56 and 85%) were studied as substitutes for 20 and 50% of the protein content in ice cream mix. The basic mix formula had 12% fat, 11% nonfat milk solids, 15% sweetener, and 0.3% stabilizer/emulsifier blend. Protein levels remained constant, and total solids were compensated for in MPC mixes by the addition of polydextrose. Physical properties investigated included apparent viscosity, fat globule size, melting rate, shape retention, and freezing behavior using differential scanning calorimetry. Milk protein concentrate formulations had higher mix viscosity, larger amount of fat destabilization, narrower ice melting curves, and greater shape retention compared with the control. Milk protein concentrates did not offer significant modifications of ice cream physical properties on a constant protein basis when substituted for up to 50% of the protein supplied by nonfat dry milk. Milk protein concentrates may offer ice cream manufacturers an alternative source of milk solids non-fat, especially in mixes reduced in lactose or fat, where higher milk solids nonfat are needed to compensate other losses of total solids.

Cast Stone Formulation At Higher Sodium Concentrations

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

Fox, K. M.; Roberts, K. A.; Edwards, T. B.

2013-09-17

A low temperature waste form known as Cast Stone is being considered to provide supplemental Low Activity Waste (LAW) immobilization capacity for the Hanford site. Formulation of Cast Stone at high sodium concentrations is of interest since a significant reduction in the necessary volume of Cast Stone and subsequent disposal costs could be achieved if an acceptable waste form can be produced with a high sodium molarity salt solution combined with a high water to premix (or dry blend) ratio. The objectives of this study were to evaluate the factors involved with increasing the sodium concentration in Cast Stone, includingmore » production and performance properties and the retention and release of specific components of interest. Three factors were identified for the experimental matrix: the concentration of sodium in the simulated salt solution, the water to premix ratio, and the blast furnace slag portion of the premix. The salt solution simulants used in this study were formulated to represent the overall average waste composition. The cement, blast furnace slag, and fly ash were sourced from a supplier in the Hanford area in order to be representative. The test mixes were prepared in the laboratory and fresh properties were measured. Fresh density increased with increasing sodium molarity and with decreasing water to premix ratio, as expected given the individual densities of these components. Rheology measurements showed that all of the test mixes produced very fluid slurries. The fresh density and rheology data are of potential value in designing a future Cast Stone production facility. Standing water and density gradient testing showed that settling is not of particular concern for the high sodium compositions studied. Heat of hydration measurements may provide some insight into the reactions that occur within the test mixes, which may in turn be related to the properties and performance of the waste form. These measurements showed that increased sodium

Cast Stone Formulation At Higher Sodium Concentrations

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

Fox, K. M.; Edwards, T. A.; Roberts, K. B.

2013-10-02

A low temperature waste form known as Cast Stone is being considered to provide supplemental Low Activity Waste (LAW) immobilization capacity for the Hanford site. Formulation of Cast Stone at high sodium concentrations is of interest since a significant reduction in the necessary volume of Cast Stone and subsequent disposal costs could be achieved if an acceptable waste form can be produced with a high sodium molarity salt solution combined with a high water to premix (or dry blend) ratio. The objectives of this study were to evaluate the factors involved with increasing the sodium concentration in Cast Stone, includingmore » production and performance properties and the retention and release of specific components of interest. Three factors were identified for the experimental matrix: the concentration of sodium in the simulated salt solution, the water to premix ratio, and the blast furnace slag portion of the premix. The salt solution simulants used in this study were formulated to represent the overall average waste composition. The cement, blast furnace slag, and fly ash were sourced from a supplier in the Hanford area in order to be representative. The test mixes were prepared in the laboratory and fresh properties were measured. Fresh density increased with increasing sodium molarity and with decreasing water to premix ratio, as expected given the individual densities of these components. Rheology measurements showed that all of the test mixes produced very fluid slurries. The fresh density and rheology data are of potential value in designing a future Cast Stone production facility. Standing water and density gradient testing showed that settling is not of particular concern for the high sodium compositions studied. Heat of hydration measurements may provide some insight into the reactions that occur within the test mixes, which may in turn be related to the properties and performance of the waste form. These measurements showed that increased sodium

Cast Stone Formulation At Higher Sodium Concentrations

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

Fox, K. M.; Roberts, K. A.; Edwards, T. B.

2014-02-28

A low temperature waste form known as Cast Stone is being considered to provide supplemental Low Activity Waste (LAW) immobilization capacity for the Hanford site. Formulation of Cast Stone at high sodium concentrations is of interest since a significant reduction in the necessary volume of Cast Stone and subsequent disposal costs could be achieved if an acceptable waste form can be produced with a high sodium molarity salt solution combined with a high water to premix (or dry blend) ratio. The objectives of this study were to evaluate the factors involved with increasing the sodium concentration in Cast Stone, includingmore » production and performance properties and the retention and release of specific components of interest. Three factors were identified for the experimental matrix: the concentration of sodium in the simulated salt solution, the water to premix ratio, and the blast furnace slag portion of the premix. The salt solution simulants used in this study were formulated to represent the overall average waste composition. The cement, blast furnace slag, and fly ash were sourced from a supplier in the Hanford area in order to be representative. The test mixes were prepared in the laboratory and fresh properties were measured. Fresh density increased with increasing sodium molarity and with decreasing water to premix ratio, as expected given the individual densities of these components. Rheology measurements showed that all of the test mixes produced very fluid slurries. The fresh density and rheology data are of potential value in designing a future Cast Stone production facility. Standing water and density gradient testing showed that settling is not of particular concern for the high sodium compositions studied. Heat of hydration measurements may provide some insight into the reactions that occur within the test mixes, which may in turn be related to the properties and performance of the waste form. These measurements showed that increased sodium

Manufacturing of High-Concentration Monoclonal Antibody Formulations via Spray Drying-the Road to Manufacturing Scale.

PubMed

Gikanga, Benson; Turok, Robert; Hui, Ada; Bowen, Mayumi; Stauch, Oliver B; Maa, Yuh-Fun

2015-01-01

Spray-dried monoclonal antibody (mAb) powders may offer applications more versatile than the freeze-dried cake, including preparing high-concentration formulations for subcutaneous administration. Published studies on this topic, however, are generally scarce. This study evaluates a pilot-scale spray dryer against a laboratory-scale dryer to spray-dry multiple mAbs in consideration of scale-up, impact on mAb stability, and feasibility of a high-concentration preparation. Under similar conditions, both dryers produced powders of similar properties-for example, water content, particle size and morphology, and mAb stability profile-despite a 4-fold faster output by the pilot-scale unit. All formulations containing arginine salt or a combination of arginine salt and trehalose were able to be spray-dried with high powder collection efficiency (>95%), but yield was adversely affected in formulations with high trehalose content due to powder sticking to the drying chamber. Spray-drying production output was dictated by the size of the dryer operated at an optimal liquid feed rate. Spray-dried powders could be reconstituted to high-viscosity liquids, >300 cP, substantially beyond what an ultrafiltration process can achieve. The molar ratio of trehalose to mAb needed to be reduced to 50:1 in consideration of isotonicity of the formulation with mAb concentration at 250 mg/mL. Even with this low level of sugar protection, long-term stability of spray-dried formulations remained superior to their liquid counterparts based on size variant and potency data. This study offers a commercially viable spray-drying process for biological bulk storage and an option for high-concentration mAb manufacturing. This study evaluates a pilot-scale spray dryer against a laboratory-scale dryer to spray-dry multiple monoclonal antibodies (mAbs) from the perspective of scale-up, impact on mAb stability, and feasibility of a high-concentration preparation. The data demonstrated that there is no

Hierarchical Cluster Formation in Concentrated Monoclonal Antibody Formulations

NASA Astrophysics Data System (ADS)

Godfrin, P. Douglas; Zarzar, Jonathan; Zarraga, Isidro Dan; Porcar, Lionel; Falus, Peter; Wagner, Norman; Liu, Yun

Reversible cluster formation has been identified as an underlying cause of large solution viscosities observed in some concentrated monoclonal antibody (mAb) formulations. As high solution viscosity prevents the use of subcutaneous injection as a delivery method for some mAbs, a fundamental understanding of the interactions responsible for high viscosities in concentrated mAb solutions is of significant relevance to mAb applications in human health care as well as of intellectual interest. Here, we present a detailed investigation of a well-studied IgG1 based mAb to relate the short time dynamics and microstructure to significant viscosity changes over a range of pharmaceutically relevant physiochemical conditions. Using a combination of experimental techniques, it is found that upon adding Na2SO4, these antibodies dimerize in solution. Proteins form strongly bounded reversible dimers at dilute concentrations that, when concentrated, interact with each other to form loosely bounded, large, transient clusters. The combined effect of forming strongly bounded dimers and a large transient network is a significant increase in the solution viscosity. Strongly bounded, reversible dimers may exist in many IgG1 based mAb systems such that these results contribute to a more comprehensive understanding of the physical mechanisms producing high viscosities in concentrated protein solutions.

Effectiveness of partially hydrolyzed rice glutelin as a food emulsifier: Comparison to whey protein.

PubMed

Xu, Xingfeng; Zhong, Junzhen; Chen, Jun; Liu, Chengmei; Luo, Liping; Luo, Shunjing; Wu, Lixin; McClements, David Julian

2016-12-15

The emulsifying properties of partially hydrolyzed rice glutelin (H-RG, 2% degree of hydrolysis) were compared to those of whey isolate protein (WPI), a commonly used protein-based emulsifier. The surface load of WPI (1% emulsifier, d32=167.5nm) was 2.8 times lower than that of H-RG (3% emulsifier, d32=159.0nm). Emulsions containing WPI-coated lipid droplets had better stability to pH changes (2-8), NaCl addition (0-500mM) and thermal processing (30-90°C, 0 or 200mM NaCl). Nevertheless, H-RG emulsions were stable over a range of conditions: pH 6-8; NaCl≤200 (pH 7); temperatures≤90°C in the absence of salt (pH 7); and temperatures≤50°C in the presence of 200mM NaCl (pH 7). This study indicates that H-RG may be utilized as a natural emulsifier in the development of label-friendly emulsion-based food products, but that further work is needed to increase the range of applications. Copyright © 2016. Published by Elsevier Ltd.

High concentration biotherapeutic formulation and ultrafiltration: Part 1 pressure limits.

PubMed

Lutz, Herb; Arias, Joshua; Zou, Yu

2017-01-01

High therapeutic dosage requirements and the desire for ease of administration drive the trend to subcutaneous administration using delivery systems such as subcutaneous pumps and prefilled syringes. Because of dosage volume limits, prefilled syringe administration requires higher concentration liquid formulations, limited to about 30 cP or roughly 100-300 g L -1 for mAb's. Ultrafiltration (UF) processes are routinely used to formulate biological therapeutics. This article considers pressure constraints on the UF process that may limit its ability to achieve high final product concentrations. A system hardware analysis shows that the ultrafiltration cassette pressure drop is the major factor limiting UF systems. Additional system design recommendations are also provided. The design and performance of a new cassette with a lower feed channel flow resistance is described along with 3D modeling of feed channel pressure drop. The implications of variations in cassette flow channel resistance for scaling up and setting specifications are considered. A recommendation for a maximum pressure specification is provided. A review of viscosity data and theory shows that molecular engineering, temperature, and the use of viscosity modifying excipients including pH adjustment can be used to achieve higher concentrations. The combined use of a low pressure drop cassette with excipients further increased final concentrations by 35%. Guidance is provided on system operation to control hydraulics during final concentration. These recommendations should allow one to design and operate systems to routinely achieve the 30 cP target final viscosity capable of delivery using a pre-filled syringe. © 2016 American Institute of Chemical Engineers Biotechnol. Prog., 33:113-124, 2017. © 2016 American Institute of Chemical Engineers.

Formulation Effects and the Off-target Transport of Pyrethroid Insecticides from Urban Hard Surfaces

PubMed Central

Jorgenson, Brant C.; Young, Thomas M.

2010-01-01

Controlled rainfall experiments utilizing drop forming rainfall simulators were conducted to study various factors contributing to off-target transport of off-the-shelf formulated pyrethroid insecticides from concrete surfaces. Factors evaluated included active ingredient, product formulation, time between application and rainfall (set time), and rainfall intensity. As much as 60% and as little as 0.8% of pyrethroid applied could be recovered in surface runoff depending primarily on product formulation, and to a lesser extent on product set time. Resulting wash-off profiles during one-hour storm simulations could be categorized based on formulation, with formulations utilizing emulsifying surfactants rather than organic solvents resulting in unique wash-off profiles with overall higher wash-off efficiency. These higher wash-off efficiency profiles were qualitatively replicated by applying formulation-free neat pyrethroid in the presence of independently applied linear alkyl benzene sulfonate (LAS) surfactant, suggesting that the surfactant component of some formulated products may be influential in pyrethroid wash-off from urban hard surfaces. PMID:20524665

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.

Airborne concentrations of benzene associated with the historical use of some formulations of liquid wrench.

PubMed

Williams, Pamela R D; Knutsen, Jeffrey S; Atkinson, Chris; Madl, Amy K; Paustenbach, Dennis J

2007-08-01

The current study characterizes potential inhalation exposures to benzene associated with the historical use of some formulations of Liquid Wrench under specific test conditions. This product is a multiuse penetrant and lubricant commonly used in a variety of consumer and industrial settings. The study entailed the remanufacturing of several product formulations to have similar physical and chemical properties to most nonaerosol Liquid Wrench formulations between 1960 and 1978. The airborne concentrations of benzene and other constituents during the simulated application of these products were measured under a range of conditions. Nearly 200 breathing zone and area bystander air samples were collected during 11 different product use scenarios. Depending on the tests performed, average airborne concentrations of benzene ranged from approximately 0.2-9.9 mg/m(3) (0.08-3.8 ppm) for the 15-min personal samples; 0.1-8 mg/m(3) (0.04-3 ppm) for the 1-hr personal samples; and 0.1-5.1 mg/m(3) (0.04-2 ppm) for the 1-hr area samples. The 1-hr personal samples encompassed two 15-min product applications and two 15-min periods of standing within 5 to 10 feet of the work area. The measured airborne concentrations of benzene varied significantly based on the benzene content of the formulation tested (1%, 3%, 14%, or 30% v/v benzene) and the indoor air exchange rate but did not vary much with the base formulation of the product or the two quantities of Liquid Wrench used. The airborne concentrations of five other volatile chemicals (ethylbenzene, toluene, total xylenes, cyclohexane, and hexane) were also measured, and the results were consistent with the volatility and concentrations of these chemicals in the product tested. A linear regression analysis of air concentration compared with the chemical mole fraction in the solution and air exchange rate provided a relatively good fit to the data. The results of this study should be useful for evaluating potential inhalation

The Assessment of Red Beet as a Natural Colorant, and Evaluation of Quality Properties of Emulsified Pork Sausage Containing Red Beet Powder during Cold Storage

PubMed Central

Jin, Sang-Keun; Choi, Jung-Seok; Moon, Sung-Sil; Jeong, Jin-Yeon

2014-01-01

The purpose of this study was to assess red beet as a natural colorant in emulsified pork sausage and to investigate the effect of red beet on quality characteristics of emulsified pork sausage during 20 d of cold storage. Red beet was prepared as a powder and a substitute with sodium nitrite at 0.5% and 1.0% levels in emulsified pork sausage. Red beet significantly increased the moisture content and pH (p<0.0001) and affected color traits. Lightness of emulsified pork sausage decreased by the addition of red beet powder (p<0.01), whereas lightness with red beet treatments slightly increased during 20 d of cold storage at 4℃ (p<0.05). Redness dramatically increased with red beet powder (p<0.0001). Color by sensory evaluation also showed a significant effect from red beet addition (p<0.05), whereas the other sensory properties such as flavor, tenderness, juiciness, and overall acceptability were not affected by the addition of red beet powder (p>0.05). Texture and 2-thiobabituric acid reactive substance were also not affected by red beet addition (p>0.05). Therefore, red beet could be a good natural colorant in emulsified pork sausage but it needs additional processing, such as betalain concentration and extraction as a juice, to be used as an antioxidant in meat products. PMID:26761285

Porous polystyrene beads as carriers for self-emulsifying system containing loratadine.

PubMed

Patil, Pradeep; Paradkar, Anant

2006-03-01

The aim of this study was to formulate a self-emulsifying system (SES) containing a lipophilic drug, loratadine, and to explore the potential of preformed porous polystyrene beads (PPB) to act as carriers for such SES. Isotropic SES was formulated, which comprised Captex 200 (63% wt/wt), Cremophore EL (16% wt/wt), Capmul MCM (16% wt/wt), and loratadine (5% wt/wt). SES was evaluated for droplet size, drug content, and in vitro drug release. SES was loaded into preformed and characterized PPB using solvent evaporation method. SES-loaded PPB were evaluated using scanning electron microscopy (SEM) for density, specific surface area (S BET ), loading efficiency, drug content, and in vitro drug release. After SES loading, specific surface area reduced drastically, indicating filling of PPB micropores with SES. Loading efficiency was least for small size (SS) and comparable for medium size (MS) and large size (LS) PPB fractions. In vitro drug release was rapid in case of SS beads due to the presence of SES near to surface. LS fraction showed inadequate drug release owing to presence of deeper micropores that resisted outward diffusion of entrapped SES. Leaching of SES from micropores was the rate-limiting step for drug release. Geometrical features such as bead size and pore architecture of PPB were found to govern the loading efficiency and in vitro drug release from SES-loaded PPB.

Porous polystyrene beads as carriers for self-emulsifying system containing loratadine.

PubMed

Patil, Pradeep; Paradkar, Anant

2006-03-24

The aim of this study was to formulate a self-emulsifying system (SES) containing a lipophilic drug, loratadine, and to explore the potential of preformed porous polystyrene beads (PPB) to act as carriers for such SES. Isotropic SES was formulated, which comprised Captex 200 (63% wt/wt), Cremophore EL (16% wt/wt), Capmul MCM (16% wt/wt), and loratadine (5% wt/wt). SES was evaluated for droplet size, drug content, and in vitro drug release. SES was loaded into preformed and characterized PPB using solvent evaporation method. SES-loaded PPB were evaluated using scanning electron microscopy (SEM) for density, specific surface area (S(BET)), loading efficiency, drug content, and in vitro drug release. After SES loading, specific surface area reduced drastically, indicating filling of PPB micropores with SES. Loading efficiency was least for small size (SS) and comparable for medium size (MS) and large size (LS) PPB fractions. In vitro drug release was rapid in case of SS beads due to the presence of SES near to surface. LS fraction showed inadequate drug release owing to presence of deeper micropores that resisted outward diffusion of entrapped SES. Leaching of SES from micropores was the rate-limiting step for drug release. Geometrical features such as bead size and pore architecture of PPB were found to govern the loading efficiency and in vitro drug release from SES-loaded PPB.

Improved oral absorption of dutasteride via Soluplus®-based supersaturable self-emulsifying drug delivery system (S-SEDDS).

PubMed

Lee, Dong Hoon; Yeom, Dong Woo; Song, Ye Seul; Cho, Ha Ra; Choi, Yong Seok; Kang, Myung Joo; Choi, Young Wook

2015-01-15

A novel supersaturable self-emulsifying drug delivery system (S-SEDDS) was formulated to improve the oral absorption of dutasteride (DTS), a 5α-reductase inhibitor that is poorly water-soluble. A supersaturable system was prepared by employing Soluplus(®) (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer) as a precipitation inhibitor with a conventional SEDDS vehicle consisted of Capryol™ 90, Cremophor(®) EL and Transcutol(®) HP (DTS:SEDDS vehicle:Soluplus(®)=1.0:67.6:10.0 w/v/w). In an in vitro dissolution test in a non-sink condition, the drug dissolution rate from SEDDS was rapidly increased to 72% for an initial period of 5min, but underwent rapid drug precipitation within 2h, decreasing the amount of drug dissolved to one-seventh of its original amount. On the other hand, S-SEDDS resulted in a slower crystallization of DTS by virtue of a precipitation inhibitor, maintaining a 3 times greater dissolution rate after 2h compared to SEDDS. In an in vivo pharmacokinetic study in rats, the S-SEDDS formulation exhibited 3.9-fold greater area-under-curve value than that of the drug suspension and 1.3-fold greater than that of SEDDS. The maximum plasma concentration of S-SEDDS was 5.6- and 2.0-fold higher compared to drug suspension and SEDDS, respectively. The results of this study suggest that the novel supersaturable system may be a promising tool for improving the physicochemical property and oral absorption of the 5α-reductase inhibitor. Copyright © 2014 Elsevier B.V. All rights reserved.

Stability and Oil Migration of Oil-in-Water Emulsions Emulsified by Phase-Separating Biopolymer Mixtures.

PubMed

Yang, Nan; Mao, Peng; Lv, Ruihe; Zhang, Ke; Fang, Yapeng; Nishinari, Katsuyoshi; Phillips, Glyn O

2016-08-01

Oil-in-water (O/W) emulsions with varying concentration of oil phase, medium-chain triglyceride (MCT), were prepared using phase-separating gum arabic (GA)/sugar beet pectin (SBP) mixture as an emulsifier. Stability of the emulsions including emulsion phase separation, droplet size change, and oil migration were investigated by means of visual observation, droplet size analysis, oil partition analysis, backscattering of light, and interfacial tension measurement. It was found that in the emulsions prepared with 4.0% GA/1.0% SBP, when the concentration of MCT was greater than 2.0%, emulsion phase separation was not observed and the emulsions were stable with droplet size unchanged during storage. This result proves the emulsification ability of phase-separating biopolymer mixtures and their potential usage as emulsifiers to prepare O/W emulsion. However, when the concentration of MCT was equal or less than 2.0%, emulsion phase separation occurred after preparation resulting in an upper SBP-rich phase and a lower GA-rich phase. The droplet size increased in the upper phase whereas decreased slightly in the lower phase with time, compared to the freshly prepared emulsions. During storage, the oil droplets exhibited a complex migration process: first moving to the SBP-rich phase, then to the GA-rich phase and finally gathering at the interface between the two phases. The mechanisms of the emulsion stability and oil migration in the phase-separated emulsions were discussed. © 2016 Institute of Food Technologists®

Effectiveness of methoprene, an insect growth regulator, against malaria vectors in Fars, Iran: a field study.

PubMed

Darabi, H; Vatandoost, H; Abaei, M R; Gharibi, O; Pakbaz, F

2011-01-01

Methoprene, an insect growth regulator, was evaluated under field conditions against the main malaria vectors in the Islamic Republic of Iran. The effect of 5, 10 and 20 kg ha(-1) concentration ofmethoprene granule formulation and 100 and 200 mL ha(-1) concentration of EC formulation was measured to determine any changes in Anophelini larval abundance and IE ratio in both rice fields and artificial ponds. In artificial ponds, granular methoprene at a dose of 20 kg ha(-1) inhibited adult emergence by 77.1% after 1 day and 65.9% after 3 days. The emulsifiable concentrate formulation of methoprene at 200 mL ha(-1) inhibited adult emergence by 83.7% after 1 day and 32.2% after 3 days. In rice fields, inhibition of emergence was 44.3% at 20 kg ha(-1) granule and 35.8% for emulsifiable concentrate at 200 mL ha(-1) after 3 days. The results vary depending on the mosquito species, treatment methods, breeding places and type of formulation.

Comparison of the single dose pharmacokinetics, pharmacodynamics, and safety of two novel oral formulations of dimethandrolone undecanoate (DMAU): a potential oral, male contraceptive.

PubMed

Ayoub, R; Page, S T; Swerdloff, R S; Liu, P Y; Amory, J K; Leung, A; Hull, L; Blithe, D; Christy, A; Chao, J H; Bremner, W J; Wang, C

2017-03-01

Dimethandrolone (DMA, 7α,11β-dimethyl-19-nortestosterone) has both androgenic and progestational activities, ideal properties for a male hormonal contraceptive. In vivo, dimethandrolone undecanoate (DMAU) is hydrolyzed to DMA. We showed previously that single oral doses of DMAU powder in capsule taken with food are well tolerated and effective at suppressing both LH and testosterone (T), but absorption was low. We compared the pharmacokinetics and pharmacodynamics of two new formulations of DMAU, in castor oil and in self-emulsifying drug delivery systems (SEDDS), with the previously tested powder formulation. DMAU was dosed orally in healthy adult male volunteers at two academic medical centers. For each formulation tested in this double-blind, placebo-controlled study, 10 men received single, escalating, oral doses of DMAU (100, 200, and 400 mg) and two subjects received placebo. All doses were evaluated for both fasting and with a high fat meal. All three formulations were well tolerated without clinically significant changes in vital signs, blood counts, or serum chemistries. For all formulations, DMA and DMAU showed higher maximum (p < 0.007) and average concentrations (p < 0.002) at the 400 mg dose, compared with the 200 mg dose. The powder formulation resulted in a lower conversion of DMAU to DMA (p = 0.027) compared with both castor oil and SEDDS formulations. DMAU in SEDDS given fasting resulted in higher serum DMA and DMAU concentrations compared to the other two formulations. Serum LH and sex hormone concentrations were suppressed by all formulations of 200 and 400 mg DMAU when administered with food, but only the SEDDS formulation was effectively suppressed serum T when given fasting. We conclude that while all three formulations of oral DMAU are effective and well tolerated when administered with food, DMAU in oil and SEDDS increased conversion to DMA, and SEDDS may have some effectiveness when given fasting. These properties might be

Applications of lipid based formulation technologies in the delivery of biotechnology-based therapeutics.

PubMed

du Plessis, Lissinda H; Marais, Etienne B; Mohammed, Faruq; Kotzé, Awie F

2014-01-01

In the last decades several new biotechnologically-based therapeutics have been developed due to progress in genetic engineering. A growing challenge facing pharmaceutical scientists is formulating these compounds into oral dosage forms with adequate bioavailability. An increasingly popular approach to formulate biotechnology-based therapeutics is the use of lipid based formulation technologies. This review highlights the importance of lipid based drug delivery systems in the formulation of oral biotechnology based therapeutics including peptides, proteins, DNA, siRNA and vaccines. The different production procedures used to achieve high encapsulation efficiencies of the bioactives are discussed, as well as the factors influencing the choice of excipient. Lipid based colloidal drug delivery systems including liposomes and solid lipid nanoparticles are reviewed with a focus on recent advances and updates. We further describe microemulsions and self-emulsifying drug delivery systems and recent findings on bioactive delivery. We conclude the review with a few examples on novel lipid based formulation technologies.

Effects of ultrasound pretreatment on the enzymatic hydrolysis of soy protein isolates and on the emulsifying properties of hydrolysates.

PubMed

Chen, Lin; Chen, Jianshe; Ren, Jiaoyan; Zhao, Mouming

2011-03-23

Soy protein isolate (SPI) was modified by ultrasound pretreatment (200 W, 400 W, 600 W) and controlled papain hydrolysis, and the emulsifying properties of SPIH (SPI hydrolysates) and USPIH (ultrasound pretreated SPIH) were investigated. Analysis of mean droplet sizes and creaming indices of emulsions formed by SPIH and USPIH showed that some USPIH had markedly improved emulsifying capability and emulsion stabilization against creaming during quiescent storage. Compared with control SPI and SPIH-0.58% degree of hydrolysis (DH), USPIH-400W-1.25% (USPIH pretreated under 400W sonication and hydrolyzed to 1.25% DH) was capable of forming a stable fine emulsion (d43=1.79 μm) at a lower concentration (3.0% w/v). A variety of physicochemical and interfacial properties of USPIH-400W products have been investigated in relation to DH and emulsifying properties. SDS-PAGE showed that ultrasound pretreatment could significantly improve the accessibility of some subunits (α-7S and A-11S) in soy proteins to papain hydrolysis, resulting in changes in DH, protein solubility (PS), surface hydrophobicity (H0), and secondary structure for USPIH-400W. Compared with control SPI and SPIH-0.58%, USPIH-400W-1.25% had a higher protein adsorption fraction (Fads) and a lower saturation surface load (Γsat), which is mainly due to its higher PS and random coil content, and may explain its markedly improved emulsifying capability. This study demonstrated that combined ultrasound pretreatment and controlled enzymatic hydrolysis could be an effective method for the functionality modification of globular proteins.

Formulation and Stabilization of Concentrated Edible Oil-in-Water Emulsions Based on Electrostatic Complexes of a Food-Grade Cationic Surfactant (Ethyl Lauroyl Arginate) and Cellulose Nanocrystals.

PubMed

Bai, Long; Xiang, Wenchao; Huan, Siqi; Rojas, Orlando J

2018-05-14

We report on high-internal-phase, oil-in-water Pickering emulsions that are stable against coalescence during storage. Viscous, edible oil (sunflower) was emulsified by combining naturally derived cellulose nanocrystals (CNCs) and a food-grade, biobased cationic surfactant obtained from lauric acid and L-arginine (ethyl lauroyl arginate, LAE). The interactions between CNC and LAE were elucidated by isothermal titration calorimetry (ITC) and supplementary techniques. LAE adsorption on CNC surfaces and its effect on nanoparticle electrostatic stabilization, aggregation state, and emulsifying ability was studied and related to the properties of resultant oil-in-water emulsions. Pickering systems with tunable droplet diameter and stability against oil coalescence during long-term storage were controllably achieved depending on LAE loading. The underlying stabilization mechanism was found to depend on the type of complex formed, the LAE structures adsorbed on the cellulose nanoparticles (as unimer or as adsorbed admicelles), the presence of free LAE in the aqueous phase, and the equivalent alkane number of the oil phase (sunflower and dodecane oils were compared). The results extend the potential of CNC in the formulation of high-quality and edible Pickering emulsions. The functional properties imparted by LAE, a highly effective molecule against food pathogens and spoilage organisms, open new opportunities in food, cosmetics, and pharmaceutical applications, where the presence of CNC plays a critical role in achieving synergistic effects with LAE.

Effect of tartarate and citrate based food additives on the micellar properties of sodium dodecylsulfate for prospective use as food emulsifier.

PubMed

Banipal, Tarlok S; Kaur, Harjinder; Kaur, Amanpreet; Banipal, Parampaul K

2016-01-01

Citrate and tartarate based food preservatives can be used to enhance the emulsifying properties of sodium dodecylsulfate (SDS) based micellar system and thus making it appropriate for food applications. Exploration of interactions between the two species is the key constraint for execution of such ideas. In this work various micellar and thermodynamic parameters of SDS like critical micellar concentration (CMC), standard Gibbs free energy of micellization (ΔG(0)mic.) etc. have been calculated in different concentrations of disodium tartarate (DST) and trisodium citrate (TSC) in the temperature range (288.15-318.15)K from the conductivity and surface tension measurements. The parameters obtained from these studies reveal the competitive nature of both the additives with SDS for available positions at the air/water interface. TSC is found to be more effective additive in order to make SDS micellar system better for its potential applications as food emulsifier. Copyright © 2015 Elsevier Ltd. All rights reserved.

Pharmacokinetics of a concentrated buprenorphine formulation in red-tailed hawks (Buteo jamaicensis).

PubMed

Gleeson, Molly D; Guzman, David Sanchez-Migallon; Knych, Heather K; Kass, Philip H; Drazenovich, Tracy L; Hawkins, Michelle G

2018-01-01

OBJECTIVE To determine the pharmacokinetics and sedative effects of 2 doses of a concentrated buprenorphine formulation after SC administration to red-tailed hawks (Buteo jamaicensis). ANIMALS 6 adult red-tailed hawks. PROCEDURES Concentrated buprenorphine (0.3 mg/kg, SC) was administered to all birds. Blood samples were collected at 10 time points over 24 hours after drug administration to determine plasma buprenorphine concentrations. After a 4-week washout period, the same birds received the same formulation at a higher dose (1.8 mg/kg, SC), and blood samples were collected at 13 time points over 96 hours. Hawks were monitored for adverse effects and assigned agitation-sedation scores at each sample collection time. Plasma buprenorphine concentrations were quantified by liquid chromatography-tandem mass spectrometry. RESULTS Mean time to maximum plasma buprenorphine concentration was 7.2 minutes and 26.1 minutes after administration of the 0.3-mg/kg and 1.8-mg/kg doses, respectively. Plasma buprenorphine concentrations were > 1 ng/mL for mean durations of 24 and 48 hours after low- and high-dose administration, respectively. Mean elimination half-life was 6.23 hours for the low dose and 7.84 hours for the high dose. Mean agitation-sedation scores were higher (indicating some degree of sedation) than the baseline values for 24 hours at both doses. No clinically important adverse effects were observed. CONCLUSIONS AND CLINICAL RELEVANCE Concentrated buprenorphine was rapidly absorbed, and plasma drug concentrations considered to have analgesic effects in other raptor species were maintained for extended periods. Most birds had mild to moderate sedation. Additional studies are needed to evaluate the pharmacodynamics of these doses of concentrated buprenorphine in red-tailed hawks.

Using Cellulose Nanofibers and Its Palm Oil Pickering Emulsion as Fat Substitutes in Emulsified Sausage.

PubMed

Wang, Yanan; Wang, Wenhang; Jia, Hongjiao; Gao, Guixian; Wang, Xiao; Zhang, Xiaowei; Wang, Yabin

2018-06-01

Nano cellulose is attracting great interest in food and nutraceutical fields and also provides a potential additive to develop functional meat products such as low fat sausage. Here, we compared 1 wt% aqueous dispersion of cellulose nanofiber (CNF) and its palm oil Pickering emulsion (CPOE) at the ratio of 1:1 (water: oil, v:v) for being fat alternatives replacing 30% and 50% of the original fat of the emulsified sausage. Replacing fat by CPOE and CNF resulted in lower fat content, lower cooking loss and higher moisture content and higher lightness values (P ≤ 0.05) at both fat levels. Textural analysis indicated that the products formulated with CPOE showed higher hardness, springiness, chewiness and the texture was enhanced by the addition of CNF, especially when 30% fat was substituted. Compared with the full-fat control, the sausages formulated with CPOE became more elastic and compact, especially by the incorporation of CNF according to the rheology and scanning electron microscope results. The reformulated products with CPOE and CNF at the 30% level showed higher sensory scores (P ≤ 0.05) while at the 50% level produced comparable quality to the control, but no significant differences were found in the overall acceptability. In summary, CNF and its Pickering emulsion provide the potential as potential fat alternatives for developing low fat meat products. Cellulose nanofibers present a variety of distinguishing properties, such as large surface area, great stability and high strength. The ability to stabilize emulsions and good biocompatibility enlarge its application in food. In this study, we attempted to use cellulose nanofibers and its palm oil Pickering emulsion as fat substitutes to partly replace the original fat of pork emulsified sausages, hoping to provide some basic information for using cellulose nanofibers and its Pickering emulsion as fat substitute to high fiber, low fat meat products. © 2018 Institute of Food Technologists®.

Emulsifier for intravenous cyclosporin inhibits neurite outgrowth, causes deficits in rapid axonal transport and leads to structural abnormalities in differentiating N1E.115 neuroblastoma.

PubMed

Brat, D J; Windebank, A J; Brimijoin, S

1992-05-01

The emulsifier for cyclosporin in clinical i.v. formulations, Cremophor EL, has recently come into question as a possible source of neurotoxic side effects in immunosuppressant therapy. To address this issue we tested Cremophor EL and cyclosporin on an in vitro neuronal model, the differentiating N1E.115 neuroblastoma cell. In terms of effects on elaboration of neurites by these cells, Cremophor accounted for nearly all the neurotoxicity of clinically formulated cyclosporin. At a concentration of 0.005% (v/v), Cremophor EL halved the number of cells that extended neurites after 48 hr in serum-free medium. Average neurite length was also reduced substantially. Inhibition of neurite outgrowth first became apparent 24 hr after exposure to Cremophor EL. Neurites that did grow in the presence of Cremophor were disfigured by a series of regularly spaced, gross dilatations (beads) filled with large (0.2-0.5 microns) lipid vesicles. Abnormalities of rapid axonal transport were documented in the beaded neurites by means of video-enhanced contrast, differential interference-contrast microscopy. Velocity of retrograde transport remained normal, but the velocity of anterograde transport and the total bidirectional flux of organelles were both reduced. It seems likely that the inhibition of neurite outgrowth, the swellings of the neurites and the abnormalities of transport are interrelated phenomena.

Comparative Emulsifying Properties of Octenyl Succinic Anhydride (OSA)-Modified Starch: Granular Form vs Dissolved State

PubMed Central

Marefati, Ali; Gutiérrez, Gemma; Wahlgren, Marie; Rayner, Marilyn

2016-01-01

The emulsifying ability of OSA-modified and native starch in the granular form, in the dissolved state and a combination of both was compared. This study aims to understand mixed systems of particles and dissolved starch with respect to what species dominates at droplet interfaces and how stability is affected by addition of one of the species to already formed emulsions. It was possible to create emulsions with OSA-modified starch isolated from Quinoa as sole emulsifier. Similar droplet sizes were obtained with emulsions prepared at 7% (w/w) oil content using OSA-modified starch in the granular form or molecularly dissolved but large differences were observed regarding stability. Pickering emulsions kept their droplet size constant after one month while emulsions formulated with OSA-modified starch dissolved exhibited coalescence. All emulsions stabilized combining OSA-modified starch in granular form and in solution showed larger mean droplet sizes with no significant differences with respect to the order of addition. These emulsions were unstable due to coalescence regarding presence of free oil. Similar results were obtained when emulsions were prepared by combining OSA-modified granules with native starch in solution. The degree of surface coverage of starch granules was much lower in presence of starch in solution which indicates that OSA-starch is more surface active in the dissolved state than in granular form, although it led to unstable systems compared to starch granule stabilized Pickering emulsions, which demonstrated to be extremely stable. PMID:27479315

Effect of nonionic compound emulsifiers Tween80 and Span80 on the properties of microencapsulated phase change materials.

PubMed

Zhan, Shiping; Zhou, Zhiyi; Wang, Weijing; Zhao, Qicheng; Hou, Weimin

2014-01-01

In this article, the nonionic compound emulsifiers Tween80 and Span80 were used to prepare microcapsules containing phase change materials (microPCMs) with melamine-formaldehyde (MF) shells by in situ polymerization method. The effects of compound emulsifiers Tween80 and Span80 on the structure, morphologies and properties of microPCMs containing paraffin were studied. SEM morphological investigation suggests that a complex of Tween80 and Span80 as emulsifiers are optimal for the fabrication of microPCMs in this study compared to Tween60 or OP-10. The diameter distributions of microPCMs synthesized with different amounts of compound emulsifiers are uniform, whereas compound emulsifiers' amount affect the mean diameter of microPCMs decreasing from 5.34 to 3.05 µm. These microPCMs with the core/shell weight ratio 3/1 have smoother surface and a higher core content of 68.7% than other core/shell ratio. Anti-osmosis measurements indicate that microPCMs have good compactness and stable performance compared to those synthesized by one type of emulsifier.

Mitigation of NOx and smoke emissions in a diesel engine using novel emulsified lemon peel oil biofuel.

PubMed

Bragadeshwaran, Ashok; Kasianantham, Nanthagopal; Balusamy, Saravanan; Muniappan, SenthilKumar; Reddy, Dandu Madhu Sudan; Subhash, Randive Vishal; Pravin, Nashte Adarsh; Subbarao, Rayapati

2018-06-25

Lemon peel oil (LPO) is considered to be a viable alternative fuel for diesel engine applications due to its wider availability, renewable nature, easy extraction process, almost equivalent calorific value as neat diesel, and low viscosity. The present work aims to investigate the effect of novel emulsified LPO in a diesel engine in order to reduce the NOx emission without compromising the engine performance. A new ionic surfactant is introduced in the present study, namely methyl-dihydroxy propyl imidazolium chloride due to its higher hydrophilic-lipophilic balance value which helps to prepare stable water in oil emulsion. Also, Span 80 has been selected as another suitable surfactant for water in oil emulsion. Four emulsified fuel samples have been prepared using LPO, water, and different concentrations of surfactants. All the fuel samples are tested for their stability through gravitational technique for 7 days. Among the emulsified samples, 92% LPO + 5% water + 2% Span 80 + 1% methyl-dihydroxy propyl imidazolium chloride by volume (LPOE2) and 93.5% LPO + 5% water + 1.5% surfactant Span 80 by volume (LPOE4) have showed better stability when compared to other emulsion fuel samples. It is also revealed that the stability of LPO emulsion is improved by the addition of two emulsions. The experimental results showed that the brake thermal efficiency of LPO emulsion is reduced to 29.87 from 34.58% of pure LPO at full load condition. Oxides of nitrogen emission and smoke emission are reduced by 21-32 and 6-15% for the LPO emulsion samples compared to pure LPO. Moreover, the diesel engine operation with emulsified form of LPO increases the HC emission about 0.1 g/kWh for LPOE4 and 0.15 g/kWh for LPOE2 fuels from 0.053 g/kW for pure LPO at maximum power output condition. The reformulation of LPO into emulsified form increases the CO emission by 25-53% compared to pure LPO. Moreover, the reformulation of LPO into emulsions has resulted in lower

Application of Emulsified Zero-Valent Iron to Marine Environments

NASA Technical Reports Server (NTRS)

Brooks, Kathleen B.; Quinn, Jacqueline W.; Clausen, Christian A.; Geiger, Cherie L.

2005-01-01

same oil/surfactant membrane used in EZVI. The removal of cadmium and lead from a seawater matrix is a unique challenge. It requires a system that is resistant to the corrosive nature of seawater while removing specific ions that are in a relatively low concentration compared to naturally occurring seawater salts. Laboratory studies conducted show greater than 99% removal of lead and 96% removal of cadmium from a seawater solution spiked at 5 mg/L that was treated with an Emulsified Zero-Valent Metal (EZVM). The cadmium and lead are removed from the solution as they transport across the emulsion membrane and plate out onto the zero-valent metal surface.

Polycyclic aromatic hydrocarbon-emulsifier protein produced by Aspergillus brasiliensis (niger) in an airlift bioreactor following an electrochemical pretreatment.

PubMed

Sánchez-Vázquez, Victor; Shirai, Keiko; González, Ignacio; Gutiérrez-Rojas, Mariano

2018-05-01

An emulsifier protein (EP) was produced and easily separated from oil-contaminated water as an economical substrate when Aspergillus brasiliensis, pretreated in a solid state culture with a controlled electric field, was used in an airlift bioreactor. The hydrocarbon-EP comprised 19.5% of the total protein, its purification enhanced the specific emulsifying activity (EA) seven times. The influence of operational conditions (pH and salt concentration) on the EA were assessed to characterise the emulsion stability. The EA was increased by 19% in alkaline environments (pH 7-11), but it was not affected by the presence of salt (0-35 g L -1 ). On the other hand, preheating the EP samples (60 °C) enhanced the EA by 2.5 times. Based on analysis of its EA, this EP can be applied as a bioremediation enhancer in contaminated soils. Copyright © 2018 Elsevier Ltd. All rights reserved.

Effects of high hydrostatic pressure on secondary structure and emulsifying behavior of sweet potato protein

NASA Astrophysics Data System (ADS)

Mehmood Khan, Nasir; Mu, Tai-Hua; Sun, Hong-Nan; Zhang, Miao; Chen, Jing-Wang

2015-04-01

In this study, secondary structures of sweet potato protein (SPP) after high hydrostatic pressure (HHP) treatment (200-600 MPa) were evaluated and emulsifying properties of emulsions with HHP-treated SPP solutions in different pH values (3, 6, and 9) were investigated. Circular dichroism analysis confirmed the modification of the SPP secondary structure. Surface hydrophobicity increased at pH 3 and decreased at 6 and 9. Emulsifying activity index at pH 6 increased with an increase in pressure, whereas emulsifying stability index increased at pH 6 and 9. Oil droplet sizes decreased, while volume frequency distribution of the smaller droplets increased at pH 3 and 6 with the HHP treatment. Emulsion viscosity increased at pH 6 and 9 and pseudo-plastic flow behaviors were not altered for all emulsions produced with HHP-treated SPP. These results suggested that HHP could modify the SPP structure for better emulsifying properties, which could increase the use of SPP emulsion in the food industry.

Influence of Emulsified Asphalt on the Mechanical Property and Microstructure of Cement-Stabilized Gravel under Freezing and Thawing Cycle Conditions.

PubMed

Wang, Yiqi; Tan, Yiqiu; Guo, Meng; Wang, Xinglong

2017-05-06

Properties of cement-stabilized gravel modified by emulsified asphalt under freezing and thawing cycle conditions were investigated by adjusting the dosage of cement. Mercury intrusion porosimetry (MIP) and Scanning electron microscopy (SEM) were introduced to analyze the influential mechanism. The results indicate that cement emulsified asphalt stabilized gravel with 5 wt % of cement performed well in both mechanics and frost-resistance. Although the addition of emulsified asphalt would lead to a partial decrease of strength, it can extend the process of strength loss and improve the freezing resistance. The main reason for this is that the permeability can be improved by the filling effects of emulsified asphalt. The frost-heave stress caused by the phase transition of water can also be remitted by emulsified asphalt, the elasticity modulus of which is much lower than the matrix. The generating speed of the micro crack can also be slowed down by emulsified asphalt.

Improvement of solubility, dissolution and stability profile of artemether solid dispersions and self emulsified solid dispersions by solvent evaporation method.

PubMed

Tayyab Ansari, Muhammad; Arshad, Muhammad Sohail; Hussain, Altaf; Ahmad, Zeeshan

2016-12-08

The purpose of this study was to investigate changes in the water solubility of artemether; a poorly soluble drug used for the treatment of malaria. Different solid dispersions (SDs) of artemether were prepared using artemether and polyethylene glycol 6000 at ratio 12:88 (Group 1), self-emulsified solid dispersions (SESDs) containing artemether, polyethylene glycol 6000, cremophor-A-25, olive oil, hydroxypropylmethylcellulose and transcutol in the ratio 12:75:5:4:2:2, respectively (Group 2). SESDs were also prepared by substituting cremophor-A-25 in Group 2 with poloxamer 188 (noted as Group 3). Each of these preparations was formulated using physical mixing and the solvent evaporation method. Aqueous solubility of artemether improved 11-, 95- and 102-fold, while dissolution (in simulated gastric fluid) increased 3-, 13- and 14-fold, for formulation groups 1, 2 and 3, respectively. X-ray diffraction patterns of SDs indicated a decrease in peak intensities at 10° implying reduced artemether crystallinity. Scanning electron micrographs invariably revealed embedment of artemether by various excipients and a glassy appearance for solvent evaporated mixtures for all three formulation Groups. Our findings indicate improved hydrophilic interactions for drug particles yield greater solubility and dissolution in the following order for artemether formulating methods: solvent evaporation mixtures > physical mixtures > pure artemether.

Development of edible films obtained from submicron emulsions based on whey protein concentrate, oil/beeswax and brea gum.

PubMed

Cecchini, Juan Pablo; Spotti, María J; Piagentini, Andrea M; Milt, Viviana G; Carrara, Carlos R

2017-06-01

Edible films with whey protein concentrate (WPC) with a lipid component, sunflower oil (O) or beeswax (W), to enhance barrier to water vapor were obtained. Brea gum was used as emulsifier and also as matrix component. In order to achieve emulsion with small and homogeneous droplet size, an ultrasonicator equipment was used after obtaining a pre-emulsion using a blender. The films were made by casting. Effects of lipid fraction on droplet size, zeta potential, mechanical properties, water vapor permeability (WVP), solubility, and optical properties were determined. The droplet size of emulsions with BG decreased when decreasing the lipid content in the formulation. The zeta potential was negative for all the formulations, since the pH was close to 6 for all of them and pI of BG is close to 2.5, and pI of ß-lactoglobulin and α-lactalbumin (main proteins in WPC) are 5.2 and 4.1, respectively. Increasing W or SO content in blended films reduced the tensile strength and puncture resistance significantly. BG and WPC films without lipid presented better mechanical properties. The presence of lipids decreased the WVP, as expected, and those films having BG improved this property. BG films were slightly amber as a result of the natural color of the gum. BG has shown to be a good polysaccharide for emulsifying the lipid fraction and improving the homogeneity and mechanical properties of the films with WPC and beeswax or oil.

Surface Enrichment by Conventional and Polymerizable Sulfated Nonylphenol Ethoxylate Emulsifiers in Water-Based Pressure-Sensitive Adhesive

Treesearch

Jilin Zhang; Yuxi Zhao; Matthew R. Dubay; Steven J. Severtson; Larry E. Gwin; Carl J. Houtman

2013-01-01

Comparisons of properties are made for pressure-sensitive adhesives (PSAs) generated via emulsion polymerization using both conventional and reactive emulsifiers. The emulsifiers are ammonium salts of sulfated nonylphenol ethoxylates with similar chemical structures and hydrophilic−lipophilic balances. The polymerizable surfactant possesses a reactive double...

Biopharmaceutical insights of particulate emulsified systems - a prospective overview.

PubMed

Katamreddy, Jyothshna Devi; Yalavarthi, Prasanna Raju; D, Subba Rao; Battu, Sowjanya; Peesa, Jaya Preethi

2018-05-10

During the twenty-first century, drug discovery is expanding rapidly and a large number of chemical moieties are recognized. Many of them are poorly soluble and hence related biopharmaceutical constraints are to be addressed systematically. Among novel approaches to resolving biopharmaceutical issues, micro- and nano-emulsified systems serve as the best strategy for delivering both hydrophobic and hydrophilic drugs owing to their greater solubilization and transportation capabilities. Of late, the unique physical and biopharmaceutical properties of these liquid isotropic homogenous systems have gained substantive research importance. In addition nano/micro lipid systems share structural and functional similarity with that of the physiological lipids which offer better tolerance ability in the body. In this context, this article provides information on the historical emergence of particulate emulsified systems, importance and rationale of selection of carriers. It also encompasses the physicochemical principles that are responsible for the elevation of therapeutic outcomes of delivery systems. Detailed and schematic absorption of these drug delivery systems is explained here. Gastro-intestinal biochemistry necessary in the understanding of digestion process, lipolytic products formed, micellar structures, enzymes, transporters, mechanism of cell uptake involved after subsequent oral absorption are also emphasized. In addition, this article also explains disposition and pharmacokinetic properties of emulsified systems with real-time therapeutic research outcomes. The influence of biochemical compositions and biopharmaceutical principles on absorption and disposition patterns of ME/NEs was described in the article for the interest of readers and young researchers.

The effect of prime emulsion components as a function of equilibrium headspace concentration of soursop flavor compounds

PubMed Central

2014-01-01

Background Perceptions of food products start when flavor compounds are released from foods, transported and appropriate senses in the oral and nose are triggered. However, the long-term stability of flavor compounds in food product has been a major concern in the food industry due to the complex interactions between key food ingredients (e.g., polysaccharides and proteins). Hence, this study was conducted to formulate emulsion-based beverage using natural food emulsifiers and to understand the interactions between emulsion compositions and flavor compounds. Results The influences of modified starch (x 1 ), whey protein isolate (x 2 ), soursop flavor oil (x 3 ) and deionized water (x 4 ) on the equilibrium headspace concentration of soursop volatile flavor compounds were evaluated using a four-component with constrained extreme vertices mixture design. The results indicated that the equilibrium headspace concentration of soursop flavor compounds were significantly (p < 0.05) influenced by the matrix and structural compositions of the beverage emulsions. Interface formed using modified starch and whey protein isolate (WPI) proved to be capable of inhibiting the release of volatile flavor compounds from the oil to the aqueous phase. Modified starch could retard the overall flavor release through its hydrophobic interactions with volatile flavor compounds and viscosity enhancement effect. Excessive amount of modified starch was also shown to be detrimental to the stability of emulsion system. However, both modified starch and WPI showed to be a much more effective barrier in inhibiting the flavor release of flavor compounds when used as individual emulsifier than as a mixture. Conclusions Overall, the mixture design can be practical in elucidating the complex interactions between key food components and volatile flavor compounds in an emulsion system. These studies will be useful for the manufacturers for the formulation of an optimum beverage emulsion with

Efficient breaking of water/oil emulsions by a newly isolated de-emulsifying bacterium, Ochrobactrum anthropi strain RIPI5-1.

