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Sample records for lipid nanoemulsion resembling

  1. Metabolism of a Lipid Nanoemulsion Resembling Low-Density Lipoprotein in Patients with Grade III Obesity

    PubMed Central

    Dantas, Simone Alves; Ficker, Elisabeth Salvatori; Vinagre, Carmen G. C.; Ianni, Barbara Maria; Maranhão, Raul Cavalcante; Mady, Charles

    2010-01-01

    INTRODUCTION: Obesity increases triglyceride levels and decreases high-density lipoprotein concentrations in plasma. Artificial emulsions resembling lipidic plasma lipoprotein structures have been used to evaluate low-density lipoprotein metabolism. In grade III obesity, low density lipoprotein metabolism is poorly understood. OBJECTIVE: To evaluate the kinetics with which a cholesterol-rich emulsion (called a low-density emulsion) binds to low-density lipoprotein receptors in a group of patients with grade III obesity by the fractional clearance rate. METHODS: A low-density emulsion was labeled with [14C]-cholesterol ester and [3H]-triglycerides and injected intravenously into ten normolipidemic non-diabetic patients with grade III obesity [body mass index higher than 40 kg/m2] and into ten non-obese healthy controls. Blood samples were collected over 24 hours to determine the plasma decay curve and to calculate the fractional clearance rate. RESULTS: There was no difference regarding plasma levels of total cholesterol or low-density lipoprotein cholesterol between the two groups. The fractional clearance rate of triglycerides was 0.086 ± 0.044 in the obese group and 0.122 ± 0.026 in the controls (p = 0.040), and the fractional clearance rate of cholesterol ester (h−1) was 0.052 ± 0.021 in the obese subjects and 0.058 ± 0.015 (p = 0.971) in the controls. CONCLUSION: Grade III obese subjects exhibited normal low-density lipoprotein removal from plasma as tested by the nanoemulsion method, but triglyceride removal was slower. PMID:20126342

  2. Tocopheryl acetate nanoemulsions stabilized with lipid-polymer hybrid emulsifiers for effective skin delivery.

    PubMed

    Nam, Yoon Sung; Kim, Jin-Woong; Park, Jaeyoon; Shim, Jongwon; Lee, Jong Suk; Han, Sang Hoon

    2012-06-01

    Tocopheryl acetate is used as the oil component of nanoemulsions using a mixture of unsaturated phospholipids and polyethylene oxide-block-poly(ε-caprolactone) (PEO-b-PCL). This study investigates the effects of the lipid-polymer composition on the size and surface charge of nanoemulsions, microviscosity of the interfacial layer, and skin absorption of tocopheryl acetate. The lipid-polymer hybrid system exhibits excellent colloidal dispersion stability, which is comparable to that of polymer-based nanoemulsions. If lipids are used as emulsifiers, nanoemulsions show poor dispersion stability despite a good skin absorption enhancing effect. The amount of tocopheryl acetate absorbed by the skin increases with an increased lipid-to-polymer ratio, as determined using the hairless guinea pig skin loaded in a Franz-type diffusion cell. An 8:2 (w/w) mixture of unsaturated phospholipids and PEO-b-PCL exhibits the most efficient delivery of tocopheryl acetate into the skin. Our results show that tocopheryl acetate is absorbed almost twice as fast by the lipid-polymer hybrid system than the nanoemulsions stabilized with PEO-b-PCL. This study suggests that the lipid-polymer hybrid system can be used as an effective means of optimizing nanoemulsions in terms of dispersion stability and skin delivery capability.

  3. Anti-inflammatory effects of intravenous methotrexate associated with lipid nanoemulsions on antigen-induced arthritis

    PubMed Central

    Mello, Suzana B V; Tavares, Elaine R; Guido, Maria Carolina; Bonfá, Eloisa; Maranhão, Raul C

    2016-01-01

    OBJECTIVE: To test the hypothesis that intravenous use of methotrexate associated with lipid nanoemulsions can achieve superior anti-inflammatory effects in the joints of rabbits with antigen-induced arthritis compared with commercial methotrexate. METHODS: Arthritis was induced in New Zealand rabbits sensitized with methylated bovine serum albumin and subsequently intra-articularly injected with the antigen. A nanoemulsion of methotrexate labeled with 3H-cholesteryl ether (4 mg/kg methotrexate) was then intravenously injected into four rabbits to determine the plasma decaying curves and the biodistribution of the methotrexate nanoemulsion by radioactive counting. Additionally, the pharmacokinetics of the methotrexate nanoemulsion were determined by high-pressure liquid chromatography. Twenty-four hours after arthritis induction, the animals were allocated into three groups, with intravenous injection with saline solution (n=9), methotrexate nanoemulsion (0.5 µmol/kg methotrexate, n=7), or commercial methotrexate (0.5 µmol/kg, n=4). The rabbits were sacrificed 24 h afterward. Synovial fluid was then collected for protein leakage and cell content analyses and synovial membranes were collected for histopathological analysis. RESULTS: The methotrexate nanoemulsion was taken up mainly by the liver and the uptake by arthritic joints was two-fold greater than that by control joints. The methotrexate nanoemulsion treatment reduced leukocyte influx into the synovial fluid by nearly 65%; in particular, mononuclear and polymorphonuclear cells were reduced by 47 and 72%, respectively. In contrast, cell influx was unaffected following treatment with commercial methotrexate. Protein leakage into the arthritic knees of the rabbits was also more limited following methotrexate nanoemulsion treatment than following commercial methotrexate treatment. CONCLUSIONS: The intravenous methotrexate nanoemulsion showed anti-inflammatory effects on the synovia of arthritic joints that were

  4. Simulation of fusion-mediated nanoemulsion interactions with model lipid bilayers

    PubMed Central

    Lee, Sun-Joo; Schlesinger, Paul H.; Wickline, Samuel A.; Lanza, Gregory M.; Baker, Nathan A.

    2012-01-01

    Perfluorocarbon-based nanoemulsion particles have become promising platforms for the delivery of therapeutic and diagnostic agents to specific target cells in a non-invasive manner. A “contact-facilitated” delivery mechanism has been proposed wherein the emulsifying phospholipid monolayer on the nanoemulsion surface contacts and forms a lipid complex with the outer monolayer of target cell plasma membrane, allowing cargo to diffuse to the surface of target cell. While this mechanism is supported by experimental evidence, its molecular details are unknown. The present study develops a coarse-grained model of nanoemulsion particles that are compatible with the MARTINI force field. Simulations using this coarse-grained model have demonstrated multiple fusion events between the particles and a model vesicular lipid bilayer. The fusion proceeds in the following sequence: dehydration at the interface, close apposition of the particles, protrusion of hydrophobic molecules to the particle surface, transient lipid complex formation, absorption of nanoemulsion into the liposome. The initial monolayer disruption acts as a rate-limiting step and is strongly influenced by particle size as well as by the presence of phospholipids supporting negative spontaneous curvature. The core-forming perfluorocarbons play critical roles in initiating the fusion process by facilitating protrusion of hydrophobic moieties into the interface between the two particles. This study directly supports the hypothesized nanoemulsion delivery mechanism and provides the underlying molecular details that enable engineering of nanoemulsions for a variety of medical applications. PMID:22712024

  5. Enhancement of indocyanine green stability and cellular uptake by incorporating cationic lipid into indocyanine green-loaded nanoemulsions.

    PubMed

    Lee, Eun-Hye; Kim, Jin-Ki; Lim, Joon-Seok; Lim, Soo-Jeong

    2015-12-01

    Indocyanine green (ICG) is a near-infrared optical dye approved by the Food and Drug Administration. ICG has been investigated as a simultaneous color and fluorescence-imaging tracer for the intraoperative identification of sentinel lymph nodes, but its use has recently expanded to include application as a photosensitizer for the local photodynamic/thermal treatment of identified lymph node metastases. The current study was designed to develop an ICG-loaded nanoemulsion as an effective agent for both the diagnosis and treatment of lymph node metastases. Incorporating the cationic lipid stearylamine (SA) together with ICG in the shell of nanoemulsions did not affect the loaded ICG concentration, but changed the surface charge of nanoemulsions from a negative to a positive value and improved the physical stability of nanoemulsions. Loading ICG into SA-incorporated nanoemulsions more effectively blocked the aggregation and degradation of ICG compared to loading in SA-free nanoemulsions. SA incorporation also enhanced tumor cell uptake of ICG-loaded nanoemulsions, resulting in greater cell killing upon light irradiation. After subcutaneous injection into the footpad of mice, SA-incorporated nanoemulsions increased the concentration of ICG accumulated in popliteal lymph nodes to a greater extent than SA-free nanoemulsions without affecting the kinetics of lymph node uptake of nanoemulsions. These multiple beneficial effects of incorporating SA in nanoemulsions are likely attributable to the electrostatic interaction between anionic ICG and cationic SA, as well as the change in the nanoemulsion surface charge from negative to positive. Our findings indicate that SA-incorporated nanoemulsions are promising ICG carriers for combined diagnosis and treatment of lymph node metastases.

  6. In vitro lipid peroxidation of intestinal bile salt-based nanoemulsions: potential role of antioxidants.

    PubMed

    Courraud, J; Charnay, C; Cristol, J P; Berger, J; Avallone, S

    2013-12-01

    Over the last decades, oxidative stress has been described as a deleterious phenomenon contributing to numerous noncommunicable diseases such as cardiovascular disease, diabetes, and cancers. As many authors ascribed the healthy effect of fruit and vegetable consumption mainly to their antioxidant contents, it has been hypothesized that their protection could occur from the gut. Therefore, the aim of this study was to develop an original and physiological model of nanoemulsions to study lipid peroxidation within the intestine and to assess the properties of potential antioxidants in this setting. Several nanoemulsions were compared in terms of physical characteristics and reactivity to 2,2'-azobis-(2-amidinopropane) hydrochloride (AAPH)-induced oxidation. Formulations included different types of lipids, a detergent (a conjugated bile salt or sodium dodecyl sulfate) and, finally, lipophilic antioxidants. Hemin and myoglobin were also tested as relevant potential oxidants. Fatty acid (FA) peroxidation was monitored by gas chromatography while malondialdehyde and antioxidant contents were measured by HPLC. Investigated nanoemulsions were composed of spherical or cylindrical mixed micelles, the latter being the least resistant to oxidation. In the experimental conditions, AAPH was the only efficient oxidant. Alpha-tocopherol and lutein significantly slowed FA degradation from 4 to 1 μM, respectively. On the contrary, beta-carotene did not show any protective capacity at 4 μM. In conclusion, the tested nanoemulsions were appropriate to assess antioxidant capacity during the intestinal phase of digestion.

  7. Plasma kinetics of an LDL-like nanoemulsion and lipid transfer to HDL in subjects with glucose intolerance

    PubMed Central

    Bertato, Marina P; Oliveira, Carolina P; Wajchenberg, Bernardo L; Lerario, Antonio C; Maranhão, Raul C

    2012-01-01

    OBJECTIVE: Glucose intolerance is frequently associated with an altered plasma lipid profile and increased cardiovascular disease risk. Nonetheless, lipid metabolism is scarcely studied in normolipidemic glucose-intolerant patients. The aim of this study was to investigate whether important lipid metabolic parameters, such as the kinetics of LDL free and esterified cholesterol and the transfer of lipids to HDL, are altered in glucose-intolerant patients with normal plasma lipids. METHODS: Fourteen glucose-intolerant patients and 15 control patients were studied; none of the patients had cardiovascular disease manifestations, and they were paired for age, sex, race and co-morbidities. A nanoemulsion resembling a LDL lipid composition (LDE) labeled with 14C-cholesteryl ester and 3H-free cholesterol was intravenously injected, and blood samples were collected over a 24-h period to determine the fractional clearance rate of the labels by compartmental analysis. The transfer of free and esterified cholesterol, triglycerides and phospholipids from the LDE to HDL was measured by the incubation of the LDE with plasma and radioactivity counting of the supernatant after chemical precipitation of non-HDL fractions. RESULTS: The levels of LDL, non-HDL and HDL cholesterol, triglycerides, apo A1 and apo B were equal in both groups. The 14C-esterified cholesterol fractional clearance rate was not different between glucose-intolerant and control patients, but the 3H-free- cholesterol fractional clearance rate was greater in glucose-intolerant patients than in control patients. The lipid transfer to HDL was equal in both groups. CONCLUSION: In these glucose-intolerant patients with normal plasma lipids, a faster removal of LDE free cholesterol was the only lipid metabolic alteration detected in our study. This finding suggests that the dissociation of free cholesterol from lipoprotein particles occurs in normolipidemic glucose intolerance and may participate in atherogenic

  8. P-Selectin Targeted Dexamethasone-Loaded Lipid Nanoemulsions: A Novel Therapy to Reduce Vascular Inflammation

    PubMed Central

    Simion, Viorel; Constantinescu, Cristina Ana; Stan, Daniela; Deleanu, Mariana; Tucureanu, Monica Madalina; Butoi, Elena; Manduteanu, Ileana; Simionescu, Maya

    2016-01-01

    Inflammation is a common process associated with numerous vascular pathologies. We hypothesized that targeting the inflamed endothelium by coupling a peptide with high affinity for P-selectin to the surface of dexamethasone-loaded lipid nanoemulsions will highly increase their specific binding to activated endothelial cells (EC) and reduce the cell activation. We developed and characterized dexamethasone-loaded lipid nanoemulsions directed towards P-selectin (PLN-Dex) and monitored their anti-inflammatory effects in vitro using cultured EC (EA.hy926 cells) and in vivo using a mouse model of acute inflammation [lipopolysaccharides (LPS) intravenously administered in C57BL/6 mice]. We found that PLN-Dex bound specifically to the surface of activated EC are efficiently internalized by EC and reduced the expression of proinflammatory genes, thus preventing the monocyte adhesion and transmigration to/through activated EC. Given intravenously in mice with acute inflammation, PLN-Dex accumulated at a significant high level in the lungs (compared to nontargeted nanoemulsions) and significantly reduced mRNA expression level of key proinflammatory cytokines such as IL-1β, IL-6, and MCP-1. In conclusion, the newly developed nanoformulation, PLN-Dex, is functional in vitro and in vivo, reducing selectively the endothelium activation and the consequent monocyte infiltration and diminishing significantly the lungs' inflammation, in a mouse model of acute inflammation. PMID:27703301

  9. Enhancement of Nutraceutical Bioavailability using Excipient Nanoemulsions: Role of Lipid Digestion Products on Bioaccessibility of Carotenoids and Phenolics from Mangoes.

    PubMed

    Liu, Xuan; Bi, Jinfeng; Xiao, Hang; McClements, David Julian

    2016-03-01

    The ability of excipient nanoemulsions to increase the bioaccessibility of different kinds of nutraceuticals (phenolics and carotenoids) in mangoes was studied. Oil-in-water excipient nanoemulsions containing small digestible lipid nanoparticles (d < 200 nm) were prepared using different oil phases: medium chain triglycerides (MCT) and long-chain triglycerides (LCT). These nanoemulsions were then mixed with pureed mango and passed through a simulated gastrointestinal tract (GIT): mouth, stomach, and small intestine. Carotenoid bioaccessibility decreased in the following order: LCT nanoemulsions > MCT nanoemulsions > buffer solution, which was attributed to differences in the solubilization capacity of the mixed micelles generated in the intestinal fluids. The digestion products of LCT formed mixed micelles with hydrophobic domains large enough to accommodate the carotenoids, whereas those of MCT did not. Excipient emulsions had much less effect on phenolic bioaccessibility, which may be because phenolics are smaller more polar molecules and are therefore more easily solubilized in aqueous intestinal fluids. These results highlight the potential of excipient nanoemulsions in boosting the bioavailability of lipophilic bioactive agents in fruits and vegetables. PMID:26816342

  10. Enhancement of Nutraceutical Bioavailability using Excipient Nanoemulsions: Role of Lipid Digestion Products on Bioaccessibility of Carotenoids and Phenolics from Mangoes.