PubMed

Mohebali, Ghasemali; Kaytash, Ashk; Etemadi, Narges

2012-10-01

Water-oil emulsions occur throughout oil production, transportation, and processing. The breaking of the water/oil emulsion improves oil quality and as a consequence chemically synthesized de-emulsifiers are commonly used in the petroleum industries. Microbial de-emulsifiers represent potential alternatives to the chemicals and may become important products for petroleum industries. The main goal of this work was isolation, identification, and characterization of an efficient de-emulsifying bacterium. Following a multi-step enrichment programme a de-emulsifying bacterium, Ochrobactrum anthropi strain RIPI5-1was isolated from the oil-polluted sandy bank of Siri Island, Iran. The presence of an oil phase in growth medium was found to be unnecessary for production of the de-emulsifier. The de-emulsifying activity of both the whole culture and the cells of this strain was examined using a model multiple water-crude oil (w/o/w) emulsion. This w/o/w emulsion was used for the first time in microbial de-emulsification research. Whole cells of strain RIPI5-1 exhibited high de-emulsifying activity during the late-exponential growth and stationary phases; de-emulsifying activity of the whole culture was highest during the early-exponential growth phase. The time course of de-emulsification by whole culture and whole cells of strain RIPI5-1 was investigated; the initial rate (DeI(1)) of breaking of the multiple water-crude oil emulsion by whole culture and whole cells was calculated as 11% and 54%, respectively. However, overall de-emulsification (DeI(8.5)) for whole culture and whole cells was calculated as 63% and 72%, respectively. A clear correlation was observed between cell surface hydrophobicity and the de-emulsifying activity of whole cells. With the water/kerosene emulsion, emulsion half-life (t(1/2)) was found to be <0.5h. The potential activity of this strain was also explained using a complex oilfield emulsion. Copyright © 2012 Elsevier B.V. All rights reserved.

Egress route of emulsified 20 centistokes silicone oil from anterior chamber of rabbit.

PubMed

Ohira, A; Chihara, E; Soji, T

1994-07-01

Silicone oil is used in recent clinical practice, however, it may cause adverse reactions in the eyes. When the high viscosity silicone oil is contaminated with low molecular weight silicone oil, the contamination may cause ocular toxicity or elevation of the intraocular pressure. To obtain information on the distribution of this preparation, emulsified 20 centistokes silicone oil was injected into the anterior chamber of rabbit eyes. The silicone oil droplets were visualized by light and electron microscopy by using oil soluble phthalocyanine blue. This copper containing dye remains in the tissue after removal of the silicone oil by organic solvents. Two and 4 weeks after an injection, the silicone emulsion was observed as numerous small vacuoles with blue precipitate at the margin of vacuoles within elongated trabecular endothelial cells, fibroblasts along the route of uveoscleral outflow and cells of the iris. Three hours after the injection, only a few vacuoles were present in these cells. These results demonstrated that the emulsified silicone oil leaves the anterior chamber through the conventional and unconventional routes. Phagocytosis by the trabecular endothelial cells and fibroblasts along the uveoscleral route caused an accumulation of the emulsified silicone oil in these cells. With chronic exposure to emulsified silicone oil, changes in the trabecular meshwork may lead to a reduction in the outflow of aqueous humor and cause glaucoma.

Food Emulsifier Glycerin Monostearate Increases Internal Exposure Levels of Six Priority Controlled Phthalate Esters and Exacerbates Their Male Reproductive Toxicities in Rats.

PubMed

Gao, Hai-Tao; Xu, Run; Cao, Wei-Xin; Zhou, Xu; Yan, Ye-Hui-Mei; Lu, Lingeng; Xu, Qian; Shen, Yang

2016-01-01

Human beings are inevitably exposed to ubiquitous phthalate esters (PAEs). Processed, packaged foods are popular nowadays, in which emulsifiers are frequently added as food additives. It is unclear how emulsifiers affect the bioavailability of ingested PAEs contaminants and their toxicities. The purposes of our study were to explore whether food emulsifier Glycerin Monostearate (GMS) could increase the internal exposure levels of six priority controlled PAEs and affect their reproductive toxicities when male rats are exposed to PAEs mixture (MIXPs). The male rats were exposed to MIXPs by gavage for thirty days in combination with or without given GMS. Phthalate monoesters (MPAEs), primary metabolites of PAEs, in rat urine were used as biomarkers to predict the internal exposure levels of the six PAEs, and their concentrations were determined using UPLC-MS. The reproductive toxicity was evaluated using serum testosterone levels test and histopathology of testes. Results showed that compared to PAEs exposure alone, the internal exposure levels of PAEs increased by 30%-49% in the presence of GMS. PAEs exposure led to the reduction of testosterone level by 23.4%-42.1% in the presence and absence of GMS, respectively, compared to the baseline. Testosterone levels in MIXPs+GMS and DEHP+GMS group were decreased by 9.1% and 13.6%, respectively, compared with MIXPs and DEHP group. Histopathology showed that injuries of testis (deciduous spermatids) were observed, and GMS exacerbated the injuries. The results indicated food emulsifiers chronically taken up might increase safety risks of food PAEs contaminants.

Influence of emulsifiers on the characteristics of polyurethane structures used as drug carrier

PubMed Central

2013-01-01

Background Emulsifiers have a significant role in the emulsion polymerization by reducing the interfacial tension thus increasing the stability of colloidal dispersions of polymer nanostructures. This study evaluates the impact of four emulsifiers on the characteristics of polyurethane hollow structures used as drug delivery system. Results Polyurethane (PU) structures with high stability and sizes ranging from nano- to micro-scale were obtained by interfacial polyaddition combined with spontaneous emulsification. The pH of PU aqueous solutions (0.1% w/w) was slightly acidic, which is acceptable for products intended to be used on human skin. Agglomerated structures with irregular shapes were observed by scanning electron microscopy. The synthesized structures have melting points between 245-265°C and reveal promising results in different evaluations (TEWL, mexametry) on murine skin. Conclusions In this study hollow PU structures of reduced noxiousness were synthesized, their size and stability being influenced by emulsifiers. Such structures could be used in the pharmaceutical field as future drug delivery systems. PMID:23575277

Emulsifying and foaming properties of commercial yellow pea (Pisum sativum L.) seed flours.

PubMed

Aluko, Rotimi E; Mofolasayo, Olawunmi A; Watts, Beverley M

2009-10-28

Commercial yellow pea seed flours prepared by a patented wet-milling process and pea protein isolate (PPI) were analyzed for emulsifying and foaming properties at pH 3.0, 5.0, and 7.0 and compared to soybean protein isolate (SPI). PPI and SPI formed emulsions with significantly smaller (p < 0.05) oil droplet sizes, 16-30 and 23-54 microm, respectively, than flours that primarily contained fiber such as Centara III and IV, or those that consisted mainly of starch: Centu-tex, Uptake 80 and Accu-gel. PPI was a better emulsifier than SPI at pH 7.0, and a better foaming agent at pH 3.0 and pH 7.0, although foaming capacity varied with sample concentration. Centu-tex and Uptake 80 have exactly the same chemical composition, but the latter has a much smaller flour particle size range, and had significantly smaller (p < 0.05) emulsion oil droplets. Incorporation of pea starch into SPI emulsions produced a synergistic effect that led to significant increases (p < 0.05) in emulsification capacity (reduced emulsion oil droplet size) when compared to SPI or starch alone. These results showed that PPI had generally significantly higher (p < 0.05) emulsion and foam forming properties than SPI, and that pea starch could be used to improve the quality of SPI-stabilized food emulsions.

Production of a Health-Beneficial Food Emulsifier by Enzymatic Partial Hydrolysis of Phospholipids Obtained from the Head of Autumn Chum Salmon.

PubMed

Shah, A K M Azad; Nagao, Toshihiro; Kurihara, Hideyuki; Takahashi, Koretaro

2017-02-01

Phospholipids and their partial hydrolysates, namely lysophospholipids (LPLs), have been widely used in food, pharmaceutical, and cosmetic products as highly efficient emulsifiers. This study was conducted to produce docosahexaenoic acid (DHA)-esterified LPLs by enzymatic modification of phospholipids obtained from the head of autumn chum salmon (Oncorhynchus keta). The emulsifying properties of the obtained LPLs were also evaluated. Two different types of substrates of salmon head phospholipids were prepared via silica gel and cold acetone precipitation. Enzymatic partial hydrolysis was carried out using immobilized phospholipase A 1 (PLA 1 ) and Lipozyme RM IM. Results showed that the increase in DHA in the LPLs was much higher in the silica-separated phospholipids than in the acetone-precipitated phospholipids. When silica-separated phospholipids were used as the substrate, the DHA content of the LPLs increased from 23.1% to 40.6% and 42.6% after 8 h of partial hydrolysis with Lipozyme RM IM and immobilized PLA 1 , respectively. The yield of the LPLs was comparatively higher in the Lipozyme RM IM than in the immobilized PLA 1 hydrolysis reaction. The critical micelle concentration values of the LPLs and purified lysophosphatidylcholine (LPC) were 100 mg/L and 5 mg/L, respectively. The surface tension values of the LPLs and LPC were reduced to 30.0 mN/m and 30.5 mN/m, respectively. The hydrophilic-lipophilic balance of the LPLs and LPC were 6.0 and 9.4, respectively. Based on the emulsifying properties observed, we conclude that LPLs derived from the phospholipids of salmon head lipids could be used as a health-beneficial emulsifier in the food industry.

[Treatment of wrinkles of the upper lip by emulsified fat or "Nanofat": Biological and clinical study about 4 cases].

PubMed

Mesguich Batel, F; Bertrand, B; Magalon, J; François, P; Velier, M; Veran, J; Mallet, S; Jouve, E; Sabatier, F; Casanova, D

2018-02-01

Emulsified fat injection showed its interest in aesthetic facial surgery. The adipose tissue harvested is mechanically emulsified and filtered. The suspension obtained is injected into the dermis through small diameter needles (27 to 30 gauges). The objective of our study was to evaluate the biological composition of emulsified fat and its clinical effectiveness in the treatment of peri-oral wrinkles in 4 patients aged 50 to 59 years. Each patient received an intradermal injection of emulsified fat in the peri-oral wrinkles prepared from abdominal fat under local anesthesia. The cell viability, stromal vascular fraction (FVS) composition in emulsified fat and the adipocyte differentiation capacity of mesenchymal stem cells (MSC) were studied. The clinical results were evaluated by standardized photographs, 3D microphotography, confocal microscopy, and self-evaluation of patient satisfaction over a period of 4 months. The biological study of the emulsified fat found a lysis of all the adipocytes. The mean number of FVS cells was 126,330±2758 cells by cc of emulsified fat with preserved cell viability (85.1±6.84 %) and a good proportion of regeneratives cells (18.77±6.2 %). The clinical study found a tendency to decrease the volume of wrinkles on standardized photography and 3D microphotography no significative. Patients were satisfied with treatment with an average score of 7±1.15/10 to 4 months. Intradermal injection of emulsified fat seems to be an interesting treatment of face wrinkles. Our study has shown its safety, but additional studies seems necessary to confirm its clinical efficacy. Copyright © 2017 Elsevier Masson SAS. All rights reserved.

Preparation and optimization of tablets containing a self-nano-emulsifying drug delivery system loaded with rosuvastatin.

PubMed

Salem, Heba F; Kharshoum, Rasha M; Halawa, Abdel Khalek A; Naguib, Demiana M

2018-06-01

Rosuvastatin (ROS) calcium is the latest synthetic drug in the statin group that has an anti-hyperlipidemic activity. It is available as tablets, and its poor aqueous solubility, slow dissolution rate and low-absorption extent result in less than 20% bioavailability and about 80% being excreted unchanged in the feces without absorption. To utilize nanotechnology to reformulate ROS as a self-nano-emulsifying drug delivery system (SNEDDS), and utilizing design optimization to fabricate the SNEDDS as a tablet. The solubility of ROS in different oils, surfactants and co-surfactants was tested. Pseudo-ternary phase diagrams were developed and various SNEDDS formulations were prepared and evaluated regarding globule size, self-emulsification, viscosity and transmittance. The optimized system was examined using transmission electron microscopy. The self-nano-emulsifying tablets were prepared using two types of nano-silica and different percentages of Avicel as a binder and Ac-Di-Sol as a disintegrant. The prepared tablets were evaluated for their physicochemical properties. Bioavailability in human volunteers was assessed. A SNEDDS system was successfully developed with a droplet size range of 15 nm and a composition of 10% Labrafac, 80% Cremophore RH40 and 10% Propylene glycol. The optimized tablet formula contained: hydrophilic nano-silica, 3% Ac-Di-Sol and 30% Avicel. The pharmacokinetic study revealed that the bioavailability was enhanced by more than 2.4-fold compared with the commercially available tablet. Tablets containing SNEDDS loaded with ROS represent a promising novel formula that has higher gastrointestinal absorption and enhanced systemic bioavailability.

Fat reduction in comminuted meat products-effects of beef fat, regular and pre-emulsified canola oil.

PubMed

Youssef, M K; Barbut, S

2011-04-01

The effects of fat reduction (25.0%, 17.5%, and 10.0%) and substituting beef fat with canola oil or pre-emulsified canola oil (using soy protein isolate, sodium caseinate or whey protein isolate) on cooking loss, texture and color of comminuted meat products were investigated. Reducing fat from 25 to 10% increased cooking loss and decreased hardness. Canola oil or pre-emulsified treatments showed a positive effect on improving yield and restoring textural parameters. Using sodium caseinate to pre-emulsify the oil resulted in the highest hardness value. Cohesiveness was affected by fat type and level. The color of reduced fat meat batters was darker for all, except the beef fat treatments. Using canola oil or pre-emulsified oil resulted in a significant reduction in redness. The results show that pre-emulsification can offset some of the changes in reduced fat meat products when more water is used to substitute for the fat and that pre-emulsification can also help to produce a more stable meat matrix. © 2010 The American Meat Science Association. Published by Elsevier Ltd. All rights reserved.

Oral formulation strategies to improve solubility of poorly water-soluble drugs.

PubMed

Singh, Abhishek; Worku, Zelalem Ayenew; Van den Mooter, Guy

2011-10-01

In the past two decades, there has been a spiraling increase in the complexity and specificity of drug-receptor targets. It is possible to design drugs for these diverse targets with advances in combinatorial chemistry and high throughput screening. Unfortunately, but not entirely unexpectedly, these advances have been accompanied by an increase in the structural complexity and a decrease in the solubility of the active pharmaceutical ingredient. Therefore, the importance of formulation strategies to improve the solubility of poorly water-soluble drugs is inevitable, thus making it crucial to understand and explore the recent trends. Drug delivery systems (DDS), such as solid dispersions, soluble complexes, self-emulsifying drug delivery systems (SEDDS), nanocrystals and mesoporous inorganic carriers, are discussed briefly in this review, along with examples of marketed products. This article provides the reader with a concise overview of currently relevant formulation strategies and proposes anticipated future trends. Today, the pharmaceutical industry has at its disposal a series of reliable and scalable formulation strategies for poorly soluble drugs. However, due to a lack of understanding of the basic physical chemistry behind these strategies, formulation development is still driven by trial and error.

Approach for energy saving and pollution reducing by fueling diesel engines with emulsified biosolution/ biodiesel/diesel blends.

PubMed

Lin, Yuan-Chung; Lee, Wen-Jhy; Chao, How-Ran; Wang, Shu-Li; Tsou, Tsui-Chun; Chang-Chien, Guo-Ping; Tsai, Perng-Jy

2008-05-15

The developments of both biodiesel and emulsified diesel are being driven by the need for reducing emissions from diesel engines and saving energy. Artificial chemical additives are also being used in diesel engines for increasing their combustion efficiencies. But the effects associated with the use of emulsified additive/biodiesel/diesel blends in diesel engines have never been assessed. In this research, the premium diesel fuel (PDF) was used as the reference fuel. A soy-biodiesel was selected as the test biodiesel. A biosolution made of 96.5 wt % natural organic enzyme-7F (NOE-7F) and 3.5 wt % water (NOE-7F water) was used as the fuel additive. By adding additional 1 vol % of surfactant into the fuel blend, a nanotechnology was used to form emulsified biosolution/soy-biodiesel/PDF blends for fueling the diesel engine. We found that the emulsified biosolution/soy-biodiesel/PDF blends did not separate after being kept motionless for 30 days. The above stability suggests that the above combinations are suitable for diesel engines as alternative fuels. Particularly, we found that the emulsified biosolution/soy-biodiesel/PDF blends did have the advantage in saving energy and reducing the emissions of both particulate matters (PM) and polycyclic aromatic hydrocarbons (PAHs) from diesel engines as compared with PDF, soy-biodiesel/PDF blends, and emulsified soy-biodiesel/ PDF blends. The results obtained from this study will provide useful approaches for reducing the petroleum reliance, pollution, and global warming. However, it should be noted that NO(x) emissions were not measured in the present study which warrants the need for future investigation.

Biowaiver extension potential and IVIVC for BCS Class II drugs by formulation design: Case study for cyclosporine self-microemulsifying formulation.

PubMed

Yang, Su-Geun

2010-11-01

The objective of this work was to suggest the biowaiver potential of biopharmaceutical classification system (BCS) Class II drugs in self-microemulsifying drug delivery systems (SMEDDS) which are known to increase the solubility, dissolution and oral absorption of water-insoluble drugs. Cyclosporine was selected as a representative BCS Class II drug. New generic candidate of cyclosporine SMEDDS (test) was applied for the study with brand SMEDDS (reference I) and cyclosporine self-emulsifying drug delivery systems (SEDDS, reference II). Solubility and dissolution of cyclosporine from SMEDDS were critically enhanced, which were the similar behaviors with BCS class I drug. The test showed the identical dissolution rate and the equivalent bioavailability (0.34, 0.42 and 0.68 of p values for AUC₀(→)₂₄(h), C(max) and T(max), respectively) with the reference I. Based on the results, level A in vitro-in vivo correlation (IVIVC) was established from these two SMEDDS formulations. This study serves as a good example for speculating the biowaiver extension potential of BCS Class II drugs specifically in solubilizing formulation such as SMEDDS.

The major proteins of the seed of the fruit of the date palm (Phoenix dactylifera L.): Characterisation and emulsifying properties.

PubMed

Akasha, Ibrahim; Campbell, Lydia; Lonchamp, Julien; Euston, Stephen R

2016-04-15

Proteins were extracted from the seeds of the fruit of the date palm. Proteomic analysis and SDS-PAGE electrophoresis of the extracted proteome suggested it is composed predominantly of the storage proteins glycinin and β-conglycinin, although over 300 proteins were detected, 91 of which were identified with confidence. In terms of protein type, the largest numbers of proteins were associated, not unexpectedly, with metabolism and energy functions, which reflected the requirements of the germinating and growing embryonic plant. The emulsifying properties of the extracted proteins were determined. Date seed protein exhibited a lower emulsifying activity than either whey protein concentrate or soy protein isolate, at each of the pH values tested. However, the stability of the emulsions produced with all three proteins was very similar at the different pH values. This combination of large emulsion droplet size and high emulsion stability properties suggested that the date proteins may adsorb as large protein oligomers. Copyright © 2015 Elsevier Ltd. All rights reserved.

FORMULATION AND STABILITY EVALUATION OF BAUHINIA VARIEGATA EXTRACT TOPICAL EMULSION.

PubMed

Mohsin, Sabeeh; Akhtar, Naveed

2017-05-01

This study presents the results for the development of water in oil (W/O) emulsion containing 2 % Bauhinia variegata (BV) extract with good antioxidant potential for cosmetic application. Different ratios of surfactant, oil and water were investigated to optimize the ratio of ingredients. It was found that emulsifier and oil4ratio were important in improving the stability of emulsion. The formulation having 2.5% Abil EM90, 12% liquid paraffin, 83.5% distilled water and 2% BV extract was found to be most stable. Stability of the formulation was further evaluated by characterizing for organoleptic, sedimentation, microscopic and rheological properties at a range of storage conditions for a period of 12 weeks. Experimental findings showed stable formulation behavior with respect to color change, liquefaction and phase separation. Centrifugation test was carried out to predict the long term stability..The rheological parameters were evaluated from Power Law and the flow index value less than 1 suggested non-Newtonian behavior of the W/O emulsion. The mean droplet size of the internal phase of freshly prepared formulation was 4.06 ? 1.99 pm that did not change significantly (p > 0.05) during the storage. The newly developed formulation exhibited promising attributes over long term storage and open opportunities for the topical delivery of natural antioxidants for cosmetic and pharmaceutical objectives.

Designing excipient emulsions to increase nutraceutical bioavailability: emulsifier type influences curcumin stability and bioaccessibility by altering gastrointestinal fate.

PubMed

Zou, Liqiang; Liu, Wei; Liu, Chengmei; Xiao, Hang; McClements, David Julian

2015-08-01

The influence of emulsifier type on the ability of excipient emulsions to improve the solubility, stability, and bioaccessibility of powdered curcumin was examined. Oil-in-water emulsions prepared using three different emulsifiers (whey protein isolate, caseinate, or Tween 80) were mixed with curcumin powder and then incubated at either 30 °C (to simulate applications of salad dressings) or 100 °C (to simulate applications of cooking sauces). The transfer of curcumin into the excipient emulsions was appreciably higher for excipient emulsions held at 100 °C than those held at 30 °C, and was appreciably higher for surfactant-stabilized emulsions than protein-stabilized emulsions. For example, the amounts of curcumin transferred into emulsions held at 30 and 100 °C were 66 and 280 μg mL(-1) for Tween 80, but only 17 and 208 μg mL(-1) for caseinate. The total curcumin concentration in the digesta and mixed micelle phases collected after excipient emulsions were exposed to a simulated gastrointestinal tract (mouth, stomach, and small intestine) depended on emulsifier type. The total amount of curcumin within the digesta was higher for protein-stabilized emulsions than surfactant-stabilized ones, which was attributed to the ability of the proteins to protect curcumin from chemical degradation. For example, the digesta contained 204 μg mL(-1) curcumin for caseinate emulsions, but only 111 μg mL(-1) for Tween 80 emulsions. This study shows the potential of designing excipient emulsions to increase the oral bioavailability of curcumin for food and pharmaceutical applications.

Effect of dynamic high pressure on emulsifying and encapsulant properties of cashew tree gum.

PubMed

Porto, Bruna Castro; Cristianini, Marcelo

2018-04-15

Dynamic high pressure (DHP) has been applied in the physical modification of biopolymers as polysaccharides, proteins and gums. It is known that DHP is able to promote degradation of polysaccharides (e.g. molecular weight reduction). However, few studies have assessed the effect of DHP on the emulsifying and encapsulating properties of polysaccharides. Thus, this study aimed to investigate the effect of DHP on the emulsifying (average droplet size and particle size distribution, optical and confocal scanning laser microscopy, rheology, zeta potential and electric conductivity, creaming index, and turbidity) and encapsulating (scanning electronic microscopy, flavor retention, average droplet size, and particle size distribution) properties of cashew tree gum (CG). The application of DHP process improved the emulsifying capacity of cashew tree gum (CG) by reducing the medium droplet size (D3,2 and D4,3), increasing the turbidity and improving the emulsion stability. However, no effect of DHP was observed on the encapsulating capacity of CG. Copyright © 2018 Elsevier Ltd. All rights reserved.

The Solid Phase Curing Time Effect of Asbuton with Texapon Emulsifier at the Optimum Bitumen Content

NASA Astrophysics Data System (ADS)

Sarwono, D.; Surya D, R.; Setyawan, A.; Djumari

2017-07-01

Buton asphalt (asbuton) could not be utilized optimally in Indonesia. Asbuton utilization rate was still low because the processed product of asbuton still have impracticable form in the term of use and also requiring high processing costs. This research aimed to obtain asphalt products from asbuton practical for be used through the extraction process and not requiring expensive processing cost. This research was done with experimental method in laboratory. The composition of emulsify asbuton were 5/20 grain, premium, texapon, HCl, and aquades. Solid phase was the mixture asbuton 5/20 grain and premium with 3 minutes mixing time. Liquid phase consisted texapon, HCl and aquades. The aging process was done after solid phase mixing process in order to reaction and tie of solid phase mixed become more optimal for high solubility level of asphalt production. Aging variable time were 30, 60, 90, 120, and 150 minutes. Solid and liquid phase was mixed for emulsify asbuton production, then extracted for 25 minutes. Solubility level of asphalt, water level, and asphalt characteristic was tested at extraction result of emulsify asbuton with most optimum ashphal level. The result of analysis tested data asphalt solubility level at extract asbuton resulted 94.77% on 120 minutes aging variable time. Water level test resulted water content reduction on emulsify asbuton more long time on occurring of aging solid phase. Examination of asphalt characteristic at extraction result of emulsify asbuton with optimum asphalt solubility level, obtain specimen that have rigid and strong texture in order that examination result have not sufficient ductility and penetration value.

Effects of vegetable juice powder concentration and storage time on some chemical and sensory quality attributes of uncured, emulsified cooked sausages.

PubMed

Sindelar, J J; Cordray, J C; Sebranek, J G; Love, J A; Ahn, D U

2007-06-01

Uncured, no-nitrate/nitrite-added meat products can be manufactured with vegetable juice powder (VJP) and a starter culture containing Staphylococcus carnosus, resulting in quality and sensory attributes similar to traditional cured products. The 1st objective of this study was to determine the effects of varying concentrations of VJP and incubation times (MIN-HOLD) on quality characteristics, including lipid oxidation, color, and cured meat pigment concentrations, of emulsified-frankfurter-style-cooked (EFSC) sausages over a 90-d storage period. The 2nd objective was to compare residual nitrate and nitrite content resulting from different processing treatments and the 3rd objective was to assess sensory properties of finished products. Four EFSC sausage treatments (TRT) (TRT 1: 0.20% VJP, 30 MIN-HOLD; TRT 2: 0.20% VJP, 120 MIN-HOLD; TRT 3: 0.40% VJP, 30 MIN-HOLD; TRT 4: 0.40% VJP, 120 MIN-HOLD) and a sodium nitrite-added control (C) were used for this study. No differences for lipid oxidation (TBARS) between any TRTs and C or over time were observed. No differences (P > 0.05) for CIE L* values were found between TRTs. CIE a* and reflectance ratio values revealed that TRTs 2, 4, and C were redder than TRTs 1 and 3 at day 0. Trained sensory intensity ratings for cured aroma, cured color, cured flavor, uniform color, and firmness determined that all but TRT 1 were similar to C. These results indicate a longer incubation time (120 compared with 30 min) was found more critical than VJP level (0.20% or 0.40%) to result in products comparable to a sodium nitrite-added control.

Emulsifying Properties of Oxidatively Stressed Myofibrillar Protein Emulsion Gels Prepared with (-)-Epigallocatechin-3-gallate and NaCl.

PubMed

Feng, Xianchao; Chen, Lin; Lei, Na; Wang, Shuangxi; Xu, Xinglian; Zhou, Guanghong; Li, Zhixi

2017-04-05

The dose-dependent effects of (-)-epigallocatechin-3-gallate (EGCG; 0, 100, or 1000 ppm) on the textural properties and stability of a myofibrillar protein (MP) emulsion gel were investigated. Addition of EGCG significantly inhibited formation of carbonyl but promoted the loss of both thiol and free amine groups. Addition of EGCG, particularly at 1000 ppm, initiated irreversible protein modifications, as evidenced by surface hydrophobicity changes, patterns in sodium dodecyl sulfate-polyacrylamide gel electrophoresis, and differential scanning calorimetry. These results indicated that MP was modified by additive reactions between the quinone of EGCG and thiols and free amines of proteins. These adducts increased cooking loss and destabilized the texture, especially with a large EGCG dose. Confocal laser scanning microscopy and scanning electron microscopy images clearly indicated the damage to the emulsifying properties and the collapse of the internal structure when the MP emulsion gel was treated with a large EGCG dose. A high concentration of NaCl (0.6 M) improved modification of MP and increased the rate of deterioration of the internal structure, especially with the large EGCG dose (1000 ppm), resulting in an MP emulsion gel with extremely unstable emulsifying properties.

Application of a biphasic test for characterization of in vitro drug release of immediate release formulations of celecoxib and its relevance to in vivo absorption.

PubMed

Shi, Yi; Gao, Ping; Gong, Yuchuan; Ping, Haili

2010-10-04

A biphasic in vitro test method was used to examine release profiles of a poorly soluble model drug, celecoxib (CEB), from its immediate release formulations. Three formulations of CEB were investigated in this study, including a commercial Celebrex capsule, a solution formulation (containing cosolvent and surfactant) and a supersaturatable self-emulsifying drug delivery system (S-SEDDS). The biphasic test system consisted of an aqueous buffer and a water-immiscible organic solvent (e.g., octanol) with the use of both USP II and IV apparatuses. The aqueous phase provided a nonsink dissolution medium for CEB, while the octanol phase acted as a sink for CEB partitioning. For comparison, CEB concentration-time profiles of these formulations in the aqueous medium under either a sink condition or a nonsink condition were also explored. CEB release profiles of these formulations observed in the aqueous medium from either the sink condition test, the nonsink condition test, or the biphasic test have little relevance to the pharmacokinetic observations (e.g., AUC, C(max)) in human subjects. In contrast, a rank order correlation among the three CEB formulations is obtained between the in vitro AUC values of CEB from the octanol phase up to t = 2 h and the in vivo mean AUC (or C(max)) values. As the biphasic test permits a rapid removal of drug from the aqueous phase by partitioning into the organic phase, the amount of drug in the organic phase represents the amount of drug accumulated in systemic circulation in vivo. This hypothesis provides the scientific rationale for the rank order relationship among these CEB formulations between their CEB concentrations in the organic phase and the relative AUC or C(max). In addition, the biphasic test method permits differentiation and discrimination of key attributes among the three different CEB formulations. This work demonstrates that the biphasic in vitro test method appears to be useful as a tool in evaluating performance of

Application of Emulsified Zero-Valent Iron to Marine Environments

NASA Technical Reports Server (NTRS)

Quinn, Jacqueline W.; Brooks, Kathleen B.; Geiger, Cherie L.; Clausen, Christian A.; Milum, Kristen M.

2006-01-01

Contamination of marine waters and sediments with heavy metals and dense non-aqueous phase liquids (DNAPLs) including chlorinated solvents, pesticides and PCBs pose ecological and human health risks through the potential of the contaminant to bioaccumulate in fish, shellfish and avian populations. The contaminants enter marine environments through improper disposal techniques and storm water runoff. Current remediation technologies for application to marine environments include costly dredging and off-site treatment of the contaminated media. Emulsified zero-valent iron (EZVI) has been proven to effectively degrade dissolved-phase and DNAPL-phase contaminants in freshwater environments on both the laboratory and field-scale level. Emulsified Zero-Valent Metal (EZVM) using metals such as iron and/or magnesium have been shown in the laboratory and on the bench scale to be effective at removing metals contamination in freshwater environments. The application to marine environments, however, is only just being explored. This paper discusses. the potential use of EZVI or EZVM in brackish and saltwater environments, with supporting laboratory data detailing its effectiveness on trichloroethylene, lead, copper, nickel and cadmium.

Turkish Tombul hazelnut (Corylus avellana L.) protein concentrates: functional and rheological properties.

PubMed

Tatar, F; Tunç, M T; Kahyaoglu, T

2015-02-01

Turkish Tombul hazelnut consumed as natural or processed forms were evaluated to obtain protein concentrate. Defatted hazelnut flour protein (DHFP) and defatted hazelnut cake protein (DHCP) were produced from defatted hazelnut flour (DHF) and defatted hazelnut cake (DHC), respectively. The functional properties (protein solubility, emulsifying properties, foaming capacity, and colour), and dynamic rheological characteristics of protein concentrates were measured. The protein contents of samples varied in the range of 35-48 % (w/w, db) and 91-92 % (w/w, db) for DHF/DHC and DHFP/DHCP samples, respectively. The significant difference for water/fat absorption capacity, emulsion stability between DHF and DHC were determined. On the other hand, the solubility and emulsion activity of DHF and DHC were not significantly different (p > 0.05). Emulsion stability of DHFP (%46) was higher than that of DHCP (%35) but other functional properties were found similar. According to these results, the DHCP could be used as DHFP in food product formulations. The DHFP and DHCP samples showed different apparent viscosity at the same temperature and concentration, the elastic modulus (G' value) of DHPC was also found higher than that of DHFP samples.

Effect of a single dose of emulsified versus capsular fish oils on plasma phospholipid fatty acids over 48 hours

USDA-ARS?s Scientific Manuscript database

Emulsified fish oil supplements provide an alternative to encapsulated fish oils. Oil-in-water emulsions may offer an advantage in digestion and absorption thereby increasing the bioavailability of fatty acids. We evaluated the effect of three oil-in-water emulsified fish oils (Emulsion B, Emulsion ...

Saving energy and reducing emissions of both polycyclic aromatic hydrocarbons and particulate matter by adding bio-solution to emulsified diesel.

PubMed

Lin, Yuan-Chung; Lee, Wen-Jhy; Chen, Chun-Chi; Chen, Chung-Bang

2006-09-01

Development of emulsified diesel has been driven by the need to reduce emissions from diesel engines and to save energy. Emulsification technology and bio-solution (NOE-7F) were used to produce emulsified diesel in this study. The experimental results indicated that there were no significant separation layers in W13 (13 wt % water + 87 wt % PDF), W16 (16 wt % water + 84 wt % PDF), W19 (19 wt % water + 81 wt % PDF), E13 (13 wt % NOE-7F water + 87 wt % PDF), E16 (16 wt % NOE-7F water + 83 wt % PDF), and E19 (19 wt % NOE-7F water + 81 wt % PDF) after premium diesel fuel (PDF) was emulsified for more than 30 days. In addition, there was no significant increase in damage from using these six emulsified fuels after the operation of the diesel generator for more than one year. The energy saving and reduction of particulate matter (PM) and total polycyclic aromatic hydrocarbons (PAHs) for W13, W16, W19, E13, E16 and E19, respectively, were 3.90%, 30.9%, 27.6%; 3.38%, 37.0%, 34.9%; 2.17%, 22.2%, 15.4%; 5.87%, 38.6%, 49.3%; 5.88%, 57.8%, 58.0%; and 4.75%, 31.1%, 47.3%, compared with PDF. The above results revealed that the bio-solution (NOE-7F) had a catalytic effect which elevated the combustion efficiency and decreased pollutant emissions during the combustion process. Furthermore, bio-solution (NOE-7F) can stabilize the emulsified fuels and enhance energy saving. Thus, emulsified fuels are highly suitable for use as alternative fuels. Due to the increasing price of diesel, emulsified diesel containing NOE-7F has potential for commercial application.

Switchable Pickering Emulsions Stabilized by Awakened TiO2 Nanoparticle Emulsifiers Using UV/Dark Actuation.

PubMed

Zhang, Qing; Bai, Rui-Xue; Guo, Ting; Meng, Tao

2015-08-26

In this work, switchable Pickering emulsions that utilize UV/dark manipulation employ a type of smart TiO2 nanoparticle as emulsifiers. The emulsifiers can be awakened when needed via UV-induced degradation of grafted silanes on TiO2 nanoparticles. By tuning the surface wettability of TiO2 nanoparticles in situ via UV/dark actuation, emulsions stabilized by the nanoparticles can be reversibly switched between the water-in-oil (W/O) type and oil-in-water (O/W) type for several cycles. Due to the convertible wettability, the smart nanoparticle emulsifiers can be settled in either the oil phase or the water phase as desired during phase separation, making it convenient for recycling. The present work provides a facile and noninvasive method to freely manipulate the formation, breakage, and switching of the emulsion; this method has promising potential as a powerful technique for use in energy-efficient and environmentally friendly industries.

Retention and release of oil-in-water emulsions from filled hydrogel beads composed of calcium alginate: impact of emulsifier type and pH.

PubMed

Zeeb, Benjamin; Saberi, Amir Hossein; Weiss, Jochen; McClements, David Julian

2015-03-21

Delivery systems based on filled hydrogel particles (microgels) can be fabricated from natural food-grade lipids and biopolymers. The potential for controlling release characteristics by modulating the electrostatic interactions between emulsifier-coated lipid droplets and the biopolymer matrix within hydrogel particles was investigated. A multistage procedure was used to fabricate calcium alginate beads filled with lipid droplets stabilized by non-ionic, cationic, anionic, or zwitterionic emulsifiers. Oil-in-water emulsions stabilized by Tween 60, DTAB, SDS, or whey protein were prepared by microfluidization, mixed with various alginate solutions, and then microgels were formed by simple extrusion into calcium solutions. The microgels were placed into a series of buffer solutions with different pH values (2 to 11). Lipid droplets remained encapsulated under acidic and neutral conditions, but were released under highly basic conditions (pH 11) due to hydrogel swelling when the alginate concentration was sufficiently high. Lipid droplet release increased with decreasing alginate concentration, which could be attributed to an increase in the pore size of the hydrogel matrix. These results have important implications for the design of delivery systems to entrap and control the release of lipophilic bioactive components within filled hydrogel particles.

21 CFR 178.3400 - Emulsifiers and/or surface-active agents.

Code of Federal Regulations, 2014 CFR

2014-04-01

... paperboard. α-[p-(1,1,3,3-Tetramethylbutyl)phenyl] omega-hydroxypoly(oxyethylene) produced by the... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Emulsifiers and/or surface-active agents. 178.3400... substances: List of substances Limitations α-Alkyl-, α-alkenyl-, and α-alkylaryl-omega-hydroxypoly...

Effect of pulsed ultrasound on the physicochemical characteristics and emulsifying properties of squid (Dosidicus gigas) mantle proteins.

PubMed

Higuera-Barraza, O A; Torres-Arreola, W; Ezquerra-Brauer, J M; Cinco-Moroyoqui, F J; Rodríguez Figueroa, J C; Marquez-Ríos, E

2017-09-01

Food technologists are always looking to improve the functional properties of proteins. In this sense, in last years ultrasound has been used to improve some functional properties. For this reason, and considering that jumbo squid is an important fishery in northwest Mexico, the purpose of this research was to determine the effect of pulsed ultrasound on the physicochemical characteristics and emulsifying properties of squid (Dosidicus gigas) mantle proteins. Pulsed ultrasound (20kHz, 20, and 40% amplitude) was applied for 30, 60, and 90s to a protein extract prepared from giant squid mantle causing an increase (p<0.05) in surface hydrophobicity (S o ) from 108.4±1.4 to 239.1±2.4 after application of pulsed ultrasound at 40% of amplitude for 90s. The electrophoretic profile and the total and reactive sulfhydryl contents were not affected (p⩾0.05) by the ultrasound treatment. The emulsifying ability of the protein solution was improved (p<0.05), whereas the Emulsifier Activity Index (EAI) varied from123.67±5.52m 2 /g for the control and increased up to 217.7±3.8m 2 /g after application of the ultrasound. The Stability Emulsifier Index (EEI) was improved at 40% of amplitude by 60 and 90s. The results suggested that pulsed ultrasound used as pretreatment induced conformational changes in giant squid proteins, which improved the interfacial association between protein-oil phases, thus contributing to the improvement of their emulsifient properties. Copyright © 2017 Elsevier B.V. All rights reserved.

Optimized formulation of solid self-microemulsifying sirolimus delivery systems

PubMed Central

Cho, Wonkyung; Kim, Min-Soo; Kim, Jeong-Soo; Park, Junsung; Park, Hee Jun; Cha, Kwang-Ho; Park, Jeong-Sook; Hwang, Sung-Joo

2013-01-01

Background The aim of this study was to develop an optimized solid self-microemulsifying drug delivery system (SMEDDS) formulation for sirolimus to enhance its solubility, stability, and bioavailability. Methods Excipients used for enhancing the solubility and stability of sirolimus were screened. A phase-separation test, visual observation for emulsifying efficiency, and droplet size analysis were performed. Ternary phase diagrams were constructed to optimize the liquid SMEDDS formulation. The selected liquid SMEDDS formulations were prepared into solid form. The dissolution profiles and pharmacokinetic profiles in rats were analyzed. Results In the results of the oil and cosolvent screening studies, Capryol™ Propylene glycol monocapry late (PGMC) and glycofurol exhibited the highest solubility of all oils and cosolvents, respectively. In the surfactant screening test, D-α-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS) was determined to be the most effective stabilizer of sirolimus in pH 1.2 simulated gastric fluids. The optimal formulation determined by the construction of ternary phase diagrams was the T32 (Capryol™ PGMC:glycofurol:vitamin E TPGS = 30:30:40 weight ratio) formulation with a mean droplet size of 108.2 ± 11.4 nm. The solid SMEDDS formulations were prepared with Sucroester 15 and mannitol. The droplet size of the reconstituted solid SMEDDS showed no significant difference compared with the liquid SMEDDS. In the dissolution study, the release amounts of sirolimus from the SMEDDS formulation were significantly higher than the raw sirolimus powder. In addition, the solid SMEDDS formulation was in a more stable state than liquid SMEDDS in pH 1.2 simulated gastric fluids. The results of the pharmacokinetic study indicate that the SMEDDS formulation shows significantly greater bioavailability than the raw sirolimus powder or commercial product (Rapamune® oral solution). Conclusion The results of this study suggest the potential use

21 CFR 178.3400 - Emulsifiers and/or surface-active agents.

Code of Federal Regulations, 2010 CFR

2010-04-01

... paperboard. α-[p-(1,1,3,3-Tetramethylbutyl)phenyl] omega-hydroxypoly(oxyethylene) produced by the... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Emulsifiers and/or surface-active agents. 178.3400...-alkylaryl-omega-hydroxypoly(oxyethylene) mixture consisting of 30 weight pct of α-(2,4,6-triisobutylphenyl...

21 CFR 178.3400 - Emulsifiers and/or surface-active agents.

Code of Federal Regulations, 2013 CFR

2013-04-01

... paperboard. α-[p-(1,1,3,3-Tetramethylbutyl)phenyl] omega-hydroxypoly(oxyethylene) produced by the... 21 Food and Drugs 3 2013-04-01 2013-04-01 false Emulsifiers and/or surface-active agents. 178.3400...-alkylaryl-omega-hydroxypoly(oxyethylene) mixture consisting of 30 weight pct of α-(2,4,6-triisobutylphenyl...

21 CFR 178.3400 - Emulsifiers and/or surface-active agents.

Code of Federal Regulations, 2011 CFR

2011-04-01

... paperboard. α-[p-(1,1,3,3-Tetramethylbutyl)phenyl] omega-hydroxypoly(oxyethylene) produced by the... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Emulsifiers and/or surface-active agents. 178.3400...-alkylaryl-omega-hydroxypoly(oxyethylene) mixture consisting of 30 weight pct of α-(2,4,6-triisobutylphenyl...

21 CFR 178.3400 - Emulsifiers and/or surface-active agents.

Code of Federal Regulations, 2012 CFR

2012-04-01

... paperboard. α-[p-(1,1,3,3-Tetramethylbutyl)phenyl] omega-hydroxypoly(oxyethylene) produced by the... 21 Food and Drugs 3 2012-04-01 2012-04-01 false Emulsifiers and/or surface-active agents. 178.3400...-alkylaryl-omega-hydroxypoly(oxyethylene) mixture consisting of 30 weight pct of α-(2,4,6-triisobutylphenyl...

Natural emulsifiers - Biosurfactants, phospholipids, biopolymers, and colloidal particles: Molecular and physicochemical basis of functional performance.

PubMed

McClements, David Julian; Gumus, Cansu Ekin

2016-08-01

There is increasing consumer pressure for commercial products that are more natural, sustainable, and environmentally friendly, including foods, cosmetics, detergents, and personal care products. Industry has responded by trying to identify natural alternatives to synthetic functional ingredients within these products. The focus of this review article is on the replacement of synthetic surfactants with natural emulsifiers, such as amphiphilic proteins, polysaccharides, biosurfactants, phospholipids, and bioparticles. In particular, the physicochemical basis of emulsion formation and stabilization by natural emulsifiers is discussed, and the benefits and limitations of different natural emulsifiers are compared. Surface-active polysaccharides typically have to be used at relatively high levels to produce small droplets, but the droplets formed are highly resistant to environmental changes. Conversely, surface-active proteins are typically utilized at low levels, but the droplets formed are highly sensitive to changes in pH, ionic strength, and temperature. Certain phospholipids are capable of producing small oil droplets during homogenization, but again the droplets formed are highly sensitive to changes in environmental conditions. Biosurfactants (saponins) can be utilized at low levels to form fine oil droplets that remain stable over a range of environmental conditions. Some nature-derived nanoparticles (e.g., cellulose, chitosan, and starch) are effective at stabilizing emulsions containing relatively large oil droplets. Future research is encouraged to identify, isolate, purify, and characterize new types of natural emulsifier, and to test their efficacy in food, cosmetic, detergent, personal care, and other products. Copyright © 2016 Elsevier B.V. All rights reserved.

Emulsifying and foaming properties of ultraviolet-irradiated egg white protein and sodium caseinate.

PubMed

Kuan, Yau-Hoong; Bhat, Rajeev; Karim, Alias A

2011-04-27

The physicochemical and functional properties of ultraviolet (UV)-treated egg white protein (EW) and sodium caseinate (SC) were investigated. UV irradiation of the proteins was carried out for 30, 60, 90, and 120 min. However, the SC samples were subjected to extended UV irradiation for 4 and 6 h as no difference was found on the initial UV exposure time. Formol titration, SDS-PAGE, and FTIR analyses indicated that UV irradiation could induce cross-linking on proteins and led to improved emulsifying and foaming properties (P < 0.05). These results indicated that the UV-irradiated EW and SC could be used as novel emulsifier and foaming agents in broad food systems for stabilizing and foaming purposes.

Antibacterial Activity of Emulsified Pomelo (Citrus grandis Osbeck) Peel Oil and Water-Soluble Chitosan on Staphylococcus aureus and Escherichia coli.

PubMed

Chen, Guan-Wen; Lin, Yu-Hsin; Lin, Chia-Hua; Jen, Hsiao-Chin

2018-04-06

This study utilized pomelo steam distillation to isolate pomelo peel essential oil. The constituents were then analyzed through gas chromatography-mass spectrometry (GC-MS), and the antibacterial activity of the essential oil emulsions at different homogenizer speed conditions and concentrations of water-soluble chitosan (degree of acetylation, DA = 54.8%) against S. aureus and E. coli was examined. Analysis of the essential oil composition identified a total of 33 compounds with the main constituent, limonene accounting for 87.5% (940.07 mg/g) of the total. The pomelo peel oil was emulsified through homogenization at 24,000 rpm, resulting in a minimal inhibitory concentration (MIC) for E. coli that was 1.9 times lower than that of the essential oil without homogenization. In addition, a mixture of 0.4% essential oil emulsion and 0.03% water-soluble chitosan had the strongest synergetic antibacterial effect on S. aureus and E. coli at pH 7.4. In comparison with chitosan alone, the MIC value of this mixture was significantly 2.4 and 2.5 times lower. Hence, this study suggests using a mixture of emulsified pomelo peel oil and water-soluble chitosan to develop a novel natural food preservative, and that the processability of food, as well as the economic value of the byproducts of the Taiwan Matou pomelo and chitosan, could be increased.

Field demonstration of DNAPL dehalogenation using emulsified zero-valent iron

NASA Technical Reports Server (NTRS)

Quinn, Jacqueline; Geiger, Cherie; Clausen, Chris; Brooks, Kathleen; Coon, Christina; O'Hara, Suzanne; Krug, Thomas; Major, David; Yoon, Woong-Sang; Gavaskar, Arun;

Field Demonstration of DNAPL Dehalogenation Using Emulsified Zero-Valent Iron

NASA Technical Reports Server (NTRS)

Quinn, Jacqueline; Geiger, Cherie; Clausen, Chris; Brooks, Kathleen; Coon, Christina; O'Hara, Suzanne; Krug, Thomas; Major, David; Yoon, Sam; Gavaskar, Arun;

Formulation and performance characterization of radio-sterilized "progestin-only" microparticles intended for contraception.

PubMed

Puthli, Shivanand; Vavia, Pradeep

2009-01-01

The aim of this study was to formulate and characterize a microparticulate system of progestin-only contraceptive. Another objective was to evaluate the effect of gamma radio-sterilization on in vitro and in vivo drug release characteristics. Levonorgestrel (LNG) microspheres were fabricated using poly(lactide-co-glycolide) (PLGA) by a novel solvent evaporation technique. The formulation was optimized for drug/polymer ratio, emulsifier concentration, and process variables like speed of agitation and evaporation method. The drug to polymer ratio of 1:5 gave the optimum encapsulation efficiency. Speed of agitation influenced the spherical shape of the microparticles, lower speeds yielding less spherical particles. The speed did not have a significant influence on the drug payloads. A combination of stabilizers viz. methyl cellulose and poly vinyl alcohol with in-water solvent evaporation technique yielded microparticles without any free drug crystals on the surface. This aspect significantly eliminated the in vitro dissolution "burst effect". The residual solvent content was well within the regulatory limits. The microparticles passed the test for sterility and absence of pyrogens. In vitro dissolution conducted on the product before and after gamma radiation sterilization at 2.5 Mrad indicated no significant difference in the drug release patterns. The drug release followed zero-order kinetics in both static and agitation conditions of dissolution testing. The in vivo studies conducted in rabbits exhibited LNG release up to 1 month duration with drug levels maintained within the effective therapeutic window.

Inhibitory effect of BCG cell-wall skeletons (BCG-CWS) emulsified in squalane on tumor growth and metastasis in mice.

PubMed

Yoo, Yung Choon; Hata, Katsusuke; Lee, Kyung Bok; Azuma, Ichiro

2002-08-01

The antimetastatic effect of BCG-CWS, which was emulsified in an oil-in-water form with either Drakeol 6VR mineral oil (BCG-CWS/DK) or squalane (BCG-CWS/SQA), on lung metastasis produced by highly metastatic murine tumor cells, Colon26-M3.1 carcinoma cells and B16-BL6 melanoma cells, was investigated in syngeneic mice. An intravenous (i.v.) administration of BCG-CWS (100 mg/mouse) 1 day after tumor inoculation significantly inhibited tumor metastasis of both Colon26-M3.1 carcinoma and B16-BL6 melanoma cells in experimental lung metastasis models. No differences in the antitumor activity of the two oil-based formulations (BCG-CWS/DK and BCG-CWS/SQA) were obverved. However, BCG-CWS/SQA administered through subcutaneous (s.c.) route was shown to be effective only when it was consecutively injected (3 times) after tumor inoculation. An in vivo analysis for tumor-induced angiogenesis showed that a single i.v. administration of BCG-CWS/SQA inhibited the number of tumor-induced blood vessels and suppressed tumor growth. Furthermore, the multiple administration of BCG-CWS/SQA given at on week intervals led to a significant reduction in spontaneous lung metastasis of B16-BL6 melanoma cells in a spontaneous metastasis model. These results suggest that BCG-CWS emulsified with squalane is a potent inhibitory agent of lung metastasis, and that the antimetastatic effect of BCG-CWS is related to the suppression of tumor growth and the inhibition of tumor-induced angiogenesis.

Identification of outer membrane proteins with emulsifying activity by prediction of beta-barrel regions.

PubMed

Walzer, Gil; Rosenberg, Eugene; Ron, Eliora Z

2009-01-01

Microbial bioemulsifiers are secreted by many bacteria and are important for bacterial interactions with hydrophobic substrates or nutrients and for a variety of biotechnological applications. We have recently shown that the OmpA protein in several members of the Acinetobacter family has emulsifying properties. These properties of OmpA depend on the amino acid composition of four putative extra-membrane loops, which in various strains of Acinetobacter, but not in E. coli, are highly hydrophobic. As many Acinetobacter strains can utilize hydrophobic carbon sources, such as oil, the emulsifying activity of their OmpA may be important for the utilization and uptake of hydrocarbons. We assumed that if outer membrane proteins with emulsifying activity are physiologically important, they may exist in additional oil degrading bacteria. In order to identify such proteins, it was necessary to obtain bioinformatics-based predictions for hydrophobic extra-membrane loops. Here we describe a method for using protein sequence data for predicting the hydrophobic properties of the extra-membrane loops of outer membrane proteins. The feasibility of this method is demonstrated by its use to identify a new microbial bioemulsifier - OprG - an outer membrane protein of the oil degrading Pseudomonas putida KT2440.

Removal of Emulsified Oil from Water by Fruiting Bodies of Macro-Fungus (Auricularia polytricha)

PubMed Central

Yang, Xunan; Guo, Mengting; Wu, Yinghai; Wu, Qunhe; Zhang, Renduo

2014-01-01

The aim of this study was to investigate the feasibility of utilizing the fruiting bodies of a jelly macro-fungus Auricularia polytricha as adsorbents to remove emulsified oil from water. The effects of several factors, including temperature, initial pH, agitation speed, and adsorbent dosage, were taken into account. Results showed that the optimized conditions for adsorption of A. polytricha were a temperature of 35°C, pH of 7.5, and agitation speed of 100 rpm. The adsorption kinetics were characterized by the pseudo-first order model, which showed the adsorption to be a fast physical process. The Langmuir-Freundlich isotherm described the adsorption very well and predicted the maximum adsorption capacity of 398 mg g−1, under optimized conditions. As illustrated by scanning electron micrographs, the oil particles were adsorbed onto the hairs covering the bottom surface and could be desorbed by normal temperature volatilization. The material could be used as an emulsified oil adsorbent at least three times, retaining more than 95% of the maximum adsorption capacity. The results demonstrated that the fruiting bodies of A. polytricha can be a useful adsorbent to remove emulsified oil from water. PMID:24743498

A 2D tank test on remediation of nitrobenzene-contaminated aquifer using in-situ reactive zone with emulsified nanoscale zero-valent iron.

PubMed

Dong, Jun; Dong, Yang; Wen, Chunyu; Gao, Song; Ren, Liming; Bao, Qiburi

2018-05-15

Nitrobenzene (NB) is one of the most challenging pollutants for groundwater remediation due to its great harm and recalcitrance. Emulsified nanoscale zero-valent iron (EZVI) is considered as a promising agent for in-situ remediation of contaminated groundwater for its high reactivity, good durability and low cost. In this paper, 2D tank experiment was conducted to evaluate the effectiveness of enhanced remediation of NB-contaminated groundwater with EZVI. 9 L of EZVI solution was injected into aquifer to establish in-situ reactive zone (IRZ) before 40 d of NB contamination. Results indicate that injection of EZVI leads to 90% reduction of total NB, which is mainly converted to aniline (AN). NB concentration decreases along the flow path in the tank. Fe 2+ is generated from Fe 0 oxidation. Significant acetate and bicarbonate are released due to emulsified oil decomposition during the whole operation time. Groundwater pH maintains in neutral value (6.6-8.2) owing to the balance between organic acids and OH - released after iron oxidation. Drastic decrease of ORP and DO indicates the transformation from oxidizing to reducing condition, leading to the reduction of oxidative species (e.g. sulfate, nitrate) in subsurface. Calculation of reducing equivalents suggests that microbial breakdown of emulsified oil provides more electrons than Fe 0 oxidation does to the system. Both biotic and abiotic processes are involved in the enhanced degradation of NB. Copyright © 2018 Elsevier Ltd. All rights reserved.

Covalent modification of soy protein isolate by (-)-epigallocatechin-3-gallate: effects on structural and emulsifying properties.

PubMed

Tao, Fei; Jiang, He; Chen, Wenwei; Zhang, Yongyong; Pan, Jiarong; Jiang, Jiaxin; Jia, Zhenbao

2018-05-07

Soy protein isolate (SPI) has promising applications in various food products because of its excellent functional properties and nutritional quality. The structural and emulsifying properties of covalently modified SPI by (-)-epigallocatechin-3-gallate (EGCG) were investigated. SPI was covalently modified by EGCG under alkaline conditions. SDS-PAGE analysis revealed that EGCG modification caused cross-linking of SPI proteins. Circular dichroism spectra demonstrated that the secondary structure of SPI proteins was changed by EGCG modification. In addition, the modifications resulted in the perturbation of the tertiary structure of SPI as evidenced by intrinsic fluorescence spectra and surface hydrophobicity measurements. Oil-in-water emulsions of modified SPI had smaller droplet sizes and better creaming stability compared to those from unmodified SPI. The covalent modification by EGCG improved the emulsifying property of SPI. This study provided an innovative approach for improving the emulsifying properties of proteins. This article is protected by copyright. All rights reserved.

Methods to obtain protein concentrates from jumbo squid (Dosidicus gigas) and evaluation of their functionality.

PubMed

Galvez-Rongel, A; Ezquerra-Brauer, J M; Ocano-Higuera, V M; Ramirez-Wong, B; Torres-Arreola, W; Rouzaud-Sandez, O; Marquez-Rios, E

2014-03-01

Jumbo squid is an important fishery resource in Mexico, and its muscle is lean and white and it has a very low price in the market. It is abundant, but with little or nothing added value, therefore is necessary to search alternatives of processing. Due to muscle characteristics, the aim of this study was to obtain protein concentrates using different methods. They were obtained by means of acidic (acid protein concentrates) and alkaline (alkaline protein concentrates) dissolution. Moreover, a protein concentrate was obtained by direct isoelectric precipitation and by the traditional method (neutral protein concentrates). The yield with better results was alkaline protein concentrates (63.58 ± 1.8%). The gel hardness was significantly different (p < 0.05), especially for the alkaline protein concentrates. The acid protein concentrates, isoelectric precipitation and alkaline protein concentrates were better with regard to the neutral protein concentrates, concerning the emulsifying and foaming properties. The protein concentrates by means of alkaline dissolution gave a better gelling property, but all the processes had the potential to obtain protein with emulsifying and foaming properties.

Volatile organic compounds in pesticide formulations: Methods to estimate ozone formation potential

NASA Astrophysics Data System (ADS)

Zeinali, Mazyar; McConnell, Laura L.; Hapeman, Cathleen J.; Nguyen, Anh; Schmidt, Walter F.; Howard, Cody J.

2011-05-01

The environmental fate and toxicity of active ingredients in pesticide formulations has been investigated for many decades, but relatively little research has been conducted on the fate of pesticide co-formulants or inerts. Some co-formulants are volatile organic compounds (VOCs) and can contribute to ground-level ozone pollution. Effective product assessment methods are required to reduce emissions of the most reactive VOCs. Six emulsifiable concentrate pesticide products were characterized for percent VOC by thermogravimetric analysis (TGA) and gas chromatography-mass spectrometry (GC-MS). TGA estimates exceeded GC-MS by 10-50% in all but one product, indicating that for some products a fraction of active ingredient is released during TGA or that VOC contribution was underestimated by GC-MS. VOC profiles were examined using TGA-Fourier transform infrared (FTIR) evolved gas analysis and were compared to GC-MS results. The TGA-FTIR method worked best for products with the simplest and most volatile formulations, but could be developed into an effective product screening tool. An ozone formation potential ( OFP) for each product was calculated using the chemical composition from GC-MS and published maximum incremental reactivity ( MIR) values. OFP values ranged from 0.1 to 3.1 g ozone g -1 product. A 24-h VOC emission simulation was developed for each product assuming a constant emission rate calculated from an equation relating maximum flux rate to vapor pressure. Results indicate 100% VOC loss for some products within a few hours, while other products containing less volatile components will remain in the field for several days after application. An alternate method to calculate a product OFP was investigated utilizing the fraction of the total mass of each chemical emitted at the end of the 24-h simulation. The ideal assessment approach will include: 1) unambiguous chemical composition information; 2) flexible simulation models to estimate emissions under

Effects of Jerusalem Artichoke Powder and Sodium Carbonate as Phosphate Replacers on the Quality Characteristics of Emulsified Chicken Meatballs

PubMed Central

2018-01-01

Today incorporation of natural ingredients as inorganic phosphate replacers has come into prominence as a novel research topic due to health concerns about phosphates. In this study, we aimed to investigate the quality of emulsified chicken meatballs produced with Jerusalem artichoke powder (JAP), either alone or in combination with sodium carbonate (SC) as sodium tripolyphosphate (STPP) replacers. The results showed that naturally dried JAP showed favorable technological properties in terms of water-oil binding and gelling. Emulsion batters formulated with JAP-SC mixture showed lower jelly and fat separation, higher water-holding capacity and higher emulsion stability than control samples with STPP. In final product, incorporation of JAP-SC mixture increased moisture and reduced lipid and energy values, and kept the pH value similar to control. Added JAP lead to increments in b* values whereas decreases L* values. Cook yield was similar to control in phosphate-free samples formulated with JAP-SC mix. Either low or medium ratios of JAP in combination with SC managed to protect most of the sensory parameters, while sensory scores tend to decrease in samples containing high levels of JAP. Addition of JAP to formulations presented samples that have equivalent behavior to phosphates in terms of lipid oxidation. In conclusion, our study confirms that utilization of JAP in combination with SC had promising effects as phosphate replacers by presenting natural solutions and providing equivalent quality to standard phosphate containing products. PMID:29725222

Effects of Jerusalem Artichoke Powder and Sodium Carbonate as Phosphate Replacers on the Quality Characteristics of Emulsified Chicken Meatballs.

PubMed

Öztürk, Burcu; Serdaroğlu, Meltem

2018-02-01

Today incorporation of natural ingredients as inorganic phosphate replacers has come into prominence as a novel research topic due to health concerns about phosphates. In this study, we aimed to investigate the quality of emulsified chicken meatballs produced with Jerusalem artichoke powder (JAP), either alone or in combination with sodium carbonate (SC) as sodium tripolyphosphate (STPP) replacers. The results showed that naturally dried JAP showed favorable technological properties in terms of water-oil binding and gelling. Emulsion batters formulated with JAP-SC mixture showed lower jelly and fat separation, higher water-holding capacity and higher emulsion stability than control samples with STPP. In final product, incorporation of JAP-SC mixture increased moisture and reduced lipid and energy values, and kept the pH value similar to control. Added JAP lead to increments in b* values whereas decreases L* values. Cook yield was similar to control in phosphate-free samples formulated with JAP-SC mix. Either low or medium ratios of JAP in combination with SC managed to protect most of the sensory parameters, while sensory scores tend to decrease in samples containing high levels of JAP. Addition of JAP to formulations presented samples that have equivalent behavior to phosphates in terms of lipid oxidation. In conclusion, our study confirms that utilization of JAP in combination with SC had promising effects as phosphate replacers by presenting natural solutions and providing equivalent quality to standard phosphate containing products.

The effect of Pro NanoLipospheres (PNL) formulation containing natural absorption enhancers on the oral bioavailability of delta-9-tetrahydrocannabinol (THC) and cannabidiol (CBD) in a rat model.

PubMed

Cherniakov, Irina; Izgelov, Dvora; Domb, Abraham J; Hoffman, Amnon

2017-11-15

The lipophilic phytocannabinoids cannabidiol (CBD) and Δ 9 -tetrahydrocannabinol (THC) show therapeutic efficacy in various medical conditions. Both molecules are poorly water soluble and subjected to extensive first pass metabolism in the gastrointestinal tract, leading to a limited oral bioavailability of approximately 9%. We have developed an advanced lipid based Self-Emulsifying Drug Delivery System termed Advanced Pro-NanoLiposphere (PNL) pre-concentrate. The PNL is composed of lipid and emulsifying excipients of GRAS status and are known to increase solubility and reduce Phase I metabolism of lipophilic active compounds. Advanced PNLs are PNLs with an incorporated natural absorption enhancers. These molecules are natural alkaloids and phenolic compounds which were reported to inhibit certain phase I and phase II metabolism processes. Here we use piperine, curcumin and resveratrol to formulate the Advanced-PNL formulations. Consequently, we have explored the utility of these Advanced-PNLs on CBD and THC oral bioavailability. Oral administration of CBD-piperine-PNL resulted in 6-fold increase in AUC compared to CBD solution, proving to be the most effective of the screened formulations. The same trend was found in pharmacokinetic experiments of THC-piperine-PNL which resulted in a 9.3-fold increase in AUC as compared to THC solution. Our Piperine-PNL can be used as a platform for synchronized delivery of piperine and CBD or THC to the enterocyte site. This co-localization provides an increase in CBD and THC bioavailability by its effect at the pre-enterocyte and the enterocyte levels of the absorption process. The extra augmentation in the absorption of CBD and THC by incorporating piperine into PNL is attributed to the inhibition of Phase I and phase II metabolism by piperine in addition to the Phase I metabolism and P-gp inhibition by PNL. These novel results pave the way to utilize piperine-PNL delivery system for other poorly soluble, highly metabolized

Lipid composition and emulsifying properties of canola lecithin from enzymatic degumming.

PubMed

Xie, Meizhen; Dunford, Nurhan Turgut

2017-03-01

This study investigated the polar lipid composition and emulsifying properties of canola lecithin from enzymatic degumming (CLED). Phospholipase A 1 was used for enzymatic degumming of crude canola oil to collect lecithin sample. Canola lecithin from water degumming (CLWD) was also collected and served as the control. The results showed that the contents of phosphatidylethanolamine (PE) (2.99%) and phosphatidylcholine (PC) (6.59%) in CLED were significantly lower than that in CLWD (PE 15.55% and PC 21.93%); while the content of lysophosphatidylcholine (LPC) (19.45%) in CLED was significantly higher than that in CLWD (3.27%). Unsaturated fatty acids accounted for a higher percentage of the total fatty acids in CLED than in CLWD. CLED promoted more stable o/w emulsions than CLWD. This study provides a better understanding of the chemical nature of CLED, and important information for utilization of CLED as o/w emulsifier. Copyright © 2016 Elsevier Ltd. All rights reserved.

Characterization of E 471 food emulsifiers by high-performance thin-layer chromatography-fluorescence detection.

PubMed

Oellig, Claudia; Brändle, Klara; Schwack, Wolfgang

2018-07-13

Mono- and diacylglycerol (MAG and DAG) emulsifiers, also known as food additive E 471, are widely used to adjust techno-functional properties in various foods. Besides MAGs and DAGs, E 471 emulsifiers additionally comprise different amounts of triacylglycerols (TAGs) and free fatty acids (FFAs). MAGs, DAGs, TAGs and FFAs are generally determined by high-performance liquid chromatography (HPLC) or gas chromatography (GC) coupled to mass selective detection, analyzing the individual representatives of the lipid classes. In this work we present a rapid and sensitive method for the determination of MAGs, DAGs, TAGs and FFAs in E 471 emulsifiers by high-performance thin-layer chromatography with fluorescence detection (HPTLC-FLD), including a response factor system for quantitation. Samples were simply dissolved and diluted with t-butyl methyl ether before a two-fold development was performed on primuline pre-impregnated LiChrospher silica gel plates with diethyl ether and n-pentane/n-hexane/diethyl ether (52:20:28, v/v/v) as the mobile phases to 18 and 75 mm, respectively. For quantitation, the plate was scanned in the fluorescence mode at UV 366/>400 nm, when the cumulative signal for each lipid class was used. Calibration was done with 1,2-distearin and amounts of lipid classes were calculated with response factors and expressed as monostearin, distearin, tristearin and stearic acid. Limits of detection and quantitation were 1 and 4 ng/zone, respectively, for 1,2-distearin. Thus, the HPTLC-FLD approach represents a simple, rapid and convenient screening alternative to HPLC and GC analysis of the individual compounds. Visual detection additionally enables an easy characterization and the direct comparison of emulsifiers through the lipid class pattern, when utilized as a fingerprint. Copyright © 2018 Elsevier B.V. All rights reserved.

Oral bioavailability of DN101, a concentrated formulation of calcitriol, in tumor-bearing dogs.

PubMed

Rassnick, Kenneth M; Muindi, Josephia R; Johnson, Candace S; Bailey, Dennis B; Trump, Donald L

2011-01-01

High-dose calcitriol (1,25-dihydroxyvitamin D(3)) has antineoplastic activity against a range of tumors and potentiates chemotherapeutic agents. In an earlier canine study, the MTD of intravenous (i.v.) calcitriol was 3.75 μg/kg, but polysorbate-associated hypersensitivity reactions were common. Use of commercially available oral calcitriol is limited by the absence of a formulation of suitable strength to allow administration of a reasonable number of caplets. This study evaluated the bioavailability of DN101, a concentrated oral calcitriol formulation specifically developed for anticancer applications. An open-label, single-dose, 2-way crossover study was conducted. Dogs randomly received a single 3.75 μg/kg dose of calcitriol either i.v. or oral (as DN101), followed by cisplatin (60 mg/m(2)). Three weeks later, the alternate form of calcitriol was given prior to another dose of cisplatin. Dogs received antihistamines and corticosteroids prior to both treatments. Food was withheld for 12 h before and after therapy. Serum calcitriol concentrations were measured by radioimmunoassay. Ten tumor-bearing dogs received both i.v. and oral calcitriol. Six dogs experienced hypersensitivity reactions during i.v. calcitriol. Sequence of calcitriol administration (day-1 vs. day-21) by either i.v. or oral routes had no effect on the major calcitriol pharmacokinetic parameters. Oral calcitriol resulted in significantly lower values for AUC (P = 0.05) and prolonged T (1/2) (P = 0.003) when compared to i.v. Calcitriol oral bioavailability was highly variable among dogs (mean ± SEM, 71 ± 12.6%). This study demonstrates that a high-dose formulation of calcitriol has a moderate bioavailability in dogs, but inter-individual variability in PK parameters is similar to that observed in people. With this bioavailability, serum concentrations of calcitriol that exhibit antitumor activity in a preclinical murine model were achieved in some dogs. Exploration of methods to minimize

Assessing the fate of an aromatic hydrocarbon fluid in agricultural spray applications using the three-stage ADVOCATE model framework

USDA-ARS?s Scientific Manuscript database

Components of emulsifiable concentrates (ECs) used in pesticide formulations may be emitted to air following application in agricultural use and contribute to ozone formation. A key consideration is the fraction of the ECs that is volatilized. This study is designed to provide a mechanistic model fr...

Concentrated formulations and methods for neutralizing chemical and biological toxants

DOEpatents

Tucker, Mark D.; Betty, Rita G.; Tadros, Maher E.

2004-04-20

A formulation and method of making and using that neutralizes the adverse health effects of both chemical and biological toxants, especially chemical warfare (CW) and biological warfare (BW) agents. The aqueous formulation is non-toxic and non-corrosive and can be delivered as a long-lasting foam, spray, or fog. The formulation includes solubilizing compounds that serve to effectively render the CW or BW toxant susceptible to attack, so that a nucleophillic agent can attack the compound via a hydrolysis or oxidation reaction. The formulation can kill up to 99.99999% of bacterial spores within one hour of exposure.

[The application of the emulsified turpentine baths for the correction of the functional state of the cross-country skiers].

PubMed

Garnov, I O; Kuchin, A V; Loginova, T P; Varlamova, N G; Boiko, E R

2016-01-01

The baths with emulsified turpentine find the wide application in balneotherapy. They produce especially pronounced beneficial prophylactic effects in the patients presenting with microtrombosis and microvascular stasis. Moreover, these baths may be prescribed to improve microcirculation, increase the functional reserves and physical capacity in the athletes. At the same time, the current literature appears to contain no scientific publications on the application of emulsified turpentine baths for the restoration of the physical capacity of the professional ski runners. The lack of relevant information motivated the study reported in the present article. The main objective of the study involving 10 subjects was to evaluate the effectiveness of the modified emulsified turpentine baths as a method by which to restore and enhance the physical capacity of the professional cross-country skiers. The physical capacity of the athletes was evaluated from the results of the bicycle ergometer exercise test with the use of the «Oxycon Pro» system. The data obtained suggest that a course of the emulsified turpentine baths increases the activity of the cardiorespiratory system, improves the physical capacity, and enhances the functional reserves of the body in the anaerobic zone.

Dorzolamide-loaded PLGA/vitamin E TPGS nanoparticles for glaucoma therapy: Pharmacoscintigraphy study and evaluation of extended ocular hypotensive effect in rabbits.

PubMed

Warsi, Musarrat H; Anwar, Mohammed; Garg, Vaidehi; Jain, Gaurav K; Talegaonkar, Sushama; Ahmad, Farhan J; Khar, Roop K

2014-10-01

Poor drug penetration and rapid clearance after topical instillation of a drug formulation into the eyes are the major causes for the lower ocular bioavailability from conventional eye drops. Along with this, poor encapsulation efficiency of hydrophilic drug in polymeric nanoparticles remains a major formulation challenge. Taking this perspective into consideration, dorzolamide (DZ)-loaded PLGA nanoparticles were developed employing two different emulsifiers (PVA and vitamin E TPGS) and the effects of various formulation and process variables on particle size and encapsulation efficiency were assessed. Nanoparticles emulsified with vitamin E TPGS (DZ-T-NPs) were found to possess enhanced drug encapsulation (59.8±6.1%) as compared to those developed with PVA as emulsifier (DZ-P-NPs). Transcorneal permeation study revealed a significant enhancement in permeation (1.8-2.5 fold) as compared to solution. In addition, ex vivo biodistribution study showed a higher concentration of drug in the aqueous humour (1.5-2.3 fold). Histological and IR-camera studies proved the non-irritant potential of the formulations. Pharmacoscintigraphic studies revealed the reduced corneal clearance, as well as naso-lachrymal drainage in comparison to drug solution. Furthermore, efficacy study revealed that DZ-P-NPs and DZ-T-NPs significantly reduced the intraocular pressure by 22.81% and 29.12%, respectively, after a single topical instillation into the eye. Copyright © 2014 Elsevier B.V. All rights reserved.

Effect of antioxidant properties of lecithin emulsifier on oxidative stability of encapsulated bioactive compounds.

PubMed

Pan, Yuanjie; Tikekar, Rohan V; Nitin, N

2013-06-25

Oxidation of encapsulated bioactive compounds in emulsions is one of the key challenges that limit shelf life of emulsion containing products. Oxidation in these emulsions is triggered by permeation of free radicals generated at the emulsion interface. The objective of this study was to evaluate the role of antioxidant properties of common emulsifiers (lecithin and Tween 20) in reducing permeation of free radicals across the emulsion interface. Radical permeation rates were correlated with oxidative stability of a model bioactive compound (curcumin) encapsulated in these emulsions. Rate of permeation of peroxyl radicals from the aqueous phase to the oil phase of emulsion was inversely proportional to the antioxidant properties of emulsifiers. The rate of radical permeation was significantly higher (p<0.05) for emulsions stabilized using Tween 20 and oxidized lecithin compared to native lecithin that showed higher antioxidant activity. Free radical permeation rate correlated with stability of curcumin in emulsions and was significantly higher (p<0.05) in lecithin stabilized emulsions as compared to Tween 20 emulsions. Overall, this study demonstrates that antioxidant activity of emulsifiers significantly influences permeation of free radicals across the emulsion interface and the rate of oxidation of bioactive encapsulant. Copyright © 2013 Elsevier B.V. All rights reserved.

Effects of rice bran on sensory and physico-chemical properties of emulsified pork meatballs.

PubMed

Huang, S C; Shiau, C Y; Liu, T E; Chu, C L; Hwang, D F

2005-08-01

Four kinds of bran, which are milled from important rice cultivators in Taiwan, have high contents of dietary fiber, fat and protein. The use of rice bran in Kung-wan, an emulsified pork meatball, was investigated. It was found that protein and fat contents, and white index of meatballs decreased as the amount of bran increased. A texture profile analysis (TPA) also indicated the hardness, gumminess and chewiness of the Kung-wan decreased. The sensory scores of taste, texture and overall acceptability of meatballs with less than 10% added bran showed no significant difference from those for meatballs without bran. However, the added amount of 15% enriched meatballs resulted in inferior sensory scores. The bran's particle size profoundly affected the sensory and physico-chemical properties of the meat products. Meatballs enriched with smaller bran particles possessed higher TPA indices and sensory scores than those added with larger ones. No significant differences in proximate composition, cooking yield, color and sensory quality were found among emulsified meatballs enriched with four different kinds of bran. Conclusively, the suitable amount of rice bran that should be added to emulsified pork meatballs was less than 10% and a smaller particle size would result in better quality.

In vivo quantification of photosensitizer concentration using fluorescence differential path-length spectroscopy: influence of photosensitizer formulation and tissue location

NASA Astrophysics Data System (ADS)

de Visscher, Sebastiaan A. H. J.; Witjes, Max J. H.; Kaščáková, Slávka; Sterenborg, Henricus J. C. M.; Robinson, Dominic J.; Roodenburg, Jan L. N.; Amelink, Arjen

2012-06-01

In vivo measurement of photosensitizer concentrations may optimize clinical photodynamic therapy (PDT). Fluorescence differential path-length spectroscopy (FDPS) is a non-invasive optical technique that has been shown to accurately quantify the concentration of Foscan® in rat liver. As a next step towards clinical translation, the effect of two liposomal formulations of mTHPC, Fospeg® and Foslip®, on FDPS response was investigated. Furthermore, FDPS was evaluated in target organs for head-and-neck PDT. Fifty-four healthy rats were intravenously injected with one of the three formulations of mTHPC at 0.15 mg kg-1. FDPS was performed on liver, tongue, and lip. The mTHPC concentrations estimated using FDPS were correlated with the results of the subsequent harvested and chemically extracted organs. An excellent goodness of fit (R2) between FDPS and extraction was found for all formulations in the liver (R2=0.79). A much lower R2 between FDPS and extraction was found in lip (R2=0.46) and tongue (R2=0.10). The lower performance in lip and in particular tongue was mainly attributed to the more layered anatomical structure, which influences scattering properties and photosensitizer distribution.

FIELD EVALUATION OF THE TREATMENT OF DNAPL USING EMULSIFIED ZERO-VALENT IRON

EPA Science Inventory

A pilot scale field demonstration of dense non-aqueous phase liquids (DNAPL) treatment using emulsified zero-valent iron (EZVI) is being conducted at Parris Island Marine Corps Recruit Depot (MCRD), Parris Island SC. The demonstration is being conducted by Geosyntec, the Nationa...

Application of multiwalled carbon nanotubes and its magnetite derivative for emulsified oil removal from produced water.

PubMed

Ibrahim, Taleb H; Sabri, Muhammad A; Khamis, Mustafa I

2018-05-10

Multiwalled carbon nanotubes and their magnetite derivatives were employed as adsorbents for emulsified oil removal from produced water. The experimental parameters for maximum emulsified oil removal efficiency and effective regeneration of these adsorbents were determined. The optimum parameters in terms of adsorbent dosage, contact time, salinity, pH and temperature were 3.0 g/L, 20.0 min, 0 ppm, 7.0 and 25°C for both adsorbents. Due to their low density, multiwalledcarbon nanotubes could not be successfully employed in packed bed columns. The magnetite derivative has a larger density and hence, for the removal of emulsified oil from produced water packed bed column studies were performed utilizing multiwalled carbon magnetite nanotubes. The packed bed column efficiency and behaviour were evaluated using Thomas, Clark, Yan et al. and Bohart and Adams models. The Yan model was found to best describe the column experimental data. The adsorbents were regenerated using n-hexane and reused several times for oil removal from produced water without any significant decrease in their initial adsorption capacities.

Enhanced bioavailability of EPA from emulsified fish oil preparations versus capsular triacylglycerol

USDA-ARS?s Scientific Manuscript database

Pre-emulsified fish oil supplements, an alternative to capsular triacylglycerol, may enhance the uptake of LCn3 fatty acids it contains. A randomized, Latin-square crossover design was used to compare the effects of four fish oil supplement preparations on phospholipid (PLFA) and chylomicron fatty ...

Development of solid self-emulsifying drug delivery system (SEDDS) I: use of poloxamer 188 as both solidifying and emulsifying agent for lipids.

PubMed

Shah, Ankita V; Serajuddin, Abu T M

2012-10-01

To develop solid self-emulsifying drug delivery systems (SEDDS) for lipids using poloxamer 188 as both solidifying and emulsifying agents. Mixtures of various lipids with poloxamer 188 and PEG 8000 were prepared at ~75°C. The molten mixtures, with and without dissolved drugs (fenofibrate and probucol), were then cooled to room temperature. When solids formed, they were characterized by powder XRD, DSC, microscopy using cross-polarization and confocal fluorescence techniques, dispersion test in water and particle size analysis of dispersions. When mixed with poloxamer 188 or PEG 8000, lipids consisting of monoesters of fatty acids with glycerol or propylene glycol formed solid systems, but not di- and tri-esters, which showed phase separation. Added to water, the solid systems containing poloxamer 188 started to disperse in water forming oil globules of 200-600 nm. No emulsification of lipids was observed from solids containing PEG 8000, indicating that the surfactant property of poloxamer 188 was responsible for emulsification. Powder XRD, DSC and microscopic examination revealed that poloxamer 188 and PEG 8000 maintained their crystallinity in solid systems, while the lipids were interspersed in between crystalline regions. The drug remained solubilized in the lipid phase. A novel solid SEDDS is developed where the drug can be solubilized in liquid lipids and then the lipidic solution can be converted to solid mass by dispersing into the microstructure of poloxamer 188.

Formulation and optimization of pH sensitive drug releasing O/W emulsions using Albizia lebbeck L. seed polysaccharide.

PubMed

Varma, Chekuri Ashok Kumar; Jayaram Kumar, K

2018-04-30

Smart polymers, one of the class of polymers with extensive growth in the last few decades due to their wide applications in drug targeting and controlled delivery systems. With this in mind, the aim of the present study is to design and formulate smart releasing o/w emulsion by using Albizia lebbeck L. seed polysaccharide (ALPS). For this purpose, the physicochemical and drug release characteristics like emulsion capacity (EC), emulsion stability (ES), viscosity, microscopy, zeta potential, polydispersity index (PDI) and in-vitro drug release were performed. The EC and ES values were found to increase with an increased concentration of ALPS. The emulsion formulations were statistically designed by using 3 2 full factorial design. All the emulsions showed a shear-thinning behavior. The zeta potential and polydispersity index were found to be in the range of -35.83 mV to -19.00 mV and 0.232-1.000 respectively. Further, the percent cumulative drug release of the emulsions at 8 h was found to be in the range of 30.19-82.65%. The drug release profile exhibited zero order release kinetics. In conclusion, the ALPS can be used as a natural emulsifier and smart polymer for the preparation of pH sensitive emulsions in drug delivery systems. Copyright © 2018 Elsevier B.V. All rights reserved.

Influence of different emulsifiers on characteristics of eggless cake containing soy milk: Modeling of physical and sensory properties by mixture experimental design.

PubMed

Rahmati, Nazanin Fatemeh; Mazaheri Tehrani, Mostafa

2014-09-01

Emulsifiers of different structures and functionalities are important ingredients usually used in baking cakes with satisfactory properties. In this study, three emulsifiers including distilled glycerol mono stearate (DGMS), lecithin and sorbitan mono stearate (SMS) were used to bake seven eggless cakes containing soy milk and optimization was performed by using mixture experimental design to produce an eggless cake sample with optimized properties. Physical properties of cake batters (viscosity, specific gravity and stability), cake quality parameters (moisture loss, density, specific volume, volume index, contour, symmetry, color and texture) and sensory attributes of eggless cakes were analyzed to investigate functional potential of the emulsifiers and results were compared with those of control cake containing egg. Almost in all cases emulsifiers, compared to the control cake, changed properties of eggless cakes significantly. Regarding models of different response variables (except for some properties) and their high R(2) (99.51-100), it could be concluded that models obtained by mixture design were significantly fitted for the studied responses.

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.

The influence of carbohydrate-based fat replacers with and without emulsifiers on the quality characteristics of lowfat cake.

PubMed

Khalil, A H

1998-01-01

Physical and sensory characteristics of cakes prepared with either the carbohydrate-based fat replacers N-Flate, Paselli MD 10 and Litesse (0, 25, 50 and 75% of fat weight) or fat replacers plus emulsifier (mono- and diglycerides; 0 and 3% of flour weight) were studied. Specific gravity of the batter was significantly (p < or = 0.05) improved by using the carbohydrate-based fat replacers, especially at the 25 and 50% replacement levels. The combination of the emulsifier with either Paselli MD 10 or Litesse also enhanced the specific gravity. Cakes prepared with fat replacers at the 25 and 50% levels had higher volumes, specific volume and standing heights than those of the control. Cakes prepared with fat replacers at the 25, 50 and 75% levels were more compressible than the control. Cakes prepared with Paselli MD 10 had the highest volumes, specific volume, standing heights and compressibilities. Incorporation of emulsifier with fat replacers improved cake volumes, standing heights and compressibilities. Cakes prepared with fat replacers exhibited higher crust and crumb color values compared to the control. Cakes prepared with 25 or 50% fat replacers had higher mean scores for flavor, softness and eating quality than the control. Incorporation of emulsifier with fat replacers did not affect the crust color, crumb color and flavor, but significantly (p < or = 0.05) improved softness and eating quality.

Distribution and persistence of emamectin benzoate at efficacious concentrations in pine tissues after injection of a liquid formulation.

PubMed

Takai, Kazuya; Suzuki, Toshio; Kawazu, Kazuyoshi

2004-01-01

In an earlier paper the authors reported the creation of a novel emamectin benzoate 40 g litre(-1) liquid formulation (Shot Wan Liquid Formulation). The injection of this formulation exerted a preventative effect against the pine wilt disease caused by the pine wood nematode, Bursaphelenchus xylophilus (Steiner & Buhrer) Nickle, and this effect lasted for at least 3 years. The present study was carried out to show experimentally that the marked effect of this formulation was due to the presence and persistence in pine tissues of sufficient amounts of emamectin benzoate to inhibit nematode propagation. A cleanup procedure prior to quantitative analysis of emamectin benzoate by fluorescence HPLC was devised. The presence of the compound in concentrations sufficient to inhibit nematode propagation in the shoots of current growth and its persistence for 3 years explained the marked preventative effect. Non-distribution of emamectin benzoate in some parts of the lower trunk suggested that the formulation should be injected at several points for large trees in order to distribute the compound uniformly to lower branches.

Field test on the treatment of source zone chloroethenes using emulsified zerovalent iron

EPA Science Inventory

This talk summarizes the research activities currently underway at the Solid Waste Management Unit 45 (Site 45), Marine Corps Recruit Depot, Parris Island, South Carolina. A pilot field test was initiated in 2005 at this site to evaluate the effectiveness of nanoscale emulsified...

Processing effects on physicochemical properties of creams formulated with modified milk fat.

PubMed

Bolling, J C; Duncan, S E; Eigel, W N; Waterman, K M

2005-04-01

Type of thermal process [high temperature, short time pasteurization (HTST) or ultra-high temperature pasteurization (UHT)] and homogenization sequence (before or after pasteurization) were examined for influence on the physicochemical properties of natural cream (20% milk fat) and creams formulated with 20% low-melt, fractionated butteroil emulsified with skim milk, or buttermilk and butter-derived aqueous phase. Homogenization sequence influenced physicochemical makeup of the creams. Creams homogenized before pasteurization contained more milk fat surface material, higher phospholipid levels, and less protein at the milk fat interface than creams homogenized after pasteurization. Phosphodiesterase I activity was higher (relative to protein on lipid globule surface) when cream was homogenized before pasteurization. Creams formulated with skim milk and modified milk fat had relatively more phospholipid adsorbed at the milk fat interface. Ultra-high-temperature-pasteurized natural and reformulated creams were higher in viscosity at all shear rates investigated compared with HTST-pasteurized creams. High-temperature, short time-pasteurized natural cream was more viscous than HTST-pasteurized reformulated creams at most shear rates investigated. High-temperature, short time-pasteurized creams had better emulsion stability than UHT-pasteurized creams. Cream formulated with buttermilk had creaming stability most comparable to natural cream, and cream formulated with skim milk and modified butteroil was least stable to creaming. Most creams feathered in a pH range of 5.00 to 5.20, indicating that they were moderately stable to slightly unstable emulsions. All processing sequences yielded creams within sensory specifications with the exception of treatments homogenized before UHT pasteurization and skim milk formulations homogenized after UHT pasteurization.

Influence of high dose of phytase and an emulsifier on performance, apparent metabolisable energy and nitrogen retention in broilers fed on diets containing soy oil or tallow.

PubMed

Zaefarian, F; Romero, L F; Ravindran, V

2015-01-01

The effects of high dose of microbial phytase and an emulsifier on the performance, apparent metabolisable energy (AME) and nitrogen (N) retention in broilers fed on diets containing different fat sources were examined in a 5-week trial. Two fat sources (soy oil and tallow), two inclusion levels of E. coli phytase (500 or 1000 phytase units (FTU)/kg diet) and two inclusion levels of lysolecithin emulsifier (0 or 3.5 g/kg of diet) were evaluated in a 2 × 2 × 2 factorial arrangement of treatments. Throughout the 5-week trial, soy oil supplementation improved weight gain and feed per gain compared with tallow, but had no effect on feed intake. The high dose of phytase increased the weight gain and feed intake and lowered the feed per gain during d 1-21, but had no effect on performance parameters over the whole trial period. An effect of emulsifier was observed for feed intake during d 1-21 and over the whole trial period. Addition of emulsifier increased feed intake compared with diets without emulsifier. During weeks 1, 2, 3 and 5, birds fed on soy oil-based diets had higher nitrogen-corrected AME (AMEN) compared with those fed on tallow-based diets. During weeks 2, 3 and 5, the effect of phytase was significant for AMEN, with the high dose increasing the AMEN. During week 2, AMEN was increased with emulsifier addition. During weeks 1, 2, 3 and 5, birds fed on soy oil-based diets had higher fat retention compared with those fed on tallow-based diets. The high dose of phytase improved the retention of fat during week 5 and the addition of emulsifier resulted in higher fat retention during week 1. During weeks 2, 3 and 5, an interaction between fat source × phytase × emulsifier was observed for N retention. In soy oil-based diets, emulsifier plus 1000 FTU/kg phytase increased N retention compared with other groups, while in tallow-based diets, emulsifier addition increased N retention in diets with 500 FTU/kg, but not in 1000 FTU/kg diet. Overall, the

Selective factors governing in vitro β-carotene bioaccessibility: negative influence of low filtration cutoffs and alterations by emulsifiers and food matrices.

PubMed

Corte-Real, Joana; Richling, Elke; Hoffmann, Lucien; Bohn, Torsten

2014-12-01

Because of their putative health benefits, the biological fate of carotenoids after digestion has been met with much interest, and ex vivo methods using carotenoid standards to study their digestion and further metabolism have been developed. In the absence of a complex food matrix, that is, when studying isolated carotenoids, protocol conditions of gastrointestinal digestion models have to be adjusted. In this investigation, we hypothesized that certain selected factors would significantly influence the bioaccessibility of β-carotene in vitro. The factors considered included (i) type of lipid matrix employed (milk, cream, or oil), (ii) presence/absence of emulsifiers (e.g. lecithin and taurocholate), (iii) addition of a gastric lipase, and (iv) final filtration (20 or 200 nm) of the digesta. Adding an emulsifier mixture (10 mg lecithin + 50 mg monoolein + 5 mg oleic acid) enhanced β-carotene bioaccessibility 3 times (P < 0.001), whereas additional taurocholate and the presence/absence of gastric lipase added before intestinal digestion had no significant effect. β-Carotene bioaccessibility was superior with oil than with milk (18.8% ± 0.7% and 6.1% ± 0.7%, respectively; P = 0.03), especially after filtration, thus suggesting incomplete micelle formation after addition of milk. Filtration through 20 nm filters reduced carotenoid concentration in the aqueous fraction (from 7.1% ± 0.2% to 5.5% ± 0.2% in samples digested with canola oil, P < 0.001), indicating that not all formed micelles compared in size with those normally formed in vivo. When studying carotenoid standards during in vitro digestion, care should be taken to separate mixed micelles by filtration, and the choice of emulsifier and matrix should be considered. Copyright © 2014 Elsevier Inc. All rights reserved.

Synthesis and characterization of fluorinated polyacrylate latex emulsified with novel surfactants.

PubMed

Zhang, Cuifeng; Xu, Tingting; Bao, Zhongbin; Chen, Lijun

2017-01-01

The fluorinated polyacrylate latex were successfully prepared with semi- continuous seeded emulsion polymerization of butyl acrylate (BA), methyl methacrylate (MMA) and hexafluorobutyl methacrylate (HFMA) which was initiated with potassium persulfate (KPS) initiator and emulsified with the novel mixed surfactants of sodium lauryl glutamate (SLG) and alkylphenol ethoxylates (OP-10). The structure of the resultant latex was confirmed by Fourier transform infrared spectroscopy (FTIR). The particle size of the latex was measured by Zetatrac dynamic light scattering detector. The film of latex was tested by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and contact angle (CA). The optimum conditions of preparing the novel fluorinated polyacrylate latex are optimized and the results are as follows: the amount of emulsifiers is 4.0%; mass ratio of SLG to OP-10 is 1:1, the amount of the initiator is 0.6%. The mass ratio of MMA to BA is 1:1 and the amount of HFMA is 7.0%. In this case, the conversion is high and the polymerization stability is good. In addition, the water resistance and thermal properties of the latex films were improved significantly in comparison with the film of the latex prepared without the fluorinated monomer.

Relation between ultrasonic properties, rheology and baking quality for bread doughs of widely differing formulation.

PubMed

Peressini, Donatella; Braunstein, Dobrila; Page, John H; Strybulevych, Anatoliy; Lagazio, Corrado; Scanlon, Martin G

2017-06-01

The objective was to evaluate whether an ultrasonic reflectance technique has predictive capacity for breadmaking performance of doughs made under a wide range of formulation conditions. Two flours of contrasting dough strength augmented with different levels of ingredients (inulin, oil, emulsifier or salt) were used to produce different bread doughs with a wide range of properties. Breadmaking performance was evaluated by conventional large-strain rheological tests on the dough and by assessment of loaf quality. The ultrasound tests were performed with a broadband reflectance technique in the frequency range of 0.3-6 MHz. Principal component analysis showed that ultrasonic attenuation and phase velocity at frequencies between 0.3 and 3 MHz are good predictors for rheological and bread scoring characteristics. Ultrasonic parameters had predictive capacity for breadmaking performance for a wide range of dough formulations. Lower frequency attenuation coefficients correlated well with conventional quality indices of both the dough and the bread. © 2016 Society of Chemical Industry. © 2016 Society of Chemical Industry.

Advanced stable lipid-based formulations for a patient-centric product design.

PubMed

Becker, Karin; Saurugger, Eva-Maria; Kienberger, Diana; Lopes, Diogo; Haack, Detlev; Köberle, Martin; Stehr, Michael; Lochmann, Dirk; Zimmer, Andreas; Salar-Behzadi, Sharareh

2016-01-30

Multiparticulate dosage forms are a recent strategy to meet the special needs of children, elderly people and patients suffering from dysphagia. Our study presents a novel and cost-efficient approach for the manufacturing of a taste-masked multiparticulate system with a stable immediate release profile by applying lipid-based excipients in a solvent-free hot melt coating process. The thermosensitive N-acetylcysteine (N-ac) was used as model drug and hot-melt coated with a mixture of tripalmitin and polysorbate 65. A predictive in vitro method for the evaluation of the taste masking efficiency was developed based on the deprotonation of the carboxyl group of N-ac and the decline of pH, responsible for the unpleasant sour taste of the compound. The method was confirmed using in vivo studies. Differential scanning calorimetry and X-ray scattering experiments revealed polymorphic transformation and its dependency on transformation time, temperature and emulsifier concentration. During the process, the coating was transformed almost completely into the stable β-polymorph, leading to an unaltered dissolution profile during storage. A statistical design was conducted that revealed the critical process parameters affecting the taste masking efficiency and drug release. This study shows the successful application of solvent-free hot-melt coating in the development of a taste-masked and stable formulation. Copyright © 2015 Elsevier B.V. All rights reserved.

Interfacial and emulsifying properties of designed β-strand peptides.

PubMed

Dexter, Annette F

2010-12-07

The structural and surfactant properties of a series of amphipathic β-strand peptides have been studied as a function of pH. Each nine-residue peptide has a framework of hydrophobic proline and phenylalanine amino acid residues, alternating with acidic or basic amino acids to give a sequence closely related to known β-sheet formers. Surface activity, interfacial mechanical properties, electronic circular dichroism (ECD), droplet sizing and zeta potential measurements were used to gain an overview of the peptide behavior as the molecular charge varied from ±4 to 0 with pH. ECD data suggest that the peptides form polyproline-type helices in bulk aqueous solution when highly charged, but may fold to β-hairpins rather than β-sheets when uncharged. In the uncharged state, the peptides adsorb readily at a macroscopic fluid interface to form mechanically strong interfacial films, but tend to give large droplet sizes on emulsification, apparently due to flocculation at a low droplet zeta potential. In contrast, highly charged peptide states gave a low interfacial coverage, but retained good emulsifying activity as judged by droplet size. Best emulsification was generally seen for intermediate charged states of the peptides, possibly representing a compromise between droplet zeta potential and interfacial binding affinity. The emulsifying properties of β-strand peptides have not been previously reported. Understanding the interfacial properties of such peptides is important to their potential development as biosurfactants.

THE INFLUENCE OF CARBON BURNOUT ON SUBMICRON PARTICLE FORMATION FROM EMULSIFIED FUEL OIL COMBUSTION

EPA Science Inventory

The paper gives results of an examination of particle behavior and particle size distributions from the combustion of different fuel oils and emulsified fuels in three experimental combusators. Results indicate that improved carbon (C) burnout from fule oil combustion, either by...

Enhanced absorption of n-3 fatty acids from emulsified compared with encapsulated fish oil

USDA-ARS?s Scientific Manuscript database

The omega-3 fatty acids, eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) have important nutrition and disease management properties. Presently fish oil (FO) supplementation relies on capsular triglyceride. Flavored emulsified lipid preparations may provide an improved approach to FO del...

In vitro digestion of the self-emulsifying lipid excipient Labrasol(®) by gastrointestinal lipases and influence of its colloidal structure on lipolysis rate.

PubMed

Fernandez, Sylvie; Jannin, Vincent; Chevrier, Stéphanie; Chavant, Yann; Demarne, Frédéric; Carrière, Frédéric

2013-12-01

Labrasol(®) is a self-emulsifying excipient used to improve the oral bioavailability of poorly water-soluble drugs. It is a mixture of acylglycerols and PEG esters, these compounds being substrates for digestive lipases. The characterization of Labrasol(®) gastrointestinal lipolysis is essential for understanding its mode of action. Labrasol(®) lipolysis was investigated using either individual enzymes (gastric lipase, pancreatic lipase-related protein 2, pancreatic carboxyl ester hydrolase) or a combination of enzymes under in vitro conditions mimicking first the gastric phase of lipolysis and second the duodenal one. Specific methods for quantifying lipolysis products were established in order to determine which compounds in Labrasol(®) were preferentially hydrolyzed. Gastric lipase showed a preference for di- and triacylglycerols and the main acylglycerols remaining after gastric lipolysis were monoacylglycerols. PEG-8 diesters were also hydrolyzed to a large extent by gastric lipase. Most of the compounds initially present in Labrasol(®) were found to be totally hydrolyzed after the duodenal phase of lipolysis. The rate of Labrasol(®) hydrolysis by individual lipases was found to vary significantly with the dilution of the excipient in water and the resulting colloidal structures (translucent dispersion; opaque emulsion; transparent microemulsion), each lipase displaying a distinct pattern depending on the particle size. The lipases with distinct substrate specificities used in this study were found to be sensitive probes of phase transitions occurring upon Labrasol(®) dilution. In addition to their use for developing in vitro digestion models, these enzymes are interesting tools for the characterization of self-emulsifying lipid-based formulations.

Integrated process for the removal of emulsified oils from effluents in the steel industry

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

Benito, J.M.; Rios, G.; Gutierrez, B.

1999-11-01

Emulsified oils contained in aqueous effluents from cold-rolling mills of the steel industry can be effectively removed via an integrated process consisting of a coagulation/flocculation stage followed by ultrafiltration of the resulting aqueous phase. The effects of CaCl{sub 2}, NaOH, and lime on the stability of different industrial effluents were studied in the coagulation experiments. The flocculants tested were inorganic prehydrolyzed aluminum salts and quaternary polyamines. Ultrafiltration of the aqueous phase from the coagulation/flocculation stage was carried out in a stirred cell using Amicon PM30 and XM300 organic membranes. Permeate fluxes were measured for industrial effluents to which the indicatedmore » coagulants and flocculants had been added. Oil concentrations in the permeate were 75% lower than the limits established by all European Union countries. Complete regeneration of the membrane was accomplished with an aqueous solution of a commercial detergent.« less

Nonlinear absorption kinetics of self-emulsifying drug delivery systems (SEDDS) containing tocotrienols as lipophilic molecules: in vivo and in vitro studies.

PubMed

Alqahtani, Saeed; Alayoubi, Alaadin; Nazzal, Sami; Sylvester, Paul W; Kaddoumi, Amal

2013-07-01

Self-emulsifying drug delivery systems (SEDDS) have been broadly used to promote the oral absorption of poorly water-soluble drugs. The purpose of the current study was to evaluate the in vivo oral bioavailability of vitamin E isoforms, δ-tocotrienol (δ-T3) and γ-tocotrienol (γ-T3) administered as SEDDS, as compared to commercially available UNIQUE E® Tocotrienols capsules. Results from studies in rats showed that low dose treatment with δ-T3 (90%) and γ-T3 (10%) formulated SEDDS showed bioavailability of 31.5% and 332%, respectively. However, bioavailability showed a progressive decrease with increased treatment dose that displayed nonlinear absorption kinetics. Additional in vitro studies examining cellular uptake studies in Caco 2 cells revealed that the SEDDS formulation increased passive permeability of δ-T3 and γ-T3 by threefold as compared to the commercial capsule formulation. These studies also showed that free surfactants decreased δ-T3 and γ-T3 absorption. Specifically, combined treatment cremophor EL or labrasol with tocotrienols caused a 60-85% reduction in the cellular uptake of δ-T3 and γ-T3 and these effects appear to result from surfactant-induced inhibition of the δ-T3 and γ-T3 transport protein Niemann-Pick C1-like 1 (NPC1L1). In summary, results showed that SEDDS formulation significantly increases the absorption and bioavailability δ-T3 and γ-T3. However, this effect is self-limiting because treatment with increasing doses of SEDDS appears to be associated with a corresponding increase in free surfactants levels that directly and negatively impact tocotrienol transport protein function and results in nonlinear absorption kinetics and a progressive decrease in δ-T3 and γ-T3 absorption and bioavailability.

FIELD EVALUATION OF THE TREATMENT OF DNAPL USING EMULSIFIED ZERO-VALENT IRON (DNAPL CONFERENCE)

EPA Science Inventory

A pilot scale field demonstration of dense non-aqueous phase liquids (DNAPL) treatment using emulsified zero-valent iron (EZVI) is being conducted at Parris Island Marine Corps Recruit Depot (MCRD), Parris Island SC. The demonstration is being conducted by Geosyntec, the Nationa...

FIELD EVALUATION OF THE TREATMENT OF DNAPL USING EMULSIFIED ZERO-VALENT IRON (Battelle Conference)

EPA Science Inventory

A pilot scale field demonstration of dense non-aqueous phase liquids (DNAPL) treatment using emulsified zero-valent iron (EZVI) was conducted at Parris Island Marine Corps Recruit Depot (MCRD), Parris Island, SC. The EZVI technology was developed at the University of Central Fl...

FIELD EVALUATION OF THE TREATMENT OF DNAPL USING EMULSIFIED ZERO-VALENT IRON (BATTELLE PRESENTATION)

EPA Science Inventory

A pilot scale field demonstration of dense non-aqueous phase liquids (DNAPL) treatment using emulsified zero-valent iron (EZVI) is being conducted at Parris Island Marine Corps Recruit Depot (MCRD), Parris Island SC. The EZVI technology was developed at the University of Central ...

Emulsifying properties of acidic subunits of soy 11S globulin.

PubMed

Liu, M; Lee, D S; Damodaran, S

1999-12-01

The emulsifying properties of the acidic subunits (AS11S) isolated from soy glycinin (11S) have been studied. The isolated AS11S existed in solution mainly as a dimer species. Circular dichroic analysis indicated only a slight increase in aperiodic structure and no significant difference in beta-sheet structure when compared with those of soy 11S. At similar experimental conditions, the emulsifying properties of AS11S were superior to those of soy 11S and heat-denatured 11S. Emulsions prepared with 1% AS11S remained very stable without any visible oil separation for more than a month under gentle agitating conditions, whereas those prepared with 1% 11S collapsed and separated into phases within 2-3 days. The AS11S-stabilized emulsions were very stable below 0.15 M ionic strength. Studies on the rate of adsorption and surface tension reduction at the air-water interface showed that AS11S was significantly more surface active than soy 11S. It is proposed that, because the mass fraction of acidic subunits in soy 11S is approximately 60% and it is relatively easy to separate the acidic subunits from soy 11S, it may be industrially feasible to develop an economical process to isolate functional acidic subunits for use in emulsion-based food products.

Enhanced emulsifying properties of wood-based cellulose nanocrystals as Pickering emulsion stabilizer.