    PubMed

    Liu, Xuan; Bi, Jinfeng; Xiao, Hang; McClements, David Julian

    2016-03-01

    The ability of excipient nanoemulsions to increase the bioaccessibility of different kinds of nutraceuticals (phenolics and carotenoids) in mangoes was studied. Oil-in-water excipient nanoemulsions containing small digestible lipid nanoparticles (d < 200 nm) were prepared using different oil phases: medium chain triglycerides (MCT) and long-chain triglycerides (LCT). These nanoemulsions were then mixed with pureed mango and passed through a simulated gastrointestinal tract (GIT): mouth, stomach, and small intestine. Carotenoid bioaccessibility decreased in the following order: LCT nanoemulsions > MCT nanoemulsions > buffer solution, which was attributed to differences in the solubilization capacity of the mixed micelles generated in the intestinal fluids. The digestion products of LCT formed mixed micelles with hydrophobic domains large enough to accommodate the carotenoids, whereas those of MCT did not. Excipient emulsions had much less effect on phenolic bioaccessibility, which may be because phenolics are smaller more polar molecules and are therefore more easily solubilized in aqueous intestinal fluids. These results highlight the potential of excipient nanoemulsions in boosting the bioavailability of lipophilic bioactive agents in fruits and vegetables.

  11. Consequences of lipidic nanoemulsions on membrane integrity and ultrastructural morphology of Staphylococcus aureus

    NASA Astrophysics Data System (ADS)

    Singh, Neeru; Manaswita Verma, Saurabh; Singh, Sandeep Kumar; Ranjan Prasad Verma, Priya

    2014-04-01

    The present study divulges the consequences of lipidic nanoemulsions (cationized and non-cationized) on morphology and membrane integrity of Staphylococcus aureus using transmission electron microscopy, scanning electron microscopy (SEM) and atomic force microscopy (AFM). Transmission electron microscopic (TEM) images reveal that the cationized lipidic emulsions (CLEs) remained adhered even after the hostile treatment to remove nanoemulsions by centrifugation owing to electrostatic attraction between CLE and negatively charged bacterial surface. TEM images portray the extensive cell lyses owing to the release of cytoplasmic content when treated with both CLE and Non-CLE (NCLE). The AFM analysis of the NCLE and CLE treated S. aureus cells showed the root mean square roughness of 11.3 ± 2.8 nm and 17.7 ± 3.2 nm, respectively. The complete losses of bacterial colonies after 45 min of contact with NCLE were observed. No viable bacterial colonies were noticeable after 10 min of contact when treated with CLE, indicating better rate of killing with respect to NCLE. Similar results were obtained in the zone of inhibition studies. Significant (p < 0.05) increase of cytoplasmic material was observed both in NCLE (0.192 ± 0.003) and CLE (0.308 ± 0.012) as compared to control (0.019 ± 0.002). The present finding illustrates that the NCLE and CLE had caused significant membrane disorganization leading to release of cytoplasmic content causing irreversible cell damage, which is in accordance with the TEM, SEM and AFM studies.

  12. Behavior of vitamin E acetate delivery systems under simulated gastrointestinal conditions: lipid digestion and bioaccessibility of low-energy nanoemulsions.

    PubMed

    Mayer, Sinja; Weiss, Jochen; McClements, David Julian

    2013-08-15

    Colloidal delivery systems are needed to incorporate oil-soluble vitamins into aqueous-based foods and beverage products. In this study, we encapsulated vitamin E acetate into oil-in-water nanoemulsions produced using either a low-energy method (Emulsion Phase Inversion, EPI) or a high energy method (microfluidization). Oil-in-water nanoemulsions (d<200 nm) could be produced using both low- and high-energy methods from a non-ionic surfactant (Tween 80) and medium chain triglycerides (MCTs). The influence of surfactant-to-oil ratio (SOR) on lipid digestion and vitamin bioaccessibility of EPI nanoemulsions was determined using a gastrointestinal tract (GIT) model that simulated the mouth, stomach, and small intestine. There were increases in the size and negative charge of the oil droplets after passage through the GIT, which was attributed to droplet coalescence and changes in interfacial composition. The rate and extent of lipid digestion decreased with increasing surfactant concentration, but the bioaccessibility of vitamin E acetate was high in all of the samples (>95%). No appreciable influence of the preparation method (low-energy versus high-energy) on lipid digestion and vitamin bioaccessibility was observed. The major advantage of the EPI method for forming nanoemulsions is that no expensive equipment is required, but relatively high surfactant concentrations are needed compared to microfluidization. PMID:23721832

  13. The preparation of magnetically guided lipid based nanoemulsions using self-emulsifying technology

    NASA Astrophysics Data System (ADS)

    Bakandritsos, Aristides; Zboril, Radek; Bouropoulos, Nikolaos; Kallinteri, Paraskevi; Favretto, Marco E.; Parker, Terry L.; Mullertz, Anette; Fatouros, Dimitrios G.

    2010-02-01

    This paper reports an easy and highly reproducible preparation route, using self-emulsifying technology, for an orally administered high quality magnetically responsive drug delivery system. Hydrophobic iron oxide nanoparticles of about 5 nm in diameter were prepared and incorporated into the lipid core of the produced oil droplets of a self-nanoemulsifying drug delivery system (MagC18/SNEDDS). The produced nanoemulsion exhibits colloidal stability at high ionic strengths and temperatures. The observed value of the saturation magnetization at 2 K is ≈4.1 emu g-1. The nanoemulsion displayed the magnetic properties of a non-interacting assembly of superparamagnetic particles and a low blocking temperature. Moreover the effect of MagC18/SNEDDS on biological systems in vitro was investigated in rodent fibroblasts (3T3 cells). The cytotoxicity studies show that none of the formulations tested affected cell activity significantly over the 24 h incubation. Such systems might have a potential use for oral delivery of poorly soluble compounds by extending the residence time of the formulation in the small intestine resulting in increased drug absorption values.

  14. The preparation of magnetically guided lipid based nanoemulsions using self-emulsifying technology.

    PubMed

    Bakandritsos, Aristides; Zboril, Radek; Bouropoulos, Nikolaos; Kallinteri, Paraskevi; Favretto, Marco E; Parker, Terry L; Mullertz, Anette; Fatouros, Dimitrios G

    2010-02-01

    This paper reports an easy and highly reproducible preparation route, using self-emulsifying technology, for an orally administered high quality magnetically responsive drug delivery system. Hydrophobic iron oxide nanoparticles of about 5 nm in diameter were prepared and incorporated into the lipid core of the produced oil droplets of a self-nanoemulsifying drug delivery system (MagC(18)/SNEDDS). The produced nanoemulsion exhibits colloidal stability at high ionic strengths and temperatures. The observed value of the saturation magnetization at 2 K is approximately 4.1 emu g(-1). The nanoemulsion displayed the magnetic properties of a non-interacting assembly of superparamagnetic particles and a low blocking temperature. Moreover the effect of MagC(18)/SNEDDS on biological systems in vitro was investigated in rodent fibroblasts (3T3 cells). The cytotoxicity studies show that none of the formulations tested affected cell activity significantly over the 24 h incubation. Such systems might have a potential use for oral delivery of poorly soluble compounds by extending the residence time of the formulation in the small intestine resulting in increased drug absorption values. PMID:20032554

  15. Coencapsulated doxorubicin and bromotetrandrine lipid nanoemulsions in reversing multidrug resistance in breast cancer in vitro and in vivo.

    PubMed

    Cao, Xi; Luo, Jingwen; Gong, Tao; Zhang, Zhi-Rong; Sun, Xun; Fu, Yao

    2015-01-01

    Multidrug resistance has remained a major cause of treatment failure in chemotherapy due to the presence of P-glycoproteins (P-gp) that actively pump drugs from inside the cell to the outside. P-gp inhibitors were developed and coadministered with chemotherapeutic drugs to overcome the effect of efflux pumps thus enhancing the chemosensitivity of therapeutics. Our study aimed at developing a lipid nanoemulsion system for the coencapsulation of doxorubicin (DOX) and bromotetrandrine (W198) to reverse multidrug resistance (MDR) in breast cancer. W198 was a potent P-gp inhibitor, and DOX was selected as a model compound which is a common substrate for P-gp. Coencapsulated DOX and W198 lipid nanoemulsions (DOX/W198-LNs) displayed significantly enhanced cytotoxicity in DOX-resistant human breast cancer cells (MCF-7/ADR) compared with DOX loaded lipid nanoemulsions (DOX-LNs) (p < 0.05), which is due to the enhanced intracellular uptake of DOX in MCF-7/ADR cells. The biodistribution study was performed using a nude mice xenograft model, which demonstrates enhanced tumor uptake of DOX in the DOX/W198-LN treated group. Compared with DOX solution, DOX/W198-LNs showed reduced cardiac toxicity and gastrointestinal injury in rats. Taken together, DOX/W198-LNs represent a promising formulation for overcoming MDR in breast cancer. PMID:25469833

  16. Functional nanoemulsion-hybrid lipid nanocarriers enhance the bioavailability and anti-cancer activity of lipophilic diferuloylmethane

    NASA Astrophysics Data System (ADS)

    Sun, Lili; Wan, Kun; Hu, Xueyuan; Zhang, Yonghong; Yan, Zijun; Feng, Jiao; Zhang, Jingqing

    2016-02-01

    The purpose of this study was to assess the enhanced physicochemical characteristics, in vitro release behavior, anti-lung cancer activity, gastrointestinal absorption, in vivo bioavailability and bioequivalence of functional nanoemulsion-hybrid lipid nanocarriers containing diferuloylmethane (DNHLNs). The DNHLNs were first fabricated by loading water-in-oil nanoemulsions into hybrid lipid nanosystems using nanoemulsion-thin film-sonication dispersion technologies. The in situ absorption and in vitro and in vivo kinetic features of DNHLNs were measured using an in situ unidirectional perfusion method, a dynamic dialysis method and a plasma concentration-time profile-based method, respectively. The cytotoxic effects of DNHLNs in lung adenocarcinoma A549 cells were examined using MTT colorimetric analysis. The absorptive constants and permeabilities of DNHLNs in four gastrointestinal sections increased by 1.43-3.23 times and by 3.10-7.76 times that of diferuloylmethane (DIF), respectively. The relative bioavailability of DNHLNs to free DIF was 855.02%. DNHLNs inhibited cancer cell growth in a time- and dose-dependent manner. DNHLNs markedly improved the absorption and bioavailability of DIF after oral administration. DNHLNs had stronger inhibitory effects on the viability of A549 cells than that of free DIF. DNHLNs might be potentially promising nanocarriers for DIF delivery via the oral route to address unmet clinical needs.

  17. Nanoemulsions (NEs), liposomes (LPs) and solid lipid nanoparticles (SLNs) for retinyl palmitate: effect on skin permeation.

    PubMed

    Clares, Beatriz; Calpena, Ana C; Parra, Alexander; Abrego, Guadalupe; Alvarado, Helen; Fangueiro, Joana F; Souto, Eliana B

    2014-10-01

    The aim of this study was to develop biocompatible lipid-based nanocarriers for retinyl palmitate (RP) to improve its skin delivery, photostability and biocompatibility, and to avoid undesirable topical side effects. RP loaded nanoemulsions (NEs), liposomes (LPs) and solid lipid nanoparticles (SLNs) were characterized in terms of size, surface electrical charge, pH, drug encapsulation efficiency and morphology. Spherical-shaped nanocarriers with a negatively charged surface (>|40|mV) and mean size lower than 275 nm were produced with adequate skin compatibility. The rheological properties showed that aqueous dispersions of SLNs followed a non-Newtonian behavior, pseudoplastic fluid adjusted to Herschel-Bulkley equation, whereas LPs and NEs exhibited a Newtonian behavior. SLNs offered significantly better photoprotection than LPs and NEs for RP. The cumulative amount of drug permeated through human skin at the end of 38 h was 6.67 ± 1.58 μg, 4.36 ± 0.21 μg and 3.64 ± 0.28 μg for NEs, LPs and SLNs, respectively. NEs flux was significantly higher than SLNs and LPs: NEs (0.37 ± 0.12 μg/h) > LPs (0.15 ± 0.09 μg/h) > SLNs (0.10 ± 0.05 μg/h). LPs offered significant higher skin retention than NEs and SLNs. Finally, even though all developed nanocarriers were found to be biocompatible, according to histological studies, NE was the system that most disrupted the skin. These encouraging findings can guide in proper selection of topical carriers among the diversity of available lipid-based nanocarriers, especially when a dermatologic or cosmetic purpose is desired. PMID:25102113

  18. Nanoemulsions (NEs), liposomes (LPs) and solid lipid nanoparticles (SLNs) for retinyl palmitate: effect on skin permeation.

    PubMed

    Clares, Beatriz; Calpena, Ana C; Parra, Alexander; Abrego, Guadalupe; Alvarado, Helen; Fangueiro, Joana F; Souto, Eliana B

    2014-10-01

    The aim of this study was to develop biocompatible lipid-based nanocarriers for retinyl palmitate (RP) to improve its skin delivery, photostability and biocompatibility, and to avoid undesirable topical side effects. RP loaded nanoemulsions (NEs), liposomes (LPs) and solid lipid nanoparticles (SLNs) were characterized in terms of size, surface electrical charge, pH, drug encapsulation efficiency and morphology. Spherical-shaped nanocarriers with a negatively charged surface (>|40|mV) and mean size lower than 275 nm were produced with adequate skin compatibility. The rheological properties showed that aqueous dispersions of SLNs followed a non-Newtonian behavior, pseudoplastic fluid adjusted to Herschel-Bulkley equation, whereas LPs and NEs exhibited a Newtonian behavior. SLNs offered significantly better photoprotection than LPs and NEs for RP. The cumulative amount of drug permeated through human skin at the end of 38 h was 6.67 ± 1.58 μg, 4.36 ± 0.21 μg and 3.64 ± 0.28 μg for NEs, LPs and SLNs, respectively. NEs flux was significantly higher than SLNs and LPs: NEs (0.37 ± 0.12 μg/h) > LPs (0.15 ± 0.09 μg/h) > SLNs (0.10 ± 0.05 μg/h). LPs offered significant higher skin retention than NEs and SLNs. Finally, even though all developed nanocarriers were found to be biocompatible, according to histological studies, NE was the system that most disrupted the skin. These encouraging findings can guide in proper selection of topical carriers among the diversity of available lipid-based nanocarriers, especially when a dermatologic or cosmetic purpose is desired.

  19. Effect of lipid-containing, positively charged nanoemulsions on skin hydration, elasticity and erythema--an in vivo study.