PubMed

Gong, Xiaoyu; Wang, Yixiang; Chen, Lingyun

2017-08-01

Cellulose nanocrystals are hydrophilic nanomaterials, which limits their applications as interfacial compounds. Herein, we propose using modified wood-based cellulose nanocrystals as Pickering emulsion stabilizer. Wood cellulose was consecutively oxidized and modified with phenyltrimethylammonium chloride to create hydrophobic domains comprised of phenyl groups. These modified oxidized cellulose nanocrystals (m-O-CNCs) were homogeneous/electrostatically stable in water and they can stabilize O/W Pickering emulsions. The dispersed phase volume fraction (DPVF) of the Pickering emulsion was 0.7 at around 1.5g/L, whereas the tween-20 control needed a 13-fold greater concentration to have a similar DPVR. In addition, these m-O-CNC stabilized Pickering emulsions also showed good mechanical and thermal stability against centrifugation and heat, as well as size controllability. In terms of stability, size controllability, surfactant-free status, these m-O-CNCs possess superior and enhanced emulsifying properties. Future research for these new interfacial materials have potential in applications, for personal care, cosmetic and pharmaceutic industries. Copyright © 2017 Elsevier Ltd. All rights reserved.

Solid lipid nanoparticles as vesicles for oral delivery of olmesartan medoxomil: formulation, optimization and in vivo evaluation.

PubMed

Nooli, Mounika; Chella, Naveen; Kulhari, Hitesh; Shastri, Nalini R; Sistla, Ramakrishna

2017-04-01

Olmesartan medoxomil (OLM) is an antihypertensive drug with low oral bioavailability (28%) resulting from poor aqueous solubility, presystemic metabolism and P-glycoprotein mediated efflux. The present investigation studies the role of lipid nanocarriers in enhancing the OLM bioavailability through oral delivery. Solid lipid nanoparticles (SLN) were prepared by solvent emulsion-evaporation method. Statistical tools like regression analysis and Pareto charts were used to detect the important factors effecting the formulations. Formulation and process parameters were then optimized using mean effect plot and contour plots. The formulations were characterized for particle size, size distribution, surface charge, percentage of drug entrapped in nanoparticles, drug-excipients interactions, powder X-ray diffraction analysis and drug release in vitro. The optimized formulation comprised glyceryl monostearate, soya phosphatidylcholine and Tween 80 as lipid, co-emulsifier and surfactant, respectively, with an average particle size of 100 nm, PDI 0.291, zeta potential of -23.4 mV and 78% entrapment efficiency. Pharmacokinetic evaluation in male Sprague Dawley rats revealed 2.32-fold enhancement in relative bioavailability of drug from SLN when compared to that of OLM plain drug on oral administration. In conclusion, SLN show promising approaches as a vehicle for oral delivery of drugs like OLM.

Synthesis and characterization of fluorinated polyacrylate latex emulsified with novel surfactants

PubMed Central

Zhang, Cuifeng; Xu, Tingting; Bao, Zhongbin; Chen, Lijun

2017-01-01

Abstract The fluorinated polyacrylate latex were successfully prepared with semi- continuous seeded emulsion polymerization of butyl acrylate (BA), methyl methacrylate (MMA) and hexafluorobutyl methacrylate (HFMA) which was initiated with potassium persulfate (KPS) initiator and emulsified with the novel mixed surfactants of sodium lauryl glutamate (SLG) and alkylphenol ethoxylates (OP-10). The structure of the resultant latex was confirmed by Fourier transform infrared spectroscopy (FTIR). The particle size of the latex was measured by Zetatrac dynamic light scattering detector. The film of latex was tested by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and contact angle (CA). The optimum conditions of preparing the novel fluorinated polyacrylate latex are optimized and the results are as follows: the amount of emulsifiers is 4.0%; mass ratio of SLG to OP-10 is 1:1, the amount of the initiator is 0.6%. The mass ratio of MMA to BA is 1:1 and the amount of HFMA is 7.0%. In this case, the conversion is high and the polymerization stability is good. In addition, the water resistance and thermal properties of the latex films were improved significantly in comparison with the film of the latex prepared without the fluorinated monomer. PMID:29491785

Toxicity of Lavandula angustifolia oil constituents and spray formulations to insecticide-susceptible and pyrethroid-resistant Plutella xylostella and its endoparasitoid Cotesia glomerata.

PubMed

Yi, Chang Geun; Hieu, Tran Trung; Lee, Si Hyeock; Choi, Byeoung-Ryeol; Kwon, Min; Ahn, Young-Joon

2016-06-01

Plutella xylostella is one of the most serious insect pests of cruciferous crops. This study was conducted to determine the toxicity of 21 constituents from Lavandula angustifolia essential oil (LA-EO) and another 16 previously known LA-EO constituents and the toxicity of six experimental spray formulations containing the oil (1-6 g L(-1) sprays) to susceptible KS-PX and pyrethroid-resistant JJ-PX P. xylostella larvae, as well as to its endoparasitoid Cotesia glomerata adults. Linalool and linalool oxide (LC50 = 0.016 mg cm(-3) ) were the most toxic fumigant compounds and were 10.7-fold less toxic than dichlorvos to KS-PX larvae. Either residual or fumigant toxicity of these compounds was almost identical against larvae from either of the two strains. Against C. glomerata, dichlorvos (LC50 = 7 × 10(-6)  mg cm(-3) ) was the most toxic insecticide. LA-EO was ∼1430 times less toxic than dichlorvos. The oil applied as 6 g L(-1) spray and emamectin benzoate 21.5 g L(-1) emulsifiable concentrate provided 100% mortality against larvae from either of the two strains. Reasonable P. xylostella control in greenhouses can be achieved by a spray formulation containing the 6 g L(-1) oil as potential contact-action fumigant. © 2015 Society of Chemical Industry. © 2015 Society of Chemical Industry.

A study of the impact of freezing on the lyophilization of a concentrated formulation with a high fill depth.

PubMed

Liu, Jinsong; Viverette, Todd; Virgin, Marlin; Anderson, Mitch; Paresh, Dalal

2005-01-01

The objective of this study was to evaluate the impact of freezing on the lyophilization of a concentrated formulation with a high fill depth. A model system consisting of a 15-mL fill of 15% (w/w) sulfobutylether 7-beta-cyclodextrin (SBECD) solution in a 30-mL vial was selected for this study. Various freezing methods including single-step freezing, two-step freezing with a super-cooling holding, annealing, vacuum-induced freezing, changing ice habit using tert-butyl-alcohol (TBA), ice nucleation with silver iodide (AgI), as well as combinations of some of the methods, were used in the lyophilization of this model system. This work demonstrated that the freezing process had a significant impact on primary drying rate and product quality of a concentrated formulation with a high fill depth. Annealing, vacuum-induced freezing, and addition of either TBA or an ice nucleating agent (AgI) to the formulation accelerated the subsequent ice sublimation process. Two-step freezing or addition of TBA improved the product quality by eliminating vertical heterogeneity within the cake. The combination of two-step freezing in conjunction with an annealing step was shown to be a method of choice for freezing in the lyophilization of a product with a high fill depth. In addition to being an effective method of freezing, it is most applicable for scaling up. An alternative approach is to add a certain amount of TBA to the formulation, if the TBA-formulation interaction or regulatory concerns can be demonstrated as not being an issue. An evaluation of vial size performed in this study showed that although utilizing large-diameter vials to reduce the fill depth can greatly shorten the cycle time of a single batch, it will substantially decrease the product throughput in a large-scale freeze-dryer.

Moisturizing effect of cosmetic formulations containing Aloe vera extract in different concentrations assessed by skin bioengineering techniques.

PubMed

Dal'Belo, Susi Elaine; Gaspar, Lorena Rigo; Maia Campos, Patrícia Maria Berardo Gonçalves

2006-11-01

The polysaccharide-rich composition of Aloe vera extracts (Aloe barbadensis Miller), often used in cosmetic formulations, may impart moisturizing properties to the product. The aim of this study was to evaluate the effect of cosmetic formulations containing different concentrations of freeze-dried Aloe vera extract on skin hydration, after a single and a 1- and 2-week period of application, by using skin bioengineering techniques. Stable formulations containing 5% (w/w) of a trilaureth-4 phosphate-based blend were supplemented with 0.10%, 0.25% or 0.50% (w/w) of freeze-dried Aloe vera extract and applied to the volar forearm of 20 female subjects. Skin conditions in terms of the water content of the stratum corneum and of transepidermal water loss (TEWL) (Corneometer CM 825 and Tewameter TM 210) were analysed before and after a single and 1- and 2-week period of daily application. After a single application, only formulations supplemented with 0.25% and 0.50% (w/w) of Aloe vera extract increased the water content of the stratum corneum, while after the 2-week period application, all formulations containing the extract (0.10%, 0.25% and 0.50%) had the same effect, in both cases as compared with the vehicle. TEWL was not modified after a single and after 1- and 2-week period of application, when compared with the vehicle. Our results show that freeze-dried Aloe vera extract is a natural effective ingredient for improving skin hydration, possibly through a humectant mechanism. Consequently, it may be used in moisturizing cosmetic formulations and also as a complement in the treatment of dry skin.

In situ bioremediation of uranium with emulsified vegetable oil as the electron donor.

PubMed

Watson, David B; Wu, Wei-Min; Mehlhorn, Tonia; Tang, Guoping; Earles, Jennifer; Lowe, Kenneth; Gihring, Thomas M; Zhang, Gengxin; Phillips, Jana; Boyanov, Maxim I; Spalding, Brian P; Schadt, Christopher; Kemner, Kenneth M; Criddle, Craig S; Jardine, Philip M; Brooks, Scott C

2013-06-18

A field test with a one-time emulsified vegetable oil (EVO) injection was conducted to assess the capacity of EVO to sustain uranium bioreduction in a high-permeability gravel layer with groundwater concentrations of (mM) U, 0.0055; Ca, 2.98; NO3(-), 0.11; HCO3(-), 5.07; and SO4(2-), 1.23. Comparison of bromide and EVO migration and distribution indicated that a majority of the injected EVO was retained in the subsurface from the injection wells to 50 m downgradient. Nitrate, uranium, and sulfate were sequentially removed from the groundwater within 1-2 weeks, accompanied by an increase in acetate, Mn, Fe, and methane concentrations. Due to the slow release and degradation of EVO with time, reducing conditions were sustained for approximately one year, and daily U discharge to a creek, located approximately 50 m from the injection wells, decreased by 80% within 100 days. Total U discharge was reduced by 50% over the one-year period. Reduction of U(VI) to U(IV) was confirmed by synchrotron analysis of recovered aquifer solids. Oxidants (e.g., dissolved oxygen, nitrate) flowing in from upgradient appeared to reoxidize and remobilize uranium after the EVO was exhausted as evidenced by a transient increase of U concentration above ambient values. Occasional (e.g., annual) EVO injection into a permeable Ca and bicarbonate-containing aquifer can sustain uranium bioreduction/immobilization and decrease U migration/discharge.

In situ SERS detection of emulsifiers at lipid interfaces using label-free amphiphilic gold nanoparticles.

PubMed

Li, Yue; Driver, Michael; Winuprasith, Thunnalin; Zheng, Jinkai; McClements, David Julian; He, Lili

2014-10-21

Herein, we fabricated amphiphilic gold nanoparticles (GNPs) that can self-assemble at oil-water interfaces. We applied those GNPs for in situ SERS detection of emulsifier molecules within the interfacial region of oil in water (O/W) emulsion systems.

Microstructural, textural, and sensory properties of whole-wheat noodle modified by enzymes and emulsifiers.

PubMed

Niu, Meng; Hou, Gary G; Kindelspire, Julie; Krishnan, Padmanaban; Zhao, Siming

2017-05-15

With the utilization of enzymes including endoxylanase, glucose oxidase (GOX) and transglutaminase (TG), and emulsifiers comprising sodium stearoyl lactate (SSL) and soy lecithin, the microstructural, textural, and sensory properties of whole-wheat noodle (WWN) were modified. The development time and stability of whole-wheat dough (WWD) were enhanced by TG due to the formation of a more compact gluten network, and by SSL resulting from the enhanced gluten strength. Microstructure graphs by scanning electron microscopy (SEM) verified that TG and SSL promoted the connectivity of gluten network and the coverage of starch granules in WWN. TG increased the hardness and elasticity of cooked WWN, while two emulsifiers increased the noodle cohesiveness. Additionally, TG and SSL improved the sensory properties of noodle such as bite, springiness, and mouth-feel. The results suggest that TG and SSL are effective ingredients in enhancing the gluten strength of WWD and improving the qualities of WWN. Copyright © 2016 Elsevier Ltd. All rights reserved.

Peroxidase mediated conjugation of corn fibeer gum and bovine serum albumin to improve emulsifying properties

USDA-ARS?s Scientific Manuscript database

The emulsifying properties of corn fiber gum (CFG), a naturally-occurring polysaccharide protein complex, were improved by kinetically controlled formation of hetero-covalent linkages with bovine serum albumin (BSA), using horseradish peroxidase. The formation of hetero-crosslinked CFG-BSA conjugate...

Emulsified Zero-Valent Nano-Scale Iron Treatment of Chlorinated Solvent DNAPL Source Areas

DTIC Science & Technology

2010-09-01

Significant laboratory and field research has demonstrated that zero-valent metals will reductively dehalogenate dissolved chlorinated solvents such as...Eekert, Servé W. M. Kengen, Gosse Schraa, and Alfons J. M. Stams. 1999. Anaerobic Microbial Reductive Dehalogenation of Chlorinated Ethenes...and T. Holdsworth. 2005. Field Demonstration of DNAPL Dehalogenation Using Emulsified Zero-Valent Iron. Environmental Science Technology, vol 39

Mycobacteria emulsified in olive oil-in-water trigger a robust immune response in bladder cancer treatment

PubMed Central

Noguera-Ortega, Estela; Blanco-Cabra, Núria; Rabanal, Rosa Maria; Sánchez-Chardi, Alejandro; Roldán, Mónica; Guallar-Garrido, Sandra; Torrents, Eduard; Luquin, Marina; Julián, Esther

2016-01-01

The hydrophobic composition of mycobacterial cell walls leads to the formation of clumps when attempting to resuspend mycobacteria in aqueous solutions. Such aggregation may interfere in the mycobacteria-host cells interaction and, consequently, influence their antitumor effect. To improve the immunotherapeutic activity of Mycobacterium brumae, we designed different emulsions and demonstrated their efficacy. The best formulation was initially selected based on homogeneity and stability. Both olive oil (OO)- and mineral oil-in-water emulsions better preserved the mycobacteria viability and provided higher disaggregation rates compared to the others. But, among both emulsions, the OO emulsion increased the mycobacteria capacity to induce cytokines’ production in bladder tumor cell cultures. The OO-mycobacteria emulsion properties: less hydrophobic, lower pH, more neutralized zeta potential, and increased affinity to fibronectin than non-emulsified mycobacteria, indicated favorable conditions for reaching the bladder epithelium in vivo. Finally, intravesical OO-M. brumae-treated mice showed a significantly higher systemic immune response, together with a trend toward increased tumor-bearing mouse survival rates compared to the rest of the treated mice. The physicochemical characteristics and the induction of a robust immune response in vitro and in vivo highlight the potential of the OO emulsion as a good delivery vehicle for the mycobacterial treatment of bladder cancer. PMID:27265565

Adelphi-Goddard emulsified fuel project. [using water/oil emulsions

NASA Technical Reports Server (NTRS)

1977-01-01

Thermal efficiency and particle emissions were studied using water/oil emulsions. These studies were done using number 2 and number 6 fuel oil. The number 6 oil had a sulfur content greater than one percent and experiments were conducted to remove the sulfur dioxide from the stack gases. Test findings include: (1) emulsion effected a reduction in soot at a low excess air levels; (2) a steam atomizing system will produce a water/oil emulsion. The fuel in the study was emulsified in the steam atomization process, hence, pre-emulsification did not yield a dramatic reduction in soot or an increase in thermal efficiency.

Nonclinical dose formulation analysis method validation and sample analysis.

PubMed

Whitmire, Monica Lee; Bryan, Peter; Henry, Teresa R; Holbrook, John; Lehmann, Paul; Mollitor, Thomas; Ohorodnik, Susan; Reed, David; Wietgrefe, Holly D

2010-12-01

Nonclinical dose formulation analysis methods are used to confirm test article concentration and homogeneity in formulations and determine formulation stability in support of regulated nonclinical studies. There is currently no regulatory guidance for nonclinical dose formulation analysis method validation or sample analysis. Regulatory guidance for the validation of analytical procedures has been developed for drug product/formulation testing; however, verification of the formulation concentrations falls under the framework of GLP regulations (not GMP). The only current related regulatory guidance is the bioanalytical guidance for method validation. The fundamental parameters for bioanalysis and formulation analysis validations that overlap include: recovery, accuracy, precision, specificity, selectivity, carryover, sensitivity, and stability. Divergence in bioanalytical and drug product validations typically center around the acceptance criteria used. As the dose formulation samples are not true "unknowns", the concept of quality control samples that cover the entire range of the standard curve serving as the indication for the confidence in the data generated from the "unknown" study samples may not always be necessary. Also, the standard bioanalytical acceptance criteria may not be directly applicable, especially when the determined concentration does not match the target concentration. This paper attempts to reconcile the different practices being performed in the community and to provide recommendations of best practices and proposed acceptance criteria for nonclinical dose formulation method validation and sample analysis.

Synthesis of pH-sensitive and recyclable magnetic nanoparticles for efficient separation of emulsified oil from aqueous environments

NASA Astrophysics Data System (ADS)

Lü, Ting; Zhang, Shuang; Qi, Dongming; Zhang, Dong; Vance, George F.; Zhao, Hongting

2017-02-01

Emulsified oil wastewaters, arisen from oil industry and oil spill accidents, cause severe environmental and ecological problems. In this study, a series of pH-sensitive magnetic nanomaterials (MNPs) were synthesized and characterized for their evaluation in separation of emulsified oil from aqueous environments. A coprecipitation method was used to produce Fe3O4 magnetic nanoparticles that were coated in a 2-step process with first silica to form a surface for anchoring an (3-aminopropyl)triethoxysilane (APTES) molecular layer. Detailed studies were conducted on effects of MNPs dosage, APTES anchoring density (DA) and pH on oil-water separation performance of the synthetic MNPs. Results showed that, under both acidic and neutral conditions, MNPs with high DA exhibited enhanced oil-water separation performance, while under alkaline condition, the oil-water separation process was minimal. Alkaline conditions allowed the MNPs to be recycled up to 9 cycles without showing any significant decrease in oil-water separation efficiency. An examination of the oil-water separation mechanism found that electrostatic interaction and interfacial activity both played important roles in oil-water separation. In conclusion, pH-sensitive MNPs can be easily synthesized and recycled, providing a promising, cost-effective and environmentally-friendly process for the efficient treatment of emulsified oil wastewater.

In vitro gastrointestinal lipolysis of four formulations of piroxicam and cinnarizine with the self emulsifying excipients Labrasol and Gelucire 44/14.

PubMed

Fernandez, Sylvie; Chevrier, Stéphanie; Ritter, Nicolas; Mahler, Bruno; Demarne, Frédéric; Carrière, Frédéric; Jannin, Vincent

2009-08-01

Labrasol and Gelucire 44/14 are defined admixtures of acylglycerols and PEG esters which are substrates for digestive lipases. We investigated their in vitro gastrointestinal lipolysis to understand which compounds are, after digestion, responsible for keeping poorly water-soluble drugs in solution. The precipitation of piroxicam and cinnarizine formulated in these excipients during the gastrointestinal lipolysis was also studied. Monoacylglycerols and PEG monoesters are the largest compounds present at the end of gastric phase whereas PEG-monoesters are the largest compounds after the duodenal phase. The precipitation of piroxicam is mainly due to the gastric lipolysis. In the control experiments performed without digestive lipases, cinnarizine formulated in Labrasol was found to precipitate upon dilution of the gastric medium to form the solution mimicking the duodenal medium. In the presence of gastric lipase, Labrasol was hydrolyzed and the precipitation of cinnarizine was not observed in this case. When the cinnarizine was formulated with Gelucire 44/14 the precipitation was only due to the dilution of the gastric medium. Our study highlights the importance of the gastrointestinal lipolysis and the associated phenomena such as the dilution of chyme by biliary and pancreatic secretions in vivo, on the solubilisation of poorly water-soluble drugs formulated with lipid-based excipients.

Protective clothing for pesticide operators: part I--selection of a reference test chemical for penetration testing.

PubMed

Shaw, Anugrah; Schiffelbein, Paul

2016-01-01

A systematic approach was taken to develop a database for protective clothing for pesticide operators; results are reported as a two-part series. Part I describes the research studies that led to identification of a pesticide formulation that could serve as a reference test chemical for further testing. Measurement of pesticide penetration was conducted using different types of pesticide formulations. Six fabrics were tested using 10 formulations at different concentrations. Three formulations were subsequently selected for further testing. Analysis of the data indicated that, when compared with other formulations, mean percent penetration of 5% Prowl 3.3 EC [emulsifiable concentrate diluted to 5% active ingredient (pendimethalin)] is either similar to or higher than most test chemicals. Those results led to choosing 5% Prowl 3.3 EC as a reference test liquid. Part II of the study, published as a separate paper, includes data on a wide range of textile materials.

Preparation and impact of multiple (water-in-oil-in-water) emulsions in meat systems.

PubMed

Cofrades, S; Antoniou, I; Solas, M T; Herrero, A M; Jiménez-Colmenero, F

2013-11-01

The aim of this paper was to prepare and characterise multiple emulsions and assess their utility as pork backfat replacers in meat gel/emulsion model systems. In order to improve the fat content (in quantitative and qualitative terms) pork backfat was replaced by a water-in-oil-in-water emulsion (W1/O/W2) prepared with olive oil (as lipid phase), polyglycerol ester of polyricinoleic acid (PGPR) as a lipophilic emulsifier, and sodium caseinate (SC) and whey protein concentrate (WP) as hydrophilic emulsifiers. The emulsion properties (particle size and distribution, stability, microstructure) and meat model system characteristics (composition, texture, fat and water binding properties, and colour) of the W1/O/W2, as affected by reformulation, were evaluated. Multiple emulsions showed a well-defined monomodal distribution. Freshly prepared multiple emulsions showed good thermal stability (better using SC) with no creaming. The meat systems had good water and fat binding properties irrespective of formulation. The effect on texture by replacement of pork backfat by W1/O/W2 emulsions generally depends on the type of double emulsion (associated with the hydrophilic emulsifier used in its formulation) and the fat level in the meat system. Copyright © 2013 Elsevier Ltd. All rights reserved.

Structural and emulsifying properties of soy protein isolate subjected to acid and alkaline pH-shifting processes.

PubMed

Jiang, Jiang; Chen, Jie; Xiong, Youling L

2009-08-26

Structural unfolding of soy protein isolate (SPI) as induced by holding (0, 0.5, 1, 2, and 4 h) in acidic (pH 1.5-3.5) and alkaline (pH 10.0-12.0) pH solutions, followed by refolding (1 h) at pH 7.0, was analyzed. Changes in emulsifying properties of treated SPI were then examined. The pH-shifting treatments resulted in a substantial increase in protein surface hydrophobicity, intrinsic tryptophan fluorescence intensity, and disulfide-mediated aggregation, along with the exposure of tyrosine. After the pH-shifting processes, soy protein adopted a molten globule-like conformation that largely maintained the original secondary structure and overall compactness but lost some tertiary structure. These structural modifications, consequently, led to markedly improved emulsifying activity of SPI as well as the emulsion stability.

Toward the establishment of standardized in vitro tests for lipid-based formulations. 2. The effect of bile salt concentration and drug loading on the performance of type I, II, IIIA, IIIB, and IV formulations during in vitro digestion.

PubMed

Williams, Hywel D; Anby, Mette U; Sassene, Philip; Kleberg, Karen; Bakala-N'Goma, Jean-Claude; Calderone, Marilyn; Jannin, Vincent; Igonin, Annabel; Partheil, Anette; Marchaud, Delphine; Jule, Eduardo; Vertommen, Jan; Maio, Mario; Blundell, Ross; Benameur, Hassan; Carrière, Frédéric; Müllertz, Anette; Pouton, Colin W; Porter, Christopher J H

2012-11-05

The LFCS Consortium was established to develop standardized in vitro tests for lipid-based formulations (LBFs) and to examine the utility of these tests to probe the fundamental mechanisms that underlie LBF performance. In this publication, the impact of bile salt (sodium taurodeoxycholate, NaTDC) concentration and drug loading on the ability of a range of representative LBFs to generate and sustain drug solubilization and supersaturation during in vitro digestion testing has been explored and a common driver of the potential for drug precipitation identified. Danazol was used as a model poorly water-soluble drug throughout. In general, increasing NaTDC concentrations increased the digestion of the most lipophilic LBFs and promoted lipid (and drug) trafficking from poorly dispersed oil phases to the aqueous colloidal phase (AP(DIGEST)). High NaTDC concentrations showed some capacity to reduce drug precipitation, although, at NaTDC concentrations ≥3 mM, NaTDC effects on either digestion or drug solubilization were modest. In contrast, increasing drug load had a marked impact on drug solubilization. For LBFs containing long-chain lipids, drug precipitation was limited even at drug loads approaching saturation in the formulation and concentrations of solubilized drug in AP(DIGEST) increased with increased drug load. For LBFs containing medium-chain lipids, however, significant precipitation was evident, especially at higher drug loads. Across all formulations a remarkably consistent trend emerged such that the likelihood of precipitation was almost entirely dependent on the maximum supersaturation ratio (SR(M)) attained on initiation of digestion. SR(M) defines the supersaturation "pressure" in the system and is calculated from the maximum attainable concentration in the AP(DIGEST) (assuming zero precipitation), divided by the solubility of the drug in the colloidal phases formed post digestion. For LBFs where phase separation of oil phases did not occur, a

Effects of sodium caseinate concentration and storage conditions on the oxidative stability of oil-in-water emulsions.

PubMed

O' Dwyer, Sandra P; O' Beirne, David; Eidhin, Deirdre Ní; O' Kennedy, Brendan T

2013-06-01

The oxidative stability of various oils (sunflower, camelina and fish) and 20% oil-in-water (O/W) emulsions, were examined. The mean particle size decreased from 1179 to 325 nm as sodium caseinate (emulsifier) concentration was increased from 0.25% to 3% in O/W emulsions (P<0.05). Increasing the microfluidisation pressure from 21 to 138 MPa, resulted in a particle size decrease from 289 to 194 nm (P<0.05). Emulsified oils had lower detectable lipid hydroperoxide and p-Anisidine values than their corresponding bulk oils (P<0.05). The lipid hydroperoxide and p-Anisidine values of emulsions generally decreased as sodium caseinate concentration increased, and similarly decreased as microfluidisation pressure increased (P<0.05). Increasing storage temperature of the emulsions from 5 to 60°C, resulted in lower detectable lipid oxidation products during storage (P<0.05). Copyright © 2012 Elsevier Ltd. All rights reserved.

Evaluation of garlic oil in nano-emulsified form: Optimization and its efficacy in high-fat diet induced dyslipidemia in Wistar rats.

PubMed

Ragavan, Gokulakannan; Muralidaran, Yuvashree; Sridharan, Badrinathan; Nachiappa Ganesh, Rajesh; Viswanathan, Pragasam

2017-07-01

Garlic oil nanoemulsion was formulated using ultrasonic emulsification and the optimized garlic oil nanoemulsion ratio (1:2) of oil: surfactant showed spherical, with tiny droplet size 24.9 ± 1.11 nm. It was observed that the prepared nanoemulsion has the zeta potential of -42.63 ± 1.58 mV and a low polydispersity index of 0.2 ± 0.09 with excellent stability. The formulation was subjected to in vivo acute and sub-acute toxicity. In acute toxicity study, single oral administration of 18.63 ml of garlic oil nanoemulsion/kg resulted in immediate mortality. However, garlic oil nanoemulsion (0.46 ml/kg) and tween 80 (0.5 ml/kg) administered rats did not exhibit any toxicity and showed no changes in hematological and histological parameters. Further, both preventive and curative studies of garlic oil nanoemulsion were evaluated in high-fat diet fed dyslipidemic Wistar rats. Garlic oil nanoemulsion administered groups showed a significant effect in reducing the levels of lipid profiles (p < 0.001) compared to atorvastatin and garlic oil. Evaluation of lipid deposits in hepatic tissues was analyzed by Oil Red O staining, which revealed that garlic oil nanoemulsion administered rats markedly reduced the fat depots. Our findings suggest that garlic oil nano-emulsified form reduced toxicity and improved efficacy in preventing and treating dyslipidemia. Copyright © 2017 Elsevier Ltd. All rights reserved.

Optimization of methylene blue removal by stable emulsified liquid membrane using Plackett–Burman and Box–Behnken designs of experiments

PubMed Central

Djenouhat, Meriem; Bendebane, Farida; Bahloul, Lynda; Samar, Mohamed E. H.

2018-01-01

The stability of an emulsified liquid membrane composed of Span80 as a surfactant, D2EHPA as an extractant and sulfuric acid as an internal phase was first studied according to different diluents and many operating parameters using the Plackett–Burman design of experiments. Then the removal of methylene blue from an aqueous solution has been carried out using this emulsified liquid membrane at its stability conditions. The effects of operating parameters were analysed from the Box–Behnken design of experiments. The optimization of the extraction has been realized applying the response surface methodology and the results showed that the dye extraction yielding 98.72% was achieved at optimized conditions. PMID:29515841

Field and Laboratory Responses of Male Leafroller Moths, Choristoneura rosaceana and Pandemis pyrusana, to Pheromone Concentrations in an Attracticide Paste Formulation

USDA-ARS?s Scientific Manuscript database

Choristoneura rosaceana and Pandemis pyrusana male responses to an attracticide paste formulation loaded with different pheromone concentrations of appropriate blends encompassing four orders of magnitude (0.01 to 16%) were evaluated under laboratory (indoor wind tunnel) and field conditions. Respon...

Formulation Studies of InhA inhibitors and Combination therapy to improve efficacy against Mycobacterium tuberculosis

PubMed Central

Knudson, Susan E.; Cummings, Jason E.; Bommineni, Gopal R.; Pan, Pan; Tonge, Peter J.; Slayden, Richard A.

2016-01-01

Summary Previously, structure-based drug design was used to develop substituted diphenyl ethers with potency against the Mycobacterium tuberculosis (Mtb) enoyl-ACP reductase (InhA), however, the highly lipophilic centroid compound, SB-PT004, lacked sufficient efficacy in the acute murine Mtb infection model. A next generation series of compounds were designed with improved specificity, potency against InhA, and reduced cytotoxicity in vitro, but these compounds also had limited solubility. Accordingly, solubility and pharmacokinetics studies were performed to develop formulations for this class and other experimental drug candidates with high logP values often encountered in drug discovery. Lead diphenyl ethers were formulated in co-solvent and Self-Dispersing Lipid Formulations (SDLFs) and evaluated in a rapid murine Mtb infection model that assesses dissemination to and bacterial burden in the spleen. In vitro synergy studies were performed with the lead diphenyl ether compounds, SB-PT070 and SB-PT091, and rifampin (RIF), which demonstrated an additive effect, and that guided the in vivo studies. Combinatorial therapy in vivo studies with these compounds delivered in our Self-Micro Emulsifying Drug Delivery System (SMEDDS) resulted in an additional 1.4 log10 CFU reduction in the spleen of animals co-treated with SB-PT091 and RIF and an additional 1.7 log10 reduction in the spleen with animals treated with both SB-PT070 and RIF. PMID:27865404

Effects of emulsifier addition on the crystallization and melting behavior of palm olein and coconut oil.

PubMed

Maruyama, Jessica Mayumi; Soares, Fabiana Andreia Schafer De Martini; D'Agostinho, Natalia Roque; Gonçalves, Maria Inês Almeida; Gioielli, Luiz Antonio; da Silva, Roberta Claro

2014-03-12

Two commercial emulsifiers (EM1 and EM2), containing predominantly monoacylglycerols (MAGs), were added in proportiond of 1.0 and 3.0% (w/w) to coconut oil and palm olein. EM1 consisted of approximately 90% MAGs, whereas EM2 consisted of approximately 50% MAGs. The crystallization behavior of these systems was evaluated by differential scanning calorimetry (DSC) and microscopy under polarized light. On the basis of DSC results, it was clear that the addition of EM2 accelerated the crystallization of coconut oil and delayed the crystallization of palm olein. In both oils EM2 addition led to the formation of smaller spherulites, and these effects improved the possibilities for using these fats as ingredients. In coconut oil the spherulites were maintained even at higher temperatures (20 °C). The addition of EM1 to coconut oil changed the crystallization pattern. In palm olein, the addition of 3.0% (w/w) of this emulsifier altered the pattern of crystallization of this fat.

Characterization of Acinetobacter baumannii strain PS3 in degradation of food emulsifiers

NASA Astrophysics Data System (ADS)

Nguyen, Ngoc Tuan; Tran, Tuyet Nhung; Ha, Thi Bich Ngoc

2018-04-01

Strain SP3 revealed the abilty to utilizes emulsifier which is widely used in the preparation of drugs, vaccines, food, cosmetics and skin care products as its sole carbon and energy source. Generation time ranges from 1.4 to 2.1 h on the polysorbate family. Strain was identified as Acinetobacter baumannii based on 16S rRNA gene and it could dispose 27 % polysorbate 80 within a day. The proposed mechanism for polysorbate utilization belongs to the β-oxidation.

Phosphate Reduction in Emulsified Meat Products: Impact of Phosphate Type and Dosage on Quality Characteristics.

PubMed

Glorieux, Seline; Goemaere, Olivier; Steen, Liselot; Fraeye, Ilse

2017-09-01

Phosphate reduction is of important industrial relevance in the manufacturing of emulsified meat products because it may give rise to a healthier product. The effect of seven different phosphate types was tested on the physicochemical and quality characteristics to select the most promising phosphate type for further cooked sausage manufacturing. Next, phosphate mass fraction was gradually reduced. Tetrasodium di- or pyrophosphate (TSPP) and sodium tripolyphosphate (STPP) increased pH, reduced structural properties, resulted in the highest emulsion stability, lowest cooking loss and had little effect on hardness. Based on the viscoelastic properties, a minimum mass fraction of 0.06% TSPP was sufficient to obtain an acceptable quality product. Rheology proved to be a very useful tool to evaluate the quality of meat products, as it gives insight in the structure of the meat product and especially the functional properties of meat proteins. Based on the obtained results, it can be concluded that the current amount of phosphate added to emulsified meat products can be significantly reduced with minimal loss of product quality.

Phosphate Reduction in Emulsified Meat Products: Impact of Phosphate Type and Dosage on Quality Characteristics

PubMed Central

2017-01-01

Summary Phosphate reduction is of important industrial relevance in the manufacturing of emulsified meat products because it may give rise to a healthier product. The effect of seven different phosphate types was tested on the physicochemical and quality characteristics to select the most promising phosphate type for further cooked sausage manufacturing. Next, phosphate mass fraction was gradually reduced. Tetrasodium di- or pyrophosphate (TSPP) and sodium tripolyphosphate (STPP) increased pH, reduced structural properties, resulted in the highest emulsion stability, lowest cooking loss and had little effect on hardness. Based on the viscoelastic properties, a minimum mass fraction of 0.06% TSPP was sufficient to obtain an acceptable quality product. Rheology proved to be a very useful tool to evaluate the quality of meat products, as it gives insight in the structure of the meat product and especially the functional properties of meat proteins. Based on the obtained results, it can be concluded that the current amount of phosphate added to emulsified meat products can be significantly reduced with minimal loss of product quality. PMID:29089852

A facile method for emulsified oil-water separation by using polyethylenimine-coated magnetic nanoparticles

NASA Astrophysics Data System (ADS)

Lü, Ting; Qi, Dongming; Zhang, Dong; Lü, Yulan; Zhao, Hongting

2018-04-01

Oil spills and oily wastewater discharges from ships and industrial activities have serious impacts on the environment and human health. In this study, a class of easy-to-synthesize polyethylenimine (PEI)-coated Fe3O4 magnetic nanoparticles (MNPs) was successfully synthesized via a one-step coprecipitation method. The synthesized PEI-coated Fe3O4 MNPs were characterized by using multiple technologies and applied in emulsified oil-water separation for the first time. It was found that the PEI effectively tuned the surface charge and wettability of MNPs. As a result, the PEI-coated MNPs could successfully assemble at the oil-water interface and promote the coalescence of oil droplets, thereby facilitating the subsequent magnetic separation. Results showed that the oil-water separation performance was superior and enhanced with the increase of ionic strength. Recycling experiment indicated that the PEI-coated MNPs could be reused up to six times without showing a significant decrease in separation efficiency. All of these results suggested that the PEI-coated MNP could potentially be used as a class of promising nanomaterials for emulsified oil-water separation. [Figure not available: see fulltext.

Dielectric properties, optimum formulation and microwave baking conditions of chickpea cakes.

PubMed

Alifakı, Yaşar Özlem; Şakıyan, Özge

2017-03-01

The aim of this study was to correlate dielectric properties with quality parameters, and to optimize cake formulation and baking conditions by response surface methodology. Weight loss, color, specific volume, hardness and porosity were evaluated. The samples with different DATEM (0.4, 0.8 and 1.2%) and chickpea flour concentrations (30, 40 and 50%) were baked in microwave oven at different power (300, 350, 400 W) and baking times (2.50, 3.0, 3.50 min). It was found that microwave power showed significant effect on color, while baking time showed effect on weight loss, porosity, hardness, specific volume and dielectric properties. Emulsifier level affected porosity, specific volume and dielectric constant. Chickpea flour level affected porosity, color, hardness and dielectric properties of cakes. The optimum microwave power, baking time, DATEM level and chickpea flour level were found as 400 W, 2.84 min, 1.2% and 30%, respectively. The comparison between conventionally baked and the microwave baked cakes at optimum points showed that color difference, weight loss, specific volume and porosity values of microwave baked cakes were less than those of conventionally baked cakes, on the other hand, hardness values were higher. Moreover, a negative correlation between dielectric constant and porosity, and weight loss values were detected for microwave baked samples. A negative correlation between dielectric loss factor and porosity was observed. These correlations indicated that quality characteristics of a microwave baked cake sample can be assessed from dielectric properties. These correlations provides understanding on the behavior of food material during microwave processing.

Pharmacokinetics of a new, nasal formulation of naloxone.

PubMed

Tylleskar, Ida; Skulberg, Arne Kristian; Nilsen, Turid; Skarra, Sissel; Jansook, Phatsawee; Dale, Ola

2017-05-01

Nasal naloxone is wanted for bystander administration in opioid overdose and as a needle-free alternative for emergency medical personnel. Epidemiologic studies have indicated a therapeutic effect of bystander administration of low-concentration/high-volume formulations. The objective for this study was to describe the nasal pharmacokinetics of a new high-concentration/low-volume nasal formulation of naloxone. This was an open, randomized triple crossover trial in healthy, human volunteers (n = 12) where two doses of nasal naloxone (0.8 and 1.6 mg) and one intravenous dose (1.0 mg) were compared. Fifteen serum samples were collected before and until 6 h after naloxone administration. Quantification of naloxone was performed by a validated liquid chromatography-tandem mass spectrometry method. Bioavailability was 0.54 (0.45-0.63) for the 0.8 mg and 0.52 (0.37-0.67) for the 1.6 mg nasal naloxone formulation. Maximum concentration levels (C max ) were 1.45 ng/ml (1.07-1.84) for 0.8 mg and 2.57 ng/ml (1.49-3.66) for the 1.6 mg. Time to maximum concentrations (T max ) were reached at 17.9 min (11.4-24.5) and 18.6 min (14.4-22.9) for the 0.8 mg and the 1.6 mg doses, respectively. This nasal naloxone formulation had a rapid, systemic uptake and higher bioavailability than naloxone formulations not designed for IN use. This indicates that an optimized high-concentration/low-volume nasal spray formulation may deliver a therapeutic dose. The 1.6 mg nasal dose provided serum concentrations that surpassed those of 1.0 mg IV after 15-20 min and stayed above for the rest of the study period.

Mimicking gluten functionality with β-conglycinin concentrate: Evaluation in gluten free yeast-leavened breads.

PubMed

Espinosa-Ramírez, Johanan; Garzon, Raquel; Serna-Saldivar, Sergio O; Rosell, Cristina M

2018-04-01

Fractionation of soy proteins has proved to produce protein concentrates with viscoelastic properties. In the present study, a β-conglycinin concentrate (βCC) obtained by a pH fractionation of soy flour was tested as structuring agent in gluten-free yeast-leavened bread model. A lean formulation with βCC and corn starch was used to produce gluten-free breads with two hydration conditions and three levels of protein (5%, 10% and 15%). Vital gluten was used to compare the functionality of βCC protein and its performance for breadmaking. Breads were characterized in moisture, color, textural parameters and image analysis. βCC presented lower hydration properties and higher emulsifying activity compared to vital gluten. Blends βCC:starch had higher water binding capacity compared to vital gluten blends. The hydration conditions tested affected the moisture, color and cell density of breads. Breads produced with βCC presented higher 2D area and height and presented higher crumb softness and cohesiveness, and did not present significant differences in springiness and resilience compared to vital gluten breads. The image analysis of crumbs showed higher cell density but lower porosity and mean cell areas in βCC breads. Thus, βCC proved to have potential as a structuring agent in gluten-free breads. Copyright © 2017 Elsevier Ltd. All rights reserved.

Pharmacokinetics of gabapentin in a novel gastric-retentive extended-release formulation: comparison with an immediate-release formulation and effect of dose escalation and food.

PubMed

Chen, Cuiping; Cowles, Verne E; Hou, Eddie

2011-03-01

The objectives of the 3 phase I studies described herein were (1) to compare the pharmacokinetics of gabapentin delivered from a novel gastric-retentive dosage form vs an immediate-release formulation, (2) to assess the dose proportionality of the gastric-retentive extended-release formulation, and (3) to determine the effect of food on the pharmacokinetics of gabapentin delivered from this formulation. The time to reach maximum plasma concentration (t(max)) was extended for gabapentin delivered from the gastric-retentive extended-release formulation compared with the immediate-release formulation. A dose-related increase in both the maximum plasma concentration (C(max)) and the area under the plasma concentration-time curve (AUC) was observed as the gabapentin dose increased from 600 to 2400 mg. Fed status and increased fat content delayed t(max) and enhanced C(max) and AUC in proportion to the fat content. The pharmacokinetics of gabapentin delivered from this extended-release formulation allows a reduced dosing frequency while maintaining bioavailability and possibly diminishing the occurrence of adverse events attributable to a slower increase to the peak concentration compared with the immediate-release dosage form.

Evaluating tretinoin formulations in the treatment of acne.

PubMed

Kircik, Leon H

2014-04-01

Topical tretinoin has been a standard treatment for acne vulgaris for more than 4 decades. While tretinoin has demonstrated proven efficacy in the treatment of acne lesions, it also is associated with the potential for skin irritation. Newer formulations have been designed to optimize both the drug concentration and the delivery vehicle with the aim to enable clinicians to provide increasingly effective acne treatment that minimizes irritation. These therapies include formulations with varying concentrations of tretinoin and vehicles that utilize a microsponge delivery system, hydrogels and micronized tretinoin, or propolymers. The purpose of this review is to evaluate different formulations and combinations of tretinoin in the treatment of acne vulgaris. While these advanced formulations were designed for controlled release of active ingredient, and have the potential to reduce cutaneous irritation relative to standard tretinoin cream and gel formulations, there is a need for comparative studies to evaluate the relative benefits of each of these advanced tretinoin formulations in optimizing acne treatment.

A novel and organic solvent-free preparation of solid lipid nanoparticles using natural biopolymers as emulsifier and stabilizer.

PubMed

Xue, Jingyi; Wang, Taoran; Hu, Qiaobin; Zhou, Mingyong; Luo, Yangchao

2017-10-05

In this work, a new and novel organic solvent-free and synthetic surfactant-free method was reported to fabricate stable solid lipid nanoparticles (SLNs) from stearic acid, sodium caseinate (NaCas) and pectin, as well as water. Melted stearic acid was directly emulsified into an aqueous phase containing NaCas and pectin, followed by pH adjustment and thermal treatment to induce the formation of a compact and dense polymeric coating which stabilized SLNs. The preparation procedures and formulations were comprehensively optimized. The inter- and intra-molecular interactions among three ingredients were characterized by fluorescence and Fourier transform infrared spectroscopies. The stability of as-prepared SLNs was evaluated under simulated gastrointestinal conditions, and compared with traditional SLNs prepared with organic solvents. Our results revealed that the SLNs prepared from this organic solvent-free method had superior physicochemical properties over the traditional SLNs, including smaller size and better stability. Furthermore, redispersible SLNs powders were obtained by nano spray drying, but only the SLNs prepared by organic solvent-free method had sub-micron scale, uniform and spherical morphology. The organic solvent-free preparation method was proved to be a promising approach to prepare stable and uniform SLNs for potential oral delivery applications. Copyright © 2017 Elsevier B.V. All rights reserved.

A novel sample preparation method using rapid nonheated saponification method for the determination of cholesterol in emulsified foods.

PubMed

Jeong, In-Seek; Kwak, Byung-Man; Ahn, Jang-Hyuk; Leem, Donggil; Yoon, Taehyung; Yoon, Changyong; Jeong, Jayoung; Park, Jung-Min; Kim, Jin-Man

2012-10-01

In this study, nonheated saponification was employed as a novel, rapid, and easy sample preparation method for the determination of cholesterol in emulsified foods. Cholesterol content was analyzed using gas chromatography with a flame ionization detector (GC-FID). The cholesterol extraction method was optimized for maximum recovery from baby food and infant formula. Under these conditions, the optimum extraction solvent was 10 mL ethyl ether per 1 to 2 g sample, and the saponification solution was 0.2 mL KOH in methanol. The cholesterol content in the products was determined to be within the certified range of certified reference materials (CRMs), NIST SRM 1544 and SRM 1849. The results of the recovery test performed using spiked materials were in the range of 98.24% to 99.45% with an relative standard devitation (RSD) between 0.83% and 1.61%. This method could be used to reduce sample pretreatment time and is expected to provide an accurate determination of cholesterol in emulsified food matrices such as infant formula and baby food. A novel, rapid, and easy sample preparation method using nonheated saponification was developed for cholesterol detection in emulsified foods. Recovery tests of CRMs were satisfactory, and the recoveries of spiked materials were accurate and precise. This method was effective and decreased the time required for analysis by 5-fold compared to the official method. © 2012 Institute of Food Technologists®

Physical, rheological, functional and film properties of a novel emulsifier: Frost grape polysaccharide (FGP) from Vitis riparia Michx

USDA-ARS?s Scientific Manuscript database

A novel emulsifier, Frost grape polysaccharide (FGP), isolated from natural exudate of the species Vitis riparia Michx, was physically and rheologically characterized. The determination of the physical, structural, thermodynamic, emulsification, film, and rheological properties of FGP provide essent...

The Influence of Tablet Formulation, Drug Concentration, and pH Modification on the Stability of Extemporaneously Compounded Levothyroxine Suspensions.

PubMed

Svirskis, Darren; Lin, Shao-Wei; Brown, Helen; Sangaroomthong, Annie; Shin, Daniel; Wang, Ziqi; Xu, Hongtao; Dean, Rebecca; Vareed, Preetika; Jensen, Maree; Wu, Zimei

2018-01-01

Three brands of levothyroxine tablets are currently available in New Zealand (Eltroxin, Mercury Pharma, Synthroid) for extemporaneous compounding into suspensions. This study aims to determine whether tablet brand (i.e., formulation), concentration, storage conditions, as well as pH, impact the stability of compounded levothyroxine suspensions. Using the three available brands of levothyroxine tablets, suspensions were compounded at concentrations of 15 µg/mL and 25 µg/mL and stored at 4°C and 22°C. Samples were withdrawn weekly for 4 weeks, and chemical stability was evaluated using high-performance liquid chromatographic analysis. Physical appearance, ease of resuspension, and pH were also monitored weekly. To evaluate the effect on drug stability, pH modifiers were added to a suspension. As demonstrated by high-performance liquid chromatographic analysis, the suspensions compounded from the Eltroxin and Mercury Pharma tablets were more stable (>90% remaining after 4 weeks) than Synthroid across both storage conditions and concentrations. The drug was more stable at the higher concentration of 25 µg/mL than at 15 µg/mL. Levothyroxine was stable when pH was increased to pH 8 through the addition of sodium citrate; stability was reduced at a lower pH. Storage temperature did not affect the stability of the suspensions during the 4-week study. This is the first study demonstrating the impact of tablet brand, with different excipients, and drug concentrations on stability, and thus the beyond-use date of the compounded levothyroxine liquid formulations. The pH control achieved by sodium citrate, either as an excipient in tablets or an additive during compounding, improved drug stability. Copyright© by International Journal of Pharmaceutical Compounding, Inc.

Development and characterization of fast-dissolving tablet formulations of glyburide based on solid self-microemulsifying systems.

PubMed

Cirri, Marzia; Roghi, Alessandra; Valleri, Maurizio; Mura, Paola

2016-07-01

The aim of this work was to develop effective fast-dissolving tablet formulations of glyburide, endowed with improved dissolution and technological properties, investigating the actual effectiveness of the Solid-Self MicroEmulsifying Drug Delivery System (S-SMEDDS) approach. An initial screening aimed to determine the solubility of the drug in different oils, Surfactants and CoSurfactants allowed the selection of the most suitable components for liquid SMEDDS, whose relative amounts were defined by the construction of pseudo-ternary phase diagrams. The selected liquid SMEDDS formulations (Capyol 90 as oil, Tween 20 as Surfactant and Glycofurol or Transcutol as CoSurfactant) were converted into Solid-SMEDDS, by adsorbing them onto Neusilin (1:1 and 1:0.8w/w S-SMEDDS:carrier), and fully characterized in terms of solid state (DSC and X-ray powder diffraction), morphological (ESEM) and dissolution properties, particle size and reconstitution ability. Finally, the 1:1 S-SMEDDS containing Glycofurol as CoSurfactant, showing the best performance, was selected to prepare two final tablet formulations. The ratio test (t10 min ratio and DE60 ratio) and pair-wise procedures (difference (f1) and similarity (f2) factors) highlighted the similarity of the new developed tablets and the marked difference between their drug dissolution profiles and those of formulations based on the micronized drug. The S-SMEDDS approach allowed to develop fast-dissolving tablets of glyburide, endowed with good technological properties and able to achieve the complete drug dissolution in a time ranging from 10 to 15min, depending on the formulation composition. Copyright © 2016 Elsevier B.V. All rights reserved.

A quality by design approach to optimization of emulsions for electrospinning using factorial and D-optimal designs.

PubMed

Badawi, Mariam A; El-Khordagui, Labiba K

2014-07-16

Emulsion electrospinning is a multifactorial process used to generate nanofibers loaded with hydrophilic drugs or macromolecules for diverse biomedical applications. Emulsion electrospinnability is greatly impacted by the emulsion pharmaceutical attributes. The aim of this study was to apply a quality by design (QbD) approach based on design of experiments as a risk-based proactive approach to achieve predictable critical quality attributes (CQAs) in w/o emulsions for electrospinning. Polycaprolactone (PCL)-thickened w/o emulsions containing doxycycline HCl were formulated using a Span 60/sodium lauryl sulfate (SLS) emulsifier blend. The identified emulsion CQAs (stability, viscosity and conductivity) were linked with electrospinnability using a 3(3) factorial design to optimize emulsion composition for phase stability and a D-optimal design to optimize stable emulsions for viscosity and conductivity after shifting the design space. The three independent variables, emulsifier blend composition, organic:aqueous phase ratio and polymer concentration, had a significant effect (p<0.05) on emulsion CQAs, the emulsifier blend composition exerting prominent main and interaction effects. Scanning electron microscopy (SEM) of emulsion-electrospun NFs and desirability functions allowed modeling of emulsion CQAs to predict electrospinnable formulations. A QbD approach successfully built quality in electrospinnable emulsions, allowing development of hydrophilic drug-loaded nanofibers with desired morphological characteristics. Copyright © 2014 Elsevier B.V. All rights reserved.

Limitations of high dose carrier based formulations.

PubMed

Yeung, Stewart; Traini, Daniela; Tweedie, Alan; Lewis, David; Church, Tanya; Young, Paul M

2018-06-10

This study was performed to investigate how increasing the active pharmaceutical ingredient (API) content within a formulation affects the dispersion of particles and the aerosol performance efficiency of a carrier based dry powder inhalable (DPI) formulation, using a custom dry powder inhaler (DPI) development rig. Five formulations with varying concentrations of API beclomethasone dipropionate (BDP) between 1% and 30% (w/w) were formulated as a multi-component carrier system containing coarse lactose and fine lactose with magnesium stearate. The morphology of the formulation and each component were investigated using scanning electron micrographs while the particle size was measured by laser diffraction. The aerosol performance, in terms of aerodynamic diameter, was assessed using the British pharmacopeia Apparatus E cascade impactor (Next generation impactor). Chemical analysis of the API was observed by high performance liquid chromatography (HPLC). Increasing the concentration of BDP in the blend resulted in increasing numbers and size of individual agglomerates and densely packed BDP multi-layers on the surface of the lactose carrier. BDP present within the multi-layer did not disperse as individual primary particles but as dense agglomerates, which led to a decrease in aerosol performance and increased percentage of BDP deposition within the Apparatus E induction port and pre-separator. As the BDP concentration in the blends increases, aerosol performance of the formulation decreases, in an inversely proportional manner. Concurrently, the percentage of API deposition in the induction port and pre-separator could also be linked to the amount of micronized particles (BDP and Micronized composite carrier) present in the formulation. The effect of such dose increase on the behaviour of aerosol dispersion was investigated to gain greater insight in the development and optimisation of higher dosed carrier-based formulations. Copyright © 2018 Elsevier B.V. All

HAZARDOUS AIR POLLUTANTS FROM THE COMBUSTION OF AN EMULSIFIED HEAVY FUEL OIL IN A FIRETUBE BOILER

EPA Science Inventory

The report gives results of measuring emissions of hazardous air pollutants (HAPs) from the combustion flue gases of a No. 6 fuel oil, both with and without an emulsifying agent, in a 2.5 million Btu/hr (732 kW) firetube boiler with the purpose of determining the impacts of the e...

Comparative viscoelasticity studies: Corn fiber gum versus commercial polysaccharide emulsifiers in bulk and at air/liquid interfaces

USDA-ARS?s Scientific Manuscript database

A comparative study of both the bulk and air/liquid interfacial rheological responses was carried out by using four kinds of high molecular weight and highly branched polysaccharide emulsifiers, (a) corn fiber gum (CFG), (b) octenyl succinate anhydride-modified starch (OSA-s), (c) gum arabic (GA) an...

Characterization and emulsifying properties of β-lactoglobulin-gum Acacia Seyal conjugates prepared via the Maillard reaction.

PubMed

Bi, Binwei; Yang, Hao; Fang, Yapeng; Nishinari, Katsuyoshi; Phillips, Glyn O

2017-01-01

Gum Acacia Seyal (ASY) is less valued than is gum Acacia Senegal, due to its poor emulsifying ability. The present study investigated the Maillard reaction between ASY and β-lactoglobulin (BLG) and its impact on the emulsifying properties of ASY. The reaction products of BLG/ASY mixture (r=1/4), prepared by dry-heating at 60°C and a relative humidity of 79%, as a function of incubation time, were characterized by SDS-PAGE, GPC-MALLS and DSC. The results showed that 12-24h of dry-heating under the given conditions was sufficient for conjugation, meanwhile avoiding the formation of deeply coloured and insoluble melanoidins. More than 64% of the protein was incorporated into ASY, resulting in a two-fold increase in arabinogalactan-protein (AGP) content and 3.5 times increase in weight-average molecular mass of ASY. The conjugation with BLG markedly improved the stability of ASY-stabilized emulsions and their resistance against severe conditions, such as low pH and high saline conditions. Copyright © 2016 Elsevier Ltd. All rights reserved.

Assessing the fate and effects of an insecticidal formulation.

PubMed

de Perre, Chloé; Williard, Karl W J; Schoonover, Jon E; Young, Bryan G; Murphy, Tracye M; Lydy, Michael J

2015-01-01

A 3-yr study was conducted on a corn field in central Illinois, USA, to understand the fate and effects of an insecticidal formulation containing the active ingredients phostebupirim and cyfluthrin. The objectives were to determine the best tillage practice (conventional vs conservation tillage) in terms of grain yields and potential environmental risk, to assess insecticidal exposure using concentrations measured in soil and runoff water and sediments, to compare measured insecticidal concentrations with predicted concentrations from selected risk assessment exposure models, and to calculate toxicity benchmarks from laboratory bioassays performed on reference aquatic and terrestrial nontarget organisms, using individual active ingredients and the formulation. Corn grain yields were not significantly different based on tillage treatment. Similarly, field concentrations of insecticides were not significantly (p > 0.05) different in strip tillage versus conventional tillage, suggesting that neither of the tillage systems would enable greater environmental risk from the insecticidal formulation. Risk quotients were calculated from field concentrations and toxicity data to determine potential risk to nontarget species. The insecticidal formulation used at the recommended rate resulted in soil, sediment, and water concentrations that were potentially harmful to aquatic and terrestrial invertebrates, if exposure occurred, with risk quotients up to 34. © 2014 SETAC.

Changes of lipid and fatty acid absorption induced by high dose of citric acid ester and lecithin emulsifiers.

PubMed

Sadouki, Mohamed; Bouchoucha, Michel

2014-09-01

To describe the effect of two food emulsifiers, lecithin (E322) and citric acid esters of mono-and diglycerides of fatty acids (E472c), on the intestinal absorption of lipids. The experiment was conducted on 24 male Wistar rats randomly assigned in three groups. For two groups of six rats, 30% of the lipid intake was replaced with lecithin (L) or citric acid ester of mono and diglycerides, (E); the remaining 12 rats were the control group (C). Diet and fecal fat analysis was used to determine the apparent lipid absorption (ALA) and fatty acids. ALA was significantly lower in the group E than in the groups C and L (p < 0.001). ALA of long saturated chain fatty acids decreased while the length of the carbon chains increased, and this decrease was higher in the group E. E472c emulsifier decreased the intestinal absorption of lipids.

Evaluation of mechanical and rheological properties of metronidazole gel as local delivery system.

PubMed

Jelvehgari, Mitra; Montazam, Hassan

2011-06-01

Rosacea is a chronic multifactorial vascular skin disorder that affects about 10 percent of the general population. Metronidazole is an effective antibiotic in the treatment of moderate-to severe rosacea. Metronidazole is a suitable drug in cases of resistance to tetracycline or erythromycin, but it has also been shown that oral metronidazole may increase the side effects (e.g., peripheral neuropathy). Oral metronidazole should not be used for more than three months, and hence topical metronidazole gel is the best therapeutic choice in rosacea (especially during pregnancy). This study examined the mechanical (adhesiveness, cohesiveness, extrudability, spreadability, homogeneity) and rheological (viscosity), skin irritant and drug release properties of different metronidazole gel formulations that contain anionic emulsifying wax, glycerin and lactic acid in different proportions. The release studies were conducted using Franz diffusion cells and Silastic membrane as a barrier. The results indicated that gel compressibility, hardness, and adhesiveness, are the factors that influence the ease of gel removal from the container, ease of gel application onto the mucosal membrane, and gel bioadhesion. The findings showed that there exists a strong negative correlation between the spreadability of a formulation and its cohesiveness, the spreadability of a formulation is inversely proportional to its cohesiveness. However, sorbitol solution (70%) concentration was not significantly correlated with drug release. In addition, drug release was significantly reduced as the concentration of anionic emulsifying wax increased and the concentration of lactic acid decreased. The maximum metronidazole release was achieved at a pH of 4-6. Data obtained from in vitro release studies were fitted to various kinetic models and high correlation was obtained in the Higuchi and first order models. The results showed that all the gel formulations showed good extrudability, viscosity

Formulation studies of InhA inhibitors and combination therapy to improve efficacy against Mycobacterium tuberculosis.

PubMed

Knudson, Susan E; Cummings, Jason E; Bommineni, Gopal R; Pan, Pan; Tonge, Peter J; Slayden, Richard A

2016-12-01

Previously, structure-based drug design was used to develop substituted diphenyl ethers with potency against the Mycobacterium tuberculosis (Mtb) enoyl-ACP reductase (InhA), however, the highly lipophilic centroid compound, SB-PT004, lacked sufficient efficacy in the acute murine Mtb infection model. A next generation series of compounds were designed with improved specificity, potency against InhA, and reduced cytotoxicity in vitro, but these compounds also had limited solubility. Accordingly, solubility and pharmacokinetics studies were performed to develop formulations for this class and other experimental drug candidates with high logP values often encountered in drug discovery. Lead diphenyl ethers were formulated in co-solvent and Self-Dispersing Lipid Formulations (SDLFs) and evaluated in a rapid murine Mtb infection model that assesses dissemination to and bacterial burden in the spleen. In vitro synergy studies were performed with the lead diphenyl ether compounds, SB-PT070 and SB-PT091, and rifampin (RIF), which demonstrated an additive effect, and that guided the in vivo studies. Combinatorial therapy in vivo studies with these compounds delivered in our Self-Micro Emulsifying Drug Delivery System (SMEDDS) resulted in an additional 1.4 log 10  CFU reduction in the spleen of animals co-treated with SB-PT091 and RIF and an additional 1.7 log 10 reduction in the spleen with animals treated with both SB-PT070 and RIF. Copyright © 2016 Elsevier Ltd. All rights reserved.

Neonates need tailored drug formulations.

PubMed

Allegaert, Karel

2013-02-08

Drugs are very strong tools used to improve outcome in neonates. Despite this fact and in contrast to tailored perfusion equipment, incubators or ventilators for neonates, we still commonly use drug formulations initially developed for adults. We would like to make the point that drug formulations given to neonates need to be tailored for this age group. Besides the obvious need to search for active compounds that take the pathophysiology of the newborn into account, this includes the dosage and formulation. The dosage or concentration should facilitate the administration of low amounts and be flexible since clearance is lower in neonates with additional extensive between-individual variability. Formulations need to be tailored for dosage variability in the low ranges and also to the clinical characteristics of neonates. A specific focus of interest during neonatal drug development therefore is a need to quantify and limit excipient exposure based on the available knowledge of their safety or toxicity. Until such tailored vials and formulations become available, compounding practices for drug formulations in neonates should be evaluated to guarantee the correct dosing, product stability and safety.

Critical Concentration of Lecithin Enhances the Antimicrobial Activity of Eugenol against Escherichia coli.

PubMed

Zhang, Haoshu; Dudley, Edward G; Davidson, P Michael; Harte, Federico

2017-04-15

Lecithin is a natural emulsifier used in a wide range of food and nonfood applications to improve physical stability, with no known bioactive effects. In this study, the effect of lecithin on the antimicrobial performance of a constant eugenol concentration was tested against three Escherichia coli strains (C600, 0.1229, and O157:H7 strain ATCC 700728). This is the first study, to our knowledge, focusing on lecithin at concentrations below those commonly used in foods to improve the stability of oil in water emulsions (≤10 mg/100 ml). For all three cultures, significant synergistic antimicrobial effects were observed when E. coli cultures were exposed to a constant eugenol concentration (ranging from 0.043 to 0.050% [wt/wt]) together with critical lecithin concentrations ranging from 0.5 to 1 mg/100 ml. Increasing the concentration of lecithin above 1 mg/100 ml (up to 10 mg/100 ml lecithin) diminished the antibacterial effect to values similar to those with eugenol-only treatments. The formation of aggregates (<100 nm) at the critical lecithin concentration was observed using cryo-transmission electron microscopy (cryo-TEM), together with a reduction in light absorbance at 284 nm. At critically low concentrations of lecithin, the formation of nanoscale aggregates is responsible for improving eugenol antimicrobial effects. IMPORTANCE Essential oils (EOs) are effective natural antimicrobials. However, their hydrophobicity and strong aromatic character limit the use of essential oils in food systems. Emulsifiers (e.g., lecithin) increase the stability of EOs in water-based systems but fail to consistently improve antimicrobial effects. We demonstrate that lecithin, within a narrow critical concentration window, can enhance the antimicrobial properties of eugenol. This study highlights the potential bioactivity of lecithin when utilized to effectively control foodborne pathogens. Copyright © 2017 American Society for Microbiology.

Critical Concentration of Lecithin Enhances the Antimicrobial Activity of Eugenol against Escherichia coli

PubMed Central

Zhang, Haoshu; Dudley, Edward G.; Davidson, P. Michael

2017-01-01

ABSTRACT Lecithin is a natural emulsifier used in a wide range of food and nonfood applications to improve physical stability, with no known bioactive effects. In this study, the effect of lecithin on the antimicrobial performance of a constant eugenol concentration was tested against three Escherichia coli strains (C600, 0.1229, and O157:H7 strain ATCC 700728). This is the first study, to our knowledge, focusing on lecithin at concentrations below those commonly used in foods to improve the stability of oil in water emulsions (≤10 mg/100 ml). For all three cultures, significant synergistic antimicrobial effects were observed when E. coli cultures were exposed to a constant eugenol concentration (ranging from 0.043 to 0.050% [wt/wt]) together with critical lecithin concentrations ranging from 0.5 to 1 mg/100 ml. Increasing the concentration of lecithin above 1 mg/100 ml (up to 10 mg/100 ml lecithin) diminished the antibacterial effect to values similar to those with eugenol-only treatments. The formation of aggregates (<100 nm) at the critical lecithin concentration was observed using cryo-transmission electron microscopy (cryo-TEM), together with a reduction in light absorbance at 284 nm. At critically low concentrations of lecithin, the formation of nanoscale aggregates is responsible for improving eugenol antimicrobial effects. IMPORTANCE Essential oils (EOs) are effective natural antimicrobials. However, their hydrophobicity and strong aromatic character limit the use of essential oils in food systems. Emulsifiers (e.g., lecithin) increase the stability of EOs in water-based systems but fail to consistently improve antimicrobial effects. We demonstrate that lecithin, within a narrow critical concentration window, can enhance the antimicrobial properties of eugenol. This study highlights the potential bioactivity of lecithin when utilized to effectively control foodborne pathogens. PMID:28213539

Formulation of multiparticulate systems as lyophilised orally disintegrating tablets.

PubMed

Alhusban, Farhan; Perrie, Yvonne; Mohammed, Afzal R

2011-11-01

The current study aimed to exploit the electrostatic associative interaction between carrageenan and gelatin to optimise a formulation of lyophilised orally disintegrating tablets (ODTs) suitable for multiparticulate delivery. A central composite face centred (CCF) design was applied to study the influence of formulation variables (gelatin, carrageenan and alanine concentrations) on the crucial responses of the formulation (disintegration time, hardness, viscosity and pH). The disintegration time and viscosity were controlled by the associative interaction between gelatin and carrageenan upon hydration which forms a strong complex that increases the viscosity of the stock solution and forms tablet with higher resistant to disintegration in aqueous medium. Therefore, the levels of carrageenan, gelatin and their interaction in the formulation were the significant factors. In terms of hardness, increasing gelatin and alanine concentration was the most effective way to improve tablet hardness. Accordingly, optimum concentrations of these excipients were needed to find the best balance that fulfilled all formulation requirements. The revised model showed high degree of predictability and optimisation reliability and therefore was successful in developing an ODT formulation with optimised properties that were able deliver enteric coated multiparticulates of omeprazole without compromising their functionality. Copyright © 2011 Elsevier B.V. All rights reserved.

Effects of aerosol formulation to amino acids and fatty acids contents in Haruan extract.

PubMed

Febriyenti; Bai-Baie, Saringat Bin; Laila, Lia

2012-01-01

Haruan (Channa striatus) extract was formulated to aerosol for wound and burn treatment. Haruan extract is containing amino acids and fatty acids that important for wound healing process. The purpose of this study is to observe the effect of formulation and other excipients in the formula to amino acids and fatty acids content in Haruan extract before and after formulated into aerosol. Precolumn derivatization with 6-aminoquinolyl-N-hydroxysuccinimidyl carbamate (AQC) method is used for amino acids analysis. Fatty acids in Haruan extract were esterified using transesterification method to form FAMEs before analyzed using GC. Boron trifluoride-methanol reagent is used for transesterification. Tyrosine and methionine concentrations were different after formulated. The concentrations were decrease. There are six fatty acids have amount that significantly different after formulated into concentrate and aerosol. Contents of these fatty acids were increase. Generally, fatty acids which had content increased after formulated were the long-chain fatty acids. This might be happen because of chain extension process. Saponification and decarboxylation would give the chain extended product. Therefore contents of long-chain fatty acids were increase. Generally, the aerosol formulation did not affect the amino acids concentrations in Haruan extract while some long-chain fatty acids concentrations were increase after formulated into concentrate and aerosol.

Groundwater Hydrology and Chemistry in and near an Emulsified Vegetable-Oil Injection Zone, Solid Waste Management Unit 17, Naval Weapons Station Charleston, North Charleston, South Carolina, 2004-2009

USGS Publications Warehouse

Vroblesky, Don A.; Petkewich, Matthew D.; Lowery, Mark A.; Conlon, Kevin J.; Casey, Clifton C.

2010-01-01

The U.S. Geological Survey and the Naval Facilities Engineering Command Southeast investigated the hydrology and groundwater chemistry in the vicinity of an emulsified vegetable-oil injection zone at Solid Waste Management Unit (SWMU) 17, Naval Weapons Station Charleston, North Charleston, South Carolina. In May 2004, Solutions-IES initiated a Phase-I pilot-scale treatability study at SWMU17 involving the injection of an edible oil emulsion into the aquifer near wells 17PS-01, 17PS-02, and 17PS-03 to treat chlorinated solvents. The Phase-I injection of emulsified vegetable oil resulted in dechlorination of trichloroethene (TCE) to cis-1,2-dichloroethene (cDCE), but the dechlorination activity appeared to stall at cDCE, with little further dechlorination of cDCE to vinyl chloride (VC) or to ethene. The purpose of the present investigation was to examine the groundwater hydrology and chemistry in and near the injection zone to gain a better understanding of the apparent remediation stall. It is unlikely that the remediation stall was due to the lack of an appropriate microbial community because groundwater samples showed the presence of Dehalococcoides species (sp.) and suitable enyzmes. The probable causes of the stall were heterogeneous distribution of the injectate and development of low-pH conditions in the injection area. Because groundwater pH values in the injection area were below the range considered optimum for dechlorination activity, a series of tests was done to examine the effect on dechlorination of increasing the pH within well 17PS-02. During and following the in-well pH-adjustment tests, VC concentrations gradually increased in some wells in the injection zone that were not part of the in-well pH-adjustment tests. These data possibly reflect a gradual microbial acclimation to the low-pH conditions produced by the injection. In contrast, a distinct increase in VC concentration was observed in well 17PS-02 following the in-well pH increase. Adjustment

Composition of legume soaking water and emulsifying properties in gluten-free bread.

PubMed

Huang, San; Liu, Yuling; Zhang, Weihan; Dale, Kylie J; Liu, Silu; Zhu, Jingnan; Serventi, Luca

2018-04-01

Soaking of legumes results in the loss of macronutrients, micronutrients and phytochemicals. Fibre, protein and phytochemicals found in legumes exert emulsifying activity that may improve the structure and texture of gluten-free bread. The legume soaking water of haricot beans, garbanzo chickpeas, whole green lentils, split yellow peas and yellow soybeans were tested in this study for functional properties and use as food ingredients. Composition, physicochemical properties and effect on the quality of gluten-free bread were determined for each legume soaking water. Haricot beans and split yellow peas released the highest amount of solids in the legume soaking water: 1.89 and 2.38 g/100 g, respectively. Insoluble fibre was the main constituent of haricot beans legume soaking water, while water-soluble carbohydrates and protein were the major fraction of split yellow peas. High quantities of phenolics (∼400 µg/g) and saponins (∼3 mg/g) were found in the legume soaking water of haricot beans, whole green lentils and split yellow peas. High emulsifying activity (46 and 50%) was found for the legume soaking water of garbanzo chickpeas and split yellow peas, probably due to their protein content and high ratio of water-soluble carbohydrates to dry matter. Such activity resulted in softer texture of the gluten-free bread. A homogeneous structure of crumb pores was found for split yellow peas, opposing that of whole green lentils. A balance between the contents of yeast nutrients and antinutrients was the likely basis of the different appearances.

Advanced protein formulations

PubMed Central

Wang, Wei

2015-01-01

It is well recognized that protein product development is far more challenging than that for small-molecule drugs. The major challenges include inherent sensitivity to different types of stresses during the drug product manufacturing process, high rate of physical and chemical degradation during long-term storage, and enhanced aggregation and/or viscosity at high protein concentrations. In the past decade, many novel formulation concepts and technologies have been or are being developed to address these product development challenges for proteins. These concepts and technologies include use of uncommon/combination of formulation stabilizers, conjugation or fusion with potential stabilizers, site-specific mutagenesis, and preparation of nontraditional types of dosage forms—semiaqueous solutions, nonfreeze-dried solid formulations, suspensions, and other emerging concepts. No one technology appears to be mature, ideal, and/or adequate to address all the challenges. These gaps will likely remain in the foreseeable future and need significant efforts for ultimate resolution. PMID:25858529

Image-guided thermal therapy with a dual-contrast magnetic nanoparticle formulation: A feasibility study

PubMed Central

Attaluri, Anilchandra; Seshadri, Madhav; Mirpour, Sahar; Wabler, Michele; Marinho, Thomas; Furqan, Muhammad; Zhou, Haoming; De Paoli, Silvia; Gruettner, Cordula; Gilson, Wesley; DeWeese, Theodore; Garcia, Monica; Ivkov, Robert; Liapi, Eleni

2016-01-01

Purpose/objective The aim of this study was to develop and investigate the properties of a magnetic iron oxide nanoparticle–ethiodised oil formulation for image-guided thermal therapy of liver cancer. Materials and methods The formulation comprises bionised nano-ferrite (BNF) nanoparticles suspended in ethiodised oil, emulsified with polysorbate 20 (BNF-lip). Nanoparticle size was measured via photon correlation spectroscopy and transmission electron microscopy. In vivo thermal therapy capability was tested in two groups of male Foxn1nu mice bearing subcutaneous HepG2 xenograft tumours. Group I (n =12) was used to screen conditions for group II (n =48). In group II, mice received one of BNF-lip (n =18), BNF alone (n =16), or PBS (n =14), followed by alternating magnetic field (AMF) hyperthermia, with either varied duration (15 or 20 min) or amplitude (0, 16, 20, or 24 kA/m). Image-guided fluoroscopic intra-arterial injection of BNF-lip was tested in New Zealand white rabbits (n =10), bearing liver VX2 tumours. The animals were subsequently imaged with CT and 3 T MRI, up to 7 days post-injection. The tumours were histopathologically evaluated for distribution of BNF-lip. Results The BNF showed larger aggregate diameters when suspended in BNF-lip, compared to clear solution. The BNF-lip formulation produced maximum tumour temperatures with AMF >20 kA/m and showed positive X-ray visibility and substantial shortening of T1 and T2 relaxation time, with sustained intratumoural retention up to 7 days post-injection. On pathology, intratumoural BNF-lip distribution correlated well with CT imaging of intratumoural BNF-lip distribution. Conclusion The BNF-lip formulation has favourable thermal and dual imaging capabilities for image-guided thermal therapy of liver cancer, suggesting further exploration for clinical applications. PMID:27151045

U(VI) bioreduction with emulsified vegetable oil as the electron donor--microcosm tests and model development.

PubMed

Tang, Guoping; Wu, Wei-Min; Watson, David B; Parker, Jack C; Schadt, Christopher W; Shi, Xiaoqing; Brooks, Scott C

2013-04-02

We conducted microcosm tests and biogeochemical modeling to study U(VI) reduction in contaminated sediments amended with emulsified vegetable oil (EVO). Indigenous microorganisms in the sediments degraded EVO and stimulated Fe(III), U(VI), and sulfate reduction, and methanogenesis. Acetate concentration peaked in 100-120 days in the EVO microcosms versus 10-20 days in the oleate microcosms, suggesting that triglyceride hydrolysis was a rate-limiting step in EVO degradation and subsequent reactions. Acetate persisted 50 days longer in oleate- and EVO- than in ethanol-amended microcosms, indicating that acetate-utilizing methanogenesis was slower in the oleate and EVO than ethanol microcosms. We developed a comprehensive biogeochemical model to couple EVO hydrolysis, production, and oxidation of long-chain fatty acids (LCFA), glycerol, acetate, and hydrogen, reduction of Fe(III), U(VI) and sulfate, and methanogenesis with growth and decay of multiple functional microbial groups. By estimating EVO, LCFA, and glycerol degradation rate coefficients, and introducing a 100 day lag time for acetoclastic methanogenesis for oleate and EVO microcosms, the model approximately matched observed sulfate, U(VI), and acetate concentrations. Our results confirmed that EVO could stimulate U(VI) bioreduction in sediments and the slow EVO hydrolysis and acetate-utilizing methanogens growth could contribute to longer term bioreduction than simple substrates (e.g., ethanol, acetate, etc.) in the subsurface.

Relative bioavailability of an extemporaneous ondansetron 4-mg capsule formulation versus solution.

PubMed

Lam, Y W Francis; Javors, Martin A; Ait-Daoud, Nassima; Roache, John D; Johnson, Bankole A

2004-04-01

To compare the relative bioavailability of an extemporaneous ondansetron capsule formulation with that of an identical dose of the commercially available solution formulation. Open-label, randomized, two-way crossover study. University-affiliated research laboratory. Sixteen (eight men, eight women) healthy, nonsmoking volunteers. Participants were randomly assigned to receive a 4-mg dose of either the commercially available ondansetron solution or the extemporaneous ondansetron capsule formulation. Blood sampling was performed over 12 hours after dosing. After a washout period of at least 3 days, each participant was switched to the alternate formulation, and blood sampling was repeated. Ondansetron was well absorbed after administration of both formulations, with the solution achieving a faster rate of drug absorption over the first hour of dosing. After the peak plasma concentration was achieved, the plasma concentration-time curves of both formulations declined at a similar steady rate. There were no significant differences in pharmacokinetic parameters between the two formulations, and the relative bioavailability of the capsule versus the solution formulation was 101%. Similar concentration-time curves and pharmacokinetic parameters were achieved with the two formulations. The commercially available solution would be a useful alternative formulation for administration of low-dose ondansetron in research and clinical settings.

UPTAKE AND EFFECTS OF DISPERSED OIL DROPLETS AND EMULSIFIED OIL BY ESTUARINE CRUSTACEANS IN THE GULF OF MEXICO

EPA Science Inventory

The results from this project will provide information on the extent of uptake of dispersed petroleum from the seawater and uptake of emulsified oil from the sediment by blue crabs and grass shrimp of different life history stages. The primary focus of the study will be eff...

Formulation and performance test of palm-based foaming agent concentrate for fire extinguisher application

NASA Astrophysics Data System (ADS)

Rivai, M.; Hambali, E.; Suryani, A.; Fitria, R.; Firmansyah, S.; Pramuhadi, G.

2018-03-01

The utilization of foaming agent for fire extinguisher application improves the efficiency of water as a fire extinguishing agent, lowers surface tension, and acts as a foaming agent. The formed foam cools the fire down and covers the burned material to avoid it from further contact with oxygen which may reignite the fire. This study aimed to produce and assess the performance of foaming agent concentrate from palm oil as a fire extinguisher agent. In the performance test, measurements were taken on foam stability, foaming ability, surface tension, interfacial tension, viscosity, contact angle, density, and specific gravity. The formulation was conducted by using the best produced potassium palmitate, potassium methyl ester, and sodium lauric combined with diluents, chelating agent, and other additives at various composition comparisons. The produced foaming agent concentrate was found to be in a rather paste and liquid form with viscosity of 2.34 – 253 cP. It was also found that the resulted foaming agent concentrate dissolved in water at the concentration rate of 1% had a foam stability level of 30-91%, foaming ability of 288 – 503%, surface tension of 19.68 – 25.05 dyne/cm, interfacial tension of 0.54 – 4,20 dyne/cm, viscosity of 1.00 – 1.05 cP, contact angles of 53.75 – 63.79° at 0 minute and 11.84 – 22.42 ° at minute 10, density of 0.99586 – 0.99612 g/cm3, and a specific gravity of 1.00021 – 1.00046. Based on foam stability, foaming ability, and surface tension parameters, it was concluded that NF5 and NF17 were the best formulas.Compared to the other formulas, NF5 formula had the best droplet diameter (minimum 0.14 mm) and droplet density (maximum 3056 droplets/cm2).

Design and characterization of emulsified spray dried alginate microparticles as a carrier for the dually acting drug roflumilast.

PubMed

Mahmoud, Azza A; Elkasabgy, Nermeen A; Abdelkhalek, Abdel Fatah A

2018-06-18

Roflumilast is a selective inhibitor of phosphodiesterase-4 isoenzyme in lung cells. Having psychiatric adverse reactions when administered orally affects negatively the patients' adherence to the drug. This work aimed to prepare emulsified spray dried alginate microparticles for the pulmonary delivery of roflumilast. Sodium alginate was used as microparticle-forming material, isopropyl myristate as an oil, Tween®80 as surfactant and calcium beta-glycerophosphate as cross-linking agent to enhance the mechanical properties of the particles. The prepared particles were evaluated for their encapsulation efficiency, particle size and in-vitro release. From the studied carriers, beta-cyclodextrin (CD) was the best regarding giving formulation smaller particle size and more sustained drug release. The inhalation profile of CD-based microparticles was investigated using Anderson cascade impactor. The aerosolization profile of CD-based microparticles suggested their efficiency to deliver the drug deep in the lung. The CD-based microparticles possessed more inhibitory effects on the viability of A549 cells and on the pro-inflammatory cytokines (TNF-α, IL-6 and IL-10) compared to the pure drug. Hence, CD-based microparticles could regulate the tumorigenesis besides tumor-associated inflammation. Finally, CD-based microparticles showed more sustained bronchodilatation properties in healthy human volunteers when compared to Ventolin®HFA. CD-based microparticles proved to be a promising carrier for inhaled roflumilast in human. Copyright © 2018. Published by Elsevier B.V.

Salting-out and salting-in: competitive effects of salt on the aggregation behavior of soy protein particles and their emulsifying properties.

PubMed

Xu, Hua-Neng; Liu, Yang; Zhang, Lianfu

2015-08-07

Emulsions stabilized by protein particles have gained increasing research attention due to their combined advantages of biocompatibility and superior stability. In this study, colloidal particles consisting of soy protein isolates (SPIs) prepared through a heat-treatment procedure are used to make oil-in-water emulsions at a protein concentration of 10 g L(-1) and a pH of 5.91. We investigate parallelly the effects of NaCl on the stability and rheological properties of the particle suspensions and their stabilized emulsions at salt concentrations of 0, 100 and 400 mM. The aggregation behavior of the particles is strongly dependent on the NaCl concentration, showing signs of sedimentation at low NaCl concentration (100 mM) but redispersion again at high NaCl concentration (400 mM). The extensive particle aggregation is beneficial to the formation of a continuous interfacial film for the emulsions, and hence results in a remarkable increase of creaming stability and interfacial viscoelastic moduli. The results can be explained in terms of two competitive effects of NaCl: salting-out and salting-in, which are attributed to complex electrostatic interactions between the particles as a function of NaCl concentration. The delicate balance between salting-out and salting-in provides an interesting insight into the nature of underlying protein particle interactions in aqueous suspensions and a possible mechanism for tailoring their emulsifying properties via salt effects.

Preparation of liposomes containing zedoary turmeric oil using freeze-drying of liposomes via TBA/water cosolvent systems and evaluation of the bioavailability of the oil.

PubMed

Yang, Zhiwen; Yu, Songlin; Fu, Dahua

2010-02-01

The purpose of this study was to enhance the absorption of zedoary turmeric oil (ZTO) in vivo and develop new formulations of a water-insoluble oily drug. This study described a method for preparing ZTO liposomes, which involved freeze-drying (FD) of liposomes with TBA/water cosolvent systems. The TBA/water cosolvent systems were used to investigate a feasible method of liposomes manufacture; the two factors, sugar/lipid mass ratio and TBA content (concentration), of the preparation process were evaluated in this study. The results showed that the addition of TBA content could significantly enhance the sublimation of ice resulting in short FD cycles time, and reduce the entrapment efficiency of liposomes. In addition, the residual TBA solvents levels were determined to be less than 0.37% under all optimum formulations and processing conditions. Several physical properties of liposomes were examined by H-600 transmission electron microscope (TEM) and zetamaster analyser system. The results revealed that the liposomes were smooth and spherical with an average particle size of 457 +/- 7.8 nm and the zeta potential was more than 3.65 Mv. The bioavailability of the liposomes was evaluated in rabbits, compared with the conventional self-emulsifying formulation for oral administration. Compared with the conventional self-emulsifying formulation, the plasma concentration-time profiles with improved sustained-release characteristics were achieved after oral administration of the liposomes with a bioavailability of 257.7% (a good strategy for improving the bioavailability of an oily drug). In conclusion, the present experimental findings clearly demonstrated the usefulness of ZTO liposome vesicles in improving therapeutic efficacy by enhancing oral bioavailability. Our study offered an alternative method for designing sustained-release preparations of oily drugs.

Emulsifying properties of legume proteins compared to β-lactoglobulin and Tween 20 and the volatile release from oil-in-water emulsions.

PubMed

Benjamin, O; Silcock, P; Beauchamp, J; Buettner, A; Everett, D W

2014-10-01

The emulsifying properties of plant legume protein isolates (soy, pea, and lupin) were compared to a milk whey protein, β-lactoglobulin (β-lg), and a nonionic surfactant (Tween 20). The protein fractional composition was characterized using sodium dodecyl sulfate-polyacrylamide gel electrophoresis analysis. The following emulsion properties were measured: particle diameter, shear surface ζ-potential, interfacial tension (IT), and creaming velocity. The effect of protein preheat treatment (90 °C for 10 min) on the emulsifying behavior and the release of selected volatile organic compounds (VOCs) from emulsions under oral conditions was also investigated in real time using proton transfer reaction-mass spectrometry. The legume proteins showed comparable results to β-lg and Tween 20, forming stable, negatively charged emulsions with particle diameter d3,2 < 0.4 μm, and maintained stability over 50 d. The relatively lower stability of lupin emulsions was significantly correlated with the low protein surface hydrophobicity and IT of the emulsion. After heating the proteins, the droplet size of pea and lupin emulsions decreased. The VOC release profile was similar between the protein-stabilized emulsions, and greater retention was observed for Tween 20-stabilized emulsions. This study demonstrates the potential application of legume proteins as alternative emulsifiers to milk proteins in emulsion products. © 2014 Institute of Food Technologists®

Concentration-effect relationship of levodopa in patients with Parkinson's disease after oral administration of an immediate release and a controlled release formulation.

PubMed Central

Harder, S; Baas, H; Bergemann, N; Demisch, L; Rietbrock, S

1995-01-01

1. The relationship between plasma concentration of levodopa and motor-response was investigated in 12 patients with Parkinson's disease who showed marked response fluctuations, after a single oral dose of an immediate release (IR) formulation (100 mg levodopa/25 mg genserazide) and a controlled release (CR) formulation (300 mg levodopa/75 mg benserazide), using a double-blind, randomized, cross-over design. 2. The sum score of the Columbia University Rating Scale (CURS sigma) was used for pharmacodynamic assessment. A sigmoidal Emax-model was fitted to the data using a semiparametric pharmacokinetic/dynamic approach. 3. The dose-corrected AUC of levodopa after the IR-formulation was 27.5 (+/- 9.1 s.d.) ng ml-1 h per mg and 23.2 (+/- 4.6 s.d.) ng ml-1 h per mg after the CR-formulation. Cmax was 1714 (+/- 1027 s.d.) ng ml-1 after the IR-formulation and 1494 (+/- 383 s.d.) ng ml-1 after the CR-formulation. 4. With both preparations, the maximal response to levodopa (Emax) was a decrease in the CURS sigma rating of about 27 scores. Estimates of the EC50 of levodopa were 495 (+/- 144 s.d.) ng ml-1 (IR) and 1024 (+/- 502 s.d.) ng ml-1 (CR), respectively (95%-CI: 1.51-2.66, point estimator 1.95). The mean duration of the motor response was 1.9 (+/- 0.5 s.d.) h (IR) and 2.8 (+/- 0.7 s.d.) h (CR), respectively (95%-CI: 1.12-2.04, point estimator 1.53).(ABSTRACT TRUNCATED AT 250 WORDS) PMID:7756097

Effects of locust bean gum and mono- and diglyceride concentrations on particle size and melting rates of ice cream.

PubMed

Cropper, S L; Kocaoglu-Vurma, N A; Tharp, B W; Harper, W J

2013-06-01

The objective of this study was to determine how varying concentrations of the stabilizer, locust bean gum (LBG), and different levels of the emulsifier, mono- and diglycerides (MDGs), influenced fat aggregation and melting characteristics of ice cream. Ice creams were made containing MDGs and LBG singly and in combination at concentrations ranging between 0.0% to 0.14% and 0.0% to 0.23%, respectively. Particle size analysis, conducted on both the mixes and ice cream, and melting rate testing on the ice cream were used to determine fat aggregation. No significant differences (P < 0.05) were found between particle size values for experimental ice cream mixes. However, higher concentrations of both LBG and MDG in the ice creams resulted in values that were larger than the control. This study also found an increase in the particle size values when MDG levels were held constant and LBG amounts were increased in the ice cream. Ice creams with higher concentrations of MDG and LBG together had the greatest difference in the rate of melting than the control. The melting rate decreased with increasing LBG concentrations at constant MDG levels. These results illustrated that fat aggregation may not only be affected by emulsifiers, but that stabilizers may play a role in contributing to the destabilization of fat globules. © 2013 Institute of Food Technologists®

Emulsifying and foaming properties of amaranth seed protein isolates.

PubMed

Fidantsi, A; Doxastakis, G

2001-07-01

The emulsifying and foaming properties of amaranth seed protein isolates prepared by wet extraction methods, such as isoelectric precipitation and dialysis, were investigated. The various isolates differ from each other in many ways. The isolate prepared by isoelectric precipitation mainly contains the globulin but not the albumin fraction and a considerable amount of polysaccharides, while the other isolate prepared by the dialysis method contains all the globulin and albumin fractions. The protein-polysaccharide complexes enhance emulsion stability due to steric repulsion effects. Measurements of the emulsion stability show that the studied protein isolates act as effective stabilizing agents. Foam expansion is dominated by the surface activity and availability of protein in the solution, while foam stability is determined by the properties of the interfacial layer. The results show that amaranth protein isolates act as an effective foaming agent. Both foaming properties intensified from the presence of protein-polysaccharide complexes.

Treatment of emulsified oils by electrocoagulation: pulsed voltage applications.

PubMed

Genc, Ayten; Bakirci, Busra

2015-01-01

The effect of pulsed voltage application on energy consumption during electrocoagulation was investigated. Three voltage profiles having the same arithmetic average with respect to time were applied to the electrodes. The specific energy consumption for these profiles were evaluated and analyzed together with oil removal efficiencies. The effects of applied voltages, electrode materials, electrode configurations, and pH on oil removal efficiency were determined. Electrocoagulation experiments were performed by using synthetic and real wastewater samples. The pulsed voltages saved energy during the electrocoagulation process. In continuous operation, energy saving was as high as 48%. Aluminum electrodes used for the treatment of emulsified oils resulted in higher oil removal efficiencies in comparison with stainless steel and iron electrodes. When the electrodes gap was less than 1 cm, higher oil removal efficiencies were obtained. The highest oil removal efficiencies were 95% and 35% for the batch and continuous operating modes, respectively.

Evaluation of the Properties Magnesium Phosphate Cement with Emulsified Asphalt

NASA Astrophysics Data System (ADS)

Du, Jia-Chong; Shen, Ruei-Siang; Zhou, Yu-Zhun

2017-10-01

Three type mixtures of magnesium phosphate cement with emulsified asphalt for evaluation their properties. The mixtures of the samples were fabricated and allowed them 2 hours, seven and twenty eight days curing before tested by compressive strength, Marshall stability and indirect tensile strength to probe into their engineering properties. The test results show that all tests have the greatest values at the 28 days curing and too much asphalt emulsion may cause too soft as result of low stability. The compressive strength of Type-III mixture has the greatest value, no matter what curing time is. The Marshall stability test and indirect tensile strength of the Type-III mixture are qualified by the specification required for fast maintenance. The more asphalt emulsion added, the less compressive strength has.

Surface-modified solid lipid nanoparticles for oral delivery of docetaxel: enhanced intestinal absorption and lymphatic uptake

PubMed Central

Cho, Hyun-Jong; Park, Jin Woo; Yoon, In-Soo; Kim, Dae-Duk

2014-01-01

Docetaxel is a potent anticancer drug, but development of an oral formulation has been hindered mainly due to its poor oral bioavailability. In this study, solid lipid nanoparticles (SLNs) surface-modified by Tween 80 or D-alpha-tocopheryl poly(ethylene glycol 1000) succinate (TPGS 1000) were prepared and evaluated in terms of their feasibility as oral delivery systems for docetaxel. Tween 80-emulsified and TPGS 1000-emulsified tristearin-based lipidic nanoparticles were prepared by a solvent-diffusion method, and their particle size distribution, zeta potential, drug loading, and particle morphology were characterized. An in vitro release study showed a sustained-release profile of docetaxel from the SLNs compared with an intravenous docetaxel formulation (Taxotere®). Tween 80-emulsified SLNs showed enhanced intestinal absorption, lymphatic uptake, and relative oral bioavailability of docetaxel compared with Taxotere in rats. These results may be attributable to the absorption-enhancing effects of the tristearin nanoparticle. Moreover, compared with Tween 80-emulsified SLNs, the intestinal absorption and relative oral bioavailability of docetaxel in rats were further improved in TPGS 1000-emulsified SLNs, probably due to better inhibition of drug efflux by TPGS 1000, along with intestinal lymphatic uptake. Taken together, it is worth noting that these surface-modified SLNs may serve as efficient oral delivery systems for docetaxel. PMID:24531717

Effect of Formulation and Process Parameters on Chitosan Microparticles Prepared by an Emulsion Crosslinking Technique.

PubMed

Rodriguez, Lidia B; Avalos, Abraham; Chiaia, Nicholas; Nadarajah, Arunan

2017-05-01

There are many studies about the synthesis of chitosan microparticles; however, most of them have very low production rate, have wide size distribution, are difficult to reproduce, and use harsh crosslinking agents. Uniform microparticles are necessary to obtain repeatable drug release behavior. The main focus of this investigation was to study the effect of the process and formulation parameters during the preparation of chitosan microparticles in order to produce particles with narrow size distribution. The technique evaluated during this study was emulsion crosslinking technique. Chitosan is a biocompatible and biodegradable material but lacks good mechanical properties; for that reason, chitosan was ionically crosslinked with sodium tripolyphosphate (TPP) at three different ratios (32, 64, and 100%). The model drug used was acetylsalicylic acid (ASA). During the preparation of the microparticles, chitosan was first mixed with ASA and then dispersed in oil containing an emulsifier. The evaporation of the solvents hardened the hydrophilic droplets forming microparticles with spherical shape. The process and formulation parameters were varied, and the microparticles were characterized by their morphology, particle size, drug loading efficiency, and drug release behavior. The higher drug loading efficiency was achieved by using 32% mass ratio of TPP to chitosan. The average microparticle size was 18.7 μm. The optimum formulation conditions to prepare uniform spherical microparticles were determined and represented by a region in a triangular phase diagram. The drug release analyses were evaluated in phosphate buffer solution at pH 7.4 and were mainly completed at 24 h.

The effect of clove bud powder at a spice level on antioxidant and quality properties of emulsified pork sausage during cold storage.

PubMed

Jin, Sang-Keun; Choi, Jung-Seok; Jeong, Jin-Yeon; Kim, Gap-Don

2016-09-01

Clove bud is a widely used spice in meat and meat products, and it contains high level of phenolic compounds. The effectiveness of the clove as a spice has not been fully studied at a general level of addition in the meat products. Therefore, in the present study, the antioxidant, antimicrobial, and nitrite scavenging abilities of clove bud powder (CBP) was assessed at spice level (0.1% and 0.2%) in emulsified pork sausage, during 6 weeks of cold storage. CBP had DPPH radical scavenging ability, but CBP addition at 0.1% and 0.2% did not decrease the TBARS value. An antimicrobial effect of CBP was also not observed during the cold storage. However, residual nitrite at storage weeks 4 and 6 was shown to be lower (P < 0.05). Addition of CBP decreased CIE L* and a* values, but it produced unacceptable sensory properties. Texture profile analysis was not affected by the addition of CBP in emulsified pork sausage (P > 0.05). The positive effect on nitrite scavenging could be expected by the addition of 0.2% CBP as a spice. However, antioxidant and antimicrobial abilities were not observed, as well as improvement in the quality of characteristics, in emulsified pork sausage. © 2016 Society of Chemical Industry. © 2016 Society of Chemical Industry.

Influence of hydrophilic surfactants on the properties of multiple W/O/W emulsions.

PubMed

Schmidts, T; Dobler, D; Nissing, C; Runkel, F

2009-10-01

Multiple W/O/W emulsions for topical application using Span 80 as a lipophilic emulsifier were prepared. Several hydrophilic emulsifiers were tested in respect of their suitability for the preparation of multiple emulsions. In addition, the effect of different oil-phase compositions on emulsion stability was investigated. The physicochemical parameters of the formulations were characterized and their long-term stability was evaluated by means of rheological measurements, droplet size observations and conductivity analysis. As discovered, the modification of an oil-phase composition results in a decrease in the diffusion coefficient of water and water-soluble substances and, consequently, in enhanced stability. The influence of the release of electrolytes from the inner to the outer water phase on the emulsion stability behaviour was investigated. It was found, that the effect of the hydrophilic emulsifiers on the formulation properties is related not only to its HLB value, but rather to its chemical composition. As a result, polyethoxylated ethers of fatty alcohols (C=16-18) with HLBs between 15.3 and 16.2 appear to be the most suitable ones for creating stable formulations.

Multimodal cues drive host-plant assessment in Asian citrus psyllid (Diaphorina citri).

PubMed

Patt, Joseph M; Meikle, William G; Mafra-Neto, Agenor; Sétamou, Mamoudou; Mangan, Robert; Yang, Chenghai; Malik, Nasir; Adamczyk, John J

2011-12-01

Asian citrus psyllid (Diaphorina citri) transmits the causal agent of Huanglongbing, a devastating disease of citrus trees. In this study we measured behavioral responses of D. citri to combinations of visual, olfactory, and gustatory stimuli in test arenas. Stimuli were presented to the psyllids in droplets or lines of an emulsified wax formulation in two different arena types in no-choice tests. First, when placed on a colored ring situated halfway between the center and perimeter of a petri dish, D. citri spent more time on yellow versus gray rings; however, this response disappeared when either gray or yellow wax droplets were applied. When the psyllids were presented with droplets scented with terpenes, the response to both scent and color was increased. The addition of a dilute (≍0.1 M) sucrose solution to the wax droplets increased the magnitude of D. citri responses. Next, groups of D. citri were placed on plastic laboratory film covering a sucrose solution, to mimic a leaf surface. Test stimuli were presented via two 'midribs' made from lines of emulsified wax formulation. Probing levels were measured as a function of color saturation and scent composition, and concentration. The test scents were based on qualitatively major volatiles emitted by Murraya paniculata (L.) Jack, Citrus aurantifolia (Christm.) Swingle, and C. sinensis (L.) Osbeck. The highest probing response was observed on the middle concentration (20-μl scent/10 ml wax formulation) of the C. aurantifolia-scented wax lines. Results indicate that there are interactive effects between the different sensory modalities in directing host-plant assessment behavior.

Bioavailability of syrup and tablet formulations of cefetamet pivoxil.

PubMed

Ducharme, M P; Edwards, D J; McNamara, P J; Stoeckel, K

1993-12-01

Two studies examining the bioavailability of cefetamet pivoxil in healthy male subjects were conducted. In the first, the bioavailabilities of the 250-mg (M250) and M500 tablet formulations of cefetamet pivoxil to be marketed were compared with that of a tablet used in clinical trials. All products were given with food at a dose of 500 mg. In the second study, the bioavailability of the syrup formulation was evaluated under both fasting and nonfasting conditions and compared with that of the M500 tablet formulation given with food. The absolute bioavailabilities of the M500 and M250 tablets (55.0% +/- 8.0% and 55.7% +/- 7.0%, respectively) were not significantly different from that of the clinical-trial formulation (49.8% +/- 8.5%). The newer tablet formulations exhibited faster absorption as evidenced by higher peak concentrations (3.8 [M500] and 3.9 [M250] mg/liter compared with 3.2 mg/liter for the clinical-trial formulation), a shorter time to peak concentration, and a shorter mean absorption time. The syrup formulation was found to have significantly lower absolute bioavailability (37.9% +/- 6.0%) compared with that of the M500 tablet (58.4% +/- 9.0%) when both were given with food. Food had no significant effect on the bioavailability of the syrup, which averaged 34.0% +/- 8.6% under fasting conditions, although absorption was delayed by food (mean absorption time increased from 2.2 to 3.9 h). This contrasts with the results of previous studies documenting significant increases in tablet bioavailability with food. Despite the lower bioavailability of the syrup, unbound-cefetamet concentrations are expected to remain above the MICs for 90% of the strains tested for susceptible organisms for approximately 10 h of the usual 12-h dosing interval with both syrup and tablet formulations of cefetamet pivoxil given with food.

Bioavailability of syrup and tablet formulations of cefetamet pivoxil.

PubMed Central

Ducharme, M P; Edwards, D J; McNamara, P J; Stoeckel, K

1993-01-01

Two studies examining the bioavailability of cefetamet pivoxil in healthy male subjects were conducted. In the first, the bioavailabilities of the 250-mg (M250) and M500 tablet formulations of cefetamet pivoxil to be marketed were compared with that of a tablet used in clinical trials. All products were given with food at a dose of 500 mg. In the second study, the bioavailability of the syrup formulation was evaluated under both fasting and nonfasting conditions and compared with that of the M500 tablet formulation given with food. The absolute bioavailabilities of the M500 and M250 tablets (55.0% +/- 8.0% and 55.7% +/- 7.0%, respectively) were not significantly different from that of the clinical-trial formulation (49.8% +/- 8.5%). The newer tablet formulations exhibited faster absorption as evidenced by higher peak concentrations (3.8 [M500] and 3.9 [M250] mg/liter compared with 3.2 mg/liter for the clinical-trial formulation), a shorter time to peak concentration, and a shorter mean absorption time. The syrup formulation was found to have significantly lower absolute bioavailability (37.9% +/- 6.0%) compared with that of the M500 tablet (58.4% +/- 9.0%) when both were given with food. Food had no significant effect on the bioavailability of the syrup, which averaged 34.0% +/- 8.6% under fasting conditions, although absorption was delayed by food (mean absorption time increased from 2.2 to 3.9 h). This contrasts with the results of previous studies documenting significant increases in tablet bioavailability with food. Despite the lower bioavailability of the syrup, unbound-cefetamet concentrations are expected to remain above the MICs for 90% of the strains tested for susceptible organisms for approximately 10 h of the usual 12-h dosing interval with both syrup and tablet formulations of cefetamet pivoxil given with food. PMID:8109939

[Relative bioavailability study of two oral formulations of mycophenolate mofetil in healthy volunteers].

PubMed

Saavedra S, Iván; Sasso A, Jaime; Quiñones S, Luis; Saavedra B, Mónica; Gaete G, Leonardo; Boza T, Ignacio; Carvajal H, Cristóbal; Soto L, Jorge

2011-07-01

The bioequivalence of different formulations of a same pharmaceutical product must be tested empirically. To evaluate the relative bioavailability for an oralformulation of mycophenolate mofetil (MMF) (Linfonex™) compared to the reference formulation (Cellcept™) to determine the bioequivalence between both formulations. A randomized, crossover, double-blind trial in 22 healthy male volunteers, who received a single oral dose of 1000 mg of Linfonex and Cellcept with a washout period of 10 days. Plasma levels of the drug were determined by high performance liquid chr ornatography. Plasma concentrations were plotted and maximum concentration, area under the plasma concentration versus time between 0 and 12 hours after administration and área under plasma concentration curve versus time after administration between 0 and infinity, were calculated for both products. The active compound, mycophenolic acid, was similarly absorbed in both formulations. No statistically significant differences were found in calculated pharmacokinetic parameters between both formulations. Linfonex™ 500 mg is bioequivalent to Cellcept™ 500 mg.

Enzymatic Preparation of a Homologous Series of Long-Chain 6- O-Acylglucose Esters and Their Evaluation as Emulsifiers.