    PubMed

    Yilmaz, Erol; Borchert, Hans-Hubert

    2006-01-13

    Dry skin and other skin disorders such as atopic dermatitis are characterized by impaired stratum corneum (SC) barrier function and by an increase in transepidermal water loss (TEWL) leading to a decrease in skin hydration. The possibility that dermatological and cosmetic products containing SC lipids could play a part in the restoration of disturbed skin barrier function is of great interest in the field of dermatology and cosmetics. The aim of the present study was to evaluate the effect of positively charged oil/water nanoemulsions (PN) containing ceramide 3B and naturally found SC lipids (PNSC) such as ceramide 3, cholesterol, and palmitic acid on skin hydration, elasticity, and erythema. Creams of PNSC were compared to PN creams, to creams with negatively charged o/w nanoemulsion and SC lipids (NNSC) and to Physiogel cream, a SC lipid containing formulation, which is already on the market. The formulations (PN, PNSC, and NNSC) were prepared by high-pressure homogenization. After adding Carbopol 940 as thickener, particle size and stability of the creams were not significantly changed compared to the nanoemulsions. The studies were carried out on three groups, each with 14 healthy female test subjects between 25 and 50 years of age, using Corneometer 825, Cutometer SEM 575 and Mexameter 18 for measurements of skin hydration, elasticity, and erythema of the skin, respectively. The creams were applied regularly and well tolerated throughout the study. All formulations increased skin hydration and elasticity. There was no significant difference between PNSC and Physiogel. However, PNSC was significantly more effective in increasing skin hydration and elasticity than PN and NNSC indicating that phytosphingosine inducing the positive charge, SC lipids and ceramide 3B are crucial for the enhanced effect on skin hydration and viscoelasticity. PMID:16289984

  20. Rationalizing lipid nanoemulsion formation for utilization in the food and beverage industry

    NASA Astrophysics Data System (ADS)

    Rao, Jiajia

    There is growing interest in the use of nanoemulsions as delivery systems for lipophilic functional agents in food and beverage products due to their high optical clarity, physical stability and bioavailability. The goal of this research is to establish quantitative structure-function relationships to allow rational formulation of food-grade nanoemulsions for food and beverage applications. Initially, formation of oil-in-water nanoemulsions using a low energy method was examined. Nanoemulsions were formed using the phase inversion temperature (PIT) method, which involves heating a surfactant, oil, water (SOW) systems near the PIT, and then cooling rapidly with stirring. Preliminary experiments were carried out using a model system consisting of a non-ionic surfactant (C12E4), hydrocarbon oil (tetradecane), and water. Nanoemulsions were formed by holding SOW mixtures near their PIT (38.5 °C) and then cooling them rapidly to 10 °C. The PIT was measured using electrical, conductivity and turbidity methods. The optimum storage temperature for PIT-nanoemulsions was about 27 °C lower than the PIT. The stability of PIT-nanoemulsions at ambient temperatures can be improved by adding either Tween 80 (0.2 wt%) or SDS (0.1 wt%) to displace the C12E4 (Brij 30) from the nano-droplet surfaces. Experiments were then carried out to establish if stable nanoemulsions could be formed using the PIT method from food-grade ingredients. Nanoemulsions were fabricated from a non-ionic surfactant (Tween 80) and flavor oil (lemon oil) by heat treatment. Different types of colloidal dispersion could be formed by simple heat treatment (90 °C, 30 minutes) depending on the surfactant-to-oil ratio (SOR): emulsions at SOR < 1; nanoemulsions at 1 < SOR < 2; microemulsions at SOR > 2. The results suggested that there was a kinetic energy barrier in the SOW system at ambient temperature that prevented it from moving from a highly unstable system into a nanoemulsion system. The conditions where

  1. Rationalizing lipid nanoemulsion formation for utilization in the food and beverage industry

    NASA Astrophysics Data System (ADS)

    Rao, Jiajia

    There is growing interest in the use of nanoemulsions as delivery systems for lipophilic functional agents in food and beverage products due to their high optical clarity, physical stability and bioavailability. The goal of this research is to establish quantitative structure-function relationships to allow rational formulation of food-grade nanoemulsions for food and beverage applications. Initially, formation of oil-in-water nanoemulsions using a low energy method was examined. Nanoemulsions were formed using the phase inversion temperature (PIT) method, which involves heating a surfactant, oil, water (SOW) systems near the PIT, and then cooling rapidly with stirring. Preliminary experiments were carried out using a model system consisting of a non-ionic surfactant (C12E4), hydrocarbon oil (tetradecane), and water. Nanoemulsions were formed by holding SOW mixtures near their PIT (38.5 °C) and then cooling them rapidly to 10 °C. The PIT was measured using electrical, conductivity and turbidity methods. The optimum storage temperature for PIT-nanoemulsions was about 27 °C lower than the PIT. The stability of PIT-nanoemulsions at ambient temperatures can be improved by adding either Tween 80 (0.2 wt%) or SDS (0.1 wt%) to displace the C12E4 (Brij 30) from the nano-droplet surfaces. Experiments were then carried out to establish if stable nanoemulsions could be formed using the PIT method from food-grade ingredients. Nanoemulsions were fabricated from a non-ionic surfactant (Tween 80) and flavor oil (lemon oil) by heat treatment. Different types of colloidal dispersion could be formed by simple heat treatment (90 °C, 30 minutes) depending on the surfactant-to-oil ratio (SOR): emulsions at SOR < 1; nanoemulsions at 1 < SOR < 2; microemulsions at SOR > 2. The results suggested that there was a kinetic energy barrier in the SOW system at ambient temperature that prevented it from moving from a highly unstable system into a nanoemulsion system. The conditions where

  2. Factorial design applied to the optimization of lipid composition of topical antiherpetic nanoemulsions containing isoflavone genistein

    PubMed Central

    Argenta, Débora Fretes; de Mattos, Cristiane Bastos; Misturini, Fabíola Dallarosa; Koester, Leticia Scherer; Bassani, Valquiria Linck; Simões, Cláudia Maria Oliveira; Teixeira, Helder Ferreira

    2014-01-01

    The aim of this study was to optimize topical nanoemulsions containing genistein, by means of a 23 full factorial design based on physicochemical properties and skin retention. The experimental arrangement was constructed using oil type (isopropyl myristate or castor oil), phospholipid type (distearoylphosphatidylcholine [DSPC] or dioleylphosphaditylcholine [DOPC]), and ionic cosurfactant type (oleic acid or oleylamine) as independent variables. The analysis of variance showed effect of third order for particle size, polydispersity index, and skin retention of genistein. Nanoemulsions composed of isopropyl myristate/DOPC/oleylamine showed the smallest diameter and highest genistein amount in porcine ear skin whereas the formulation composed of isopropyl myristate/DSPC/oleylamine exhibited the lowest polydispersity index. Thus, these two formulations were selected for further studies. The formulations presented positive ζ potential values (>25 mV) and genistein content close to 100% (at 1 mg/mL). The incorporation of genistein in nanoemulsions significantly increased the retention of this isoflavone in epidermis and dermis, especially when the formulation composed by isopropyl myristate/DOPC/oleylamine was used. These results were supported by confocal images. Such formulations exhibited antiherpetic activity in vitro against herpes simplex virus 1 (strain KOS) and herpes simplex virus 22 (strain 333). Taken together, the results show that the genistein-loaded nanoemulsions developed in this study are promising options in herpes treatment. PMID:25336951

  3. Simvastatin increases the antineoplastic actions of paclitaxel carried in lipid nanoemulsions in melanoma-bearing mice

    PubMed Central

    Kretzer, Iara F; Maria, Durvanei A; Guido, Maria C; Contente, Thaís C; Maranhão, Raul C

    2016-01-01

    Purpose Lipid nanoemulsions (LDEs) that bind to low-density lipoprotein (LDL) receptors used as carriers of paclitaxel (PTX) can decrease toxicity and increase PTX antitumoral action. The administration of simvastatin (Simva), which lowers LDL-cholesterol, was tested as an adjuvant to commercial PTX and to PTX associated with LDE (LDE-PTX). Materials and methods B16F10 melanoma-bearing mice were treated with saline solution or LDE (controls), Simva, PTX, PTX and Simva, LDE-PTX, and LDE-PTX and Simva: PTX dose 17.5 μmol/kg (three intraperitoneal injections, 3 alternate days): Simva 50 mg/kg/day by gavage, 9 consecutive days. Results Compared with saline controls, 95% tumor-growth inhibition was achieved by LDE-PTX and Simva, 61% by LDE-PTX, 44% by PTX and Simva, and 43% by PTX. Simva alone had no effect. Metastasis developed in only 37% of the LDE-PTX and Simva, 60% in LDE-PTX, and 90% in PTX and Simva groups. Survival rates were higher in LDE-PTX and Simva and in LDE-PTX groups. The LDE-PTX and Simva group presented tumors with reduced cellular density and increased collagen fibers I and III. Tumors from all groups showed reduction in immunohistochemical expression of ICAM, MCP-1, and MMP-9; LDE-PTX and Simva presented the lowest MMP-9 expression. Expression of p21 was increased in the Simva, LDE-PTX, and LDE-PTX and Simva groups. In the Simva and LDE-PTX and Simva groups, expression of cyclin D1, a proliferation and survival promoter of tumor cells, was decreased. Therapy with LDE-PTX and Simva showed negligible toxicity compared with PTX and Simva, which resulted in weight loss and myelosuppression. Conclusion Simva increased the antitumor activity of PTX carried in LDE but not of PTX commercial presentation, possibly because statins increase the expression of LDL receptors that internalize LDE-PTX. PMID:27022257

  4. A New Application of Lipid Nanoemulsions as Coating Agent, Providing Zero-Order Hydrophilic Drug Release from Tablets

    PubMed Central

    Anton, Nicolas; de Crevoisier, Astrid; Schmitt, Sabrina; Vandamme, Thierry

    2012-01-01

    The objective of the present investigation was to evaluate potential of nanoemulsions as a coating material for the tablets. The nanoemulsion of size less than 100 nm was prepared using a simple and low-energy spontaneous emulsification method. Conventional tablets containing theophylline as a model hydrophilic drug were prepared. The theophylline tablets were coated with the nanoemulsion using a fluid bed coater. The effect of different levels of the nanoemulsion coating on the theophylline release was evaluated. The theophylline tablets containing different levels of the nanoemulsion coating could be successfully prepared. Interestingly, the coating of tablet with the nanoemulsion resulted in zero-order release of theophylline from the tablets. The noncoated theophylline tablets release the entire drug in less than 2 minutes, whereas nanoemulsion coating delayed the release of theophylline from tablets. This investigation establishes the proof of concept for the potential of nanoemulsions as a coating material for tablets. PMID:22272376

  5. Advanced Nanoemulsions

    NASA Astrophysics Data System (ADS)

    Fryd, Michael M.; Mason, Thomas G.

    2012-05-01

    Recent advances in the growing field of nanoemulsions are opening up new applications in many areas such as pharmaceuticals, foods, and cosmetics. Moreover, highly controlled nanoemulsions can also serve as excellent model systems for investigating basic scientific questions about soft matter. Here, we highlight some of the most recent developments in nanoemulsions, focusing on methods of formation, surface modification, material properties, and characterization. These developments provide insight into the substantial advantages that nanoemulsions can offer over their microscale emulsion counterparts.

  6. Preparation of lipid nanoemulsions by premix membrane emulsification with disposable materials.

    PubMed

    Gehrmann, Sandra; Bunjes, Heike

    2016-09-25

    The possibility to prepare nanoemulsions as drug carrier systems on small scale was investigated with disposable materials. For this purpose premix membrane emulsification (premix ME) as a preparation method for nanoemulsions with narrow particle size distributions on small scale was used. The basic principle of premix ME is that the droplets of a coarse pre-emulsion get disrupted by the extrusion through a porous membrane. In order to implement the common preparation setup for premix ME with disposable materials, the suitability of different syringe filters (made from polyethersulfone, cellulose acetate, cellulose ester and nylon) and different pharmaceutically relevant emulsifiers (phospholipids, polysorbate 80 and sucrose laurate) for the preparation of nanoemulsions was investigated. Already the preparation of the premix could be realized by emulsification with the help of two disposable syringes. As shown for a phospholipid-stabilized emulsion, the polyethersulfone filter was the most appropriate one and was used for the study with different emulsifiers. With this syringe filter, the median particle size of all investigated emulsions was below 500nm after 21 extrusion cycles through a 200nm filter and a subsequent extrusion cycle through a 100nm filter. Furthermore, the particle size distribution of the polysorbate 80- and sucrose laurate-stabilized emulsions prepared this way was very narrow (span value of 0.7). PMID:27477104

  7. Nanoemulsion delivery systems for oil-soluble vitamins: Influence of carrier oil type on lipid digestion and vitamin D3 bioaccessibility.

    PubMed

    Ozturk, Bengu; Argin, Sanem; Ozilgen, Mustafa; McClements, David Julian

    2015-11-15

    The influence of carrier oil type on the bioaccessibility of vitamin D3 encapsulated within oil-in-water nanoemulsions prepared using a natural surfactant (quillaja saponin) was studied using a simulated gastrointestinal tract (GIT) model: mouth; stomach; small intestine. The rate of free fatty acid release during lipid digestion decreased in the following order: medium chain triglycerides (MCT) > corn oil ≈ fish oil > orange oil > mineral oil. Conversely, the measured bioaccessibility of vitamin D3 decreased in the following order: corn oil ≈ fish oil > orange oil > mineral oil > MCT. These results show that carrier oil type has a considerable impact on lipid digestion and vitamin bioaccessibility, which was attributed to differences in the release of bioactives from lipid droplets, and their solubilization in mixed micelles. Nanoemulsions prepared using long chain triglycerides (corn or fish oil) were most effective at increasing vitamin bioaccessibility. PMID:25977056

  8. Nanoemulsion delivery systems for oil-soluble vitamins: Influence of carrier oil type on lipid digestion and vitamin D3 bioaccessibility.

    PubMed

    Ozturk, Bengu; Argin, Sanem; Ozilgen, Mustafa; McClements, David Julian

    2015-11-15

    The influence of carrier oil type on the bioaccessibility of vitamin D3 encapsulated within oil-in-water nanoemulsions prepared using a natural surfactant (quillaja saponin) was studied using a simulated gastrointestinal tract (GIT) model: mouth; stomach; small intestine. The rate of free fatty acid release during lipid digestion decreased in the following order: medium chain triglycerides (MCT) > corn oil ≈ fish oil > orange oil > mineral oil. Conversely, the measured bioaccessibility of vitamin D3 decreased in the following order: corn oil ≈ fish oil > orange oil > mineral oil > MCT. These results show that carrier oil type has a considerable impact on lipid digestion and vitamin bioaccessibility, which was attributed to differences in the release of bioactives from lipid droplets, and their solubilization in mixed micelles. Nanoemulsions prepared using long chain triglycerides (corn or fish oil) were most effective at increasing vitamin bioaccessibility.