PubMed

Liang, Min-Yi; Chen, Yongsheng; Banwell, Martin G; Wang, Yong; Lan, Ping

2018-04-18

Sugar fatty acid esters are nonionic surfactants that are widely exploited in the food and cosmetics industries, as well as in the oral care and medical supply fields. Accordingly, new methods for their selective synthesis and the "tuning" of their emulsifying properties are of considerable interest. Herein we report simple and irreversible enzymatic esterifications of d-glucose with seven fatty acid vinyl esters. The foaming and emulsifying effects of the resulting 6- O-acylglucose esters were then evaluated. In accord with expectations, when the length of the alkyl side chain associated with the 6- O-acylglucose esters increases, then their hydrophilic-lipophilic balance (HLB) values decrease, while the stabilities of the derived emulsions improve. In order to maintain good foaming properties, alkyl side chains of at least 9 to 11 carbons in length are required. In the first such assays on 6- O-acylglucose esters, most of those described herein are shown to be nontoxic to the HepG2, MCF-7, LNacp, SW549, and LO-2 cell lines.

Sintering of wax for controlling release from pellets.

PubMed

Singh, Reena; Poddar, S S; Chivate, Amit

2007-09-14

The purpose of the present study was to investigate incorporation of hydrophobic (ie, waxy) material into pellets using a thermal sintering technique and to evaluate the pellets in vitro for controlled release. Pellets prepared by extrusion-spheronization technology were formulated with a water-soluble drug, microcrystalline cellulose, and carnauba wax. Powdered carnauba wax (4%-20%) prepared by grinding or by emulsification was studied with an attempt to retard the drug release. The inclusion of ground or emulsified carnauba wax did not sustain the release of theophylline for more than 3 hours. Matrix pellets of theophylline prepared with various concentrations of carnauba wax were sintered thermally at various times and temperatures. In vitro drug release profiles indicated an increase in drug release retardation with increasing carnauba wax concentration. Pellets prepared with ground wax showed a higher standard deviation than did those prepared with emulsified wax. There was incomplete release at the end of 12 hours for pellets prepared with 20% ground or emulsified wax. The sintering temperature and duration were optimized to allow for a sustained release lasting at least 12 hours. The optimized temperature and duration were found to be 100 degrees C and 140 seconds, respectively. The sintered pellets had a higher hydrophobicity than did the unsintered pellets. Scanning electron micrographs indicated that the carnauba wax moved internally, thereby increasing the surface area of wax within the pellets.

Emulsifier-free emulsion polymerization produces highly charged, monodisperse particles for near infrared photonic crystals.

PubMed

Reese, Chad E; Asher, Sanford A

2002-04-01

We have developed emulsifier-free, emulsion polymerization recipes for the synthesis of highly charged, monodisperse latex particles of diameters between 500 and 1100 nm. These latexes consist of poly[styrene-(co-2-hydroxyethyl methacrylate)] spherical particles whose surfaces are functionalized with sulfate and carboxylic acid groups. These highly charged, monodisperse particles readily self-assemble into robust, three-dimensionally ordered crystalline colloidal array photonic crystals that Bragg diffract light in the near infrared spectral region. By altering the particle number density, the diffraction wavelength can be tuned from approximately 1000 to approximately 4000 nm.

Solubility of ocular therapeutic agents in self-emulsifying oils. I. Self-emulsifying oils for ocular drug delivery: solubility of indomethacin, aciclovir and hydrocortisone.

PubMed

Czajkowska-Kośnik, Anna; Sznitowska, Małgorzata

2009-01-01

Self-emulsifying drug delivery systems (SEDDS) were prepared by dissolving Cremophor EL, Tween 20, Tween 80 and Span 80 (1% or 5%) in oils (Miglyol 812 or castor oil). Solubilities of three ophthalmic drugs, namely aciclovir, hydrocortisone and indomethacin were determined in these systems. In addition, the effect of a small amount of water (0.5% and 2%) on solubilization properties of the systems was estimated. Of the three substances, indomethacin showed the best solubility in Miglyol while aciclovir was practically insoluble in this oil. The surfactants usually increased drug solubility in the oily phase. Only Tween 20 was found to decrease the solubility of aciclovir and hydrocortisone in Miglyol. Addition of a small amount of water to the oil/surfactant system increased solubility of hydrocortisone, but not of indomethacin. The results of the current study may be utilized to design a suitable composition of SEDDS and allow continuation of research on this type of drug carriers.

A Comparison between Use of Spray and Freeze Drying Techniques for Preparation of Solid Self-Microemulsifying Formulation of Valsartan and In Vitro and In Vivo Evaluation

PubMed Central

Singh, Sanjay Kumar; Vuddanda, Parameswara Rao; Singh, Sanjay; Srivastava, Anand Kumar

2013-01-01

The objective of the present study was to develop self micro emulsifying formulation (SMEF) of valsartan to improve its oral bioavailability. The formulations were screened on the basis of solubility, stability, emulsification efficiency, particle size and zeta potential. The optimized liquid SMEF contains valsartan (20% w/w), Capmul MCM C8 (16% w/w), Tween 80 (42.66% w/w) and PEG 400 (21.33% w/w) as drug, oil, surfactant and co-surfactant, respectively. Further, Liquid SMEF was adsorbed on Aerosol 200 by spray and freeze drying methods in the ratio of 2 : 1 and transformed into free flowing powder. Both the optimized liquid and solid SMEF had the particle size <200 nm with rapid reconstitution properties. Both drying methods are equally capable for producing stable solid SMEF and immediate release of drug in in vitro and in vivo conditions. However, the solid SMEF produced by spray drying method showed high flowability and compressibility. The solid state characterization employing the FTIR, DSC and XRD studies indicated insignificant interaction of drug with lipid and adsorbed excipient. The relative bioavailability of solid SMEF was approximately 1.5 to 3.0 folds higher than marketed formulation and pure drug. Thus, the developed solid SMEF illustrates an alternative delivery of valsartan as compared to existing formulations with improved bioavailability. PMID:23971048

High drug loading self-microemulsifying/micelle formulation: design by high-throughput formulation screening system and in vivo evaluation.

PubMed

Sakai, Kenichi; Obata, Kouki; Yoshikawa, Mayumi; Takano, Ryusuke; Shibata, Masaki; Maeda, Hiroyuki; Mizutani, Akihiko; Terada, Katsuhide

2012-10-01

To design a high drug loading formulation of self-microemulsifying/micelle system. A poorly-soluble model drug (CH5137291), 8 hydrophilic surfactants (HS), 10 lipophilic surfactants (LS), 5 oils, and PEG400 were used. A high loading formulation was designed by a following stepwise approach using a high-throughput formulation screening (HTFS) system: (1) an oil/solvent was selected by solubility of the drug; (2) a suitable HS for highly loading was selected by the screenings of emulsion/micelle size and phase stability in binary systems (HS, oil/solvent) with increasing loading levels; (3) a LS that formed a broad SMEDDS/micelle area on a phase diagram containing the HS and oil/solvent was selected by the same screenings; (4) an optimized formulation was selected by evaluating the loading capacity of the crystalline drug. Aqueous solubility behavior and oral absorption (Beagle dog) of the optimized formulation were compared with conventional formulations (jet-milled, PEG400). As an optimized formulation, d-α-tocopheryl polyoxyethylene 1000 succinic ester: PEG400 = 8:2 was selected, and achieved the target loading level (200 mg/mL). The formulation formed fine emulsion/micelle (49.1 nm), and generated and maintained a supersaturated state at a higher level compared with the conventional formulations. In the oral absorption test, the area under the plasma concentration-time curve of the optimized formulation was 16.5-fold higher than that of the jet-milled formulation. The high loading formulation designed by the stepwise approach using the HTFS system improved the oral absorption of the poorly-soluble model drug.

Self-emulsifying drug delivery systems (SEDDS): Proof-of-concept how to make them mucoadhesive.

PubMed

Leonaviciute, Gintare; Adamovic, Nada Trivic; Lam, Hung Thanh; Rohrer, Julia; Partenhauser, Alexandra; Bernkop-Schnürch, Andreas

2017-03-01

The objective of this study was to provide a proof-of-concept that self-emulsifying drug delivery systems can be made mucoadhesive by the incorporation of hydrophobic mucoadhesive polymers. In order to obtain such a hydrophobic mucoadhesive polymer, Eudragit® S100 was thiolated by covalent attachment of cysteamine. After determination of the thiol group content, in vitro mucoadhesion studies (rotating cylinder and rheological measurements) were performed. Then, synthesized conjugate was incorporated into self-emulsifying drug delivery systems (SEDDS) and their toxic potential as well as that of unmodified and thiolated Eudragit® S100 was examined on Caco-2 cell line. Lastly, the mucoadhesiveness of developed SEDDS on porcine intestinal mucosa was determined. Generated thiolated Eudragit® S100 displaying 235±14μmol of free thiol groups and 878±101μmol of disulfide bonds per gram polymer showed a great improvement in both: dynamic viscosity with mucus and adhesion time on mucosal tissue compared to the unmodified polymer. Resazurin assay revealed that unmodified and thiolated polymers and also SEDDS dispersions were non-toxic over Caco-2 cells. Furthermore, the incorporation of 1.5% (w/w) of such thiomer into SEDDS led to remarkably improved mucoadhesiveness. Blank SEDDS were completely removed from the mucosa within 15min, whereas >60% of SEDDS containing thiolated Eudragit® S100 were still attached to it. These results provide evidence that SEDDS can be made mucoadhesive by the incorporation of hydrophobic mucoadhesive polymers. Copyright © 2016 Elsevier B.V. All rights reserved.

[Comparison of dissolution profile and plasma concentration-time profile of the thalidomide formulations made by Japanese, Mexican and British companies].

PubMed

Fujita, Yukiyoshi; Yamamoto, Koujirou; Aomori, Tohru; Murakami, Hirokazu; Horiuchi, Ryuya

2008-10-01

Thalidomide is an important advance in the treatment of multiple myeloma. In Japan thalidomide is now on the approval step for the treatment of multiple myeloma. The drug has some bothersome side effects such as defect of organogenesis, neuropathy, constipation and fatigue, but is likely more effective than standard chemotherapy and is changing multiple myeloma treatment. At this moment, Japanese patients must import the thalidomide preparations from Mexico, Britain and elsewhere, but after approval, they patients will be able to get the new Japanese thalidomide capsules. In order to determine appropriate amounts of Japanese thalidomide capsules in the treatment of multiple myeloma, we compared the dissolution profile and plasma thalidomide concentrations of Japanese and British capsules and Mexican tablets. The dissolution test was performed according to the Japanese and the United States Pharmacopoeia. The pharmacokinetic data for Japanese capsules were obtained from the clinical trial in Japanese subjects and compared with those data published for other formulations. The dissolution rate of the Japanese capsule was the fastest, followed by British and Mexican formulations. The pharmacokinetic profiles of Japanese and British capsules were similar, while the 100 mg Japanese thalidomide capsule demonstrated a 1.6-fold higher maximum plasma concentration than the 200 mg Mexican thalidomide tablet (1.7 vs. 1.1 microg/ml), greatly shortened t(max) (4.5 vs. 6.2 h), and the apparent half life was only one-third of the Mexican tablet (4.8 vs. 13.5 h). A comparison of the dissolution and the pharmacokinetic absorption profiles demonstrated a rank-order correlation. Physicians and pharmacists should be aware of the probable alteration in plasma thalidomide concentration when switching to the Japanese capsule, especially from the Mexican tablet, and should monitor clinical response carefully.

Comparative bioavailability of two oral formulations of ketorolac tromethamine: Dolac and Exodol.

PubMed

Flores-Murrieta, F J; Granados-Soto, V; Castañeda-Hernández, G; Herrera, J E; Hong, E

1994-03-01

The bioavailability of ketorolac after administration of two oral formulations containing 10 mg of ketorolac tromethamine, Exodol and Dolac, to 12 healthy Mexican volunteers was compared. Subjects received both formulations according to a randomized crossover design and blood samples were drawn at selected times during 24 h. Ketorolac plasma concentrations were determined by HPLC and individual plasma-concentration-against-time curves were constructed. Maximal plasma concentration and AUC0-24 values were compared by analysis of variance followed by Westlake's confidence interval test. 90% confidence limits ranged from 80 to 125% for Cmax and from 85 to 118% for AUC0-24. It is concluded that the two assayed formulations are bioequivalent.

[Functional properties and protein concentrate of Pigeon pea (Cajanus cajan (I.) Millsp) flour].

PubMed

Mizubuti, I Y; Biondo Júnior, O; Souza, L W; da Silva, R S; Ida, E I

2000-09-01

The objective of this investigation was to study the functional properties of Pigeon pea (Cajanus cajan (L.) Millsp) flour and protein concentrate. The solubility of both samples were superior than 70% at pH above 6.7 and below 3.5. The water and oil absorption were 1.2 and 1.07 ml/g of sample and 0.87 and 1.73 ml/g of flour and protein concentrate samples, respectively. The minimum concentration of flour and protein concentrate needed for gelation was 20% and 12%, respectively. The emulsifying capacity of flour and concentrate was 129.35 g and 191.66 g oil/g of protein and the emulsion stability 87.50 and 97.97%, respectively, after 780 minutes. The foam capacity and stability of flour foam were 36.0% and 18.61, while of the concentrate were 44.70% and 78.97% after 90 minutes. These properties indicate that the flour as well as the concentrate could have application in various food systems.

Rapidly disintegrating vagina retentive cream suppositories of progesterone: development, patient satisfaction and in vitro/in vivo studies.

PubMed

Bendas, Ehab Rasmy; Basalious, Emad B

2016-01-01

Our objective was to develop novel vagina retentive cream suppositories (VRCS) of progesterone having rapid disintegration and good vaginal retention. VRCS of progesterone were prepared using oil in water (o/w) emulsion of mineral oil or theobroma oil in hard fat and compared with conventional vaginal suppositories (CVS) prepared by hard fat. VRCS formulations were tested for content uniformity, disintegration, melting range, in vitro release and stability studies. The most stable formulation (VRCS I) was subjected to scaling-up manufacturing and patients' satisfaction test. The rapid disintegration, good retentive properties are applicable through the inclusion of emulsified theobroma oil rather than hydrophilic surfactant into the hard fat bases. The release profile of progesterone from VRCS I showed a biphasic pattern due to the formation of progesterone reservoir in the emulsified theobroma oil. All volunteers involved in patients' satisfaction test showed high satisfactory response to the tested formulation (VRCS). The in vivo pharmacokinetic study suggests that VRCS of progesterone provided higher rate and extent of absorption compared to hard fat based suppositories. Our results proposed that emulsified theobroma oil could be promising to solve the problems of poor patients' satisfaction and variability of drug absorption associated with hard fat suppositories.

Mechanism research on starting residual oil migration in ASP flooding with different Alkali concentration

NASA Astrophysics Data System (ADS)

Xia, Huifen; Pan, Junliang; Niu, Lijuan; Xu, Tianhan

2018-02-01

The results illustrate that under the condition of the same viscosity of ASP system, oil displacement efficiency is different while the ASP system with different alkali concentration has the same order of magnitude as the interfacial tension of oil. In this paper, the microscopic simulation visual model is used to study the mechanism of starting migration of residual oil by doing ASP flooding experiments with different alkali concentration. The results indicate that the migration of residual oil is different from that in the ASP systems with different alkali concentration. ASP system with high alkali concentration can start the migration by means of emulsifying residual oil into oil droplets and oil threads, on this account, increasing the alkali concentration can make the recovery degree of ASP system higher, which will finally be beneficial to the oil recovery.

Polar Quassinoids in Standardized Eurycoma longifolia Extract Formulated into a Lipid-Based Solid Dispersion to Improve Rat Sperm Count.

PubMed

Ma, Hai-Qiu; Ebrahimi, Forough; Low, Bin-Seng; Khan, Nurzalina Abdul Karim; Chan, Kit-Lam

2017-12-01

Eurycoma longifolia Jack is popularly sought in Southeast Asian countries for traditional remedies to improve sexual performance and fertility. 13α(21)-Epoxyeurycomanone and eurycomanone, two major quassinoids in a root extract (TAF2) were reported to improve rat spermatogenesis and fertility. Unfortunately, these quassinoids possess low bioavailability because of high aqueous solubility and low lipid membrane permeability. Often, other possible barriers may be P-glycoprotein (P-gp) efflux in the gut and presystemic hepatic metabolism. The present study attempted to solve these problems by formulating a lipid-based solid dispersion (TAF2-SD) of optimized mixture of TAF2 and emulsifiers, which was then orally administered to rats prior to sperm count analysis. The TAF2-SD-treated rats showed significantly twofold (p < 0.001) and fourfold (p < 0.001) higher sperm count than did TAF2-treated and vehicle-treated (control) rats, respectively. The study also demonstrated no significant in vitro ileal absorption changes of the quassinoids by P-gp efflux inhibitors and concentration change or secondary metabolite formation upon in vitro incubation with rat liver homogenates, suggesting that P-gp-mediated efflux and presystemic metabolism were not limiting their bioavailability. Further study on orally TAF2-treated rats confirmed that the area under the curve and bioavailability curve of each quassinoid in the absence and presence of ketoconazole were unchanged. Copyright © 2017 John Wiley & Sons, Ltd. Copyright © 2017 John Wiley & Sons, Ltd.

Pharmaceutical study of suppository formulations for improved in vivo kinetics of rifampicin.

PubMed

Taki, Hisashi; Ogawa, Kenji; Nikai, Toshiaki

2008-06-01

To study rifampicin (RFP) suppository formulations that were prepared by adding an absorption promoter and a holding agent to conventional rifampicin suppositories in order to achieve higher blood drug levels. The subjects were 3 healthy volunteers who gave consent to participate in this study. Suppository formulations were prepared by adding sodium caprinate (the absorption promoter) to 600 mg, 750 mg, or 900 mg of RFP at about 3% of the suppository weight and sodium alginate (the holding agent) at 25% of the RFP content. Serum samples collected at 2, 6, and 10 hours after insertion of a suppository were subjected to RFP concentration analysis. In subject no. 1, the maximum concentration was 0.807 Lg/ml, 1.093 microg/ml, and 1.291 microg/ml after administration of a suppository containing 600 mg, 750 mg, or 900 mg of RFP, respectively. Since an injectable RFP formulation has not been approved in Japan, formulation studies of RFP suppositories are important to achieve a better clinical response and to prevent the development of resistance. The present formulation that delivered a blood concentration of RFP considerably higher than 1 microg/ml was considered to have therapeutic potential. Its clinical utility will be examined in further formulation studies.

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.

Conference report: formulating better medicines for children: 4th European Paediatric Formulation Initiative conference.

PubMed

Walsh, Jennifer; Mills, Simon

2013-01-01

The fourth annual European Paediatric Formulation Initiative (EuPFI) conference on Formulating Better Medicines for Children was held on 19-20 September 2012 at the Institute of Molecular Genetics Congress Centre, Prague, Czech Republic. The 2-day conference concentrated on the latest advances, challenges and opportunities for developing medicinal products and administration devices for pediatric use, both from European and US perspectives. It was aimed specifically at providing exposure to emerging practical applications, and for illustrating remedies utilized by pediatric drug-development teams to overcome hurdles faced in developing medicines for pediatric patients. The conference format included plenary talks, focus sessions on each of the EuPFI work streams (extemporaneous preparations, excipients, pediatric administration devices, taste masking and taste assessment, age-appropriate formulations), case studies, soapbox sessions and a parallel poster display. This conference report summarizes the keynote lectures and also gives a flavor of other presentations and posters from the conference.

Preparation of Nanoemulsions by Premix Membrane Emulsification: Which Parameters Have a Significant Influence on the Resulting Particle Size?

PubMed

Gehrmann, Sandra; Bunjes, Heike

2017-08-01

Oil-in-water emulsions with particle sizes smaller than 200 nm are interesting carrier systems for poorly water-soluble drugs. Such emulsions can be produced by premix membrane emulsification. In this study, it was systematically investigated which process and formulation parameters have a strong influence on the resulting quality of a triglyceride emulsion. The influence of the pre-emulsion quality and the emulsifier concentration was examined. Also a design of experiments (DoE) approach was carried out: variables included were emulsifier (poloxamer 188, Tween 80, and sucrose laurate [SL]), flow rate, cycle number, and membrane material (polyester, nylon, cellulose acetate, and aluminum oxide; pore sizes, 200 nm), and responses were d 50 value and span for particle size and distribution width. The quality of the pre-emulsion had no influence on the quality of the nanoemulsion after 5 extrusion cycles. The DoE evaluation indicated that an increase in flow rate was of minor importance, whereas an increase in cycle number had a strong impact on the decrease of particle size. The very hydrophilic alumina membrane in combination with the emulsifier which caused the lowest interfacial tension (SL) was the most suitable combination. However, in general, the favorable emulsifier was membrane dependent. Even smaller particle sizes (∼100 nm) could be achieved by using an alumina membrane with smaller pore sizes (100 nm). Copyright © 2017 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved.

Concentrated Protein Body Product Derived from Rice Endosperm as an Oral Tolerogen for Allergen-Specific Immunotherapy—A New Mucosal Vaccine Formulation against Japanese Cedar Pollen Allergy

PubMed Central

Wakasa, Yuhya; Takagi, Hidenori; Watanabe, Nobumasa; Kitamura, Noriko; Fujiwara, Yoshihiro; Ogo, Yuko; Hayashi, Shimpei; Yang, Lijun; Ohta, Masaru; Thet Tin, Wai Wai; Sekikawa, Kenji; Takano, Makoto; Ozawa, Kenjirou; Hiroi, Takachika; Takaiwa, Fumio

2015-01-01

The endoplasmic reticulum-derived type-I protein body (PB-I) from rice endosperm cells is an ideal candidate formulation for the oral delivery of bioencapsulated peptides as tolerogens for allergen-specific immunotherapy. In the present study, PBs containing the deconstructed Japanese cedar pollen allergens Cryptomeria japonica 1 (Cry j 1) and Cry j 2 were concentrated by treatment with thermostable α-amylase at 90°C to remove the starch from milled rice powder, which resulted in a 12.5-fold reduction of dry weight compared to the starting material. The modified Cry j 1 and Cry j 2 antigens in this concentrated PB product were more resistant to enzymatic digestion than those in the milled seed powder despite the absence of intact cell wall and starch, and remained stable for at least 10 months at room temperature without detectable loss or degradation. The high resistance of these allergens could be attributed to changes in protein physicochemical properties induced by the high temperature concentration process, as suggested by the decreased solubility of the antigens and seed proteins in PBs in step-wise-extraction experiments. Confocal microscopy showed that the morphology of antigen-containing PB-Is was preserved in the concentrated PB product. The concentrated PB product induced specific immune tolerance against Cry j 1 and Cry j 2 in mice when orally administered, supporting its potential use as a novel oral tolerogen formulation. PMID:25774686

Solid self-nanoemulsifying delivery systems as a platform technology for formulation of poorly soluble drugs.

PubMed

Bansal, Tripta; Mustafa, Gulam; Khan, Zeenat I; Ahmad, Farhaan J; Khar, Roop K; Talegaonkar, Sushama

2008-01-01

New drug discovery programs produce molecules with poor physico-chemical properties, making delivery of these molecules at the right proportion into the body a big challenge to the formulation scientist. The various options available to overcome the hurdle include solvent precipitation, micronisation/nanonization using high-pressure homogenization or jet milling, salt formation, use of microspheres, solid dispersions, cogrinding, complexation, and many others. Self-nanoemulsifying systems (SNES) form one of the most popular and commercially viable approaches for delivery of poorly soluble drugs exhibiting dissolution rate limited absorption, especially those belonging to the Biopharmaceutics Classification System II/IV. SNES are essentially an isotropic blend of oils, surfactants, and/or cosolvents that emulsify spontaneously to produce oil in water nanoemulsion when introduced into aqueous phase under gentle agitation. Conventional SNES consist of liquid forms filled in hard or soft gelatin capsules, which are least preferred due to leaching and leakage phenomenon, interaction with capsule shell components, handling difficulties, machinability, and stability problems. Solidification of these liquid systems to yield solid self-nanoemulsifying systems (SSNES) offer a possible solution to the mentioned complications, and that is why these systems have attracted wide attention. Other than the advantages and wide application of SSNEDS, the present paper focuses on formulation considerations, selection, and function of solidifying excipients; techniques of preparation; and case studies of drugs selected from different therapeutic categories. Developments in the techniques for in vitro evaluation of SSNEDS have also been discussed.

Composition analysis and material characterization of an emulsifying extracellular polysaccharide (EPS) produced by Bacillus megaterium RB-05: a hydrodynamic sediment-attached isolate of freshwater origin.

PubMed

Chowdhury, S R; Manna, S; Saha, P; Basak, R K; Sen, R; Roy, D; Adhikari, B

2011-12-01

This work was aimed to isolate, purify and characterize an extracellular polysaccharide (EPS) produced by a freshwater dynamic sediment-attached micro-organism, Bacillus megaterium RB-05, and study its emulsifying potential in different hydrocarbon media. Bacillus megaterium RB-05 was found to produce EPSs in glucose mineral salts medium, and maximum yield (0.864 g l(-1) ) was achieved after 24-h incubation. The recovery rates of the polysaccharide material by ion-exchange and gel filtration chromatography were around 67 and 93%, respectively. As evident from HPLC and FT-IR analyses, the polysaccharide was found to be a heteropolymer-containing glucose, galactose, mannose, arabinose, fucose and N-acetyl glucosamine. Different oligosaccharide combinations namely hexose(3), hexose(4), hexose(5) deoxyhexose(1) and hexose(5) deoxyhexose(1) pentose(3) were obtained after partial hydrolysis of the polymer using MALDI-ToF-MS. The polysaccharide with an average molecular weight of 170 kDa and thermal stability up to 180°C showed pseudoplastic rheology and significant emulsifying activity in hydrocarbon media. Isolated polysaccharide was found to be of high molecular weight and thermally stable. The purified EPS fraction was composed of hexose, pentose and deoxyhexose sugar residues, which is a rare combination for bacterial polysaccharides. Emulsifying property was either better or comparable to that of other commercially available natural gums and polysaccharides. This is probably one of the few reports about characterizing an emulsifying EPS produced by a freshwater sediment-attached bacterium. The results of this study contribute to understand the influence of chemical composition and material properties of a new microbial polysaccharide on its application in industrial biotechnology. Furthermore, this work reconfirms freshwater dynamic sediment as a potential habitat for bioprospecting extracellular polymer-producing bacteria. This study will improve our knowledge on

Factors Contributing to the Off-Target Transport of Pyrethroid Insecticides From Urban Surfaces

PubMed Central

Jorgenson, Brant C.; Wissel-Tyson, Christopher; Young, Thomas M.

2013-01-01

Pyrethroid insecticides used in an urban and suburban context have been found in urban creek sediments and associated with toxicity in aquatic bioassays. The objectives of this study were to evaluate the main factors contributing to the off-target transport of pyrethroid insecticides from surfaces typical of residential landscapes. Controlled rainfall simulations over concrete, bare soil, and turf plots treated individually with pyrethroid insecticides in a suspension concentrate, an emulsifiable concentrate, or a granule formulation were conducted at different rainfall intensities and different product set-time intervals. Pyrethroid mass washoff varied by several orders of magnitude between experimental treatments. Suspension concentrate product application to concrete yielded significantly greater washoff than any other treatment; granule product application to turf yielded the least washoff. Fractional losses at 10 L of runoff ranged from 25.9% to 0.011% of pyrethroid mass applied and 10 L nominal mass losses ranged from 3,970 to 0.18 μg. Mass washoff depended principally on formulation and surface type combination and to a lesser degree set-time interval and rainfall intensity. Treatment effects were analyzed by ANOVA on main factors of formulation, surface type, and set time. Factor effects were not purely additive; a significant interaction between formulation and surface type was noted. PMID:22784034

Drug utilization review of potassium chloride injection formulations available in a private hospital in kuching, sarawak, malaysia.

PubMed

Melissa, Mohammad Hirman; Azmi, Sarriff

2013-07-01

The concentrated potassium chloride injection is a high-alert medication and replacing it with a pre-mixed formulation can reduce the risks associated with its use. The aim of this study was to determine the clinical characteristics of patients receiving different potassium chloride formulations available at a private institution. The study also assessed the effectiveness and safety of pre-mixed formulations in the correction of hypokalaemia. This was a retrospective observational study consisting of 296 cases using concentrated and pre-mixed potassium chloride injections in 2011 in a private hospital in Kuching, Sarawak, Malaysia. There were 135 (45.6%) cases that received concentrated potassium chloride, and 161 (54.4%) cases that received pre-mixed formulations. The patients' clinical characteristics that were significantly related to the utilization of the different formulations were diagnosis (P < 0.001), potassium serum blood concentration (P < 0.05), and fluid overload risk (P < 0.05). The difference observed for the cases that achieved or maintained normokalaemia was statistically insignificant (P = 0.172). Infusion-related adverse effects were seen more in pre-mixes compared to concentrated formulations (6.8% versus 2.2%, P < 0.05). This study provides insight into the utilization of potassium chloride injections at this specific institution. The results support current recommendations to use pre-mixed formulations whenever possible.

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.

Preparation of rich handles soft cellulosic fabric using amino silicone based softener. Part-I: Surface smoothness and softness properties.

PubMed

Zia, Khalid Mahmood; Tabassum, Shazia; Barkaat-ul-Hasin, Syed; Zuber, Mohammad; Jamil, Tahir; Jamal, Muhammad Asghar

2011-04-01

A series of amino silicone based softeners with different emulsifiers were prepared and adsorbed onto the surfaces of cotton and blends of cotton/polyester fabrics. Factors affecting the performance properties of the finished substrate such as post-treatment with amino functional silicone based softener varying different emulsifiers in their formulations and its concentration on different processed fabrics were studied. Fixation of the amino-functional silicone softener onto/or within the cellulose structure is accompanied by the formation of semi-inter-penetrated network structure thereby enhancing both the extent of crosslinking and networking as well as providing very high softness. The results of the experiments indicate that the amino silicone can form a hydrophobic film on both cotton and blends of cotton/polyester fabrics and its coating reduces the surface roughness significantly. Furthermore, the roughness becomes lesser with an increase in the applied strength of amino silicone based softener. Copyright © 2011 Elsevier B.V. All rights reserved.

Rheological behavior, emulsifying properties and structural characterization of phosphorylated fish gelatin.

PubMed

Huang, Tao; Tu, Zong-Cai; Shangguan, Xinchen; Wang, Hui; Sha, Xiaomei; Bansal, Nidhi

2018-04-25

Rheological, microstructural and emulsifying properties of fish gelatin phosphorylated using sodium trimetaphosphate (STMP) were studied. Phosphorylation was carried out at 50 °C for 0, 0.5, 1 or 2 h. Rheological behaviors indicated that phosphorylation decreased gelation rate constant (k gel ) and apparent viscosity of gelatin solutions. Phosphorylation time was inversely proportional to tan δ; gelling and melting points of fish gelatin gels; however gel properties could be improved by short time of phosphorylation. Scanning electron microscopy and atomic force microscopy revealed that longer time of phosphorylation resulted in looser gel network with more aggregation. Longer phosphorylation time could stabilize fish gelatin emulsions, and endowed emulsions with smaller particle size and lower coefficient viscosity, but higher ζ-potential values. These results suggested that phosphorylation could be applied to obtain fish gelatin with varying functional properties suitable for numerous industrial applications. Copyright © 2017 Elsevier Ltd. All rights reserved.

Whey protein/polysaccharide-stabilized emulsions: Effect of polymer type and pH on release and topical delivery of salicylic acid.

PubMed

Combrinck, Johann; Otto, Anja; du Plessis, Jeanetta

2014-06-01

Emulsions are widely used as topical formulations in the pharmaceutical and cosmetic industries. They are thermodynamically unstable and require emulsifiers for stabilization. Studies have indicated that emulsifiers could affect topical delivery of actives, and this study was therefore designed to investigate the effects of different polymers, applied as emulsifiers, as well as the effects of pH on the release and topical delivery of the active. O/w emulsions were prepared by the layer-by-layer technique, with whey protein forming the first layer around the oil droplets, while either chitosan or carrageenan was subsequently adsorbed to the protein at the interface. Additionally, the emulsions were prepared at three different pH values to introduce different charges to the polymers. The active ingredient, salicylic acid, was incorporated into the oil phase of the emulsions. Physical characterization of the resulting formulations, i.e., droplet size, zeta potential, stability, and turbidity in the water phase, was performed. Release studies were conducted, after which skin absorption studies were performed on the five most stable emulsions, by using Franz type diffusion cells and utilizing human, abdominal skin membranes. It was found that an increase in emulsion droplet charge could negatively affect the release of salicylic acid from these formulations. Contrary, positively charged emulsion droplets were found to enhance dermal and transdermal delivery of salicylic acid from emulsions. It was hypothesized that electrostatic complex formation between the emulsifier and salicylic acid could affect its release, whereas electrostatic interaction between the emulsion droplets and skin could influence dermal/transdermal delivery of the active.

Larvicidal effects of a neem (Azadirachta indica) oil formulation on the malaria vector Anopheles gambiae

PubMed Central

Okumu, Fredros O; Knols, Bart GJ; Fillinger, Ulrike

2007-01-01

Background Larviciding is a key strategy used in many vector control programmes around the world. Costs could be reduced if larvicides could be manufactured locally. The potential of natural products as larvicides against the main African malaria vector, Anopheles gambiae s.s was evaluated. Methods To assess the larvicidal efficacy of a neem (Azadirachta indica) oil formulation (azadirachtin content of 0.03% w/v) on An. gambiae s.s., larvae were exposed as third and fourth instars to a normal diet supplemented with the neem oil formulations in different concentrations. A control group of larvae was exposed to a corn oil formulation in similar concentrations. Results Neem oil had an LC50 value of 11 ppm after 8 days, which was nearly five times more toxic than the corn oil formulation. Adult emergence was inhibited by 50% at a concentration of 6 ppm. Significant reductions on growth indices and pupation, besides prolonged larval periods, were observed at neem oil concentrations above 8 ppm. The corn oil formulation, in contrast, produced no growth disruption within the tested range of concentrations. Conclusion Neem oil has good larvicidal properties for An. gambiae s.s. and suppresses successful adult emergence at very low concentrations. Considering the wide distribution and availability of this tree and its products along the East African coast, this may prove a readily available and cheap alternative to conventional larvicides. PMID:17519000

Larvicidal effects of a neem (Azadirachta indica) oil formulation on the malaria vector Anopheles gambiae.

PubMed

Okumu, Fredros O; Knols, Bart G J; Fillinger, Ulrike

2007-05-22

Larviciding is a key strategy used in many vector control programmes around the world. Costs could be reduced if larvicides could be manufactured locally. The potential of natural products as larvicides against the main African malaria vector, Anopheles gambiae s.s was evaluated. To assess the larvicidal efficacy of a neem (Azadirachta indica) oil formulation (azadirachtin content of 0.03% w/v) on An. gambiae s.s., larvae were exposed as third and fourth instars to a normal diet supplemented with the neem oil formulations in different concentrations. A control group of larvae was exposed to a corn oil formulation in similar concentrations. Neem oil had an LC50 value of 11 ppm after 8 days, which was nearly five times more toxic than the corn oil formulation. Adult emergence was inhibited by 50% at a concentration of 6 ppm. Significant reductions on growth indices and pupation, besides prolonged larval periods, were observed at neem oil concentrations above 8 ppm. The corn oil formulation, in contrast, produced no growth disruption within the tested range of concentrations. Neem oil has good larvicidal properties for An. gambiae s.s. and suppresses successful adult emergence at very low concentrations. Considering the wide distribution and availability of this tree and its products along the East African coast, this may prove a readily available and cheap alternative to conventional larvicides.

Formulation of medicines for children

PubMed Central

Nunn, Tony; Williams, Julie

2005-01-01

The development of age-adapted dosage forms and taste-masking of bitter-tasting drugs administered orally for children, are formidable challenges for formulation scientists. Childhood is a period of maturation requiring knowledge of developmental pharmacology to establish dose but the ability of the child to manage different dosage forms and devices also changes. Paediatric formulations must allow accurate administration of the dose to children of widely varying age and weight. Whilst the oral route will be preferred for long term use and the intravenous route for the acutely ill, many of the dosage forms designed for adults, such as oro-dispersible tablets, buccal gels and transdermal patches, would also benefit children if they contained an appropriate paediatric dose. The age at which children can swallow conventional tablets is of great importance for their safety. Liquid medicines are usually recommended for infants and younger dhildren so the ability to mask unpleasant taste with sweeteners and flavours is crucial. More sophisticated formulations such as granules and oro-dispersible tablets may be required but there will be limitations on choice and concentration of excipients. There are many gaps in our knowledge about paediatric formulations and many challenges for the industry if suitable preparations are to be available for all ranges. A CHMP points to consider document is soon to be released. More research and clinical feedback are important because a formulation with poor acceptability may affect compliance, prescribing practice and ultimately commercial viability. PMID:15948931

Bioaccessibility and Cellular Uptake of β-Carotene Encapsulated in Model O/W Emulsions: Influence of Initial Droplet Size and Emulsifiers

PubMed Central

Kelly, Alan L.

2017-01-01

The effects of the initial emulsion structure (droplet size and emulsifier) on the properties of β-carotene-loaded emulsions and the bioavailability of β-carotene after passing through simulated gastrointestinal tract (GIT) digestion were investigated. Exposure to GIT significantly changed the droplet size, surface charge and composition of all emulsions, and these changes were dependent on their initial droplet size and the emulsifiers used. Whey protein isolate (WPI)-stabilized emulsion showed the highest β-carotene bioaccessibility, while sodium caseinate (SCN)-stabilized emulsion showed the highest cellular uptake of β-carotene. The bioavailability of emulsion-encapsulated β-carotene based on the results of bioaccessibility and cellular uptake showed the same order with the results of cellular uptake being SCN > TW80 > WPI. An inconsistency between the results of bioaccessibility and bioavailability was observed, indicating that the cellular uptake assay is necessary for a reliable evaluation of the bioavailability of emulsion-encapsulated compounds. The findings in this study contribute to a better understanding of the correlation between emulsion structure and the digestive fate of emulsion-encapsulated nutrients, which make it possible to achieve controlled or potential targeted delivery of nutrients by designing the structure of emulsion-based carriers. PMID:28930195

Preparation and Evaluation of Multiple Nanoemulsions Containing Gadolinium (III) Chelate as a Potential Magnetic Resonance Imaging (MRI) Contrast Agent.

PubMed

Sigward, Estelle; Corvis, Yohann; Doan, Bich-Thuy; Kindsiko, Kadri; Seguin, Johanne; Scherman, Daniel; Brossard, Denis; Mignet, Nathalie; Espeau, Philippe; Crauste-Manciet, Sylvie

2015-09-01

The objective was to develop, characterize and assess the potentiality of W1/O/W2 self-emulsifying multiple nanoemulsions to enhance signal/noise ratio for Magnetic Resonance Imaging (MRI). For this purpose, a new formulation, was designed for encapsulation efficiency and stability. Various methods were used to characterize encapsulation efficiency ,in particular calorimetric methods (Differential Scanning Calorimetry (DSC), thermogravimetry analysis) and ultrafiltration. MRI in vitro relaxivities were assessed on loaded DTPA-Gd multiple nanoemulsions. Characterization of the formulation, in particular of encapsulation efficiency was a challenge due to interactions found with ultrafiltration method. Thanks to the specifically developed DSC protocol, we were able to confirm the formation of multiple nanoemulsions, differentiate loaded from unloaded nanoemulsions and measure the encapsulation efficiency which was found to be quite high with a 68% of drug loaded. Relaxivity studies showed that the self-emulsifying W/O/W nanoemulsions were positive contrast agents, exhibiting higher relaxivities than those of the DTPA-Gd solution taken as a reference. New self-emulsifying multiple nanoemulsions that were able to load satisfactory amounts of contrasting agent were successfully developed as potential MRI contrasting agents. A specific DSC protocol was needed to be developed to characterize these complex systems as it would be useful to develop these self-formation formulations.

Changes in secondary structure of gluten proteins due to emulsifiers

NASA Astrophysics Data System (ADS)

Gómez, Analía V.; Ferrer, Evelina G.; Añón, María C.; Puppo, María C.

2013-02-01

Changes in the secondary structure of gluten proteins due to emulsifiers were analyzed by Raman Spectroscopy. The protein folding induced by 0.25% SSL (Sodium Stearoyl Lactylate) (GS0.25, Gluten + 0.25% SSL) included an increase in α-helix conformation and a decrease in β-sheet, turns and random coil. The same behavior, although in a less degree, was observed for 0.5% gluten-DATEM (Diacetyl Tartaric Acid Esters of Monoglycerides) system. The low burial of Tryptophan residues to a more hydrophobic environment and the low percentage area of the C-H stretching band for GS0.25 (Gluten + 0.25% SSL), could be related to the increased in α-helix conformation. This behavior was also confirmed by changes in stretching vibrational modes of disulfide bridges (S-S) and the low exposure of Tyrosine residues. High levels of SSL (0.5% and 1.0%) and DATEM (1.0%) led to more disordered protein structures, with different gluten networks. SSL (1.0%) formed a more disordered and opened gluten matrix than DATEM, the last one being laminar and homogeneous.

Dietary emulsifiers from milk and soybean differently impact adiposity and inflammation in association with modulation of colonic goblet cells in high-fat fed mice.

PubMed

Lecomte, Manon; Couëdelo, Leslie; Meugnier, Emmanuelle; Plaisancié, Pascale; Létisse, Marion; Benoit, Bérengère; Gabert, Laure; Penhoat, Armelle; Durand, Annie; Pineau, Gaëlle; Joffre, Florent; Géloën, Alain; Vaysse, Carole; Laugerette, Fabienne; Michalski, Marie-Caroline

2016-03-01

Enhanced adiposity and metabolic inflammation are major features of obesity that could be impacted by dietary emulsifiers. We investigated in high-fat fed mice the effects of using a new polar lipid (PL) emulsifier from milk (MPL) instead of soybean lecithin (soybean PL [SPL]) on adipose tissue and intestinal mucosa function. Four groups of C57BL6 mice received for 8 wks a low-fat (LF) diet or a high-fat diet devoid of PLs or an high-fat diet including MPL (high-fat-MPL) or SPL (high-fat-SPL). Compared with high-fat diet, high-fat-SPL diet increased white adipose tissue (WAT) mass (p < 0.05), with larger adipocytes (p < 0.05) and increased expression of tumor necrosis factor alpha, monochemoattractant protein-1, LPS-binding protein, and leptin (p < 0.05). This was not observed with high-fat-MPL diet despite similar dietary intakes and increased expression of fatty acid transport protein 4 and microsomal TG transfer protein, involved in lipid absorption, in upper intestine (p < 0.05). High-fat-MPL mice had a lower expression in WAT of cluster of differentiation 68, marker of macrophage infiltration, versus high-fat and high-fat-SPL mice (p < 0.05), and more goblet cells in the colon (p < 0.05). Unlike SPL, MPL in the high-fat diet did not induce WAT hypertrophy and inflammation but increased colonic goblet cells. This supports further clinical exploration of different sources of dietary emulsifiers in the frame of obesity outbreak. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Stability of an alternative extemporaneous captopril fast-dispersing tablet formulation versus an extemporaneous oral liquid formulation.

PubMed

Pabari, Ritesh M; McDermott, Claire; Barlow, James; Ramtoola, Zebunnissa

2012-11-01

Administration of medications to pediatric patients is challenging because many drugs are not commercially available in appropriate dosage formulations and/or strengths. Consequently, these drugs are prepared extemporaneously as oral liquid (OL) formulations using marketed tablets or capsules. In many cases, the stability of these extemporaneous preparations, which may affect their tolerability, has not been documented. An alternative extemporaneous solid formulation, such as a fast-dispersing tablet (FDT), may offer enhanced stability as well as dosing flexibility because it may be administered as an orodispersible tablet or as a reconstituted suspension/solution. Although FDTs are available increasingly as patient-friendly oral dosage formulations, and their simple method of manufacture can be applied to extemporaneous formulations, such applications have not been explored to date. The use of extemporaneous captopril OL formulations in hospitals in Ireland was surveyed, and the stability of the most commonly used captopril formulation (reference) was investigated and compared with that of a newly available extemporaneous FDT formulation. The survey was carried out in 120 hospitals in the Republic of Ireland. The 56-day stability of the most commonly used formulation was compared with that of a newly available extemporaneous captopril FDT preparation. The captopril content of the formulations was measured by high-performance liquid chromatography analysis. Formulations were also monitored for changes in appearance, including color; odor; and pH (OLs only). The survey showed that extemporaneously prepared captopril OLs were extensively used, particularly in specialist children's hospitals. The most commonly used preparation was a xanthan gum-based oral suspension. Analysis of these OL preparations showed the OLs to have been stable up to day 7, but that the captopril concentration decreased to 72% to 84% at day 14 and to 59% to 68% at day 56; this decrease was

Green clay and aloe vera peel-off facial masks: response surface methodology applied to the formulation design.

PubMed

O'Reilly Beringhs, André; Rosa, Julia Macedo; Stulzer, Hellen Karine; Budal, Rosane Maria; Sonaglio, Diva

2013-03-01

This article describes the optimization of a peel-off facial mask formulation. An investigation was carried out on the parameters of the formulation that most affect the desirable characteristics of peel-off facial masks. Cereal alcohol had a significant effect on the drying time at concentrations of 1-12% (w/w). The applicability of the evaluated formulations was influenced by both carbomer (0-2.4%; w/w) and polyvinyl alcohol (PVA; 2.5-17.5%; w/w) content due to their ability to alter the formulation viscosity. Inverse concentrations of carbomer and PVA led to formulations with optimum viscosity for facial application. Film-forming performance was influenced only by the PVA concentration, achieving maximum levels at concentrations of around 11% (w/w). The optimized formulation, determined mathematically, contained 13% (w/w) PVA and 10% (w/w) cereal alcohol with no addition of carbomer. This formulation provided high levels of applicability and film-forming performance, the lowest drying time possible and excellent homogeneity of the green clay particles and aloe vera before and after drying. The preliminary stability study indicated that the optimized formulation is stable under normal storage conditions. The microbiological stability evaluation indicated that the preservative was efficient in terms of avoiding microbial growth. RSM was shown to be a useful statistical tool for the determination of the behavior of different compounds and their concentrations for the responses studied, allowing the investigation of the optimum conditions for the production of green clay and aloe vera peel-off facial masks.

Oral apomorphine delivery from solid lipid nanoparticles with different monostearate emulsifiers: pharmacokinetic and behavioral evaluations.

PubMed

Tsai, Ming-Jun; Huang, Yaw-Bin; Wu, Pao-Chu; Fu, Yaw-Syan; Kao, Yao-Ren; Fang, Jia-You; Tsai, Yi-Hung

2011-02-01

Apomorphine, a dopamine receptor agonist for treating Parkinson's disease, has very poor oral bioavailability (<2%) due to the first-pass effect. The aim of this work was to investigate whether the oral bioavailability and brain regional distribution of apomorphine could be improved by utilizing solid lipid nanoparticles (SLNs). Glyceryl monostearate (GMS) and polyethylene glycol monostearate (PMS) were individually incorporated into SLNs as emulsifiers. It was found that variations in the emulsifiers had profound effects on the physicochemical characteristics. Mean diameters of the GMS and PMS systems were 155 and 63 nm, respectively. More than 90% of the apomorphine was entrapped in the SLNs. The interfacial film was the likely location for most of apomorphine molecules. The PMS system, when incubated in simulated intestinal medium, was found to be more stable in terms of particle size and encapsulation efficiency than the GMS system. Using the GMS and PMS systems to orally administer apomorphine (26 mg/kg) equally enhanced the bioavailability in rats. SLNs showed 12- to 13-fold higher bioavailability than the reference solution. The drug distribution in the striatum, the predominant site of therapeutic action, also increased when using the SLNs. The anti-Parkinsonian activity of apomorphine was evaluated in rats with 6-hydroxydopamine-induced lesions, a model of Parkinson's disease. The contralateral rotation behavior was examined after oral apomorphine delivery. The total number of rotations increased from 20 to 94 and from 20 to 115 when the drug was administered from SLNs containing GMS and PMS, respectively. The experimental results suggest that SLNs may offer a promising strategy for apomorphine delivery via oral ingestion. Copyright © 2010 Wiley-Liss, Inc.

Doxycycline concentration over time after storage in a compounded veterinary preparation.

PubMed

Papich, Mark G; Davidson, Gigi S; Fortier, Lisa A

2013-06-15

To determine the concentration of doxycycline compounded from doxycycline hyclate tablets into liquid formulations for oral administration in veterinary species and stored for 28 days. Evaluation study. Doxycycline hyclate tablets (100 mg) crushed and mixed with a 50:50 mixture of syrup and suspension vehicles for oral administration to produce 3 batches each of 2 doxycycline formulations: 33.3 and 166.7 mg/mL. Formulations were stored, protected from light, at room temperature (22° to 26°C [71.6° to 78.8°F]) and at a controlled cold temperature (refrigerated 2° to 8°C [35.6° to 46.4°F]). Doxycycline was extracted from the formulations, and concentration was measured by high-pressure liquid chromatography on days 0 (date of preparation), 1, 4, 7, 14, 21, and 28. Concentrations were compared with those of a US Pharmacopeial Convention reference standard. Formulation quality at each point was also assessed through color change, formulation consistency, and suspension uniformity. On days 0, 1, 4, and 7, the concentration of each formulation was within 90% to 110% of the reference standard (range, 93% to 109%), which was deemed acceptable. However, doxycycline concentrations had decreased dramatically by day 14 and remained low for the duration of the study period. Doxycycline concentrations on days 14, 21, and 28 were all < 20% (range, 14% to 18%) of the reference standard, and the quality of the formulations decreased as well. No effect of storage temperatures on doxycycline concentration was identified. The concentration of doxycycline, compounded from commercial tablets in the vehicles evaluated to yield doses of 33.3 and 166.7 mg/mL, cannot be assured beyond 7 days.

Bioequivalence of a new cyclosporine a formulation to Neoral.

PubMed

David-Neto, Elias; Kakehashi, Erica; Alves, Cristiane Feres; Pereira, Lilian M; de Castro, Maria Cristina R; de Mattos, Renata Maciel; Sumita, Nairo Massakazu; Romano, Paschoalina; Mendes, Maria Elizabete; Nahas, William Carlos; Ianhez, Luiz Estevam

2004-02-01

New cyclosporine A (CsA) formulations must prove their bioequivalence to Neoral, the reference CsA formulation, to allow free prescription for the patients. The aim of this study was to compare the pharmacokinetics (PK) of a new CsA formulation (Zinograf-ME), produced by Strides-Arcolab, to Neoral and to demonstrate their interchangeability in stable renal transplant recipients. Twelve-hour PK studies were obtained from 18 (13 M/5 F) adult patients (mean age 44.7 +/- 12 years). They received their renal allografts from 13 cadaver and 5 living donors. Before enrollment, all patients were receiving a third generic CsA for a mean of 48 months. Nine patients were also under azathioprine and 9 under mycophenolate mofetil; 17 received prednisone. A single oral dose of either Zinograf or Neoral was administered. The first PK study was performed with one formulation, and 1 week later, a second PK was done with the other formulation. During the washout period, patients continued taking the third CsA formulation. The drug substitution was done milligram-for-milligram. The CsA whole-blood level was measured by TDx immunoassay. Mean +/- SD of area under the curve (AUC), maximum concentration (C(max)), and concentration at the second hour (C2) of Zinograf were not statistically different from those with Neoral (4019 +/- 1466 vs 3971 +/- 1325 ng x h/mL, 998 +/- 376 vs 1021 +/- 356 ng/mL, and 707 +/- 254 vs 734 +/- 229 ng/mL, respectively). In the same way, the Zinograf 90% confidence interval for either C(max) (-123, +77 ng/mL) or AUC (-214, +311 ng.mL/h) were within the Neoral bioequivalence interval for the same parameters (+/-204 ng/mL and +/-794 ng x mL/h, respectively). These data demonstrate that the ZinografME CsA formulation is bioequivalent to Neoral.

Application of a non-invasive method to study the moisturizing effect of formulations containing vitamins A or E or ceramide on human skin.

PubMed

Leonardi, Gislaine Ricci; Gaspar, Lorena Rigo; Maia Campos, Patrícia M B G

2002-01-01

Moisturizers containing vitamins A and E as well as ceramides are believed to improve the skin condition by increasing the water content of the stratum corneum. The aim of this research was to evaluate, through the capacitance method (a non-invasive method), the moisturizing effect of an O/W emulsion (non-ionic self-emulsifying base) containing vitamin A palmitate, vitamin E acetate, and ceramide III on human skin. The studies were carried out on a group of 40 healthy Caucasian female test subjects between 30 and 45 years of age, using the Corneometer CM 825 PC. Skin measurements were taken from the volunteers at 7 and 30 days after daily use (twice a day) of the tested products. The presence of vitamins A and E or ceramide III did not cause an improvement in the hydration of the stratum corneum, which means that none of those compounds strengthens the hydration effectiveness of the base formulations used, at least at the doses tested. The interpretation of electrical measurement regarding skin moisture should be made with caution; thus the results observed in this study show the importance of using different approaches (or methodologies) to verify the performance of the formulas tested. We conclude that, at the low doses typically used in cosmetic formulations, vitamins A and E and ceramide III are not likely to contribute to the hydrating effects of the base moisturizing formulation when assessed by capacitance.

Formulation and Evaluation of Mouth Disintegrating Tablets of Atenolol and Atorvastatin

PubMed Central

Sarfraz, R. M.; Khan, H. U.; Mahmood, A.; Ahmad, M.; Maheen, S.; Sher, M.

2015-01-01

In this study, mouth-disintegrating tablets of atenolol and atorvastatin combination were formulated using superdisintegrants to impart fast disintegration. Fifteen formulations were prepared based on different concentrations of two superdisintegrants, croscarmellose sodium and Kyron-T134. Three different techniques such as direct compression, effervescent and sublimation were used to study the effect of manufacturing processes, nature and concentration of superdisintegrants on various features of these tablets. Five formulations were made using each method. Precompression studies like bulk density, tapped density, angle of repose, Carr's compressibility index, Hausner's ratio and compatibility studies such as Fourier transform infrared spectroscopy and differential scanning calorimetry were performed. Various features such as hardness, thickness, diameter, weight variation, friability, disintegration time, dissolution studies, wetting time, wetting volume, water absorption ratio, modified disintegration, uniformity of contents and stability were evaluated. Finally results were statistically analyzed by the application of one way ANOVA test. Formulation F13 containing Kyron-T134 (6%) and croscarmellose sodium (2%) was found to be the best among all fifteen formulations prepared in all aspects evaluated. Sublimation method is found to be the best among three methods of preparation used. PMID:25767322

Modified EVA Encapsulant Formulations for Low Temperature Processing: Preprint

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

Mei, Z.; Pern, F. J.; Glick, S. H.

2001-10-01

Presented at the 2001 NCPV Program Review Meeting: We have developed several new ethylene-vinyl acetate (EVA) formulations modified on the basis of NREL patented EVA formulations [1]. The new formulations can be cured to a desired gel content of {approx}80% in the ambient at temperatures 20-30 C lower than the typical conditions in vacuum (i.e. {approx}150 C). Glass/glass laminates showed transmittance spectra that are essentially the same as that of EVA 15295P in the visible and NIR regions but higher in the UV region. Results of fluorescence analysis of the ambient-processed new EVA formulations showed the concentrations of the curing-generatedmore » {alpha},{beta}-unsaturated carbonyl chromophores, which are responsible for the UV induced EVA discoloration and photodegradation, were considerably lower than that of EVA 15295P, therefore suggesting a better photochemical stability of new EVA formulations.« less

Evaluation of alternative Plutella xylostella control by two Isaria fumosorosea conidial formulations - oil-based formulation and wettable powder - combined with Bacillus thuringiensis.

PubMed

Nian, Xiao-Ge; He, Yu-Rong; Lu, Li-Hua; Zhao, Rui

2015-12-01

Entomopathogenic fungi are potential candidates for controlling the diamondback moth Plutella xylostella (L.) (Lepidoptera: Plutellidae). The control efficacy of two Isaria fumosorosea conidial formulations - wettable powder and oil-based formulation - combined with Bacillus thuringiensis against P. xylostella was tested. In the laboratory, the combined application of two pathogens increased larval mortality either in an additive or a synergistic way. P. xylostella larvae treated with oil-based formulation died sooner than larvae infected with wettable powder. For pot and field experiments, each formulation was applied alone or combined with B. thuringiensis 668 µg mL(-1) , and then larval mortality, pupation rate, adult emergence rate, female longevity and fecundity were recorded. In pot experiments there was no evidence of any antagonistic effects between the two pathogens. Combined application of B. thuringiensis and a high concentration of the two I. fumosorosea formulations resulted in higher mortality (84.4 and 86.2%) with minimum pupation (15.6 and 11.9%) and adult emergence rates (8.7 and 7.0%). Female longevity and fecundity were significantly reduced by the two formulations at high concentration compared with the control. Similar results were also observed in field experiments. The combined application of I. fumosorosea and B. thuringiensis is a promising alternative strategy for P. xylostella control. © 2015 Society of Chemical Industry. © 2015 Society of Chemical Industry.

Dissolution of three insensitive munitions formulations.

PubMed

Taylor, Susan; Park, Eileen; Bullion, Katherine; Dontsova, Katerina

2015-01-01

The US military fires live munitions during training. To save soldiers lives both during training and war, the military is developing insensitive munitions (IM) that minimize unintentional detonations. Some of the compounds in the IM formulation are, however, very soluble in water, raising environmental concerns about their fate and transport. We measured the dissolution of three of these IM formulations, IMX101, IMX104 and PAX21 using laboratory drip tests and studied the accompanying changes in particle structure using micro computed tomography. Our laboratory drip tests mimic conditions on training ranges, where spatially isolated particles of explosives scattered by partial detonations are dissolved by rainfall. We found that the constituents of these IM formulations dissolve sequentially and in the order predicted by their aqueous solubility. The order of magnitude differences in solubility among their constituents produce water solutions whose compositions and concentrations vary with time. For IMX101 and IMX104, that contain 3-nitro-1,2,4-triazol-5-one (NTO), the solutions also vary in pH. The good mass balances measured for the drip tests indicate that the formulations are not being photo-or bio-transformed under laboratory conditions. Published by Elsevier Ltd.

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.

Poly (amidoamine) dendrimer-mediated hybrid formulation for combination therapy of ramipril and hydrochlorothiazide.

PubMed

Singh, Mayank Kumar; Pooja, Deep; Kulhari, Hitesh; Jain, Sanjay Kumar; Sistla, Ramakrishna; Chauhan, Abhay Singh

2017-01-01

We present a dendrimer-based hybrid formulation strategy to explore the potential of poly (amidoamine) PAMAM dendrimers to be used as drug carriers for combination therapy of an anti-hypertensive drug ramipril (RAPL) and a diuretic hydrochlorothiazide (HCTZ). The drug-dendrimer complexes were prepared by phase-equilibration method. The results showed that the solubility of RAPL and HCTZ was dependent on dendrimer concentration and pH of dendrimer solution. The solubility profile of both RAPL and HCTZ dendrimer complexes illustrated a non-linear relationship with dendrimer concentration. At 0.8% (w/v) dendrimer concentration, solubility of RAPL was increased 4.91 folds with amine-terminated while for HCTZ, solubility enhancement was highest (3.72 folds) with carboxy-terminated. The complexes were characterized by Fourier transform infrared spectroscopy, nuclear magnetic resonance analysis and high performance liquid chromatography. In-vitro drug dissolution performance of pure drugs, individual drug loaded dendrimer formulations and hybrid formulations was studied in USP dissolution medium (pH7.0) and in simulated gastric fluid (pH1.2). Dendrimer mediated formulations showed faster and complete dissolution compared to pure RAPL or HCTZ. Surprisingly, similar pattern of dissolution profile was established with hybrid formulations as compared to individual drug loaded dendrimers. The dendrimer-based hybrid formulations were found to be stable at dark and refrigerated conditions up to 5weeks. Conclusively, the proposed formulation strategy establishes a novel multitasking platform using dendrimer for simultaneous loading and delivery of multiple drugs for pharmaceutical applications. Copyright © 2016 Elsevier B.V. All rights reserved.

Sorbitol crystallization-induced aggregation in frozen mAb formulations.

PubMed

Piedmonte, Deirdre Murphy; Hair, Alison; Baker, Priti; Brych, Lejla; Nagapudi, Karthik; Lin, Hong; Cao, Wenjin; Hershenson, Susan; Ratnaswamy, Gayathri

2015-02-01

Sorbitol crystallization-induced aggregation of mAbs in the frozen state was evaluated. The effect of protein aggregation resulting from sorbitol crystallization was measured as a function of formulation variables such as protein concentration and pH. Long-term studies were performed on both IgG1 and IgG2 mAbs over the protein concentration range of 0.1-120 mg/mL. Protein aggregation was measured by size-exclusion HPLC (SE-HPLC) and further characterized by capillary-electrophoresis SDS. Sorbitol crystallization was monitored and characterized by subambient differential scanning calorimetry and X-ray diffraction. Aggregation due to sorbitol crystallization is inversely proportional to both protein concentration and formulation pH. At high protein concentrations, sorbitol crystallization was suppressed, and minimal aggregation by SE-HPLC resulted, presumably because of self-stabilization of the mAbs. The glass transition temperature (Tg ') and fragility index measurements were made to assess the influence of molecular mobility on the crystallization of sorbitol. Tg ' increased with increasing protein concentration for both mAbs. The fragility index decreased with increasing protein concentration, suggesting that it is increasingly difficult for sorbitol to crystallize at high protein concentrations. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.

Topical Vehicle Formulations in the Treatment of Acne.

PubMed

Hoffman, Lauren K; Bhatia, Neal; Zeichner, Joshua; Kircik, Leon H

2018-06-01

Topical treatment is the mainstay of acne therapy. The most commonly prescribed topical medications for acne include benzoyl peroxide, clindamycin, and retinoids. Despite their effectiveness in treating mild to moderate acne vulgaris, these topical medications are found to be irritating, and are historically associated with poor tolerability and diminished patient adherence. Thus, choosing the right formulation that will be effective and well tolerated is essential. Novel formulations that optimize drug concentration and utilize improved delivery vehicles have helped to enhance the tolerability and efficacy, and allow for less frequent application or co-application of drugs that were previously considered incompatible. This article will review the goals of topical therapy for the treatment of acne, in addition to common therapies and their challenges. Advanced formulations and combination formulations of benzoyl peroxide, clindamycin, and tretinoin will also be discussed. J Drugs Dermatol. 2018;17(6 Suppl):s6-10.

ABC Triblock Copolymer Worms: Synthesis, Characterization, and Evaluation as Pickering Emulsifiers for Millimeter-Sized Droplets

PubMed Central

2016-01-01

Polymerization-induced self-assembly (PISA) is used to prepare linear poly(glycerol monomethacrylate)–poly(2-hydroxypropyl methacrylate)–poly(benzyl methacrylate) [PGMA–PHPMA–PBzMA] triblock copolymer nano-objects in the form of a concentrated aqueous dispersion via a three-step synthesis based on reversible addition–fragmentation chain transfer (RAFT) polymerization. First, GMA is polymerized via RAFT solution polymerization in ethanol, then HPMA is polymerized via RAFT aqueous solution polymerization, and finally BzMA is polymerized via “seeded” RAFT aqueous emulsion polymerization. For certain block compositions, highly anisotropic worm-like particles are obtained, which are characterized by small-angle X-ray scattering (SAXS) and transmission electron microscopy (TEM). The design rules for accessing higher order morphologies (i.e., worms or vesicles) are briefly explored. Surprisingly, vesicular morphologies cannot be accessed by targeting longer PBzMA blocks—instead, only spherical nanoparticles are formed. SAXS is used to rationalize these counterintuitive observations, which are best explained by considering subtle changes in the relative enthalpic incompatibilities between the three blocks during the growth of the PBzMA block. Finally, the PGMA–PHPMA–PBzMA worms are evaluated as Pickering emulsifiers for the stabilization of oil-in-water emulsions. Millimeter-sized oil droplets can be obtained using low-shear homogenization (hand-shaking) in the presence of 20 vol % n-dodecane. In contrast, control experiments performed using PGMA–PHPMA diblock copolymer worms indicate that these more delicate nanostructures do not survive even these mild conditions. PMID:27795581

Pharmacokinetic and pharmacodynamic comparison of hydrofluoroalkane and chlorofluorocarbon formulations of budesonide

PubMed Central

Clearie, Karine L; Williamson, Peter A; Meldrum, Karen; Gillen, Michael; Carlsson, Lars-Goran; Carlholm, Marie; Ekelund, Jan; Lipworth, Brian J

2011-01-01

AIMS A hydrofluoroalkane formulation of budesonide pressurized metered-dose inhaler has been developed to replace the existing chlorofluorocarbon one. The aim of this study was to evaluate the pharmacokinetic and pharmacodynamic characteristics of both formulations. METHODS Systemic bioavailability and bioactivity of both hydrofluoroalkane and chlorofluorocarbon pressurized metered-dose inhaler formulations at 800 µg twice daily was determined during a randomized crossover systemic pharmacokinetic/pharmacodynamic study at steady state in healthy volunteers. Measurements included the following: plasma cortisol AUC24h[area under the concentration-time curve (0–24 h)], budesonide AUC0–12h and Cmax. Clinical efficacy was determined during a randomized crossover pharmacodynamic study in asthmatic patients receiving 200 µg followed by 800 µg budesonide via chlorofluorocarbon or hydrofluoroalkane pressurized metered-dose inhaler each for 4 weeks. Methacholine PC20 (primary outcome), exhaled nitric oxide, spirometry, peak expiratory flow and symptoms were evaluated. RESULTS In the pharmacokinetic study, there were no differences in cortisol, AUC0–12h[area under the concentration-time curve (0–12 h)], Tmax (time to maximum concentration) or Cmax (peak serum concentration) between the hydrofluoroalkane and chlorofluorocarbon pressurized metered-dose inhaler. The ratio of budesonide hydrofluoroalkane vs. chlorofluorocarbon pressurized metered-dose inhaler for cortisol AUC24h was 1.02 (95% confidence interval 0.93–1.11) and budesonide AUC0–12h was 1.03 (90% confidence interval 0.9–1.18). In the asthma pharmacodynamic study, there was a significant dose response (P < 0.0001) for methacholine PC20 (provocative concentration of methacholine needed to produce a 20% fall in FEV1) with a relative potency ratio of 1.10 (95% confidence interval 0.49–2.66), and no difference at either dose. No significant differences between formulations were seen with the secondary

Evaluation of the enzymatic activity and stability of commercial bromelain incorporated in topical formulations.

PubMed

Lourenço, C B; Ataide, J A; Cefali, L C; Novaes, L C D L; Moriel, P; Silveira, E; Tambourgi, E B; Mazzola, P G

2016-10-01

Bromelain is a mixture of proteolytic enzymes found in various tissues of the pineapple plant (Ananas comosus) and other species of Bromeliaceae. Owing to its proteolytic activity, bromelain has been used in the food, medical, pharmaceutical and cosmetic industries, for its cell renewal, anti-ageing, whitening and anti-cellulite properties. This study evaluated the stability of bromelain (commercial powder) incorporated in topical formulations. Bromelain was incorporated at three concentrations, 0.5%, 1.0% and 2.0%, in oil-in-water emulsion and gel, and stored for six months at varying stress conditions. Stability was accessed by measuring the changes in the protein content, enzymatic activity, viscosity, rheology, pH and colour of the selected formulations. The colour of all the samples changed after 180 days of incubation, indicating the concentration-dependence and temperature-sensitive nature of these formulations. No relationship was observed between the changes in the pH, temperature and luminosity exposure in all the samples. Gels proved to be the least preferred base for incorporation of bromelain for use as a topical formulation, owing to its inability to maintain the integrity of bromelain, thereby affecting the formulation characteristics. The emulsion-based formulations at all the concentrations of bromelain were more stable than the gel-based formulation over 180 days of evaluation, at a temperature of 5°C, protected from light. © 2016 Society of Cosmetic Scientists and the Société Française de Cosmétologie.

SPE-UPLC-MS/MS for the determination of phthalate monoesters in rats urine and its application to study the effects of food emulsifier on the bioavailability of priority controlling PAEs.

PubMed

Xu, R; Gao, H T; Zhu, F; Cao, W X; Yan, Y H M; Zhou, X; Xu, Q; Ji, W L

2016-02-15

This research was mainly focused on the effects of food emulsifier on the bioavailability of six priority controlling phthalate acid esters (PAEs) for the further accurate assessment of their toxic effects, using the corresponding phthalate acid monoesters (PAMEs) in rats urine as biomarkers. Glycerin monostearate was chosen as typical food emulsifier. A method was established to determine PAMEs in urine from rats either in experimental group (integrated gavaged with glycerin monostearate and PAEs) or in control group (gavaged with PAEs only), by using solid-phase extraction (SPE) coupled with ultra performance liquid chromatography tandem mass spectrometry (SPE-UPLC-MS/MS). Extraction recoveries were more than 75% for all the PAMEs; the calibration curve was linear in the range of 1.0-1000.0ng/mL with R(2)>0.995; the limits of detection (LOD) were 0.30ng/mL-0.50ng/mL. In addition, by analysing quality control (QC) urine samples in 3 days, it showed that the method was precise and accurate, for the intra-day and inter-day RSD within 16%, and the accuracy more than 82%. Internal exposure amount of all PAEs in experimental group was significantly higher than that in control group with p values of less than 0.05 except for butyl benzyl phthalates (BBP) (P=0.07). The bioavailability of all PAEs ranged from 5.03% to 109.35% with the presence of food emulsifiers glycerin monostearate, observably higher than that without glycerin monostearate (1.12% to 54.39%). It indicated that food emulsifiers increased the bioavailability of PAEs and may lead to potential food safety risk, which should bring awareness and be further studied. Copyright © 2016 Elsevier B.V. All rights reserved.

CMC determination of nonionic surfactants in protein formulations using ultrasonic resonance technology.

PubMed

Horiuchi, Shohei; Winter, Gerhard

2015-05-01

Biological products often contain surfactants as stabilizers in their formulations to avoid surface adsorption, interfacial denaturation and aggregation of the protein drug and thereby improve the overall pharmaceutical quality of the product. On the other hand, when the surfactant concentration exceeds the critical micelle concentration (CMC) in a protein formulation, protein-loaded micelles could be formed which could potentially be the cause of immunogenicity. Therefore, the actual CMC and the presence of micelles generally need to be confirmed for each protein formulation because the CMC is affected by the presence of protein and other formulation factors. In this study, the ultrasonic resonance technology (URT) was applied to determine CMC of surfactants in pharmaceutical protein solutions in comparison with surface tensiometry (TE) and dynamic light scattering (DLS). According to our results, the ultrasonic resonance technology can easily and precisely provide CMCs of surfactants in protein formulations while it is not working for protein-free formulations. This indicates that the signal we measure with ultrasonic velocity comes from complex micelles composed of surfactant and protein molecules. DLS did not provide reliable data for protein/surfactant systems. Interestingly, a protein formulation with arginine and polysorbate 20 behaved differently when studied with TE and URT allowing us to see that arginine is bound to protein and that the complex interacts with the surfactant. Copyright © 2015 Elsevier B.V. All rights reserved.

Toxicological evaluation of aerosols of a tobacco extract formulation and nicotine formulation in acute and short-term inhalation studies.

PubMed

Werley, Michael S; Jerome, Ann M; Oldham, Michael J

2014-03-01

A formulation of tobacco extract containing 4% nicotine (TE) and similar nicotine formulation containing vehicle and 4% nicotine (NF) were evaluated using animal inhalation assays. Two 4-h inhalation exposures at 1 and 2 mg/L aerosol exposure concentrations, respectively, of the tobacco extract with 4% nicotine formulation showed that the LC50 was greater than 2 mg/L, the maximum concentration tested. All inhalation exposures were conducted using the capillary aerosol generator (CAG). Increasing aerosol TPM concentrations (0, 10, 50, 200, 1000 mg/m(3) TE and 0, 50, 200, 500, 1000 mg/m(3) NF) were generated via the CAG and used to expose groups of male and female rats for 4-h per day for 14 days. In life monitors for potential effects included clinical observations, weekly body weights and food consumption. Post mortem evaluations included gross tissue findings, hematology, clinical chemistry, serum plasma and nicotine levels, absolute and normalized organ and tissue weights, and histopathology of target organs. Treatment-related changes were observed in body weights, hematology, clinical chemistry, organ weights and histopathological findings for TE at the 200 and 1000 mg/m(3) exposure levels, and in the 500 and 1000 mg/m(3) exposure groups for NF. Under the conditions of these studies, the no-observed-adverse-effect level in the rat was approximately 50 mg/m(3) for the TE aerosol-exposed groups, and approximately 200 mg/m(3) in the NF aerosol-exposed groups.

Decontamination formulation with additive for enhanced mold remediation

DOEpatents

Tucker, Mark D [Albuquerque, NM; Irvine, Kevin [Huntsville, AL; Berger, Paul [Rome, NY; Comstock, Robert [Bel Air, MD

2010-02-16

Decontamination formulations with an additive for enhancing mold remediation. The formulations include a solubilizing agent (e.g., a cationic surfactant), a reactive compound (e.g., hydrogen peroxide), a carbonate or bicarbonate salt, a water-soluble bleaching activator (e.g., propylene glycol diacetate or glycerol diacetate), a mold remediation enhancer containing Fe or Mn, and water. The concentration of Fe.sup.2+ or Mn.sup.2+ ions in the aqueous mixture is in the range of about 0.0001% to about 0.001%. The enhanced formulations can be delivered, for example, as a foam, spray, liquid, fog, mist, or aerosol for neutralization of chemical compounds, and for killing certain biological compounds or agents and mold spores, on contaminated surfaces and materials.

DEMONSTRATION OF IN SITU DEHALOGENATION OF DNAPL THROUGH INJECTION OF EMULSIFIED ZERO-VALIENT IRON AT LAUNCH COMPLEX 34 IN CAPE CANAVERAL AIR FORCE STATION, FLORIDA

EPA Science Inventory

The purpose of this project was to evaluate the technical and cost performance of emulsified zero-valent iron (EZVI) technology when applied to DNAPL contaminants in the saturated zone. This demonstration was conducted at Launch Complex 34, Cape Canaveral Air Force Station, FL, w...

Anaerobic digestion of thermal pre-treated emulsified slaughterhouse wastes (TESW): Effect of trace element limitation on process efficiency and sludge metabolic properties.

PubMed

Eftaxias, Alexandros; Diamantis, Vasileios; Aivasidis, Alexandros

2018-06-01

Slaughterhouse solid wastes, characterized by a high lipid content, are considered a valuable resource for energy production by means of anaerobic digestion technologies. Aim of this study was to examine the effect of trace element limitation on the mesophilic anaerobic digestion of thermally pre-treated emulsified slaughterhouse wastes (TESW). Under two distinct experimental periods (Period I - low and Period II - high trace element dosage respectively) a CSTR with sludge recirculation was operated at increasing organic loading rate (OLR) from 1.5 to 10 g L -1  d -1 . Under optimum conditions, COD removal was higher than 96%, biogas yield equal to 0.53 L g -1  COD feed and the biogas methane content 77%. Trace element limitation however, resulted in a dramatic decline in process efficiency, with VFA accumulation and events of extreme sludge flotation, despite that the soluble concentration of Ni, Co and Mo were between 12 and 28 μg L -1 . This is indicative of mass transfer limitations caused by lipids adsorption onto the anaerobic biomass. Copyright © 2018 Elsevier Ltd. All rights reserved.

Investigation of the Effects of Inulin and β-Glucan on the Physical and Sensory Properties of Low-Fat Beef Burgers Containing Vegetable Oils: Optimisation of the Formulation Using D-Optimal Mixture Design

PubMed Central

Afshari, Roya; Khaksar, Ramin; Mohammadifar, Mohammad Amin; Amiri, Zohre; Komeili, Rozita; Khaneghah, Amin Mousavi

2015-01-01

Summary In this study, the D-optimal mixture design methodology was applied to determine the optimised proportions of inulin, β-glucan and breadcrumbs in formulation of low-fat beef burgers containing pre-emulsified canola and olive oil blend. Also, the effect of each of the ingredients individually as well as their interactions on cooking characteristics, texture, colour and sensory properties of low-fat beef burgers were investigated. The results of this study revealed that the increase of inulin content in the formulations of burgers led to lower cooking yield, moisture retention and increased lightness, overall acceptability, mouldability and desired textural parameters. In contrast, incorporation of β-glucan increased the cooking yield, moisture retention and decreased lightness, overall acceptability, mouldability and desired textural parameters of burger patties. The interaction between inulin and β-glucan improved the cooking characteristics of the burgers without significantly negative effect on the colour or sensory properties. The results of the study clearly stated that the optimum mixture for the burger formulation consisted of (in g per 100 g): inulin 3.1, β-glucan 2.2 and breadcrumbs 2.7. The texture parameters and cooking characteristics were improved by using the mixture of inulin, β-glucan and breadcrumbs, without any negative effects on the sensory properties of the burgers. PMID:27904378

Benzathine penicillin G: a model for long-term pharmacokinetic comparison of parenteral long-acting formulations.

PubMed

Shahbazi, M A; Azimi, K; Hamidi, M

2013-04-01

  Long-acting intramuscular penicillin G injection is an important product for the management of some severe infections. However, testing the bioequivalence of such long-acting formulations is difficult. Our aim was to undertake such a test using a generic formulation containing 1 200 000 IU of benzathine penicillin G powder and an innovator's product (Retarpen(®) 1·2 million units; Sandoz, Switzerland).   In an open, double-blind, randomized, two-periods, two-group crossover study, 12 healthy male volunteers received both formulations of benzathine penicillin G on two different days with a 5-month washout period between the doses and a sampling period of over 500 h. A simple, sensitive and rapid high-performance liquid chromatography (HPLC)-UV method was developed and validated for determination of penicillin G plasma concentrations and other pharmacokinetic (PK) parameters.   The analytical method used produced linear responses within a wide analyte concentration range with average within-run and between-run variations of below 15% with acceptable recovery, accuracy and sensitivity. The primary PK parameters we used were maximum plasma concentration (Cmax ), time to reach the maximal concentration (Tmax ) and the area under the plasma concentration vs. time curve from time zero to the last sampling time (AUC0→t ) using a standard non-compartmental approach. Based on these parameters, the two formulations were bioequivalent.   We illustrate the bioequivalence testing of a very long-acting product. The data indicate that the generic test formulation and the branded reference formulation were bioequivalent in fasting healthy Iranian male volunteers. © 2013 Blackwell Publishing Ltd.

Pharmacokinetic evaluation of novel midazolam gel formulations following buccal administration to healthy dogs.

PubMed

Aldawsari, Mohammed F; Lau, Vivian W; Babu, Ramapuram J; Arnold, Robert D; Platt, Simon R

2018-01-01

OBJECTIVE To determine the physiochemical properties and pharmacokinetics of 3 midazolam gel formulations following buccal administration to dogs. ANIMALS 5 healthy adult hounds. PROCEDURES In phase 1 of a 2-phase study, 2 gel formulations were developed that contained 1% midazolam in a poloxamer 407 (P1) or hydroxypropyl methylcellulose (H1) base and underwent rheological and in vitro release analyses. Each formulation was buccally administered to 5 dogs such that 0.3 mg of midazolam/kg was delivered. Each dog also received midazolam hydrochloride (0.3 mg/kg, IV). There was a 3-day interval between treatments. Blood samples were collected immediately before and at predetermined times for 8 hours after drug administration for determination of plasma midazolam concentration and pharmacokinetic analysis. During phase 2, a gel containing 2% midazolam in a hydroxypropyl methylcellulose base (H2) was developed on the basis of phase 1 results. That gel was buccally administered such that midazolam doses of 0.3 and 0.6 mg/kg were delivered. Each dog also received midazolam (0.3 mg/kg, IV). All posttreatment procedures were the same as those for phase 1. RESULTS The H1 and H2 formulations had lower viscosity, greater bioavailability, and peak plasma midazolam concentrations that were approximately 2-fold as high, compared with those for the P1 formulation. The mean peak plasma midazolam concentration for the H2 formulation was 187.0 and 106.3 ng/mL when the midazolam dose administered was 0.6 and 0.3 mg/kg, respectively. CONCLUSIONS AND CLINICAL RELEVANCE Results indicated that buccal administration of gel formulations might be a viable alternative for midazolam administration to dogs.

A pyrene formulation for fluorometric visualization of latent fingermarks

NASA Astrophysics Data System (ADS)

Kumari Sharma, Kirti; Harsha Kannikanti, Gavash; Ramachandra Rao Baggi, Tulsidas; Rao Vaidya, Jayathirtha

2018-07-01

Present work is conducted to demonstrate the use of pyrene for the development of latent fingermarks. Pyrene formulation with binders can be efficiently used for developing latent fingermarks on porous, non-porous and semi-porous surfaces. The effectiveness of pyrene formulation for the detection of latent fingermarks present on a large variety of objects was systematically and comparatively carried out. To optimize the working formulation, studies were carried out using different pyrene concentrations followed by various substrate study, time dependent study, temperature study, depleted fingermark development and the stability of the proposed formulation. When illuminated at 366 nm, the developed fingermarks showed clear, high contrast primary, secondary and tertiary level ridge details. This work reveals that the fluorescent molecules having high quantum yield are a versatile fluorescent label and can find their applications in forensic latent fingermark development.

Development, characterization, and evaluation of sunscreen cream containing solid lipid nanoparticles of silymarin.

PubMed

Netto MPharm, Gladyston; Jose, Jobin

2017-12-10

Most of the sunscreen formulations mainly contain chemicals or synthetic molecules. Nowadays, researchers are mainly focussing on herbal formulations due to toxicity of the synthetic molecules. Silymarin is a natural flavonoids having excellent antioxidant properties. Solid lipid nanoparticles are novel drug carriers which improve the drug stability and tolerance effect and also enhance the permeation effect. This study aimed at the preparation of solid lipid nanoparticles containing silymarin that will be incorporated into a sunscreen cream and determine its sun protection factor. The solid lipid nanoparticles were prepared by micro-emulsion method; here, the glyceryl monostearate was used as lipid, and Tween 80 was used as an emulsifier. The solid lipid nanoparticles were evaluated for drug entrapment, particle size and morphology, zeta potential, and polydispersity index. The dispersion was formulated into sunscreen cream and evaluated for various parameters, such as extrudability, viscosity, spreadability, drug content, in vitro drug release, ex vivo permeation of drug, in vitro and in vivo sun protection factor determination, in vivo skin irritation test, and accelerated stability studies. The results suggested that as the concentration of emulsifier increased, the entrapment efficiency of silymarin increased. In vitro and in vivo sun protection factor determination showed that SPF of 13.80 and 14.1, respectively. Stability studies were performed under accelerated conditions, and it did not show any appreciable change in parameters. These results indicated that the sunscreen containing silymarin solid lipid nanoparticles exhibited better photoprotective action. © 2017 Wiley Periodicals, Inc.

Biotherapeutic formulation factors affecting metal leachables from stainless steel studied by design of experiments.

PubMed

Zhou, Shuxia; Evans, Brad; Schöneich, Christian; Singh, Satish K

2012-03-01

Trace amounts of metals are inevitably present in biotherapeutic products. They can arise from various sources. The impact of common formulation factors such as protein concentration, antioxidant, metal chelator concentration and type, surfactant, pH, and contact time with stainless steel on metal leachables was investigated by a design of experiments approach. Three major metal leachables, iron, chromium, and nickel were monitored by inductively coupled plasma-mass spectrometry. It was observed that among all the tested factors, contact time, metal chelator concentration, and protein concentration were statistically significant factors with higher temperature resulting in higher levels of leached metals. Within a pH range of 5.5-6.5, solution pH played a minor role for chromium leaching at 25°C. No statistically significant difference was observed due to type of chelator, presence of antioxidant, or surfactant. In order to optimize a biotherapeutic formulation to achieve a target drug product shelf life with acceptable quality, each formulation component must be evaluated for its impact.

Comprehensive evaluation of formulation factors for ocular penetration of fluoroquinolones in rabbits using cassette dosing technique.

PubMed

Sharma, Charu; Biswas, Nihar R; Ojha, Shreesh; Velpandian, Thirumurthy

2016-01-01

Corneal permeability of drugs is an important factor used to assess the efficacy of topical preparations. Transcorneal penetration of drugs from aqueous formulation is governed by various physiological, physiochemical, and formulation factors. In the present study, we investigated the effect of formulation factors like concentration, pH, and volume of instillation across the cornea using cassette dosing technique for ophthalmic fluoroquinolones (FQs). Sterile cocktail formulations were prepared using four congeneric ophthalmic FQs (ofloxacin, sparfloxacin, pefloxacin mesylate, and gatifloxacin) at concentrations of 0.025%, 0.5%, and 0.1%. Each formulation was adjusted to different pH ranges (4.5, 7.0, and 8.0) and assessed for transcorneal penetration in vivo in rabbit's cornea (n=4 eyes) at three different volumes (12.5, 25, and 50 μL). Aqueous humor was aspirated through paracentesis after applying local anesthesia at 0, 5, 15, 30, 60, 120, and 240 minutes postdosing. The biosamples collected from a total of 27 groups were analyzed using liquid chromatography-tandem mass spectroscopy to determine transcorneal permeability of all four FQs individually. Increase in concentration showed an increase in penetration up to 0.05%; thereafter, the effect of concentration was found to be dependent on volume of instillation as we observed a decrease in transcorneal penetration. The highest transcorneal penetration of all FQs was observed at pH 7.0 at concentration 0.05% followed by 0.025% at pH 4.5. Lastly, increasing the volume of instillation from 12.5 to 50 μL showed a significant fall in transcorneal penetration. The study concludes that formulation factors showed discernible effect on transcorneal permeation; therefore, due emphasis should be given on drug development and design of ophthalmic formulation.

Whey protein phospholipid concentrate and delactosed permeate: Applications in caramel, ice cream, and cake.

PubMed

Levin, M A; Burrington, K J; Hartel, R W

2016-09-01

Whey protein phospholipid concentrate (WPPC) and delactosed permeate (DLP) are 2 coproducts of cheese whey processing that are currently underutilized. Past research has shown that WPPC and DLP can be used together as a functional dairy ingredient in foods such as ice cream, soup, and caramel. However, the scope of the research has been limited to a single WPPC supplier. The variability of the composition and functionality of WPPC was previously studied. The objective of this research was to expand on the previous study and examine the potential applications of WPPC and DLP blends in foods. In ice cream, WPPC was added as a natural emulsifier to replace synthetic emulsifiers. The WPPC decreased the amount of partially coalesced fat and increased the drip-through rate. In caramel, DLP and WPPC replaced sweetened condensed skim milk and lecithin. Cold flow increased significantly, and hardness and stickiness decreased. In cake, DLP and WPPC were added as a total replacement of eggs, with no change in yield, color, or texture. Overall, WPPC and DLP can be utilized as functional dairy ingredients at a lower cost in ice cream and cake but not in chewy caramel. Copyright © 2016 American Dairy Science Association. Published by Elsevier Inc. All rights reserved.

Cardiocerebral protection by emulsified isoflurane during cardiopulmonary resuscitation.

PubMed

Zhang, Ya-Jie; Wu, Meng-Jun; Li, Yi; Yu, Hai

2015-01-01

Although improvement in cardiopulmonary resuscitation (CPR) performance and the increasing success at achieving return of spontaneous circulation (ROSC) have been possible in recent years, the survival and discharge rates of post-cardiac arrest (CA) patients remain disappointing. The high mortality rate is attributed to whole-body ischemia/reperfusion (I/R) induced multi-organ dysfunction that is well known as post-cardiac arrest syndrome. Post-cardiac arrest myocardial dysfunction and brain injury are the main clinical features of this complex pathophysiological process. Previous evidences have shown that volatile anesthetics, such as isoflurane, trigger a powerful and highly integrated cell survival response during I/R period in multiple organs, including heart and brain, which reduces I/R injury. This effect that called anesthetic-induced postconditioning can be shown when volatile anesthetics are administered after the onset of ischemia and at the time of reperfusion. Emulsified isoflurane (EIso) is a new anesthetic for intravenous administration, which is conveniently feasible outside operating room. Therefore, we hypothesize that EIso postconditioning could provide the cardiocerebral protection, and combined with therapeutic hypothermia as sedative agent could produce enhanced cardiocerebral protection, which can result in significant improvement of neurologically intact post-cardiac arrest survival. We consider that it would become a feasible, safe and efficient cardiocerebral protective intervention in the prevention and alleviation of post-cardiac arrest syndrome, which would also improve the outcomes after CA. Copyright © 2014 Elsevier Ltd. All rights reserved.

Physicochemical and sensory properties of ice-cream formulated with virgin coconut oil.

PubMed

Choo, S Y; Leong, S K; Henna Lu, F S

2010-12-01

The substitution of milk fat with virgin coconut oil (VCO) was used to produce nutritious ice cream with pleasant coconut flavor and aroma. Three formulations were developed whereby formulation VCO4, VCO8 and VCO12 was substituted with 4%, 8% and 12% of VCO, respectively. The physicochemical properties of ice creams analyzed include overrun, meltdown, pH, titratable acidity, total solid, protein and fat content. The fatty acids profile of VCO formulated ice creams and their stabilities over 3 and 6 weeks storage were studied respectively using gas chromatography (GC). Qualitative descriptive analysis (QDA) and consumer affective test were performed among the trained and untrained panelists. Significant differences (p < 0.05) of overrun, pH, total solid, protein and fat content between ice cream formulations were observed except titratable acidity. Increased VCO content in ice cream formulations lowered the melting resistance of ice cream. For GC analysis, the major fatty acid identified was lauric acid. Upon storage time, the concentration of unsaturated fatty acid decreased but the concentration of saturated fatty acid increased. The result of QDA showed that formulation VCO4, VCO8 and VCO12 were significantly (p < 0.05) different in attributes of color, firmness and smoothness as compared to the control ice cream. Formulation VCO12 was highly accepted by panelists in terms of the acceptance level of appearance, aroma, texture, flavor and overall acceptability. Hence, it has a potential marketable value.

Percutaneous penetration, melanin activation and toxicity evaluation of a phytotherapic formulation for vitiligo therapeutic.

PubMed

Truite, Cecília Valente Rodrigues; Philippsen, Gisele Strieder; Ueda-Nakamura, Tânia; Natali, Maria Raquel Marçal; Dias Filho, Benedito Prado; Bento, Antonio Carlos; Baesso, Mauro Luciano; Nakamura, Celso Vataru

2007-01-01

The aim of this work was to apply photoacoustic spectroscopy for the ex vivo determination of the penetration rate of a phytotherapic formulation for vitiligo therapeutic, with or without salicylic acid as the promoter agent. In addition, the compound toxicity and morphophysiology effects were evaluated for different concentrations of salicylic acid. The experiments were performed as a function of the period of time of treatment in a well-controlled group of rabbits. Toxic effects were not observed with any of the tested products. All formulations containing salicylic acid induced cutaneous reaction which was dose dependent. The histological analysis showed that the use of the medication was associated with an increased comedogenic effect in relation to the control group, regardless of salicylic acid concentration. Inflammatory reactions and acanthosis were observed only in the animals treated with formulations containing higher concentrations of salicylic acid, while none of these effects were detected with the use of the formulation containing 2.5% (wt/vol) of salicylic acid. Photoacoustic depth monitoring showed that both formulations, with or without salicylic acid, propagated through the skin up to the melanocytes region, suggesting that the transport of the active agent may occur through the epithelial structure without the need of using queratinolitic substances, which are known to induce side effects in the animals.

Emulsion Stability Modulates Gastric Secretion and Its Mixing with Emulsified Fat in Healthy Adults in a Randomized Magnetic Resonance Imaging Study.

PubMed

Liu, Dian; Parker, Helen L; Curcic, Jelena; Kozerke, Sebastian; Steingoetter, Andreas

2016-10-01

Oil-in-water emulsions have recently become of interest to nutritional sciences because of their ability to influence gastrointestinal digestive processes and ultimately benefit human health. MRI offers the potential to noninvasively characterize the interaction between emulsified lipids and gastric secretion within the stomach. We determined noninvasively how emulsion stability modulates volumes of fat and secretion, layering of fat, and the mixing of emulsified fat with secretion within the stomach. This required the development of MRI technology for quantifying fat and secretion concentrations inside the stomach. Twenty-one healthy adults [13 men, mean ± SD age: 22.5 ± 2.5 y, mean ± SD body mass index (in kg/m 2 ): 22.7 ± 1.8] were analyzed in a single-blind, randomized, parallel design. MRI was used to acquire the distributions of fat and secretion in the stomach after ingestion of 2 emulsions: a stable emulsion (E1) or an unstable emulsion (E4) with 20% fat fraction and ∼0.3 mm droplet sizes. Layer, volume, and mixing variables were fitted to the data and compared between the 2 emulsions. The intragastric mixing between fat and secretion was better with the E4 than the E1 [increase in content heterogeneity of 17.1% (95% CI: 12.3%, 21.9%)]. The E4 demonstrated a linear relation [slope 1.57 (95% CI: 0.86, 2.29)] between the degree of layering and mixing. In contrast, no such relation was detected for the E1. Accumulated secretion volume in the stomach was lower with the E4 [decrease in volume variable k s of 2.3 (95% CI: -3.9, -0.7)] and correlated with the degree of layering (r = 0.62, P < 0.001). In healthy adults, intragastric fat layering was influenced mainly by the degree of intragastric mixing, rather than the overall dominance of secretion. The E1 triggered a higher accumulation of gastric secretion, which in turn facilitated homogenization of intragastric content in comparison with its unstable counterpart. This trial was registered at

New approach for dry formulation techniques for rhizobacteria

NASA Astrophysics Data System (ADS)

Elchin, A. A.; Mashinistova, A. V.; Gorbunova, N. V.; Muratov, V. S.; Kydralieva, K. A.; Jorobekova, Sh. J.

2009-04-01

Two beneficial Pseudomonas isolates selected from rhizosphere of abundant weed - couch-grass Elytrigia repens L. Nevski have been found to have biocontrol activity. An adequate biocontrol effect requires high yield and long stability of the bacterial preparation [1], which could be achieved by an effective and stable formulation. This study was aimed to test various approaches to dry formulation techniques for Pseudomonas- based preparations. To reach this goal, two drying formulation techniques have been tested: the first one, spray drying and the second, low-temperature contact-convective drying in fluidized bed. The optimal temperature parameters for each technique were estimated. Main merits of the selected approach to dry technique are high yield, moderate specific energy expenditures per 1 kg of evaporated moisture, minimal time of contact of the drying product with drying agent. The technological process for dry formulation included the following stages: the obtaining of cell liquids, the low-temperature concentrating and the subsequent drying of a concentrate. The preliminary technological stages consist in cultivation of the rhizobacteria cultures and concentrating the cell liquids. The following requirements for cultivation regime in laboratory conditions were proposed: optimal temperatures are 26-28°С in 3 days, concentration of viable cells in cell liquid makes 1010-1011 cell/g of absolutely dry substance (ADS). For concentrating the cell liquids the method of a vacuum evaporation, which preserves both rhizobacteria cells and the secondary metabolites of cell liquid, has been used. The process of concentrating was conducted at the minimum possible temperature, i.e. not above 30-33°С. In this case the concentration of viable cells has decreased up to 109-1010 cell/g of ADS. For spray drying the laboratory up-dated drier BUCHI 190, intended for the drying of thermolabile products, was used. The temperatures of an in- and outcoming air did not exceed

Nanoemulsions of thymol and eugenol co-emulsified by lauric arginate and lecithin.

PubMed

Ma, Qiumin; Davidson, P Michael; Zhong, Qixin

2016-09-01

Lauric arginate (LAE) is a cationic surfactant with excellent antimicrobial activities. To incorporate essential oil components (EOCs) in aqueous systems, properties of EOC nanoemulsions prepared with a LAE and lecithin mixture were studied. The LAE-lecithin mixture resulted in stable translucent nanoemulsions of thymol and eugenol with spherical droplets smaller than 100nm, contrasting with the turbid emulsions prepared with individual emulsifiers. Zeta-potential data suggested the formation of LAE-lecithin complexes probably through hydrophobic interaction. Negligible difference was observed for antimicrobial activities of nanoemulsions and LAE in tryptic soy broth. In 2% reduced fat milk, nanoemulsions showed similar antilisterial activities compared to free LAE in inhibiting Listeria monocytogenes, but was less effective against Escherichia coli O157:H7 than free LAE, which was correlated with the availability of LAE as observed in release kinetics. Therefore, mixing LAE with lecithin improved the physical properties of EOC nanoemulsions but did not improve antimicrobial activities, especially against Gram-negative bacteria. Copyright © 2016 Elsevier Ltd. All rights reserved.

Boron concentration measurements by alpha spectrometry and quantitative neutron autoradiography in cells and tissues treated with different boronated formulations and administration protocols.

PubMed

Bortolussi, Silva; Ciani, Laura; Postuma, Ian; Protti, Nicoletta; Luca Reversi; Bruschi, Piero; Ferrari, Cinzia; Cansolino, Laura; Panza, Luigi; Ristori, Sandra; Altieri, Saverio

2014-06-01

The possibility to measure boron concentration with high precision in tissues that will be irradiated represents a fundamental step for a safe and effective BNCT treatment. In Pavia, two techniques have been used for this purpose, a quantitative method based on charged particles spectrometry and a boron biodistribution imaging based on neutron autoradiography. A quantitative method to determine boron concentration by neutron autoradiography has been recently set-up and calibrated for the measurement of biological samples, both solid and liquid, in the frame of the feasibility study of BNCT. This technique was calibrated and the obtained results were cross checked with those of α spectrometry, in order to validate them. The comparisons were performed using tissues taken form animals treated with different boron administration protocols. Subsequently the quantitative neutron autoradiography was employed to measure osteosarcoma cell samples treated with BPA and with new boronated formulations. © 2013 Published by Elsevier Ltd.

21 CFR 172.846 - Sodium stearoyl lactylate.

Code of Federal Regulations, 2012 CFR

2012-04-01

...) As an emulsifier or stabilizer in liquid and solid edible fat-water emulsions intended for use as... finished edible fat-water emulsion. (4) As a formulation aid, processing aid, or surface-active agent in...

Formulation Development and Evaluation of the Therapeutic Efficacy of Brinzolamide Containing Nanoemulsions

PubMed Central

Mahboobian, Mohammad Mehdi; Seyfoddin, Ali; Rupenthal, Ilva D.; Aboofazeli, Reza; Foroutan, Seyed Mohsen

2017-01-01

Brinzolamide (BZ) is an intraocular pressure reducing agent with low bioavailability. The purpose of the present study was to overcome this issue by development of BZ containing nanoemulsions (NEs) as an ocular drug delivery system with desirable therapeutic efficacy. Brinzolamide NEs were prepared by the spontaneous emulsification method. Based on initial release studies, twelve formulations with the slowest release characteristics were subjected to further physicochemical investigations such as particle size, polydispersity index, pH, refractive index, osmolality and viscosity. The therapeutic efficacy of these formulations was assessed by measuring the intraocular pressure after instillation of the prepared NEs in normotensive albino rabbit eyes. Nanoemulsions with suitable physicochemical properties exhibited high formulation stability under different conditions. more over biological evaluations indicated that using lower drug concentrations in NE formulations (0.4%) had a similar or even better pharmacodynamic effect compared to the commercial suspension with a higher drug concentration (1%). Our findings suggest that NEs could be effectively used as carriers for enhancing the bioavailability of topically applied ophthalmic drugs. PMID:29201076

Structural, physicochemical and antioxidant properties of sodium alginate isolated from a Tunisian brown seaweed.

PubMed

Sellimi, Sabrine; Younes, Islem; Ayed, Hanen Ben; Maalej, Hana; Montero, Veronique; Rinaudo, Marguerite; Dahia, Mostefa; Mechichi, Tahar; Hajji, Mohamed; Nasri, Moncef

2015-01-01

An original sodium alginate from Tunisian seaweed (Cystoseira barbata) was purified and characterized by circular dichroism (CD) and ATR-FTIR spectroscopies. ATR-FTIR spectrum of C. barbata sodium alginate (CBSA) showed the characteristic bands of mannuronic (M) and guluronic acids (G). The M/G ratio was estimated by CD (M/G = 0.59) indicating that CBSA was composed of 37% mannuronic acid and 63% guluronic acid. The analysis of viscosity of CBSA showed evidence of pseudoplastic fluid behaviour. The emulsifying capacity of CBSA was evaluated at different concentrations (0.25-3%), temperatures (25-100 °C) and pH (3.0-11.0). Compared to most commercial emulsifiers, the emulsion formulated by CBSA was found to be less sensitive to temperature changes and more stable at acidic pH. CBSA was examined for antioxidant properties using various antioxidant assays. CBSA exhibited important DPPH radical-scavenging activity (74% inhibition at a concentration of 0.5 mg/ml) and considerable ferric reducing potential. Effective hydroxyl-radical scavenging activity (82% at a concentration of 5 mg/ml) and potent protection activity against DNA breakage were also recorded for CBSA. However, in the linoleate-β-carotene system, CBSA exerted moderate antioxidant activity (60% at a concentration of 1.5 mg/ml). Therefore, CBSA can be used as a natural ingredient in food industry or in the pharmaceutical field. Copyright © 2014 Elsevier B.V. All rights reserved.

Mechanism for enhanced absorption of a solid dispersion formulation of LY2300559 using the artificial stomach duodenum model.

PubMed

Polster, Christopher S; Wu, Sy-Juen; Gueorguieva, Ivelina; Sperry, David C

2015-04-06

An artificial stomach duodenum (ASD) model has been used to demonstrate the performance difference between two formulations of LY2300559, a low-solubility acidic developmental drug. The two formulations investigated were a conventional high-shear wet granulation (HSWG) formulation and a solid dispersion formulation. A pharmacokinetic study in humans demonstrated the enhanced performance of the solid dispersion formulation relative to the HSWG formulation. The Cmax and AUC of the solid dispersion was 2.6 and 1.9 times greater, respectively, compared to the HSWG formulation. In the ASD, the solid dispersion formulation performance was characterized by three main phases: (1) rapid release in the stomach, creating a supersaturated concentration of drug, (2) precipitation in the stomach, and (3) rapid redissolution of the precipitate in the duodenum to concentration levels that are supersaturated relative to crystalline drug. A series of complementary experiments were employed to describe this performance behavior mechanistically. Imaging experiments with a pH indicating dye showed that local pH gradients from meglumine in the solid dispersion formulation were responsible for creating a high initial supersaturation concentration in the stomach. Upon dissipation of meglumine, the drug precipitated in the stomach as an amorphous solid. Because the precipitated drug is in an amorphous form, it can then rapidly redissolve as it transits to the more neutral environment of the duodenum. This unexpected sequence of physical state changes gives a mechanistic explanation for the enhanced in vivo performance of the solid dispersion formulation relative to the HSWG formulation.

Formulation effects on the mechanical and release properties of metronidazole suppositories.

PubMed

Adegboye, T A; Itiola, O A

2003-09-01

A study of the effects of Tween 20 and Tween 80 non-ionic surfactants, and witepsol H15 and polyethylene glycol (PEG) 2850 bases, on the mechanical and release properties of metronidazole suppositories was made. Mechanical strength was assessed by breaking strength values F. The values of F increased with increase in concentration of surfactant. The values of F for formulations containing Tween 20 were higher than those obtained for formulations containing Tween 80. Witepsol bases gave higher values of F than corresponding PEG bases. Release characteristics were assessed by the time for 80% drug release (t80), values of dissolution rate constants, k1 and k2 and the time of intersection, t1. The values of t80 decreased while those of k1 and k2 increased with increase in surfactant concentration. The values of t80 were lower, while those of k1 and k2 were higher, for formulations containing Tween 20 than for those formulations containing Tween 80. Witepsol bases gave lower t80 values and higher k1 and k2 values than their corresponding PEG bases. The concentration of surfactant, C, had the largest individual effect on the mechanical and release parameters while the nature of surfactant, S, had the lowest. The ranking for the individual effects of the variables on F and k1 was C > N > S, on t80 and k2 was C > N approximately = S, was on t1 was C = N = S. The interactions between S and C were largest for F, t80 and k2, and lowest for k1 and t1. The ranking of the interaction effects of the variables on F and k2 was S-C > N-C > N-S, on t80 was S-C > N-S approximately = N-C, on k1 was N-C > N-S > S-C, and on t1 was N-S = N-C > S-C. The results suggest that the individual and interaction effects of formulation variables would provide useful guides in optimizing metronidazole suppository formulations.

Emulsifying and Foaming Properties of Different Protein Fractions Obtained from a Novel Lupin Variety AluProt-CGNA(®) (Lupinus luteus).