  9. Anti-Lipid IgG Antibodies Are Produced via Germinal Centers in a Murine Model Resembling Human Lupus

    PubMed Central

    Wong-Baeza, Carlos; Reséndiz-Mora, Albany; Donis-Maturano, Luis; Wong-Baeza, Isabel; Zárate-Neira, Luz; Yam-Puc, Juan Carlos; Calderón-Amador, Juana; Medina, Yolanda; Wong, Carlos; Baeza, Isabel; Flores-Romo, Leopoldo

    2016-01-01

    Anti-lipid IgG antibodies are produced in some mycobacterial infections and in certain autoimmune diseases [such as anti-phospholipid syndrome, systemic lupus erythematosus (SLE)]. However, few studies have addressed the B cell responses underlying the production of these immunoglobulins. Anti-lipid IgG antibodies are consistently found in a murine model resembling human lupus induced by chlorpromazine-stabilized non-bilayer phospholipid arrangements (NPA). NPA are transitory lipid associations found in the membranes of most cells; when NPA are stabilized they can become immunogenic and induce specific IgG antibodies, which appear to be involved in the development of the mouse model of lupus. Of note, anti-NPA antibodies are also detected in patients with SLE and leprosy. We used this model of lupus to investigate in vivo the cellular mechanisms that lead to the production of anti-lipid, class-switched IgG antibodies. In this murine lupus model, we found plasma cells (Gr1−, CD19−, CD138+) producing NPA-specific IgGs in the draining lymph nodes, the spleen, and the bone marrow. We also found a significant number of germinal center B cells (IgD−, CD19+, PNA+) specific for NPA in the draining lymph nodes and the spleen, and we identified in situ the presence of NPA in these germinal centers. By contrast, very few NPA-specific, extrafollicular reaction B cells (B220+, Blimp1+) were found. Moreover, when assessing the anti-NPA IgG antibodies produced during the experimental protocol, we found that the affinity of these antibodies progressively increased over time. Altogether, our data indicate that, in this murine model resembling human lupus, B cells produce anti-NPA IgG antibodies mainly via germinal centers. PMID:27746783

  10. Design and evaluation of lipoprotein resembling curcumin-encapsulated protein-free nanostructured lipid carrier for brain targeting.

    PubMed

    Meng, Fanfei; Asghar, Sajid; Xu, Yurui; Wang, Jianping; Jin, Xin; Wang, Zhilin; Wang, Jing; Ping, Qineng; Zhou, Jianping; Xiao, Yanyu

    2016-06-15

    Many nanoparticle matrixes have been demonstrated to be efficient in brain targeting, but there are still certain limitations for them. To overcome the shortcomings of the existing nanoparticulate systems for brain-targeted delivery, a lipoprotein resembling protein-free nanostructured lipid carrier (PS80-NLC) loaded with curcumin was constructed and assessed for in vitro and in vivo performance. Firstly, single factor at a time approach was employed to investigate the effects of various formulation factors. Mean particle sizes of ≤100nm, high entrapment efficiency (EE, about 95%) and drug loading (DL, >3%) were obtained for the optimized formulations. In vitro release studies in the presence of plasma indicated stability of the formulation under physiological condition. Compared with NLC, PS80-NLC showed noticeably higher affinity for bEnd.3 cells (1.56 folds greater than NLC) but with lower uptake in macrophages. The brain coronal sections showed strong and widely distributed fluorescence intensity of PS80-NLC than that of NLC in the cortex. Ex vivo imaging studies further confirmed that PS80-NLC could effectively permeate BBB and preferentially accumulate in the brain (2.38 times greater than NLC). The considerable in vitro and in vivo performance of the safe and biocompatible PS80-NLC makes it a suitable option for further investigations in brain targeted drug delivery.

  11. Effects of Lipids on in Vitro Release and Cellular Uptake of β-Carotene in Nanoemulsion-Based Delivery Systems.

    PubMed

    Yi, Jiang; Zhong, Fang; Zhang, Yuzhu; Yokoyama, Wallace; Zhao, Liqing

    2015-12-23

    β-Carotene (BC) nanoemulsions were successfully prepared by microfluidization. BC micellarization was significantly affected by bile salts and pancreatin concentration. Positive and linear correlation was observed between BC release and bile salts concentration. Pancreatin facilitated BC's release in simulated digestion. Compared to the control (bulk oil) (4.6%), nanoemulsion delivery systems significantly improved the micellarization of BC (70.9%). The amount of BC partitioned into micelles was positively proportional to the length of carrier oils. Unsaturated fatty acid (UFA)-rich oils were better than saturated fatty acid (SFA)-rich oils in transferring BC (p < 0.05). No significant difference was observed between monounsaturated fatty acid (MUFA)-rich oils and polyunsaturated fatty acid (PUFA)-rich oils (p > 0.05). A positive and linear relationship between the degree of lipolysis and the release of BC in vitro digestion was observed. Bile salts showed cytotoxicity to Caco-2 cells below 20 times dilution. BC uptake by Caco-2 cells was not affected by fatty acid (FA) compositions in micelles, but BC uptake was proportional to its concentration in the diluted micelle fraction. The results obtained are beneficial to encapsulate and deliver BC or other bioactive lipophilic carotenoids in a wide range of commercial products. PMID:26629789

  12. Nanoemulsion: for improved oral delivery of repaglinide.

    PubMed

    Akhtar, Juber; Siddiqui, Hefazat Hussain; Fareed, Sheeba; Badruddeen; Khalid, Mohammad; Aqil, Mohammed

    2016-07-01

    Repaglinide (RPG) is a fast-acting prandial glucose regulator. It acts by stimulating insulin release from pancreatic β-cells. Recurrent dosing of RPG before each meal is burdensome remedy. Hence the plan of the present study was to evaluate nanoemulsion as a hopeful carrier for RPG for persistent hypoglycemic effect. The drug was incorporated into oil phase of nanoemulsion to give improved biopharmaceutical properties as compared to the lipid-based systems. Pseudo ternary phase diagrams were prepared by aqueous titration method. Formulations were selected at a difference of 5% w/w of oil from the o/w nanoemulsion region of phase diagrams. The optimized nanoemulsion formulation constituted sefsol-218 (5% v/v) as an oil phase, 30% v/v of Tween-80 and transcutol as a surfactant and co-surfactant to restrain nanodroplet size and low viscosity and distilled water (65%). In vitro dissolution studies showed higher drug release (98.22%), finest droplet size (76.23 nm), slightest polydispersity value (0.183), least viscosity (21.45 cps) and immeasurable dilution capability from the nanoemulsion as compared with existing oral tablet formulation. The optimized RPG nanoemulsion formulation showed better hypoglycemic effect in comparison to tablet formulation in experimental diabetic rats. No significant variations were also observed in the optimized formulation when subjected to accelerated stability study at different temperature and relative humidity over a period of 3 months. PMID:27187792

  13. Localization and reactivity of a hydrophobic solute in lecithin and caseinate stabilized solid lipid nanoparticles and nanoemulsions.

    PubMed

    Yucel, Umut; Elias, Ryan J; Coupland, John N

    2013-03-15

    The distribution and reactivity of the lipophilic spin probe 4-phenyl-2,2,5,5-tetramethyl-3-imidazoline-1-oxyl nitroxide (PTMIO) in tetradecane (C14)- and eicosane (C20)-in-water emulsions and solid lipid nanoparticles (SLN) respectively, were investigated by electron paramagnetic resonance (EPR) spectroscopy. The lipid phase (10 wt% C14 or C20) was emulsified into either caseinate solutions (1 wt%) or lecithin+bile salt dispersions (2.4 wt%+0.6 wt%) at 70-75 °C. In C14 emulsions stabilized with lecithin+bile salt, three populations of PTMIO were observed: a population in the lipid phase (~60%, a(N)~13.9 G), an aqueous phase population (~20%, a(N)~15.4 G) with high mobility, and an immobilized surface layer population (~20%, a(N)~14.2 G) with low mobility. However, in C14 emulsions stabilized by caseinate, only two distinct populations of PTMIO were seen: a lipid phase population (~70%, a(N)~13.8 G) and an aqueous phase population (~30%, a(N)~15.5 G) with high mobility. In C20 SLN stabilized with either lecithin+bile salt or caseinate, PTMIO was excluded from the lipid phase. In lecithin+bile salt-stabilized C20 SLN, the majority of the probe (~77%) was in the interfacial layer. For both surfactant systems the rate of PTMIO reduction by aqueous iron/ascorbate was greater for C20 SLN than C14 emulsions. Lecithin affects the properties of emulsions and SLN as delivery systems by providing a distinct environment for small molecules. PMID:23352869

  14. Skin permeation mechanism of aceclofenac using novel nanoemulsion formulation.

    PubMed

    Shakeel, F; Baboota, S; Ahuja, A; All, J; Shafiq, S

    2008-08-01

    The aim of the present study was to investigate the skin permeation mechanism of aceclofenac using a novel nanoemulsion formulation. An optimized oil-in-water nanoemulsion of aceclofenac was prepared by the spontaneous emulsification method. The optimized nanoemulsion contained 2% w/w aceclofenac, 10% w/w Labrafil, 5% w/w Triacetin, 35.33% w/w Tween 80, 17.66% w/w Transcutol P and 32% w/w distilled water. The skin permeation mechanism was evaluated by FTIR spectroscopy, DSC thermography, activation energy measurement and histopathological examination. FTIR spectra of skin treated with the nanoemulsion formulation indicated breaking of the hydrogen bond network at the head of ceramides. DSC thermograms indicated that intracellular transport could be a possible mechanism of permeation enhancement and that permeation occurred due to the extraction of SC lipids by the nanoemulsion. The significant decrease in activation energy for aceclofenac permeation across rat skin indicated that the SC lipid bilayers were significantly disrupted (p < 0.05). Photomicrography of skin showed disruption and extraction of lipid bilayers as distinct voids and empty spaces visible in the epidermal region. Overall these findings indicated that nanoemulsions can be successfully used to enhance skin permeation of drugs.

  15. Biosynthetic mechanism for L-Gulose in main polar lipids of Thermoplasma acidophilum and possible resemblance to plant ascorbic acid biosynthesis.

    PubMed

    Yamauchi, Noriaki; Nakayama, Yusuke

    2013-01-01

    L-Gulose is a very rare sugar, but appears as a sugar component of the main polar lipids characteristic in such a thermophilic archaeon as Thermoplasma acidophilum that lives without cell walls in a highly acidic environment. The biosynthesis of L-gulose in this thermophilic organism was investigated with deuterium-labeling experiments. L-Gulose was found to be biosynthesized from D-glucose via stepwise stereochemical inversion at C-2 and C-5. The involvement of an epimerase related to GDP-mannose 3,5-epimerase, the key enzyme of plant ascorbate biosynthesis, was also suggested in this C-5 inversion. The resemblance of L-gulose biosynthesis in archaea and plants might be suggested from these results.

  16. Nanoemulsion: a promising tool for solubility and dissolution enhancement of celecoxib.

    PubMed

    Shakeel, Faiyaz; Faisal, Mohammed S

    2010-01-01

    The solubility and dissolution of the poorly soluble drug celecoxib (CXB) was enhanced using many techniques like nanoemulsion, solid lipid nanoparticle and solid dispersion in the present investigation. The solubility of CXB in each formulation was determined using the reported HPLC method at the wavelength of 250 nm. Dissolution studies of pure CXB and its formulations were performed using USP dissolution apparatus in distilled water. The highest solubility (228. 24 mg/mL) as well as % dissolution (99.9) of CXB was obtained with nanoemulsion technique. The results of solubility and dissolution were highly significant using the nanoemulsion technique as compared to other techniques (P < 0.01). All three formulations showed a sustained type of drug release. The best sustained type drug release was obtained with nanoemulsion. This indicated that nanoemulsion can be successfully used for sustained and controlled drug delivery of CXB. Overall these findings suggested that nanoemulsion is a promising vehicle for solubility and dissolution enhancement of CXB.

  17. Improvement of β-Carotene Bioaccessibility from Dietary Supplements Using Excipient Nanoemulsions.

    PubMed

    Salvia-Trujillo, Laura; McClements, David Julian

    2016-06-01

    The influence of excipient nanoemulsions on β-carotene bioaccessibility from commercial dietary supplements (tablets or soft gels) was studied employing an in vitro gastrointestinal tract (GIT) model. Excipient nanoemulsions were formulated from long or medium chain triglycerides (LCT or MCT) to determine the impact of lipid type on carotenoid bioaccessibility. Dietary supplements were tested using the GIT model in the absence or presence of excipient nanoemulsions. β-carotene bioaccessibility from tablets (0.3%) or soft gels (2.4%) was low when tested in isolation. LCT nanoemulsions greatly improved β-carotene bioaccessibility from tablets (20%) and slightly improved it from soft gels (5%), whereas MCT nanoemulsions only slightly improved bioaccessibility. These results were attributed to the ability of large carotenoid molecules to be incorporated into large mixed micelles formed by LCT digestion but not by small ones formed by MCT digestion. Our results indicate that excipient nanoemulsions have considerable potential for improving nutraceutical bioavailability from dietary supplements. PMID:27198626

  18. Physical properties and antimicrobial efficacy of thyme oil nanoemulsions: influence of ripening inhibitors.

    PubMed

    Chang, Yuhua; McLandsborough, Lynne; McClements, David Julian

    2012-12-01

    Thyme oil-in-water nanoemulsions (pH 3.5) were prepared as potential antimicrobial delivery systems. The nanoemulsions were highly unstable to droplet growth and phase separation, which was attributed to Ostwald ripening due to the relatively high water solubility of thyme oil. Ostwald ripening could be inhibited by mixing thyme oil with a water-insoluble ripening inhibitor (≥60 wt % corn oil or ≥50 wt % MCT in the lipid phase) before homogenization, yielding nanoemulsions with good physical stability. Physically stable thyme oil nanoemulsions were examined for their antimicrobial activities against an acid-resistant spoilage yeast, Zygosaccharomyces bailii (ZB). Oil phase composition (ripening inhibitor type and concentration) had an appreciable influence on the antimicrobial activity of the thyme oil nanoemulsions. In general, increasing the ripening inhibitor levels in the lipid phase reduced the antimicrobial efficacy of nanoemulsions. For example, for nanoemulsions containing 60 wt % corn oil in the lipid phase, the minimum inhibitory concentration (MIC) of thyme oil to inhibit ZB growth was 375 μg/mL, while for nanoemulsions containing 90 wt % corn oil in the lipid phase, even 6000 μg/mL thyme oil could not inhibit ZB growth. This effect is also dependent on ripening inhibitor types: at the same concentration in the lipid phase, MCT decreased the antimicrobial efficacy of thyme oil more than corn oil. For instance, when the level of ripening inhibitor in the lipid phase was 70 wt %, the MICs of thyme oil for nanoemulsions containing corn oil and MCT were 750 and 3000 μg/mL, respectively. The results of this study have important implications for the design and utilization of nanoemulsions as antimicrobial delivery systems in the food and other industries.

  19. Physical properties and antimicrobial efficacy of thyme oil nanoemulsions: influence of ripening inhibitors.

    PubMed

    Chang, Yuhua; McLandsborough, Lynne; McClements, David Julian

    2012-12-01

    Thyme oil-in-water nanoemulsions (pH 3.5) were prepared as potential antimicrobial delivery systems. The nanoemulsions were highly unstable to droplet growth and phase separation, which was attributed to Ostwald ripening due to the relatively high water solubility of thyme oil. Ostwald ripening could be inhibited by mixing thyme oil with a water-insoluble ripening inhibitor (≥60 wt % corn oil or ≥50 wt % MCT in the lipid phase) before homogenization, yielding nanoemulsions with good physical stability. Physically stable thyme oil nanoemulsions were examined for their antimicrobial activities against an acid-resistant spoilage yeast, Zygosaccharomyces bailii (ZB). Oil phase composition (ripening inhibitor type and concentration) had an appreciable influence on the antimicrobial activity of the thyme oil nanoemulsions. In general, increasing the ripening inhibitor levels in the lipid phase reduced the antimicrobial efficacy of nanoemulsions. For example, for nanoemulsions containing 60 wt % corn oil in the lipid phase, the minimum inhibitory concentration (MIC) of thyme oil to inhibit ZB growth was 375 μg/mL, while for nanoemulsions containing 90 wt % corn oil in the lipid phase, even 6000 μg/mL thyme oil could not inhibit ZB growth. This effect is also dependent on ripening inhibitor types: at the same concentration in the lipid phase, MCT decreased the antimicrobial efficacy of thyme oil more than corn oil. For instance, when the level of ripening inhibitor in the lipid phase was 70 wt %, the MICs of thyme oil for nanoemulsions containing corn oil and MCT were 750 and 3000 μg/mL, respectively. The results of this study have important implications for the design and utilization of nanoemulsions as antimicrobial delivery systems in the food and other industries. PMID:23140446

  20. A nanoemulsion formulation of tamoxifen increases its efficacy in a breast cancer cell line.

    PubMed

    Tagne, Jean-Bosco; Kakumanu, Srikanth; Ortiz, Daniela; Shea, Thomas; Nicolosi, Robert J

    2008-01-01

    This paper reports on the preparation of a water-soluble nanoemulsion of the highly lipid-soluble drug tamoxifen (TAM). In addition, relative to a suspension of TAM, the nanoemulsion preparation demonstrated a greater zeta potential (increased negative charge) which has previously been associated with increasing drug/membrane permeability. This study also reports that relative to suspensions of TAM with particle sizes greater than 6000 nm, nanoemulsions of TAM, having mean particle sizes of 47 nm, inhibited cell proliferation 20-fold greater and increased cell apoptosis 4-fold greater in the HTB-20 breast cancer cell line. Thus, this work suggests that a nanoemulsion compared to a suspension preparation of TAM increases its anticancer properties relative to breast cancer. PMID:18171014

  1. Development of nanoemulsions for topical delivery of vitamin K1.

    PubMed

    Campani, Virginia; Biondi, Marco; Mayol, Laura; Cilurzo, Francesco; Pitaro, Michele; De Rosa, Giuseppe

    2016-09-10

    Vitamin K1 (VK1) is a natural and lipophilic compound currently used in dermatological formulations. In this work, nanoemulsions containing VK1 have been proposed to overcome some issues associated to semisolid VK1-incorporating formulations. The study has been focused on the design of a lipid-free aqueous formulation, easy to prepare and with low cost of production. Thus, a simply protocol, using a low-energy method, has been used to spontaneously form the nanoemulsions. The nanoemulsion composition has been optimized to improve its physical stability during storage in different conditions. Then, the possibility to administer VK1-containing nanoemulsions by nebulization without significant alteration of the formulation was tested. Moreover, the VK1 accumulation into the skin layers have been evaluated through permeation experiments on Franz cells, ATR-FITR analysis, confocal laser scanning microscopy (CLSM) observations, and high performance liquid chromatography (HPLC) analysis. The study demonstrated that NEs represent an interesting option for the commercial development of an aqueous spray formulation for the topical delivery of VK1.

  2. Study on antimicrobial potential of neem oil nanoemulsion against Pseudomonas aeruginosa infection in Labeo rohita.

    PubMed

    Mishra, Prabhakar; R S, Suresh Kumar; Jerobin, Jayakumar; Thomas, John; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2014-01-01

    Presence of several biochemical constituents in neem makes it an efficient antimicrobial agent for pathogenic diseases. The current investigation was aimed to assess the therapeutic potential of neem nanoemulsion as a control measure for Pseudomonas aeruginosa infection in freshwater fish Labeo rohita. The median lethal concentration (LC50) for the neem oil and neem nanoemulsion was 73.9 and 160.3 mg/L, respectively. The biomarker enzymes of treated fish tissues showed a significant difference in the level of glutathione reductase, catalase, and lipid peroxidation in neem oil-treated samples than in neem nanoemulsion-treated samples at P<0.05. The results were corroborative with histopathology and ultrastructural analysis. The bacterial infection of P. aeruginosa treated using neem nanoemulsion was more effective in both in vitro and in vivo methods. Present findings suggest that neem-based nanoemulsion has negligible toxicity to Rohu fishes. This makes neem-based nanoemulsion as an efficient therapeutic agent against P. aeruginosa infection, leading to its possible usage in the aquaculture industry.

  3. Study on antimicrobial potential of neem oil nanoemulsion against Pseudomonas aeruginosa infection in Labeo rohita.

    PubMed

    Mishra, Prabhakar; R S, Suresh Kumar; Jerobin, Jayakumar; Thomas, John; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2014-01-01

    Presence of several biochemical constituents in neem makes it an efficient antimicrobial agent for pathogenic diseases. The current investigation was aimed to assess the therapeutic potential of neem nanoemulsion as a control measure for Pseudomonas aeruginosa infection in freshwater fish Labeo rohita. The median lethal concentration (LC50) for the neem oil and neem nanoemulsion was 73.9 and 160.3 mg/L, respectively. The biomarker enzymes of treated fish tissues showed a significant difference in the level of glutathione reductase, catalase, and lipid peroxidation in neem oil-treated samples than in neem nanoemulsion-treated samples at P<0.05. The results were corroborative with histopathology and ultrastructural analysis. The bacterial infection of P. aeruginosa treated using neem nanoemulsion was more effective in both in vitro and in vivo methods. Present findings suggest that neem-based nanoemulsion has negligible toxicity to Rohu fishes. This makes neem-based nanoemulsion as an efficient therapeutic agent against P. aeruginosa infection, leading to its possible usage in the aquaculture industry. PMID:24502533

  4. Tuneable stability of nanoemulsions fabricated using spontaneous emulsification by biopolymer electrostatic deposition.

    PubMed

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

    2015-10-01

    Nanoemulsions can be formed spontaneously from surfactant-oil-water systems using low energy methods. In this work, we showed that the droplets in oil-in-water nanoemulsions fabricated by spontaneous emulsification could be coated with an anionic biopolymer (beet pectin) using electrostatic deposition. Nanoemulsions were formed by titrating oil (medium chain triglycerides) and surfactant (polyoxyethylene sorbitan monostearate+lauric arginate) mixtures into an aqueous solution (10 mM citrate buffer, pH 4). Lauric arginate was used to generate a positive charge on the droplet surfaces, thereby enabling subsequent electrostatic deposition of anionic pectin. Extensive droplet aggregation occurred when intermediate pectin concentrations were used due to bridging flocculation. However, stable anionic pectin-coated lipid droplets could be formed at high pectin concentrations. These results demonstrate the possibility of tailoring the functionality of lipid nanodroplets produced by spontaneous emulsification.

  5. Tuneable stability of nanoemulsions fabricated using spontaneous emulsification by biopolymer electrostatic deposition.

    PubMed

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

    2015-10-01

    Nanoemulsions can be formed spontaneously from surfactant-oil-water systems using low energy methods. In this work, we showed that the droplets in oil-in-water nanoemulsions fabricated by spontaneous emulsification could be coated with an anionic biopolymer (beet pectin) using electrostatic deposition. Nanoemulsions were formed by titrating oil (medium chain triglycerides) and surfactant (polyoxyethylene sorbitan monostearate+lauric arginate) mixtures into an aqueous solution (10 mM citrate buffer, pH 4). Lauric arginate was used to generate a positive charge on the droplet surfaces, thereby enabling subsequent electrostatic deposition of anionic pectin. Extensive droplet aggregation occurred when intermediate pectin concentrations were used due to bridging flocculation. However, stable anionic pectin-coated lipid droplets could be formed at high pectin concentrations. These results demonstrate the possibility of tailoring the functionality of lipid nanodroplets produced by spontaneous emulsification. PMID:26070187

  6. Nanoemulsions prepared by a low-energy emulsification method applied to edible films

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Catastrophic phase inversion (CPI) was used as a low-energy emulsification method to prepare oil-in-water (O/W) nanoemulsions in a lipid (Acetem)/water/nonionic surfactant (Tween 60) system. CPIs in which water-in-oil emulsions (W/O) are transformed into oil-in-water emulsions (O/W) were induced by ...

  7. Physical Factors Affecting Plasmid DNA Compaction in Stearylamine-Containing Nanoemulsions Intended for Gene Delivery

    PubMed Central

    Silva, André Leandro; Júnior, Francisco Alexandrino; Verissimo, Lourena Mafra; Agnez-Lima, Lucymara Fassarella; Egito, Lucila Carmem Monte; de Oliveira, Anselmo Gomes; do Egito, Eryvaldo Socrates Tabosa

    2012-01-01

    Cationic lipids have been used in the development of non-viral gene delivery systems as lipoplexes. Stearylamine, a cationic lipid that presents a primary amine group when in solution, is able to compact genetic material by electrostatic interactions. In dispersed systems such as nanoemulsions this lipid anchors on the oil/water interface confering a positive charge to them. The aim of this work was to evaluate factors that influence DNA compaction in cationic nanoemulsions containing stearylamine. The influence of the stearylamine incorporation phase (water or oil), time of complexation, and different incubation temperatures were studied. The complexation rate was assessed by electrophoresis migration on agarose gel 0.7%, and nanoemulsion and lipoplex characterization was done by Dynamic Light Scattering (DLS). The results demonstrate that the best DNA compaction process occurs after 120 min of complexation, at low temperature (4 ± 1 °C), and after incorporation of the cationic lipid into the aqueous phase. Although the zeta potential of lipoplexes was lower than the results found for basic nanoemulsions, the granulometry did not change. Moreover, it was demonstrated that lipoplexes are suitable vehicles for gene delivery. PMID:24281666

  8. Fabrication, stability and efficacy of dual-component antimicrobial nanoemulsions: essential oil (thyme oil) and cationic surfactant (lauric arginate).

    PubMed

    Chang, Yuhua; McLandsborough, Lynne; McClements, David Julian

    2015-04-01

    The influence of a cationic surfactant (lauric arginate, LAE) on the physical properties and antimicrobial efficacy of thyme oil nanoemulsions was investigated. Nanoemulsions prepared from pure thyme oil were highly unstable due to Ostwald ripening, but they could be stabilized by adding a ripening inhibitor (corn oil) to the oil phase prior to homogenisation. The loading capacity and antimicrobial efficacy of thyme oil nanoemulsions were significantly increased by adding LAE. In the absence of LAE, at least 60 wt% corn oil had to be added to the lipid phase to inhibit Ostwald ripening; but in the presence of 0.1 wt% LAE, only 30 wt% corn oil was needed. LAE addition substantially increased the antimicrobial efficacy of the thyme oil nanoemulsions: 200 μg/ml thyme oil was needed to inhibit growth of a spoilage yeast (Zygosaccharomyces bailii) if LAE was added, whereas ⩾ 400 μg/ml was needed in the absence of LAE.

  9. Physical Stability, Autoxidation, and Photosensitized Oxidation of ω-3 Oils in Nanoemulsions Prepared with Natural and Synthetic Surfactants.

    PubMed

    Uluata, Sibel; McClements, D Julian; Decker, Eric A

    2015-10-28

    The food industry is interested in the utilization of nanoemulsions stabilized by natural emulsifiers, but little research has been conducted to determine the oxidative stability of such emulsions. In this study, two natural (lecithin and quillaja saponin) and two synthetic (Tween 80 and sodium dodecyl sulfate) surfactants were used to fabricate omega-3 nanoemulsion using high pressure homogenization (microfluidization). Initially, all the nanoemulsions contained small (d from 45 to 89 nm) and anionic (ζ-potential from -8 to -65 mV) lipid droplets (pH 7). The effect of pH, ionic strength, and temperature on the physical stability of the nanoemulsion system was examined. Nanoemulsion stabilized with Tween 80, quillaja saponin, or sodium dodecyl sulfate (SDS) exhibited no major changes in particle size or visible creaming in the pH range of 3 to 8. All nanoemulsions were relatively stable to salt addition (0 to 500 mM NaCl, pH 7.0). Nanoemulsions stabilized with SDS and quillaja saponin were stable to heating (30 to 90 °C). The impact of surfactant type on lipid oxidation was determined in the presence and absence of the singlet oxygen photosensitizers, riboflavin, and rose bengal. Riboflavin and rose bengal accelerated lipid oxidation when compare to samples without photosensitizers. Lipid hydroperoxide formation followed the order Tween 80 > SDS > lecithin > quillaja saponin, and propanal formation followed the order lecithin > Tween 80 > SDS > quillaja saponin at 37 °C for autoxidation. The same order of oxidative stability was observed in the presence of photosensitized oxidation promoted by riboflavin. Quillaja saponin consistently produced the most oxidatively stable emulsions, which could be due to its high free radical scavenging capacity. PMID:26452408

  10. Protection against oxidative damage in human erythrocytes and preliminary photosafety assessment of Punica granatum seed oil nanoemulsions entrapping polyphenol-rich ethyl acetate fraction.

    PubMed

    Baccarin, Thaisa; Mitjans, Montserrat; Lemos-Senna, Elenara; Vinardell, Maria Pilar

    2015-12-25

    The main purpose of the present study is to evaluate the ability of nanoemulsion entrapping pomegranate peel polyphenol-rich ethyl acetate fraction (EAF) prepared from pomegranate seed oil and medium chain triglyceride to protect human erythrocyte membrane from oxidative damage and to assess preliminary in vitro photosafety. In order to evaluate the phototoxic effect of nanoemulsions, human red blood cells (RBCs) are used as a biological model and the rate of haemolysis and photohaemolysis (5 J cm(-2) UVA) is assessed in vitro. The level of protection against oxidative damage caused by the peroxyl radical generator AAPH in human RBCs as well as its effects on bilayer membrane characteristics such as fluidity, protein profile and RBCs morphology are determined. EAF-loaded nanoemulsions do not promote haemolysis or photohaemolysis. Anisotropy measurements show that nanoemulsions significantly retrain the increase in membrane fluidity caused by AAPH. SDS-PAGE analysis reveals that AAPH induced degradation of membrane proteins, but that nanoemulsions reduce the extension of degradation. Scanning electron microscopy examinations corroborate the interaction between AAPH, nanoemulsions and the RBC membrane bilayer. Our work demonstrates that Punica granatum nanoemulsions are photosafe and protect RBCs against oxidative damage and possible disturbance of the lipid bilayer of biomembranes. Moreover it suggests that these nanoemulsions could be promising new topical products to reduce the effects of sunlight on skin.

  11. Protection against oxidative damage in human erythrocytes and preliminary photosafety assessment of Punica granatum seed oil nanoemulsions entrapping polyphenol-rich ethyl acetate fraction.