PubMed

Burgos-Díaz, César; Piornos, José A; Wandersleben, Traudy; Ogura, Takahiro; Hernández, Xaviera; Rubilar, Mónica

2016-07-01

The use of vegetable proteins as food ingredient is becoming increasingly important due to their high versatility and environmental acceptability. This work describes a chemical characterization and techno-functional properties (emulsifying and foaming properties) of 3 protein fractions obtained from a protein-rich novel lupin variety, AluProt-CGNA(®) . This nongenetically modified variety have a great protein content in dehulled seeds (60.6 g protein/100 g, dry matter), which is higher than soybean and other lupin varieties. A simple procedure was utilized to obtain 3 different fractions by using alkali solubilization and isoelectric precipitation. Fractions 1 and 3 were mainly composed of protein and polysaccharides (NNE), whereas fraction 2 was mainly composed by protein (97%, w/w). Fraction 3 presented interesting and potential foaming properties in comparison to the other fractions evaluated in the study. Besides, its solubility, foaming and emulsifying capacity were practically not affected by pH variations. The 3 fractions also presented good emulsion stability, reaching values above a 95%. SDS-PAGE showed that fractions 1 and 2 contained mainly conglutin α, β, and δ, but in different ratios, whereas fraction 3 contained mainly conglutin γ and albumins. The results of this work will provide better understanding for the utilization of each protein fractions as potential ingredients in food industry. © 2016 Institute of Food Technologists®

Effect of pigment concentration on fastness and color values of thermal and UV curable pigment printing

NASA Astrophysics Data System (ADS)

Baysal, Gulcin; Kalav, Berdan; Karagüzel Kayaoğlu, Burçak

2017-10-01

In the current study, it is aimed to determine the effect of pigment concentration on fastness and colour values of thermal and ultraviolet (UV) curable pigment printing on synthetic leather. For this purpose, thermal curable solvent-based and UV curable water-based formulations were prepared with different pigment concentrations (3, 5 and 7%) separately and applied by screen printing technique using a screen printing machine. Samples printed with solvent-based formulations were thermally cured and samples printed with water-based formulations were cured using a UV curing machine equipped with gallium and mercury (Ga/Hg) lamps at room temperature. The crock fastness values of samples printed with solvent-based formulations showed that increase in pigment concentration was not effective on both dry and wet crock fastness values. On the other hand, in samples printed with UV curable water-based formulations, dry crock fastness was improved and evaluated as very good for all pigment concentrations. However, increasing the pigment concentration affected the wet crock fastness values adversely and lower values were observed. As the energy level increased for each irradiation source, the fastness values were improved. In comparison with samples printed with solvent-based formulations, samples printed with UV curable water-based formulations yielded higher K/S values at all pigment concentrations. The results suggested that, higher K/S values can be obtained in samples printed with UV curable water-based formulations at a lower pigment concentration compared to samples printed with solvent-based formulations.

Application of hanging drop technique to optimize human IgG formulations.

PubMed

Li, Guohua; Kasha, Purna C; Late, Sameer; Banga, Ajay K

2010-01-01

The purpose of this work is to assess the hanging drop technique in screening excipients to develop optimal formulations for human immunoglobulin G (IgG). A microdrop of human IgG and test solution hanging from a cover slide and undergoing vapour diffusion was monitored by a stereomicroscope. Aqueous solutions of IgG in the presence of different pH, salt concentrations and excipients were prepared and characterized. Low concentration of either sodium/potassium phosphate or McIlvaine buffer favoured the solubility of IgG. Addition of sucrose favoured the stability of this antibody while addition of NaCl caused more aggregation. Antimicrobial preservatives were also screened and a complex effect at different buffer conditions was observed. Dynamic light scattering, differential scanning calorimetry and size exclusion chromatography studies were performed to further validate the results. In conclusion, hanging drop is a very easy and effective approach to screen protein formulations in the early stage of formulation development.

Environmental relevant concentrations of a chlorpyrifos commercial formulation affect two neotropical fish species, Cheirodon interruptus and Cnesterodon decemmaculatus.

PubMed

Bonifacio, Alejo Fabian; Ballesteros, María Laura; Bonansea, Rocío Inés; Filippi, Iohanna; Amé, María Valeria; Hued, Andrea Cecilia

2017-12-01

The increase of cultivated areas together with the intensive use of pesticides have greatly contributed to impair the quality of aquatic systems along different areas of South America. The main goal of the present study was to assess the effects of a commercial formulation of chlorpyrifos at environmentally relevant concentrations on two native fish species, Cheirodon interruptus and Cnesterodon decemmaculatus. Adult individuals were exposed during 48 h to the following concentrations: 0.084 nl/l (Ci-Cf 1) and 0.84 nl/l (Ci-CF 2) in C. interruptus (Ci) of Clorfox (CF), and 0.84 nl/l (Cd-CF 1) and 8.4 nl/l (Cd-CF 2) in C. decemmaculatus (Cd). Fish behavior was evaluated through locomotor activity and space usage variables. The activity of acetylcholinesterase (AChE) in brain and muscle, catalase (CAT) and glutathione-S-transferase (GST) in brain, liver, muscle and gills, and aspartate amino-transferase (AST), alanine amino-transferase (ALT), AST/ALT ratio and alkaline phosphatase (ALP) in liver, were measured. Both locomotor activity and space usage varied between the two species studied and between CF treatments. The enzyme activities showed significant variations in CAT for C. interruptus and in CAT, GST, AChE, AST, and AST/ALT for C. decemmaculatus under the exposure conditions. Given that both species responded to CF and the concentrations we tested are environmentally relevant, the presence of this pesticide in freshwater systems could impose a risk for populations of both native fish studied at field. Copyright © 2017 Elsevier Ltd. All rights reserved.

Active immunization with GnRH-tandem-dimer peptide in young male rats reduces serum reproductive hormone concentrations, testicular development and spermatogenesis.

PubMed

Han, Xing-Fa; Li, Jun-Li; Zhou, Yu-Qin; Ren, Xiao-Hua; Liu, Gong-Cheng; Cao, Xiao-Han; Du, Xiao-Gang; Zeng, Xian-Yin

2016-01-01

GnRH sterilization vaccines have been developed for various practical and clinical reasons. However, conjugation of GnRH peptide to carrier protein has many drawbacks, hampering the further commercialization of GnRH vaccines. In this study, a new nonconjugated GnRH vaccine, D-Lys6-GnRH-tandem-dimer peptide (TDK), emulsified in Specol adjuvant was investigated for its immunocastration efficacy in young male rats. Prepubertal male rats were randomly allocated into three groups (n = 12): control (no treatment), surgically castrated or immunized against 100 μg TDK in Specol adjuvant at 6 weeks of age (with a booster 8 weeks later). Blood samples (for antibody titers and hormone concentrations) were collected at 2-week intervals until rats were killed (18 weeks of age). Compared to intact controls, active immunization against TDK reduced (P < 0.05) serum concentrations of testosterone, inhibin B, LH and FSH, prevented the onset of spermatogenesis at puberty. Furthermore, mRNA expressions of GnRH receptor, LH-β and FSH-β in the pituitary, LH receptor, FSH receptor, inhibin α, βA and βB subunit in the testes were decreased in immunocastrated rats compared to intact controls (P < 0.05). These results demonstrate for the first time that GnRH-tandem-dimer peptide emulsified in Specol is a promising veterinary sterilization medicine.

Emulsion of an in-situ surfactant in petroleum. Final report

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

Not Available

1983-12-01

Three emulsifiers were tested for their ability to reduce the viscosity of heavy oils. A reduction of 25% viscosity is achieved using polybutene. A reduction of 50% viscosity is achieved using a concentrated ionic detergent obtained from SANDOZ. The most promising emulsifiers is a lipopeptide. Preliminary studies show this emulsifier reduces the viscosity of heavy oils by as much as 80%. It is also able to reduce the surface tension of water by 35%. This emulsifier is also biodegradable and less toxic than synthetic surfactants. (DMC)

Pharmacodynamic comparison of two formulations of Acarbose 100-mg tablets.

PubMed

Lee, S; Chung, J Y; Hong, K S; Yang, S-H; Byun, S-Y; Lim, H-S; Shin, S-G; Jang, I-J; Yu, K-S

2012-10-01

Acarbose, an α-glycosidase inhibitor, is used to treat diabetic patients. Pharmacokinetic evaluation of acarbose is difficult because <2% is absorbed systemically. The current investigation evaluated the bioequivalence of two formulations of acarbose through pharmacodynamic comparison. This investigation consisted of a pilot study and a main study. The pilot study had an open, single-dose, single-sequence design. Subjects received placebo and then two tablets of reference formulation (Glucobay(®) 100 mg tablet; Bayer Healthcare) on two consecutive days with sucrose. The main study was an open, randomized, two-period, two-sequence crossover study. Subjects randomly received placebo and two tablets of either test formulation (generic acarbose 100-mg tablet) or reference formulation with sucrose on two consecutive days in the first period. In the second period, placebo and alternative formulation were administered. Serial blood samples for pharmacodynamic assessment were taken after each administration. The maximum serum glucose concentration (G(max)) and the area under the serum glucose concentration-time profile (AUC(gluc)) were determined and compared. Five subjects completed the pilot study. The AUC(gluc) from dosing until 1 h post-dose (AUC(gluc,1 h)) was significantly different between the placebo and acarbose. A total of 33 subjects completed the main study. The mean differences in G(max) (ΔG(max)) and AUC(gluc,1 h) (ΔAUC(gluc,1 h)) for the reference formulation compared with placebo were 22·0 ± 18·3 mg/dL and 928·2 ± 756·0 mg min/dL, respectively. The corresponding values for the test formulation were 23·3 ± 21·2 mg/dL and 923·0 ± 991·4 0 mg min/dL, respectively. The geometric mean ratios (GMRs) of the test formulation to the reference formulation for ΔG(max) and ΔAUC(gluc, 1 h) were 1·06 and 1·00, respectively, and the 90% confidence intervals (CIs) corresponding values were 0·79-1·39 and 0·64-1·36, respectively. The 90% CIs of GMRs

Preparation of Emulsifying Wax/GMO Nanoparticles and Evaluation as a Delivery System for Repurposing Simvastatin in Bone Regeneration.

PubMed

Eskinazi-Budge, Aaron; Manickavasagam, Dharani; Czech, Tori; Novak, Kimberly; Kunzler, James; Oyewumi, Moses O

2018-05-30

Simvastatin (Sim) is a widely known drug in the treatment of hyperlipidemia that has attracted so much attention in bone regeneration based on its potential osteoanabolic effect. However, repurposing of Sim in bone regeneration will require suitable delivery systems that can negate undesirable off-target/side effects. In this study, we have investigated a new lipid nanoparticle (NP) platform that was fabricated using a binary blend of emulsifying wax (Ewax) and glyceryl monooleate (GMO). Using the binary matrix materials, NPs loaded with Sim (0-500 µg/mL) were prepared and showed an average particle size of about 150 nm. NP size stability was dependent on Sim concentration loaded in NPs. The suitability of NPs prepared with the binary matrix materials in Sim delivery for potential application in bone regeneration was supported by biocompatibility in pre-osteoclastic and pre-osteoblastic cells. Additional data demonstrated that biofunctional Sim was released from NPs that facilitated differentiation of osteoblasts (cells that form bones) while inhibiting differentiation of osteoclasts (cells that resorb bones). The overall work demonstrated the preparation of NPs from Ewax/GMO blends and characterization to ascertain potential suitability in Sim delivery for bone regeneration. Additional studies on osteoblast and osteoclast functions are warranted to fully evaluate the efficacy simvastatin-loaded Ewax/GMO NPs using in-vitro and in-vivo approaches.

Microbial biodiversity of Tang and Pirgal mud volcanoes and evaluation of bio-emulsifier and bio-demulsifier activities of Capnophile bacteria.

PubMed

Parsia, Yasaman; Sorooshian, Shahryar

2017-12-01

The data presented in this article is related to the Master thesis; entitled "Survey Aerobic Microbial Diversity Mud Volcanoes in Chabahar and Khash Ports in Southern Iran" by the first author of this article, year 2011, Islamic Azad University, Iran (reference number (Parsia, 2011) [1] of this article). This article shows microbial biodiversity and evaluates bio-emulsifier and bio-demulsifier abilities of capnophile isolates, in order to introduce a superior isolate for the Microbial Enhanced Oil Recovery (MEOR) process in the petrochemical industry.

A Two and Half-Year-Performance Evaluation of a Field Test on Treatment of Source Zone Tetrachloroethene and Its Chlorinated Daughter Products Using Emulsified Zaro Valent Iron Nanoparticles

EPA Science Inventory

A field test of emulsified zero valent iron (EZVI) nanoparticles was conducted at Parris Island, SC, USA and was monitored for two and half years to assess the treatment of subsurface-source zone chlorinated volatile organic compounds (CVOCs) dominated by tetrachloroethene (PCE) ...

Effect of processing on functional properties of animal blood plasma.

PubMed

Del Hoyo, P; Rendueles, M; Díaz, M

2008-04-01

A number of functional and physical properties such as solubility, foam capacity, emulsifying stability and interfacial tension were compared for standard plasma, plasma decationed by ion exchange and plasma deionized by ultrafiltration (UF). The changes in functional properties can determine the use of a protein as an additive to a food product or invalidate its use. All samples had good functional properties and hence could be used in the formulation of food products. Results showed that ion exchange and UF improved emulsifying capacity while having little effect on the other functional properties.

Microsphere based improved sunscreen formulation of ethylhexyl methoxycinnamate.

PubMed

Gogna, Deepak; Jain, Sunil K; Yadav, Awesh K; Agrawal, G P

2007-04-01

Polymethylmethacrylate (PMMA) microspheres of ethylhexyl methoxycinnamate (EHM) were prepared by emulsion solvent evaporation method to improve its photostability and effectiveness as sunscreening agent. Process parameters like stirring speed and aqueous polyvinyl alcohol (PVA) concentration were analyzed in order to optimize the formulations. Shape and surface morphology of the microspheres were examined using scanning electron microscopy. Particle size of the microspheres was determined using laser diffraction particle size analyzer. The PMMA microspheres of EHM were incorporated in water-removable cream base. The in vitro drug release of EHM in pH 7.4 was performed using dialysis membrane. Thin layer chromatography was performed to determine photostability of EHM inside the microspheres. The formulations were evaluated for sun protection factor (SPF) and minimum erythema dose (MED) in albino rats. Cream base formulation containing microspheres prepared using EHM:PMMA in ratio of 1:3 (C(3)) showed slowest drug (EHM) release and those prepared with EHM: PMMA in ratio of 1:1 showed fastest release. The cream base formulations containing EHM loaded microspheres had shown better SPF (more than 16.0) as compared to formulation C(d) that contained 3% free EHM as sunscreen agent and showed SPF 4.66. These studies revealed that the incorporation of EHM loaded PMMA microspheres into cream base had greatly increased the efficacy of sunscreen formulation approximately four times. Further, photostability was also shown to be improved in PMMA microspheres.

Feeding deterrent and growth inhibitory activities of PONNEEM, a newly developed phytopesticidal formulation against Helicoverpa armigera (Hubner)

PubMed Central

Packiam, Soosaimanickam Maria; Baskar, Kathirvelu; Ignacimuthu, Savarimuthu

2014-01-01

Objective To assess the feeding deterrent, growth inhibitory and egg hatchability effects of PONNEEM on Helicoverpa armigera (H. armigera). Methods Five oil formulations were prepared at different ratios to assess the feeding deterrent, growth inhibitory and egg hatchability effects on H. armigera. Results Invariably all the newly formulated phytopesticidal oil formulations showed the feeding deterrent and growth inhibitory activities against H. armigera. The maximum feeding deterrent activity of 88.44% was observed at 15 µL/L concentration of PONNEEM followed by formulation A (74.54%). PONNEEM was found to be effective in growth inhibitory activities and egg hatchability at 10 µL/L concentration. It exhibited statistically significant feeding deterrent activity and growth inhibitory activity compared with all the other treatments. Conclusions PONNEEM was found to be effective phytopesticidal formulation to control the larval stage of H. armigera. This is the first report for the feeding deterrent activity of PONNEEM against H. armigera. This newly formulated phytopesticide was patented in India. PMID:25183105

Preparation of ophthalmic formulations containing cilostazol as an anti-glaucoma agent and improvement in its permeability through the rabbit cornea.

PubMed

Okamoto, Norio; Ito, Yoshimasa; Nagai, Noriaki; Murao, Takatoshi; Takiguchi, Yusuke; Kurimoto, Takuji; Mimura, Osamu

2010-01-01

To evaluate the pharmacological properties of cilostazol (CLZ), we examined its intraocular pressure (IOP) -lowering effect. CLZ is an inhibitor of Type III phosphodiesterase that increases intracellular cyclic AMP levels by restraining platelet aggregation, and has a potential protective effect against atherosclerosis. We attempted to apply it for use as an anti-glaucoma agent; however, the application of CLZ in the ophthalmic field is limited due to its poor water solubility. We attempted to enhance CLZ solubility using 2-hydroxypropyl-beta-cyclodextrin (HPbetaCD). The solubility of CLZ increased with increasing HPbetaCD concentrations, and 0.05% CLZ was dissolved in 10% HPbetaCD. Moreover, fine particle suspension of 0.5% CLZ in 5% HPbetaCD (soluble CLZ: ca. 0.027%) were prepared using a Microfluidizer, an impact-type emulsifying comminution device. In an in vitro transcorneal penetration experiment through the rabbit cornea, the CLZ penetration rate was dependent on the CLZ content of the solutions and suspensions. When a 0.05% CLZ ophthalmic solution was instilled into a rabbit eye, the absorption rate constant for CLZ into an aqueous humor was 0.0059+/-0.001 min(-1), and the elimination rate constant was 0.048+/-0.024 min(-1). Also CLZ ophthalmic solutions and fine particle suspension were examined to for their ability to reduce enhanced intraocular pressure (IOP) of rabbits in a darkroom. The instillation of 0.05% CLZ ophthalmic solutions and 0.5% CLZ fine particle suspensions into rabbit eyes reduced the enhanced IOP. These results demonstrate that the instillation of CLZ ophthalmic solutions and fine particle suspensions may represent an effective anti-glaucoma formulation.

Biopharmaceutical formulations for pre-filled delivery devices.

PubMed

Jezek, Jan; Darton, Nicholas J; Derham, Barry K; Royle, Nikki; Simpson, Iain

2013-06-01

Pre-filled syringes are becoming an increasingly popular format for delivering biotherapeutics conveniently and cost effectively. The device design and stable liquid formulations required to enable this pre-filled syringe format are technically challenging. In choosing the materials and process conditions to fabricate the syringe unit, their compatibility with the biotherapeutic needs to be carefully assessed. The biothereaputic stability demanded for the production of syringe-compatible low-viscosity liquid solutions requires critical excipient choices to be made. The purpose of this review is to discuss key issues related to the stability aspects of biotherapeutics in pre-filled devices. This includes effects on both physical and chemical stability due to a number of stress conditions the product is subjected to, as well as interactions with the packaging system. Particular attention is paid to the control of stability by formulation. We anticipate that there will be a significant move towards polymer primary packaging for most drugs in the longer term. The timescales for this will depend on a number of factors and hence will be hard to predict. Formulation will play a critical role in developing successful products in the pre-filled syringe format, particularly with the trend towards concentrated biotherapeutics. Development of novel, smart formulation technologies will, therefore, be increasingly important.

Formulation and Evaluation of Mouth Dissolving Tablets of Cinnarizine

PubMed Central

Patel, B. P.; Patel, J. K.; Rajput, G. C.; Thakor, R. S.

2010-01-01

The purpose of this research was to develop mouth dissolve tablets of cinnarizine by effervescent, superdisintegrant addition and sublimation methods. All the three formulations were evaluated for disintegration time, hardness and friability, among these superdisintegrant addition method showed lowest disintegration time; hence it was selected for further studies. Further nine batches (B1-B9) were prepared by using crospovidone, croscarmellose sodium and L-HPC in different concentrations such as 5, 7.5 and 10%. All the formulations were evaluated for weight variation, hardness, friability, drug content, in vitro disintegration time, wetting time, in vitro dissolution. Formulation with 10% L-HPC showed the less disintegration time (25.3 s) and less wetting time (29.1 s). In vitro dissolution studies showed total drug release at the end of 6 min. PMID:21218071

Experimental evaluation of oxygen-enriched air and emulsified fuels in a six-cylinder diesel engine

NASA Astrophysics Data System (ADS)

Sekar, R. R.; Marr, W. W.; Cole, R. L.; Marciniak, T. J.; Longman, D. E.

1993-01-01

The objectives of this investigation are to (1) determine the technical feasibility of using oxygen-enriched air to increase the efficiency of and reduce emissions from diesel engines, (2) examine the effects of water-emulsified fuel on the formation of nitrogen oxides in oxygen-enriched combustion, and (3) investigate the use of lower-grade fuels in high-speed diesel engines by emulsifying the fuel with water. These tests, completed on a Caterpillar model 3406B, six-cylinder engine are a scale-up from previous, single-cylinder-engine tests. The engine was tested with (1) intake-air oxygen levels up to 30%, (2) water content up to 20% of the fuel, (3) three fuel-injection timings, and (4) three fuel-flow rates (power levels). The Taguchi technique for experimental design was used to minimize the number of experimental points in the test matrix. Four separate test matrices were run to cover two different fuel-flow-rate strategies and two different fuels (No. 2 diesel and No. 6 diesel). A liquid-oxygen tank located outside the test cell supplied the oxygen for the tests. The only modification of the engine was installation of a pressure transducer in one cylinder. All tests were run at 1800 rpm, which corresponds to the synchronous speed of a 60-Hz generator. Test results show that oxygen enrichment results in power increases of 50% or more while significantly decreasing the levels of smoke and particulates emitted. The increase in power was accompanied by a small increase in thermal efficiency. Maximum engine power was limited by the test-cell dynamometer capacity and the capacity of the fuel-injection pump. Oxygen enrichment increases nitrogen-oxide emissions significantly. No adverse effects of oxygen enrichment on the turbocharger were observed. The engine operated successfully with No. 6 fuel, but it operated at a lower thermal efficiency and emitted more smoke and particulates than with No. 2 fuel.

[Glyphosate and its formulations--toxicity, occupational and environmental exposure].

PubMed

Kwiatkowska, Marta; Paweł, Jarosiewicz; Bukowska, Bozena

2013-01-01

Glyphosate (N-(phosphonomethyl)glycine) is an active ingredient of the most widely used herbicide formulations in protecting agricultural and horticultural crops. Numerous results (mostly published in the years 2010-2013) concerning the action of glyphosate and its formulations in the recent decade were analyzed. Initial reports about alleged biodegradability of glyphosate in the environment turned out to be wrong. It has been shown that glyphosate remains in the soil and can reach people by spreading along with groundwater. Recent publications have shown that glyphosate is detected at low concentrations in the human blood. Publications cited in this article, which indicate a possible induction of neoplastic changes by glyphosate formulation, have raised great concern and controversy in the scientific world. Presenting adverse effects of glyphosate and its formulations we focused on the role of glyphosate formulations in hormonal disorders by impeding the expression of steroidogenic acute regulatory protein and the inhibition of aromatase activity. The impact of glyphosate on oxygen reactive species formation, changes in redox system and the effect on necrosis and apoptosis in various types of cells was shown. We also revealed that glyphosate as a phosphonate herbicide does not inhibit directly the activity of acetylcholinesterase. Based on numerous studies it was noted that commercial formulations of glyphosate exhibit higher toxicity than that of the active substance itself. The discussed problems clearly show the need to evaluate the toxicity of glyphosate and its formulations and related potential threat to humans.

Laboratory evaluation of lambda-cyhalothrin a microencapsulated formulation on mosquito nets for control of vector mosquitos.

PubMed

Vythilingam, I; Zainal, A R; Hamidah, T

1999-03-01

Two formulations of lambda-cyhalothrin (EC-Emulsion concentrate and MC-Microencapsulated) were impregnated into bednets made of polyethylene and polyester. The nets were treated at a dosage of 15 mg/m2. For bioassay of insecticidal efficacy, female Anopheles maculatus and Aedes aegypti were exposed to the nets for two minutes and mortality was scored 24 hours later. The nets were also tested after repeated washings with water and with soap and water. Microencapsulated (2.5CS) formulation was more effective than emulsion concentrate (2.5EC) formulation on both net materials--polyethylene and polyester. Repeated washing with water and soap reduces the efficacy of all bednet treatment combinations. Microencapsulated formulation on polyethylene gave best results; it could sustain up to five washes with water and two with soap and water.

Retaining Oxidative Stability of Emulsified Foods by Novel Nonmigratory Polyphenol Coated Active Packaging.

PubMed

Roman, Maxine J; Decker, Eric A; Goddard, Julie M

2016-07-13

Oxidation causes lipid rancidity, discoloration, and nutrient degradation that decrease shelf life of packaged foods. Synthetic additives are effective oxidation inhibitors, but are undesirable to consumers who prefer "clean" label products. The aim of this study was to improve oxidative stability of emulsified foods by a novel nonmigratory polyphenol coated active packaging. Polyphenol coatings were applied to chitosan functionalized polypropylene (PP) by laccase assisted polymerization of catechol and catechin. Polyphenol coated PP exhibited both metal chelating (39.3 ± 2.5 nmol Fe(3+) cm(-2), pH 4.0) and radical scavenging (up to 52.9 ± 1.8 nmol Trolox eq cm(-2)) capacity, resulting in dual antioxidant functionality to inhibit lipid oxidation and lycopene degradation in emulsions. Nonmigratory polyphenol coated PP inhibited ferric iron promoted degradation better than soluble chelators, potentially by partitioning iron from the emulsion droplet interface. This work demonstrates that polyphenol coatings can be designed for advanced material chemistry solutions in active food packaging.

Cellulose nanofibers from banana peels as a Pickering emulsifier: High-energy emulsification processes.

PubMed

Costa, Ana Letícia Rodrigues; Gomes, Andresa; Tibolla, Heloisa; Menegalli, Florencia Cecilia; Cunha, Rosiane Lopes

2018-08-15

Cellulose nanofibers (CNFs) from banana peels was evaluated as promising stabilizer for oil-in-water emulsions. CNFs were treated using ultrasound and high-pressure homogenizer. Changes on the size, crystallinity index and zeta potential of CNFs were associated with the intense effects of cavitation phenomenon and shear forces promoted by mechanical treatments. CNFs-stabilized emulsions were produced under the same process conditions as the particles. Coalescence phenomenon was observed in the emulsions produced using high-pressure homogenizer, whereas droplets flocculation occurred in emulsions processed by ultrasound. In the latter, coalescence stability was associated with effects of cavitation forces acting on the CNFs breakup. Thus, smaller droplets created during the ultrasonication process could be recovered by particles that acted as an effective barrier against droplets coalescence. Our results improved understanding about the relationship between the choice of emulsification process and their effects on the CNFs properties influencing the potential application of CNFs as a food emulsifier. Copyright © 2018 Elsevier Ltd. All rights reserved.

Gastroretentive behavior of orally administered radiolabeled tamarind seed formulations in rabbits validated by gamma scintigraphy.

PubMed

Razavi, Mahboubeh; Karimian, Hamed; Yeong, Chai Hong; Fadaeinasab, Mehran; Khaing, Si Lay; Chung, Lip Yong; Mohamad Haron, Didi Erwandi B; Noordin, Mohamed Ibrahim

2017-01-01

This study aimed to formulate floating gastroretentive tablets containing metformin hydrochloric acid (HCl), using various grades of hydrogel such as tamarind powders and xanthan to overcome short gastric residence time of the conventional dosage forms. Different concentrations of the hydrogels were tested to determine the formulation that could provide a sustained release of 12 h. Eleven formulations with different ratios of tamarind seed powder/tamarind kernel powder (TKP):xanthan were prepared. The physical parameters were observed, and in vitro drug-release studies of the prepared formulations were carried out. Optimal formulation was assessed for physicochemical properties, thermal stability, and chemical interaction followed by in vivo gamma scintigraphy study. MKP3 formulation with a TKP:xanthan ratio of 3:2 was found to have 99.87% release over 12 h. Furthermore, in vivo gamma scintigraphy study was carried out for the optimized formulation in healthy New Zealand White rabbits, and the pharmacokinetic parameters of developed formulations were obtained. 153 Sm 2 O 3 was used to trace the profile of release in the gastrointestinal tract of the rabbits, and the drug release was analyzed. The time ( T max ) at which the maximum concentration of metformin HCl in the blood ( C max ) was observed, and it was extended four times for the gastroretentive formulation in comparison with the formulation without polymers. C max and the half-life were found to be within an acceptable range. It is therefore concluded that MKP3 is the optimal formulation for sustained release of metformin HCl over a period of 12 h as a result of its floating properties in the gastric region.

Gastroretentive behavior of orally administered radiolabeled tamarind seed formulations in rabbits validated by gamma scintigraphy

PubMed Central

Razavi, Mahboubeh; Karimian, Hamed; Yeong, Chai Hong; Fadaeinasab, Mehran; Khaing, Si Lay; Chung, Lip Yong; Mohamad Haron, Didi Erwandi B; Noordin, Mohamed Ibrahim

2017-01-01

This study aimed to formulate floating gastroretentive tablets containing metformin hydrochloric acid (HCl), using various grades of hydrogel such as tamarind powders and xanthan to overcome short gastric residence time of the conventional dosage forms. Different concentrations of the hydrogels were tested to determine the formulation that could provide a sustained release of 12 h. Eleven formulations with different ratios of tamarind seed powder/tamarind kernel powder (TKP):xanthan were prepared. The physical parameters were observed, and in vitro drug-release studies of the prepared formulations were carried out. Optimal formulation was assessed for physicochemical properties, thermal stability, and chemical interaction followed by in vivo gamma scintigraphy study. MKP3 formulation with a TKP:xanthan ratio of 3:2 was found to have 99.87% release over 12 h. Furthermore, in vivo gamma scintigraphy study was carried out for the optimized formulation in healthy New Zealand White rabbits, and the pharmacokinetic parameters of developed formulations were obtained. 153Sm2O3 was used to trace the profile of release in the gastrointestinal tract of the rabbits, and the drug release was analyzed. The time (Tmax) at which the maximum concentration of metformin HCl in the blood (Cmax) was observed, and it was extended four times for the gastroretentive formulation in comparison with the formulation without polymers. Cmax and the half-life were found to be within an acceptable range. It is therefore concluded that MKP3 is the optimal formulation for sustained release of metformin HCl over a period of 12 h as a result of its floating properties in the gastric region. PMID:28031701

Comparative toxicity of two glyphosate-based formulations to Eisenia andrei under laboratory conditions.

PubMed

Piola, Lucas; Fuchs, Julio; Oneto, María Luisa; Basack, Silvana; Kesten, Eva; Casabé, Norma

2013-04-01

Glyphosate-based products are the leading post-emergent agricultural herbicides in the world, particularly in association with glyphosate tolerant crops. However, studies on the effects of glyphosate-based formulations on terrestrial receptors are scarce. This study was conducted to evaluate the comparative toxicity of two glyphosate-based products: Roundup FG (monoammonium salt, 72% acid equivalent, glyphosate-A) and Mon 8750 (monoammonium salt, 85.4% acid equivalent, glyphosate-B), towards the earthworm Eisenia andrei. Median lethal concentration (LC50) showed that glyphosate-A was 4.5-fold more toxic than glyphosate-B. Sublethal concentrations caused a concentration-dependent weight loss, consistent with the reported effect of glyphosate as uncoupler of oxidative phosphorylation. Glyphosate-A showed deleterious effects on DNA and lysosomal damage at concentrations close to the applied environmental concentrations (14.4 μg ae cm(-2)). With glyphosate-B toxic effects were observed at higher doses, close to its LC50, suggesting that the higher toxicity of formulate A could be attributed to the effects of some of the so-called "inert ingredients", either due to a direct intrinsic toxicity, or to an enhancement in the bioavailability and/or bioaccumulation of the active ingredient. Our results highlight the importance of ecotoxicological assessment not only of the active ingredients, but also of the different formulations usually employed in agricultural practices. Copyright © 2012 Elsevier Ltd. All rights reserved.

Commercial formulations of Bacillus thuringiensis for control of Indian meal moth.

PubMed Central

Schesser, J H

1976-01-01

Doses of four commercial formulations and one experimental formulation of Bacillus thuringiensis Berliner were mixed with the diet used to rear colonies of the Indian meal moth Plodia interpunctella (Hübner). Indian meal moth eggs were introduced to the treated diet, and the resultant adult emergence was tabulated. The experimental formulations ranked as follows in efficacy in controlling the Indian meal moth: Dipel (50% lethal concentration [LC50], 25 mg/kg) greater than Bactospeine WP (LC50, 100 mg/kg) greater than Thuricide (LC50, 150 mg/kg) greater than IMC 90007 (LC30, 180 mg/kg) greater than Bactospeine Flowable (LC50, 440 mg/kg). PMID:984828

Commercial formulations of Bacillus thuringiensis for control of Indian meal moth.

PubMed

Schesser, J H

1976-10-01

Doses of four commercial formulations and one experimental formulation of Bacillus thuringiensis Berliner were mixed with the diet used to rear colonies of the Indian meal moth Plodia interpunctella (Hübner). Indian meal moth eggs were introduced to the treated diet, and the resultant adult emergence was tabulated. The experimental formulations ranked as follows in efficacy in controlling the Indian meal moth: Dipel (50% lethal concentration [LC50], 25 mg/kg) greater than Bactospeine WP (LC50, 100 mg/kg) greater than Thuricide (LC50, 150 mg/kg) greater than IMC 90007 (LC30, 180 mg/kg) greater than Bactospeine Flowable (LC50, 440 mg/kg).

Thermoreversible gel formulation containing sodium lauryl sulfate as a potential contraceptive device.

PubMed

Haineault, Caroline; Gourde, Pierrette; Perron, Sylvie; Désormeaux, André; Piret, Jocelyne; Omar, Rabeea F; Tremblay, Roland R; Bergeron, Michel G

2003-08-01

The contraceptive properties of a gel formulation containing sodium lauryl sulfate were investigated in both in vitro and in vivo models. Results showed that sodium lauryl sulfate inhibited, in a concentration-dependent manner, the activity of sheep testicular hyaluronidase. Sodium lauryl sulfate also completely inhibited human sperm motility as evaluated by the 30-sec Sander-Cramer test. The acid-buffering capacity of gel formulations containing sodium lauryl sulfate increased with the molarity of the citrate buffers used for their preparations. Furthermore, experiments in which semen was mixed with undiluted gel formulations in different proportions confirmed their physiologically relevant buffering capacity. Intravaginal application of the gel formulation containing sodium lauryl sulfate to rabbits before their artificial insemination with freshly ejaculated semen completely prevented egg fertilization. The gel formulation containing sodium lauryl sulfate was fully compatible with nonlubricated latex condoms. Taken together, these results suggest that the gel formulation containing sodium lauryl sulfate could represent a potential candidate for use as a topical vaginal spermicidal formulation to provide fertility control in women.

Combined high-power ultrasound and high-pressure homogenization nanoemulsification: The effect of energy density, oil content and emulsifier type and content.

PubMed

Calligaris, Sonia; Plazzotta, Stella; Valoppi, Fabio; Anese, Monica

2018-05-01

Combinations of ultrasound (US) and high-pressure homogenization (HPH) at low-medium energy densities were studied as alternative processes to individual US and HPH to produce Tween 80 and whey protein stabilized nanoemulsions, while reducing the energy input. To this aim, preliminary trials were performed to compare emulsification efficacy of single and combined HPH and US treatments delivering low-medium energy densities. Results highlighted the efficacy of US-HPH combined process in reducing the energy required to produce nanoemulsions stabilized with both Tween 80 and whey protein isolate. Subsequently, the effect of emulsifier content (1-3% w/w), oil amount (10-20% w/w) and energy density (47-175 MJ/m 3 ) on emulsion mean particle diameter was evaluated by means of a central composite design. Particles of 140-190 nm were obtained by delivering 175 MJ/m 3 energy density at emulsions containing 3% (w/w) Tween 80 and 10% (w/w) oil. In the case of whey protein isolate stabilized emulsions, a reduced emulsifier amount (1% w/w) and intermediate energy density (120 MJ/m 3 ) allowed a minimum droplet size around 220-250 nm to be achieved. Results showed that, in both cases, at least 50% of the energy density should be delivered by HPH to obtain the minimum particle diameter. Copyright © 2018 Elsevier Ltd. All rights reserved.

Fabrication, characterization, and evaluation of microsponge delivery system for facilitated fungal therapy

PubMed Central

Moin, Afrasim; Deb, Tamal K.; Osmani, Riyaz Ali M.; Bhosale, Rohit R.; Hani, Umme

2016-01-01

Objective: The rationale behind present research vocation was to develop and investigate a novel microsponge based gel as a topical carrier for the prolonged release and cutaneous drug deposition of fluconazole (FLZ); destined for facilitated fungal therapy. Materials and Methods: Microsponges were prepared using quasi-emulsion solvent diffusion method using Eudragit S-100. In the direction of optimization, the effect of formulation variables (drug-polymer ratio and amount of emulsifier) and diverse factors affecting physical characteristics of microsponge were investigated as well. Fabricated microsponges were characterized by differential scanning calorimetry, Fourier transform-infrared, scanning electron microscopy (SEM), particle size analysis, and also evaluated for drug content, encapsulation efficiency, in vitro drug release and in vitro antifungal activity. Results: Compatibility studies results reflected no sign of any chemical interaction between the drug and polymers used. Whereas, varied drug-polymer ratios and emulsifier concentration indicated significant effect on production yield, drug content, encapsulation efficiency, particle size and drug release. Spherical microsponges with a porous surface and 29.327 ± 0.31 μm mean particle size were evident from SEM micrographs. In vitro release outcomes, from microsponge loaded gels depicted that F1 formulation was more efficient to give extended drug release of 85.38% at the end of 8 h, while conventional formulation by releasing 83.17% of drug got exhausted incredibly earlier at the end of 4 h merely. Moreover, microsponge gels demonstrated substantial spreadability and extrudability along with promising antifungal activity. Conclusions: Fabricated microsponges would be impending pharmaceutical topical carriers of FLZ and a leading alternative to conventional therapy for efficient, safe and facilitated eradication of fungal infections. PMID:27057125

Effect of new Vacutainer blood collection tubes on plasma lidocaine concentrations.

PubMed

Lopez, L M; Sen, A; Robinson, J D; Curry, R W

1987-12-01

This study was designed to establish whether plasma lidocaine concentrations changed subsequent to contact with a new formulation of rubber-stopper Vacutainer collection tubes. Plasma lidocaine concentrations from blood samples exposed to rubber stoppers for one hour were compared with concentrations from blood samples which were not exposed to rubber stoppers. Plasma lidocaine concentrations remained essentially unchanged following one-hour exposure to Vacutainer rubber stoppers. The new formulation of "red-top" Vacutainer may be used reliably in lidocaine therapeutic drug monitoring.

Comparative bioavailability of two formulations of sibutramine.

PubMed

Franco Spínola, A C; Almeida, S; Filipe, A; Neves, R; Abolfathi, Z; Yritia, M; Anctil, D

2009-10-01

This study was conducted in order to compare the bioavailability of two capsule formulations containing 15 mg of sibutramine, N-{1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl}-N,N-dimethylamine hydrochloride monohydrate, 84485-00-7 CAS registry number. 62 healthy subjects were enrolled in a single-center, randomized, single-dose, open-label, 2-way crossover study, with a minimum washout period of 14 days. Plasma samples were collected up to 72.0 hours post-dosing. R-sibutramine, S-sibutramine, N-mono-desmethyl-sibutramine (M1) and N-di-desmethyl-sibutramine (M2) levels were determined by reverse liquid chromatography and detected by tandem mass spectrometry detection, LC/MS/MS method. Pharmacokinetic parameters used for bioequivalence assessment were the area under the concentration-time curve from time zero to time of last non-zero concentration (AUC0-t) and the maximum observed concentration (Cmax). These parameters were determined from sibutramine enantiomers as well from M1 and M2 concentration data using non-compartmental analysis. The 90% confidence intervals obtained by analysis of variance were 89.25 - 122.88% for Cmax, 90.37 - 123.18% for AUC0-t and 91.20 - 122.38% for AUCinf for R-sibutramine and 88.27 - 124.08% for Cmax, 86.15 - 121.78% for AUC0-t and 88.02 - 120.96% for AUCinf for S-sibutramine. These results were all within the range of 80.00 - 125.00% established by regulatory requirements. Bioequivalence between formulations was concluded both in terms of rate and extent of absorption.

Design, formulation, and evaluation of ginger medicated chewing gum

PubMed Central

Aslani, Abolfazl; Ghannadi, Alireza; Rostami, Farnaz

2016-01-01

Background: Various ginger compounds improve gastrointestinal problems and motion sickness. The main effects of ginger allocate to some phenolics such as gingerols and shogaols that act as their active agents. Chewing gums are among convenient dosage forms which patients prefer due to their advantages. Hence, this study tried to design, formulate, and evaluate ginger chewing gum of favorable taste and texture to avoid motion sickness and have gastro-protective and anti-oxidant effect. Materials and Methods: Dried ginger rhizomes were percolated to extract ginger compounds. Total phenolics were measured in 70% hydro-alcoholic extract of ginger by gallic and tannic acid standards using Folin–Ciocalteu’s reagent. Chewing gums containing 50 mg of concentrated extract were prepared. Content uniformity, weight variation, release pattern, organoleptic, and mechanical properties were evaluated. Results: Phenolic content was measured 61.50 ± 5.27 mg/g and 76.75 ± 5.45 mg/g of concentrated extract as gallic acid and tannic acid equivalents, respectively. Release pattern of formulations with different gum bases and sweeteners demonstrated almost 100% release of drug. Evaluation of organoleptic properties was on 10 healthy volunteers and later prepared formulations exhibited better characteristics. Formulations without any flavorants have higher acceptability. Evaluation of mechanical properties showed higher stiffness of F15. Conclusion: Ginger chewing gum comprises admissible properties to be used as a modern drug delivery system due to its advantageous results in motion sickness. It passed all the specified tests for an acceptable chewing gum. Thus, it may be successfully produced to help GI problems. PMID:27563640

Persistence of two neem formulations on peach leaves and fruit: effect of the distribution.

PubMed

Sarais, Giorgia; Angioni, Alberto; Lai, Francesco; Cabras, Paolo; Caboni, Pierluigi

2009-03-25

Persistence of azadirachtins (A+B) and of the other limonoids (nimbin, salannin, deacetylnimbin, and deacetylsalannin) on peach leaves and fruits was studied using a commercial formulation (form. C) compared with an experimental formulation (form. E) prepared with coformulations allowed in organic culture. Field experiments were carried out using three concentrations: 1x, 5x, and 10x the dose recommended by the manufacturer. The EU maximum residue level (MRL) in fruits and vegetables for azadirachtin A is 1 mg/kg with a preharvest interval (PHI) of 3 days. At the recommended dose, azadirachtin A residue on fruits was not detectable (LOQ < 0.8 microg/kg). After field treatment at the 5x concentration, azadirachtoids were found with 22% in the epicuticular waxes and the remaining 78% on the fruit surface. No residues were found in the fruit pulp. The experimental formulation (E) produced lower residues on leaves and fruit compared with the commercial formulation (C), although formulation E showed greater stability. This is probably due to the amount of the active ingredients that diffuse into the epicuticular wax layer thus enhancing photostability of azadirachtoids.

Infrared study of structural characteristics of Frankfurters formulated with olive oil-in-water emulsions stabilized with casein as pork backfat replacer.

PubMed

Carmona, P; Ruiz-Capillas, C; Jiménez-Colmenero, F; Pintado, T; Herrero, A M

2011-12-28

This article reports an infrared spectroscopic (FT-IR) study on lipids and protein structural characteristics in frankfurters as affected by an emulsified olive oil stabilizing system used as a pork backfat replacer. The oil-in-water emulsions were stabilized with sodium caseinate, without (F/SC) and with microbial transglutaminase (F/SC+MTG). Proximate composition and textural characteristics were also evaluated. Frankfurters F/SC+MTG showed the highest (P < 0.05) hardness and lowest (P < 0.05) adhesiveness. These products also showed the lowest (P < 0.05) half-bandwidth of the 2922 cm(-1) band, which could be related to the fact that the lipid chain was more orderly than that in the frankfurters formulated with animal fat and F/SC. The spectral results revealed modifications in the amide I band profile when the olive oil-in-water emulsion replaced animal fat. This fact is indicative of a greater content of aggregated intermolecular β-sheets. Structural characteristics in both proteins and lipids could be associated with the specific textural properties of frankfurters.

Comparative applications of azadirachtin- and Brevibacillus laterosporus-based formulations for house fly management experiments in dairy farms.

PubMed

Ruiu, L; Satta, A; Floris, I

2011-03-01

The potential of two bioinsecticidal formulations containing Brevibacillus laterosporus spores and azadirachtin, respectively, was assayed in laboratory and in comparative field treatments for the management of immature house flies on dairy farms. As already known for B. laterosporus, preliminary laboratory experiments with azadirachtin evidenced a concentration-dependent effect. Azadirachtin median lethal concentration (LC50) value determined for second instar larvae was 24.5 microg/g diet. Applications in dairy farms were performed at dosages and concentrations predetermined in laboratory experiments, to employ the two formulations at an equal insecticidal potential. Repeated applications on the cow pen caused a significant fly development depression in areas treated with azadirachtin (63%) and B. laterosporus (46%), compared with the control. Formulations were applied at a dosage of 3 liters/m2, and concentrations of 2 x 10(8) B. laterosporus spores/ml and 25 microg azadirachtin/ml, respectively.

Modified formulation of CPDA for storage of whole blood, and of SAGM for storage of red blood cells, to maintain the concentration of 2,3-diphosphoglycerate.

PubMed

Kurup, P A; Arun, P; Gayathri, N S; Dhanya, C R; Indu, A R

2003-11-01

A dramatic decrease in the level of 2,3-diphosphoglycerate (2,3-DPG) takes place during the storage of whole blood (WB) in CPDA (citrate-phosphate-dextrose-adenine) and a similar decrease occurs during the storage of red blood cells (RBCs) in SAGM (saline-adenine-glucose-mannitol). The aim of the present study was to prevent this decrease by modifying CPDA and SAGM. The pH of WB anticoagulant or RBC preservative solution was maintained at 7.6 by autoclaving the dextrose solution separately, by incorporating ascorbic acid and nicotinic acid into both CPDA and SAGM (to produce modified CPDA and SAGM solutions), and by reducing the concentration of adenine and adding citrate to the modified SAGM solution. The concentration of 2,3-DPG in WB after 28 days of storage in modified CPDA, and in RBCs stored in modified SAGM, was compared with that in WB or RBCs stored in unmodified solutions. The initial 2,3-DPG levels were maintained after 28 days in the modified formulations [10.63 +/- 2.58 microM/g of haemoglobin (Hb) in the case of modified CPDA and 12.07 +/- 1.47 microM/g of Hb in the case of modified SAGM], whereas in standard CPDA and SAGM solutions, the concentration of 2,3-DPG decreased to very low levels (0.86 +/- 0.97 microM/g Hb for CPDA and 0.12 +/- 0.008 for SAGM). Our modification in the formulation of CPDA or SAGM is effective in arresting the dramatic decrease in the level of 2,3-DPG that occurs during storage of WB and RBCs in unmodified solutions.

Lipolysis of the semi-solid self-emulsifying excipient Gelucire 44/14 by digestive lipases.

PubMed

Fernandez, Sylvie; Rodier, Jean-David; Ritter, Nicolas; Mahler, Bruno; Demarne, Frédéric; Carrière, Frédéric; Jannin, Vincent

2008-08-01

Gelucire 44/14 is a semi-solid self-emulsifying excipient used for the oral delivery of poorly water-soluble drugs. It is composed of C8-C18 acylglycerols and PEG-32 esters, all of which are potential substrates for digestive lipases. Here we studied the lipolysis of Gelucire 44/14 by porcine pancreatic extracts, human pancreatic juice and several purified digestive lipases. Human pancreatic lipase (HPL), the main lipase involved in the digestion of triacylglycerols, did not show any significant activity on Gelucire 44/14 or on either of its individual compounds, C8-C18 acylglycerols and PEG-32 esters. Other pancreatic lipases such as human pancreatic lipase-related protein 2 (HPLRP2) showed low activity on Gelucire 44/14 although the highest activity of HPLRP2 was that observed on the C8-C18 acylglycerol fraction, which accounts for 20% (w/w) of Gelucire 44/14. In addition, HPLRP2 showed low activities on the PEG-32 esters, whether these were tested individually or mixed together. Carboxyl ester hydrolase (CEH) showed high activity on Gelucire 44/14, and the highest activities of CEH were those recorded on the total PEG-32 ester fraction and on each individual PEG-32 ester, except for PEG-32 monostearate. The highest activity of all the enzymes tested was that of dog gastric lipase (DGL) on Gelucire 44/14, although DGL showed low activity on the PEG-32 ester fraction and on each individual PEG-32 ester. We compared the lipolysis of Gelucire 44/14 with that of Labrasol, another self-emulsifying excipient, which is liquid at room temperature. Human pancreatic juice showed similar rates of activity on both Gelucire 44/14 and Labrasol. This finding means that these excipients are hydrolyzed in vivo during pancreatic digestion, mainly by CEH in the case of Gelucire 44/14 and by both HPLRP2 and CEH in that of Labrasol, whereas HPL showed very low activities on each of these two excipients. This is the first time the effects of PEG and acyl chain length on the lipolytic

Nanoemulsion as pharmaceutical carrier for dermal and transdermal drug delivery: Formulation development, stability issues, basic considerations and applications.

PubMed

Rai, Vineet Kumar; Mishra, Nidhi; Yadav, Kuldeep Singh; Yadav, Narayan Prasad

2018-01-28

The use of nanoemulsion in augmenting dermal and transdermal effectiveness of drugs has now well established. The development of nanoemulsion based semisolid dosage forms is an active area of present research. However, thickening or liquid-to-semisolid conversion of the nanoemulsions provides opportunities to the formulation scientist to explore novel means of solving instability issues during transformation. Extending knowledge about the explicit role of nature/magnitude of zeta potential, types of emulsifiers and selection of appropriate semisolid bases could place these versatile carriers from laboratory to industrial scale. This article reviews the progressive advancement in the delivery of medicament via nanoemulsion with special reference to the dermal and transdermal administration. It is attempted to explore the most suitable semi solid dosage form for the particular type of nanoemulsion (o/w, w/o and others) and effect of particle size and zeta potential on the delivery of drugs through dermal or transdermal route. Finally, this review also highlights the basic principles and fundamental considerations of nanoemulsion manufacture, application of nanoemulsion based semisolid dosage forms in the dermal/transdermal administration and basic considerations during the nanoemulsion absorption into and through skin. Copyright © 2017 Elsevier B.V. All rights reserved.

Effect of a labile methyl donor on the transformation of 5-demethyltangeretin and the related implication on bioactivity.

PubMed

Ting, Yuwen; Li, Colin C; Pan, Min-Hsiung; Ho, Chi-Tang; Huang, Qingrong

2013-08-28

Polymethoxyflavones (PMFs) belong to a subgroup of flavonoids that particularly exist in the peels of citrus fruits. Despite their many health-beneficial biofunctionalities, the lipophilic nature of PMFs limits their water solubility and oral bioavailability. To investigate the effect of the delivery system on the improvement of PMF bioavailibility, a lecithin-based emulsion was formulated for the delivery of two PMF compounds, tangeretin and 5-demethyltangeretin. While the emulsion system improved the digestion kinetics and the total solubilized PMF concentrations in in vitro lipolysis studies, the concentration of 5-demethyltangeretin decreased due to chemical transformation to its permethoxylated counterpart, tangeretin. The emulsifier lecithin used in this emulsion formulation contained a choline headgroup as a labile methyl group donor. The presence of a methyl donor potentially caused the transformation of 5-demethyltangeretin and reduced its anti-cancer-cell-proliferation activities. Moreover, this is the first report in the literature of the transformation from 5-demethyltangeretin to tangeretin in a lecithin-based emulsion during lipolysis, and the mechanism underlying this phenomenon has also been proposed for the first time.

Field and Laboratory Responses of Male Leaf Roller Moths, Choristoneura rosaceana and Pandemis pyrusana, to Pheromone Concentrations in an Attracticide Paste Formulation

PubMed Central

Curkovic, Tomislav; Brunner, Jay F.; Landolt, Peter J.