    PubMed

    Baccarin, Thaisa; Mitjans, Montserrat; Lemos-Senna, Elenara; Vinardell, Maria Pilar

    2015-12-25

    The main purpose of the present study is to evaluate the ability of nanoemulsion entrapping pomegranate peel polyphenol-rich ethyl acetate fraction (EAF) prepared from pomegranate seed oil and medium chain triglyceride to protect human erythrocyte membrane from oxidative damage and to assess preliminary in vitro photosafety. In order to evaluate the phototoxic effect of nanoemulsions, human red blood cells (RBCs) are used as a biological model and the rate of haemolysis and photohaemolysis (5 J cm(-2) UVA) is assessed in vitro. The level of protection against oxidative damage caused by the peroxyl radical generator AAPH in human RBCs as well as its effects on bilayer membrane characteristics such as fluidity, protein profile and RBCs morphology are determined. EAF-loaded nanoemulsions do not promote haemolysis or photohaemolysis. Anisotropy measurements show that nanoemulsions significantly retrain the increase in membrane fluidity caused by AAPH. SDS-PAGE analysis reveals that AAPH induced degradation of membrane proteins, but that nanoemulsions reduce the extension of degradation. Scanning electron microscopy examinations corroborate the interaction between AAPH, nanoemulsions and the RBC membrane bilayer. Our work demonstrates that Punica granatum nanoemulsions are photosafe and protect RBCs against oxidative damage and possible disturbance of the lipid bilayer of biomembranes. Moreover it suggests that these nanoemulsions could be promising new topical products to reduce the effects of sunlight on skin. PMID:26407526

  12. Crystal structures and morphologies of fractionated milk fat in nanoemulsions.

    PubMed

    Truong, Tuyen; Morgan, Garry P; Bansal, Nidhi; Palmer, Martin; Bhandari, Bhesh

    2015-03-15

    The triacylglycerol (TAG) crystal structures and morphologies of fractionated milk lipids in nanoemulsions were investigated at 4°C. Droplet size (0.17 versus 1.20 μm), lipid composition (stearin versus olein) and cooling rate (1 versus 10°C min(-1)) had an influence on the structural properties. Five crystal polymorphs (α, β'1, β'2, β1, and β2) were formed with either triple and/or double chain length structures in the solid phases of the emulsified systems. X-ray scattering peak intensities were reduced with the nanoemulsion particles. The internal structure of TAG exhibited stacking of individual lamellar layers (3.8-4.2 nm). Various anisometric shapes of fat nanoparticles were formed due to a highly sharp curvature of the nano-size droplets. The shape of olein nanoparticles was more polyhedral compared to the stearin. TAG crystals arranged in a planar-layered organisation at the slower cooling rate. These differences imply that the nanometric confinement of oil droplets modifies the fat crystal habit.

  13. Nano-Emulsions:. Overview and Applications

    NASA Astrophysics Data System (ADS)

    Li, Xiang; Anton, Nicolas; Vandamme, Thierry

    2013-09-01

    Nano-emulsions, also called sub-micrometer emulsions, are one of the most important nanocarriers in nanomedicine. More than 40% active susbtances are hydrophobic and therefore they are difficult to be formulated using conventional approaches. Nano-emulsion systems are considered as new vehicles for hydrophobic drug administration because they can enhance the penetration and absorption of these hydrophobic active compounds and provide safer and more patient-compliant dosage forms. This chapter describes the conception and methods of preparation of nano-emulsions, their characterization methods and their applications in pharmacetical areas.

  14. Phytosterol structured algae oil nanoemulsions and powders: improving antioxidant and flavor properties.

    PubMed

    Chen, Xiao-Wei; Chen, Ya-Jun; Wang, Jin-Mei; Guo, Jian; Yin, Shou-Wei; Yang, Xiao-Quan

    2016-09-14

    Algae oil, enriched with omega-3 long-chain polyunsaturated fatty acids (ω-3 LC-PUFA), is known for its health benefits. However, protection against lipid oxidation as well as masking of unpleasant fishy malodors in algae oil enriched foods is a big challenge to achieve. In this study, we firstly achieved a one-pot ultrasound emulsification strategy (alternative heating-homogenization) to prepare phytosterol structured thermosensitive algae oil-in-water nanoemulsion stabilized by quillaja saponin. After spray drying, the resulting algae oil powders from the structured nanoemulsion templates exhibit an excellent reconstructed behavior, even after 30 d of storage. Furthermore, an enhanced oxidative stability was obtained by reducing both the primary and secondary oxidation products through formulation with β-sitosterol and γ-oryzanol, which are natural antioxidants. Following the results of headspace volatiles using dynamic headspace-gas chromatography-mass spectrometry (DHS-GC-MS), it was clear that the structured algae oil-loaded nanoemulsion and powder had lower levels of fishy off-flavour (e.g., (Z)-heptenal, decanal, ethanone, and hexadecenoic acid), whereas the control emulsion and oil powder without structure performed worse. This study demonstrated that the structure from phytosterols is an effective strategy to minimize the fishy off-flavour and maximize oxidative stability of both algae oil nanoemulsions and spray-dried powders, and opens up the possibility of formulation design in polyunsaturated oil encapsulates as novel delivery systems to apply in functional foods and beverages. PMID:27501908

  15. Impact of alcohols on the formation and stability of protein-stabilized nanoemulsions.

    PubMed

    Zeeb, Benjamin; Herz, Eva; McClements, David Julian; Weiss, Jochen

    2014-11-01

    Nanoemulsions are increasingly being used for encapsulation, protection, and delivery of bioactive lipids, however, their formation from natural emulsifiers is still challenging. We investigated the impact of alcohol on the formation and stability of protein-stabilized oil-in-water nanoemulsions prepared by high-pressure homogenization. The influence of different alcohols (ethanol, 1-propanol, and 1-butanol) at various concentrations (0-25% w/w) on the formation and stability of emulsions stabilized by sodium caseinate, whey protein isolate, and fish gelatin was investigated. The mean particle diameter decreased with increasing alcohol concentrations from 0 to 10%w/w, but extensive droplet aggregation occurred at higher levels. This phenomenon was attributed to enhanced protein-protein interactions between the adsorbed emulsifier molecules in the presence of alcohol leading to droplet flocculation. The smallest droplets (d<100nm) were obtained when 10%w/w 1-butanol was added to sodium caseinate-stabilized nanoemulsions, but relatively small droplets (d<150nm) could also be obtained in the presence of a food-grade alcohol (ethanol). This study demonstrated that alcohol addition might be a useful tool for producing protein-stabilized nanoemulsions suitable for use as delivery systems of lipophilic bioactive agents. PMID:25129338

  16. Phytosterol structured algae oil nanoemulsions and powders: improving antioxidant and flavor properties.

    PubMed

    Chen, Xiao-Wei; Chen, Ya-Jun; Wang, Jin-Mei; Guo, Jian; Yin, Shou-Wei; Yang, Xiao-Quan

    2016-09-14

    Algae oil, enriched with omega-3 long-chain polyunsaturated fatty acids (ω-3 LC-PUFA), is known for its health benefits. However, protection against lipid oxidation as well as masking of unpleasant fishy malodors in algae oil enriched foods is a big challenge to achieve. In this study, we firstly achieved a one-pot ultrasound emulsification strategy (alternative heating-homogenization) to prepare phytosterol structured thermosensitive algae oil-in-water nanoemulsion stabilized by quillaja saponin. After spray drying, the resulting algae oil powders from the structured nanoemulsion templates exhibit an excellent reconstructed behavior, even after 30 d of storage. Furthermore, an enhanced oxidative stability was obtained by reducing both the primary and secondary oxidation products through formulation with β-sitosterol and γ-oryzanol, which are natural antioxidants. Following the results of headspace volatiles using dynamic headspace-gas chromatography-mass spectrometry (DHS-GC-MS), it was clear that the structured algae oil-loaded nanoemulsion and powder had lower levels of fishy off-flavour (e.g., (Z)-heptenal, decanal, ethanone, and hexadecenoic acid), whereas the control emulsion and oil powder without structure performed worse. This study demonstrated that the structure from phytosterols is an effective strategy to minimize the fishy off-flavour and maximize oxidative stability of both algae oil nanoemulsions and spray-dried powders, and opens up the possibility of formulation design in polyunsaturated oil encapsulates as novel delivery systems to apply in functional foods and beverages.

  17. Children's Explanations of Family Resemblances.

    ERIC Educational Resources Information Center

    Horobin, Karen D.

    Four studies investigated children's explanations for family resemblance and species-typical characteristics, under different conditions of biological parentage and rearing environment. Participating were 226 children between 3 and 11 years. Children Children were presented with a number of different tasks, some involving people and some domestic…

  18. Nanoemulsion: process selection and application in cosmetics--a review.

    PubMed

    Yukuyama, M N; Ghisleni, D D M; Pinto, T J A; Bou-Chacra, N A

    2016-02-01

    In recent decades, considerable and continuous growth in consumer demand in the cosmetics field has spurred the development of sophisticated formulations, aiming at high performance, attractive appearance, sensorial benefit and safety. Yet despite increasing demand from consumers, the formulator faces certain restrictions regarding the optimum equilibrium between the active compound concentration and the formulation base taking into account the nature of the skin structure, mainly concerning to the ideal penetration of the active compound, due to the natural skin barrier. Emulsion is a mixture of two immiscible phases, and the interest in nanoscale emulsion has been growing considerably in recent decades due to its specific attributes such as high stability, attractive appearance and drug delivery properties; therefore, performance is expected to improve using a lipid-based nanocarrier. Nanoemulsions are generated by different approaches: the so-called high-energy and low-energy methods. The global overview of these mechanisms and different alternatives for each method are presented in this paper, along with their benefits and drawbacks. As a cosmetics formulation is reflected in product delivery to consumers, nanoemulsion development with prospects for large-scale production is one of the key attributes in the method selection process. Thus, the aim of this review was to highlight the main high- and low-energy methods applicable in cosmetics and dermatological product development, their specificities, recent research on these methods in the cosmetics and consideration for the process selection optimization. The specific process with regard to inorganic nanoparticles, polymer nanoparticles and nanocapsule formulation is not considered in this paper.

  19. Nanoemulsions as vehicles for transdermal delivery of aceclofenac.

    PubMed

    Shakeel, Faiyaz; Baboota, Sanjula; Ahuja, Alka; Ali, Javed; Aqil, Mohammed; Shafiq, Sheikh

    2007-12-14

    The aim of the present study was to investigate the potential of a nanoemulsion formulation for transdermal delivery of aceclofenac. Various oil-in-water nanoemulsions were prepared by the spontaneous emulsification method. The nanoemulsion area was identified by constructing pseudoternary phase diagrams. The prepared nanoemulsions were subjected to different thermodynamic stability tests. The nanoemulsion formulations that passed thermodynamic stability tests were characterized for viscosity, droplet size, transmission electron microscopy, and refractive index. Transdermal permeation of aceclofenac through rat abdominal skin was determined by Franz diffusion cell. The in vitro skin permeation profile of optimized formulations was compared with that of aceclofenac conventional gel and nanoemulsion gel. A significant increase in permeability parameters such as steady-state flux (J(ss)), permeability coefficient (K(p)), and enhancement ratio (E(r)) was observed in optimized nanoemulsion formulation F1, which consisted of 2% wt/wt of aceclofenac, 10% wt/wt of Labrafil, 5% wt/wt of Triacetin, 35.33% wt/wt of Tween 80, 17.66% wt/wt of Transcutol P, and 32% wt/wt of distilled water. The anti-inflammatory effects of formulation F1 showed a significant increase (P < .05) in percent inhibition value after 24 hours when compared with aceclofenac conventional gel and nanoemulsion gel on carrageenan-induced paw edema in rats. These results suggested that nanoemulsions are potential vehicles for improved transdermal delivery of aceclofenac.

  20. Slow, nondiffusive dynamics in concentrated nanoemulsions

    NASA Astrophysics Data System (ADS)

    Guo, H.; Wilking, J. N.; Liang, D.; Mason, T. G.; Harden, J. L.; Leheny, R. L.

    2007-04-01

    Using multispeckle x-ray photon correlation spectroscopy, we have measured the slow, wave-vector-dependent dynamics of concentrated, disordered nanoemulsions composed of silicone oil droplets in water. The intermediate scattering function possesses a compressed exponential line shape and a relaxation time that varies inversely with wave vector. We interpret this dynamics as strain in response to local stress relaxation. The motion includes a transient component whose characteristic velocity decays exponentially with time following a mechanical perturbation of the nanoemulsions and a second component whose characteristic velocity is essentially independent of time. The steady-state characteristic velocity is surprisingly insensitive to the droplet volume fraction in the concentrated regime, indicating that the strain motion is only weakly dependent on the droplet-droplet interactions.

  1. Mesoporous organohydrogels from thermogelling photocrosslinkable nanoemulsions

    NASA Astrophysics Data System (ADS)

    Helgeson, Matthew E.; Moran, Shannon E.; An, Harry Z.; Doyle, Patrick S.

    2012-04-01

    We report the formation of mesoporous organohydrogels from oil-in-water nanoemulsions containing an end-functionalized oligomeric gelator in the aqueous phase. The nanoemulsions exhibit an abrupt thermoreversible transition from a low-viscosity liquid to a fractal-like colloidal gel of droplets with mesoscale porosity and solid-like viscoelasticity with moduli approaching 100 kPa, possibly the highest reported for an emulsion-based system. We hypothesize that gelation is brought about by temperature-induced interdroplet bridging of the gelator, as shown by its dependence on the gelator chemistry. The use of photocrosslinkable gelators enables the freezing of the nanoemulsion’s microstructure into a soft hydrogel nanocomposite containing a large fraction of dispersed liquid hydrophobic compartments, and we show its use in the encapsulation and release of lipophilic biomolecules. The tunable structural, mechanical and optical properties of these organohydrogels make them a robust material platform suitable for a wide range of applications.

  2. In vitro scleral lutein distribution by cyclodextrin containing nanoemulsions.

    PubMed

    Liu, Chi-Hsien; Lai, Kuan-Yu; Wu, Wei-Chi; Chen, Yu-Jui; Lee, Wei-Shiou; Hsu, Ching-Yun

    2015-01-01

    Lutein is a macular pigment that contributes to maintaining eye health. The development of lutein-laden nanocarriers for ocular delivery would have the advantages of user friendliness and cost-effectiveness. Nano-scaled vehicles such as cyclodextrin (CD) and nanoemulsion could overcome the barriers caused by the scleral structure. This study focused on the development of hybrid nanocarriers containing nanoemulsion and CD for scleral lutein accumulation. In the presence of the nanoemulsion, CD forms such as βCD and hydroxyethyl (HE) βCD increased the partition of lutein into the porcine sclera. A combination of nanoemulsion and 2% HEβCD enhanced lutein accumulation to 119±6 µg g(-1) h(-1), which was 9.2-fold higher than that with lutein suspension alone. We explored the dose effect of CD in nanoemulsion on scleral lutein and found that the scleral accumulation of lutein was enhanced by increasing the CD content. The novel nanoemulsion had 95% drug-loading efficiency and low cytotoxicity in retinal cells. The CD-modified nanoemulsion not only improved the stability and entrapment efficacy of lutein in the aqueous system but also enhanced scleral lutein accumulation. An increase in the partition coefficient of lutein in porcine sclera when using the CD-modified nanoemulsion was also confirmed.

  3. Archaic artifacts resembling celestial spheres

    NASA Astrophysics Data System (ADS)

    Dimitrakoudis, S.; Papaspyrou, P.; Petoussis, V.; Moussas, X.

    We present several bronze artifacts from the Archaic Age in Greece (750-480 BC) that resemble celestial spheres or forms of other astronomical significance. They are studied in the context of the Dark Age transition from Mycenaean Age astronomical themes to the philosophical and practical revival of astronomy in the Classical Age with its plethora of astronomical devices. These artifacts, mostly votive in nature are spherical in shape and appear in a variety of forms their most striking characteristic being the depiction of meridians and/or an equator. Most of those artifacts come from Thessaly, and more specifically from the temple of Itonia Athena at Philia, a religious center of pan-Hellenic significance. Celestial spheres, similar in form to the small artifacts presented in this study, could be used to measure latitudes, or estimate the time at a known place, and were thus very useful in navigation.

  4. The First Scale-Up Production of Theranostic Nanoemulsions

    PubMed Central

    Liu, Lu; Bagia, Christina; Janjic, Jelena M.

    2015-01-01

    Abstract Theranostic nanomedicines are a promising new technological advancement toward personalized medicine. Although much progress has been made in pre-clinical studies, their clinical utilization is still under development. A key ingredient for successful theranostic clinical translation is pharmaceutical process design for production on a sufficient scale for clinical testing. In this study, we report, for the first time, a successful scale-up of a model theranostic nanoemulsion. Celecoxib-loaded near-infrared-labeled perfluorocarbon nanoemulsion was produced on three levels of scale (small at 54 mL, medium at 270 mL, and large at 1,000 mL) using microfluidization. The average size and polydispersity were not affected by the equipment used or production scale. The overall nanoemulsion stability was maintained for 90 days upon storage and was not impacted by nanoemulsion production scale or composition. Cell-based evaluations show comparable results for all nanoemulsions with no significant impact of nanoemulsion scale on cell toxicity and their pharmacological effects. This report serves as the first example of a successful scale-up of a theranostic nanoemulsion and a model for future studies on theranostic nanomedicine production and development. PMID:26309798

  5. Effect of PEG surface conformation on anticancer activity and blood circulation of nanoemulsions loaded with tocotrienol-rich fraction of palm oil.

    PubMed

    Alayoubi, Alaadin; Alqahtani, Saeed; Kaddoumi, Amal; Nazzal, Sami

    2013-10-01

    Tocotrienol-rich fraction of palm oil, which contains the isomers of vitamin E, was shown to possess potent anticancer activity against mammary adenocarcinoma cell lines. Its clinical use, however, is limited by poor oral bioavailability and short half-life. Previously, we developed tocotrienol-rich lipid nanoemulsions for intravenous administration. The objective of this study was to investigate the effect of surface grafted polyethylene glycol (PEG) on the properties of the nanoemulsions. PEGylation was achieved by the addition of equimolar PEG groups using poloxamer or 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(polyethylene glycol)2000] (PEG2000-DSPE). The effect of PEG surface topography on the antiproliferative activity of nanoemulsions against mammary adenocarcinoma cells, their susceptibility to protein adsorption, and its effect on blood hemolysis and circulation time was investigated. Nanoemulsions PEGylated with poloxamer or PEG2000-DSPE were stable under physical stress. Poloxamer nanoemulsion, however, displayed higher uptake and potency against MCF-7 tumor cells in 2D and 3D culture and increased hemolytic effect and susceptibility to IgG adsorption, which was reflected in its rapid clearance and short circulation half-life (1.7 h). Conversely, PEGylation with PEG2000-DSPE led to a 7-fold increase in mean residence time (12.3 h) after IV injection in rats. Reduced activity in vitro and improved circulation time suggested strong shielding of plasma proteins from the droplets. Differences between the nanoemulsions were attributed to polymer imbibitions and the differences in PEG conformation and density on the surface of the droplets.

  6. Droplet microfluidics with a nanoemulsion continuous phase.

    PubMed

    Gu, Tonghan; Yeap, Eunice W Q; Somasundar, Ambika; Chen, Ran; Hatton, T Alan; Khan, Saif A

    2016-07-01

    We present the first study of a novel, generalizable method that uses a water-in-oil nanoemulsion as the continuous phase to generate uniform aqueous micro-droplets in a capillary-based microfluidic system. We first study the droplet generation mechanism in this system and compare it to the more conventional case where a simple oil/solvent (with surfactant) is used as the continuous phase. Next, we present two versatile methods - adding demulsifying chemicals and heat treatment - to allow active online chemical interaction between the continuous and dispersed phases. These methods allow each generated micro-droplet to act as a well-mixed micro-reactor with walls that are 'permeable' to the nanoemulsion droplets and their contents. Finally, we demonstrate an application of this system in the fabrication of uniform hydrogel (alginate) micro-beads with control over particle properties such as size and swelling. Our work expands the toolbox of droplet-based microfluidics, enabling new opportunities and applications involving active colloidal continuous phases carrying chemical payloads, both in advanced materials synthesis and droplet-based screening and diagnostic methods.

  7. Pentyl Gallate Nanoemulsions as Potential Topical Treatment of Herpes Labialis.

    PubMed

    Kelmann, Regina G; Colombo, Mariana; De Araújo Lopes, Sávia Caldeira; Nunes, Ricardo J; Pistore, Morgana; Dall Agnol, Daniele; Rigotto, Caroline; Silva, Izabella Thais; Roman, Silvane S; Teixeira, Helder F; Oliveira Simões, Cláudia M; Koester, Letícia S

    2016-07-01

    Previous studies have demonstrated the antiherpes activity of pentyl gallate (PG), suggesting that it could be a promising candidate for the topical treatment of human herpes labialis. PG low aqueous solubility represents a major drawback to its incorporation in topical dosage forms. Hence, the feasibility of incorporating PG into nanoemulsions, the ability to penetrate the skin, to inhibit herpes simplex virus (HSV)-1 replication, and to cause dermal sensitization or toxicity were evaluated. Oil/water nanoemulsions containing 0.5% PG were prepared by spontaneous emulsification. The in vitro PG distribution into porcine ear skin after topical application of nanoemulsions was assessed, and the in vitro antiviral activity against HSV-1 replication was evaluated. Acute dermal toxicity and risk of dermal sensitization were evaluated in rat model. Nanoemulsions presented nanometric particle size (from 124.8 to 143.7 nm), high zeta potential (from -50.1 to -66.1 mV), loading efficiency above 99%, and adequate stability during 12 months. All formulations presented anti-HSV-1 activity. PG was able to reach deeper into the dermis more efficiently from the nanoemulsion F4. This formulation as well as PG were considered safe for topical use. Nanoemulsions seem to be a safe and effective approach for topically delivering PG in the treatment of human herpes labialis infection.

  8. Evaluation of the versatile character of a nanoemulsion formulation.

    PubMed

    Gué, E; Since, M; Ropars, S; Herbinet, R; Le Pluart, L; Malzert-Fréon, A

    2016-02-10

    The formulate-ability of six model active pharmaceutical ingredients (API), with different physico-chemical profiles, in a nanoemulsion designed to be intraveinously administrable was explored. Nanoemulsions were spontaneously generated at room temperature by pouring a phosphate buffer in an anhydrous mixture containing pharmaceutically acceptable triglycerides and non-ionic surfactants. After determination of the apparent solubility of each API in excipients and characterization of mixtures by DSC, API-loaded nanoemulsions were formulated and characterized in terms of granulometric properties, surface potential, drug recovery efficiency, pH, osmolarity, in vitro drug release, and stability. Except ciprofloxacin, a BCS class IV drug, all studied APIs were soluble in at least one excipient used, i.e. Labrasol. At 2 wt% API, all drug-loaded nanoemulsions present properties compatible with i.v. administration. The formulation should permit to increase apparent solubility of poorly water-soluble APIs, and also to prolong delivery of hydrophobic as well of more hydrophilic compounds. Herein, the relative affinity of the API for nanodroplets and the release medium would directly influence drug release profiles. Nanoemulsions were stable for 7 days. They could also been extemporaneously reconstituted before use. Such a versatile nanoemulsion would provide a valuable option as formulation strategy for improvement of drug properties. PMID:26685727

  9. Cationic nanoemulsions as potential carriers for intracellular delivery

    PubMed Central

    Khachane, P.V.; Jain, A.S.; Dhawan, V.V.; Joshi, G.V.; Date, A.A.; Mulherkar, R.; Nagarsenker, M.S.

    2014-01-01

    Successful cytosolic delivery enables opportunities for improved treatment of various genetic disorders, infectious diseases and cancer. Cationic nanoemulsions were designed using alternative excipients and evaluated for particle size, charge, effect of sterilization on its stability, DNA condensation potential and cellular uptake efficiency. Various concentrations of non-ionic and ionic stabilizers were evaluated to design formula for colloidally stable cationic nanoemulsion. The nanoemulsion comprised of 5% Capmul MCM, 0.5% didodecyldimethylammonium bromide (DDAB), 1% phospholipid, 1% Poloxamer 188 and 2.25% glycerol and possessed particle size of 81.6 ± 3.56 nm and 137.1 ± 1.57 nm before and after steam sterilization, respectively. DNA condensation studies were carried out at various nanoemulsion: DNA ratios ranging from 1:1 to 10:1. Cell uptake studies were conducted on human embryonic kidney (HEK) cell lines which are widely reported for transfection studies. The nanoemulsions showed excellent cellular uptake as evaluated by fluorescence microscopy and flow cytometry. Overall, a colloidally stable cationic nanoemulsion with good DNA condensation ability was successfully fabricated for efficient cytosolic delivery and potential for in vivo effectiveness. PMID:25972740

  10. Cationic nanoemulsions as potential carriers for intracellular delivery.

    PubMed

    Khachane, P V; Jain, A S; Dhawan, V V; Joshi, G V; Date, A A; Mulherkar, R; Nagarsenker, M S

    2015-04-01

    Successful cytosolic delivery enables opportunities for improved treatment of various genetic disorders, infectious diseases and cancer. Cationic nanoemulsions were designed using alternative excipients and evaluated for particle size, charge, effect of sterilization on its stability, DNA condensation potential and cellular uptake efficiency. Various concentrations of non-ionic and ionic stabilizers were evaluated to design formula for colloidally stable cationic nanoemulsion. The nanoemulsion comprised of 5% Capmul MCM, 0.5% didodecyldimethylammonium bromide (DDAB), 1% phospholipid, 1% Poloxamer 188 and 2.25% glycerol and possessed particle size of 81.6 ± 3.56 nm and 137.1 ± 1.57 nm before and after steam sterilization, respectively. DNA condensation studies were carried out at various nanoemulsion: DNA ratios ranging from 1:1 to 10:1. Cell uptake studies were conducted on human embryonic kidney (HEK) cell lines which are widely reported for transfection studies. The nanoemulsions showed excellent cellular uptake as evaluated by fluorescence microscopy and flow cytometry. Overall, a colloidally stable cationic nanoemulsion with good DNA condensation ability was successfully fabricated for efficient cytosolic delivery and potential for in vivo effectiveness.

  11. Lipid nanoparticles for the topical delivery of retinoids and derivatives.

    PubMed

    Morales, Javier O; Valdés, Karina; Morales, Javier; Oyarzun-Ampuero, Felipe

    2015-01-01

    Retinoids are lipophilic compounds that are highly used in cosmetics/therapeutics for skin disorders. Conventional formulations are limited by poor water solubility, high chemical/photochemical instability and the irritation of retinoids. Interestingly, lipid nanoparticles enable the administration of retinoids in aqueous media, providing drug stabilization and controlled release. Recently, it has been demonstrated that retinoids in solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions and nanocapsules can decrease degradation, improve targeting and enhance efficacy for the treatment of skin disorders. This article focuses on the formulation, fabrication, characterization and in vitro/in vivo evaluation of solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions and nanocapsules loaded with retinoids for skin administration. Furthermore, the incorporation of these lipid nanoparticles into secondary vehicles is discussed. PMID:25600970

  12. Development of a frozen yogurt fortified with a nano-emulsion containing purple rice bran oil

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The objectives of this study were to develop and evaluate a frozen yogurt (FY) fortified with a nano-emulsion containing purple rice bran oil (NPRBO). A nano-emulsion with a droplet size range of 150-300 nm was produced by sonication followed by ultra-shear homogenization. The nano-emulsion was mi...

  13. Encapsulation and Delivery of Crystalline Hydrophobic Nutraceuticals using Nanoemulsions: Factors Affecting Polymethoxyflavone Solubility.

    PubMed

    Li, Yan; Xiao, Hang; McClements, David Julian

    2012-12-01

    Polymethoxyflavones (PMF) isolated from citrus peel have potent anti-cancer activity, however their utilization as functional ingredients in foods is currently limited because of their high melting point and poor water-solubility. The influence of oil type and concentration, hydrophilic polymer addition, and simulated intestinal conditions on PMF (5-hydroxytangeretin) solubility in solutions and nanoemulsions was examined. The saturation concentration of PMF in water was relatively low (0.93 µM), but could be increased appreciably by adding certain hydrophilic polymers: polyethylene glycol (PEG) and β-cyclodextrin (CD) were ineffective at increasing solubility, but poly(vinyl alcohol) (PVA) and hydroxypropyl methylcellulose (HPMC) greatly enhanced solubility (e.g., > 6 µM for 0.5 % polymer). PMF was more soluble in medium chain triglycerides (MCT, 6.1 mM) than long chain triglycerides (LCT, 4.2 mM). The encapsulation efficiency of PMF in oil-in-water nanoemulsions was higher when MCT was used as the oil phase rather than LCT, and could be increased by increasing the oil droplet content. The solubility of PMF in simulated small intestinal fluids was increased by solubilization in bile micelles and mixed micelles formed during lipid digestion. These results have important implications for the development of functional foods fortified with bioactive hydrophobic components aimed at improving human health and wellness. PMID:23646037

  14. Potential of nanoemulsions for intravenous delivery of rifampicin.

    PubMed

    Ahmed, M; Ramadan, W; Rambhu, D; Shakeel, F

    2008-11-01

    The aim of the present study was to develop, characterize and evaluate nanoemulsion formulations for intravenous delivery of rifampicin (RIF). Different oil-in-water (o/w) nanoemulsions were prepared by the aqueous phase titration method. Prepared nanoemulsions were subjected to thermodynamic stability tests for phase separation, creaming, cracking, coalescence or phase inversion and dispersibility test for dilution capacity. Nanoemulsion formulations which passed these tests were characterized in terms of droplet size, viscosity, entrapment efficiency, homogeneity and pH. The selected formulations were subjected to in vitro dissolution studies using a dissolution apparatus-XXIII in dialysis bag. Best results were obtained with the formulation which consisted of 150 mg of RIF, 15% w/w of Sefsol 218, 18.75% w/w of Tween 80, 6.25% w/w of Tween 85 and 60% w/w of normal saline. The optimized formulation was also subjected to stability studies according to the ICH guidelines. The formulation was found to be stable for more than19 months. These results indicated the potential of nanoemulsions for intravenous delivery of RIF.

  15. Thyme oil nanoemulsions coemulsified by sodium caseinate and lecithin.

    PubMed

    Xue, Jia; Zhong, Qixin

    2014-10-01

    Many nanoemulsions are currently formulated with synthetic surfactants. The objective of the present work was to study the possibility of blending sodium caseinate (NaCas) and lecithin to prepare transparent thyme oil nanoemulsions. Thyme oil was emulsified using NaCas and soy lecithin individually or in combination at neutral pH by shear homogenization. The surfactant combination improved the oil content in transparent/translucent nanoemulsions, from 1.0% to 2.5% w/v for 5% NaCas with and without 1% lecithin, respectively. Nanoemulsions prepared with the NaCas-lecithin blend had hydrodynamic diameters smaller than 100 nm and had significantly smaller and more narrowly distributed droplets than those prepared with NaCas or lecithin alone. Particle dimension and protein surface load data suggested the coadsorption of both surfactants on oil droplets. These characteristics of nanoemulsions minimized destabilization mechanisms of creaming, coalescence, and Ostwald ripening, as evidenced by no significant changes in appearance and particle dimension after 120-day storage at 21 °C.

  16. Characteristics of Nano-emulsion for Cold Thermal Storage

    NASA Astrophysics Data System (ADS)

    Fumoto, Koji; Kawaji, Masahiro; Kawanami, Tsuyoshi

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

  17. Mucoadhesive dexamethasone acetate-polymyxin B sulfate cationic ocular nanoemulsion--novel combinatorial formulation concept.

    PubMed

    Li, X; Müller, R H; Keck, C M; Bou-Chacra, N A

    2016-06-01

    Dexamethasone acetate (DEX) and polymyxin B sulfate (polymyxin B) were formulated as a cationic nanoemulsion for the treatment of ophthalmic infections. As novel concept, the positive charge to achieve mucoadhesion was not generated by toxicologically and regulatorily problematic cationic lipids or polymers, but by using a positively charged drug in combination with positively charged preservatives. The preservative also acts as co-surfactant to stabilize the emulsion. Nanoemulsions with the lipid phase Eutanol G-Lipoid S 100 (70%:30%) containing 0.05% (w/w) DEX were produced by high pressure homogenization, followed by dissolving the hydrophilic molecules in the water phase, e.g. polymyxin B (0.1%, w/w), cetylpyridinium chloride (0.01%, w/w) and glycerol (2.6%, w/w) to yield a combination product. The particles were below 200 nm with narrow size distribution. The osmolality (374 mOsm/kg), pH (5.31) and viscosity (2.45 mPa s at 37 degrees C) were compatible to the ocular administration. The zeta potential of the optimized formulation was shifted from approx. +9 mV to -11 mV after mucin incubation. The in vitro test revealed no potential cytotoxicity. The final products were stable after 180 days of storage at 4 degrees C and room temperature. The developed product is a viable alternative to the commercial ophthalmic suspensions. Moreover, this concept of generating the positive charge by cationic drug and/or preservative addition can be transferred to other ophthalmic products. PMID:27455551

  18. Antimicrobial Activity of Nanoemulsion on Cariogenic Planktonic and Biofilm Organisms

    PubMed Central

    Amaechi, Bennett T.; Rawls, H Ralph; Valerie, A Lee

    2011-01-01

    Introduction Nanoemulsions (NE) are a unique class of disinfectants produced by mixing a water immiscible liquid phase into an aqueous phase under high shear forces. NE have antimicrobial properties and are also effective anti-biofilm agents. Materials and Methods The effectiveness of nanoemulsion and its components was determined against Streptococcus mutans and Lactobacillus casei by live/dead staining. In vitro antimicrobial effectiveness of nanoemulsion against planktonic Streptococcus mutans, Lactobacillus casei, Actinomyces viscosus, Candida albicans and mixed culture was determined by a serial dilution technique to obtain minimum inhibitory concentration and minimum bactericidal concentration (MIC/MBC). In addition, efficacy was investigated by kinetics of killing, adherence and biofilm assays. Results Compared to its components, nanoemulsion showed notable antimicrobial activity against biofilm organisms, up to 83.0% kill within 1 min. NE dilutions ranging from 243 to 19683 were effective against planktonic S. mutans, L. casei, A. viscosus, C. albicans and mixed culture of these four strains as shown through MIC/MBC assays. NE showed antimicrobial activity against planktonic cells at high dilutions, confirmed by time kill studies. The level of adhesion on glass surface was reduced by 94.2 to 99.5 % in nanoemulsion treated groups (p < 0.001). 4-day-old S. mutans, L. casei, A. viscosus, C. albicans and mixed cultures biofilms treated with NE showed reductions of bacterial counts with decreasing dilutions (p < 0.001). Conclusion These results suggest that nanoemulsion has effective anti-cariogenic activity against cariogenic microorganisms and may be a useful medication in the prevention of caries. PMID:21807359

  19. Development of an insecticidal nanoemulsion with Manilkara subsericea (Sapotaceae) extract

    PubMed Central

    2014-01-01

    Background Plants have been recognized as a good source of insecticidal agents, since they are able to produce their own defensives to insect attack. Moreover, there is a growing concern worldwide to develop pesticides with low impact to environment and non-target organisms. Hexane-soluble fraction from ethanolic crude extract from fruits of Manilkara subsericea and its triterpenes were considered active against a cotton pest (Dysdercus peruvianus). Several natural products with insecticidal activity have poor water solubility, including triterpenes, and nanotechnology has emerged as a good alternative to solve this main problem. On this context, the aim of the present study was to develop an insecticidal nanoemulsion containing apolar fraction from fruits of Manilkara subsericea. Results It was obtained a formulation constituted by 5% of oil (octyldodecyl myristate), 5% of surfactants (sorbitan monooleate/polysorbate 80), 5% of apolar fraction from M. subsericea and 85% of water. Analysis of mean droplet diameter (155.2 ± 3.8 nm) confirmed this formulation as a nanoemulsion. It was able to induce mortality in D. peruvianus. It was observed no effect against acetylcholinesterase or mortality in mice induced by the formulation, suggesting the safety of this nanoemulsion for non-target organisms. Conclusions The present study suggests that the obtained O/A nanoemulsion may be useful to enhance water solubility of poor water soluble natural products with insecticidal activity, including the hexane-soluble fraction from ethanolic crude extract from fruits of Manilkara subsericea. PMID:24886215

  20. Essential oil nanoemulsions as antimicrobial agents in food.

    PubMed

    Donsì, Francesco; Ferrari, Giovanna

    2016-09-10

    The crescent interest in the use of essential oils (EOs) as natural antimicrobials and preservatives in the food industry has been driven in the last years by the growing consumers' demand for natural products with improved microbial safety, and fresh-like organoleptic properties. Nanoemulsions efficiently contribute to support the use of EOs in foods by increasing their dispersibility in the food areas where microorganisms grow and proliferate, by reducing the impact on the quality attributes of the product, as well as by enhancing their antimicrobial activity. Understanding how nanoemulsions intervene on the mass transfer of EOs to the cell membrane and on the mechanism of antimicrobial action will support the engineering of more effective delivery systems and foster the application of EOs in real food systems. This review focuses on the enabling contribution of nanoemulsions to the use of EOs as natural preservative agents in food, (a) specifically addressing the formulation and fabrication of stable EO nanoemulsions, (b) critically analyzing the reported antimicrobial activity data, both in vitro and in product, to infer the impact of the delivery system on the mechanisms of action of EOs, as well as (c) discussing the regulatory issues associated with their use in food systems. PMID:27416793

  1. Characterization of rice bran wax policosanol and its nanoemulsion formulation.

    PubMed

    Ishaka, Aminu; Umar Imam, Mustapha; Mahamud, Rozi; Zuki, Abu Bakar Zakaria; Maznah, Ismail

    2014-01-01

    Policosanol, a mixture of long-chain alcohols found in animal and plant waxes, has several biological effects; however, it has a bioavailability of less than 10%. Therefore, there is a need to improve its bioavailability, and one of the ways of doing this is by nanoemulsion formulation. Different droplet size distributions are usually achieved when emulsions are formed, which solely depends on the preparation method used. Mostly, emulsions are intended for better delivery with maintenance of the characteristics and properties of the leading components. In this study, policosanol was extracted from rice bran wax, its composition was determined by gas chromatography mass spectrophotometry, nanoemulsion was made, and the physical stability characteristics were determined. The results showed that policosanol nanoemulsion has a nanosize particle distribution below 100 nm (92.56-94.52 nm), with optimum charge distribution (-55.8 to -45.12 mV), pH (6.79-6.92) and refractive index (1.50); these were monitored and found to be stable for 8 weeks. The stability of policosanol nanoemulsion confers the potential to withstand long storage times. PMID:24872689

  2. Characterization of rice bran wax policosanol and its nanoemulsion formulation.

    PubMed

    Ishaka, Aminu; Umar Imam, Mustapha; Mahamud, Rozi; Zuki, Abu Bakar Zakaria; Maznah, Ismail

    2014-01-01

    Policosanol, a mixture of long-chain alcohols found in animal and plant waxes, has several biological effects; however, it has a bioavailability of less than 10%. Therefore, there is a need to improve its bioavailability, and one of the ways of doing this is by nanoemulsion formulation. Different droplet size distributions are usually achieved when emulsions are formed, which solely depends on the preparation method used. Mostly, emulsions are intended for better delivery with maintenance of the characteristics and properties of the leading components. In this study, policosanol was extracted from rice bran wax, its composition was determined by gas chromatography mass spectrophotometry, nanoemulsion was made, and the physical stability characteristics were determined. The results showed that policosanol nanoemulsion has a nanosize particle distribution below 100 nm (92.56-94.52 nm), with optimum charge distribution (-55.8 to -45.12 mV), pH (6.79-6.92) and refractive index (1.50); these were monitored and found to be stable for 8 weeks. The stability of policosanol nanoemulsion confers the potential to withstand long storage times.

  3. Characterization of rice bran wax policosanol and its nanoemulsion formulation

    PubMed Central

    Ishaka, Aminu; Umar Imam, Mustapha; Mahamud, Rozi; Zuki, Abu Bakar Zakaria; Maznah, Ismail

    2014-01-01

    Policosanol, a mixture of long-chain alcohols found in animal and plant waxes, has several biological effects; however, it has a bioavailability of less than 10%. Therefore, there is a need to improve its bioavailability, and one of the ways of doing this is by nanoemulsion formulation. Different droplet size distributions are usually achieved when emulsions are formed, which solely depends on the preparation method used. Mostly, emulsions are intended for better delivery with maintenance of the characteristics and properties of the leading components. In this study, policosanol was extracted from rice bran wax, its composition was determined by gas chromatography mass spectrophotometry, nanoemulsion was made, and the physical stability characteristics were determined. The results showed that policosanol nanoemulsion has a nanosize particle distribution below 100 nm (92.56–94.52 nm), with optimum charge distribution (−55.8 to −45.12 mV), pH (6.79–6.92) and refractive index (1.50); these were monitored and found to be stable for 8 weeks. The stability of policosanol nanoemulsion confers the potential to withstand long storage times. PMID:24872689

  4. Essential oil nanoemulsions as antimicrobial agents in food.

    PubMed

    Donsì, Francesco; Ferrari, Giovanna

    2016-09-10

    The crescent interest in the use of essential oils (EOs) as natural antimicrobials and preservatives in the food industry has been driven in the last years by the growing consumers' demand for natural products with improved microbial safety, and fresh-like organoleptic properties. Nanoemulsions efficiently contribute to support the use of EOs in foods by increasing their dispersibility in the food areas where microorganisms grow and proliferate, by reducing the impact on the quality attributes of the product, as well as by enhancing their antimicrobial activity. Understanding how nanoemulsions intervene on the mass transfer of EOs to the cell membrane and on the mechanism of antimicrobial action will support the engineering of more effective delivery systems and foster the application of EOs in real food systems. This review focuses on the enabling contribution of nanoemulsions to the use of EOs as natural preservative agents in food, (a) specifically addressing the formulation and fabrication of stable EO nanoemulsions, (b) critically analyzing the reported antimicrobial activity data, both in vitro and in product, to infer the impact of the delivery system on the mechanisms of action of EOs, as well as (c) discussing the regulatory issues associated with their use in food systems.

  5. The preparation of 3,5-dihydroxy-4-isopropylstilbene nanoemulsion and in vitro release

    PubMed Central

    Zhang, Yue; Gao, Jungang; Zheng, Hetang; Zhang, Ran; Han, Yucui

    2011-01-01

    We have reported a novel procedure to prepare 3,5-dihydroxy-4-isopropylstilbene (DHPS) nanoemulsion, using a low-energy emulsification method. Based on the phase diagram, the optimum prescription of nanoemulsion preparation was screened. With polyoxyethylenated castor oil (EL-40) as the surfactant, ethanol as the co-surfactant, and isopropyl myristate (IPM) as the oil phase, the DHPS nanoemulsion was obtained with a transparent appearance, little viscosity, and spherically uniform distribution verified by transmission electron microscopy and laser scattering analyzer. The nanoemulsion was also determined by FT-Raman spectroscopy. The DHPS nanoemulsion demonstrated good stability and stable physical and chemical properties. The nanoemulsion dramatically improved the transdermal release of DHPS (from 8.02 μg · cm−2 to 273.15 μg · cm−2) and could become a favorable new dosage form for DHPS. PMID:21674020

  6. Nanoemulsion of eucalyptus oil and its larvicidal activity against Culex quinquefasciatus.

    PubMed

    Sugumar, S; Clarke, S K; Nirmala, M J; Tyagi, B K; Mukherjee, A; Chandrasekaran, N

    2014-06-01

    Filariasis is a mosquito-borne disease that causes lymphedema and the main vector is Culex quinquefasciatus. A simple measure was taken to eradicate the vector using nanoemulsion. Eucalyptus oil nanoemulsion was formulated in various ratios comprising of eucalyptus oil, tween 80 and water by ultrasonication. The stability of nanoemulsion was observed over a period of time and 1:2 ratios of eucalyptus oil (6%) and surfactant (12%) was found to be stable. The formulated eucalyptus oil nanoemulsion was characterized by transmission electron microscopy and dynamic light scattering. The nanoemulsion droplets were found to have a Z-average diameter of 9.4 nm and were spherical in shape. The larvicidal activity of eucalyptus oil nanoemulsion and bulk emulsion was tested and compared. Our nanoemulsion showed higher activity when compared to bulk emulsion. The histopathology of larvae-treated and untreated nanoemulsion was analyzed. Furthermore, biochemical assays were carried out to examine the effect of nanoemulsion on biochemical characteristics of larvae. The treated larval homogenate showed decrease in total protein content and a significant reduction in the levels of acetylcholinesterase. The levels of acid and alkaline phosphatase also showed reduction as compared to control larval homogenate.

  7. Eugenol-loaded antimicrobial nanoemulsion preserves fruit juice against, microbial spoilage.

    PubMed

    Ghosh, Vijayalakshmi; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2014-02-01

    Oil-in-water nanoemulsion was formulated using sesame oil, non-ionic surfactant (Tween20/Tween80) and water by ultrasound cavitation method. Development of nanoemulsion was optimized for process parameters such as surfactant type, surfactant concentration and emulsification time to obtain lower droplet diameter with greater stability. Increase in surfactant concentration and emulsification time resulted in nanoemulsion with minimized droplet diameter. Tween80 was more effective in reducing droplet size when compared to that of Tween20. Selected formulation with optimized process parameter (with oil-surfactant mixing ratio of 1:3 v/v and Tween80 as surfactant) was used for delivery of eugenol. Eugenol-loaded nanoemulsion was formulated with droplet diameter of 13 nm and was stable for more than 1 month. Sesame oil blended eugenol-loaded nanoemulsion demonstrated lower droplet size and higher stability than only-eugenol (without sesame oil) nanoemulsion. Eugenol-loaded nanoemulsion S3E3 exhibited antibacterial activity against Staphylococcus aureus. Inactivation kinetics of S. aureus showed time and concentration killing of bacteria upon treatment with S3E3 nanoemulsion. Fluorescence microscopy results demonstrated that S3E3 nanoemulsion treatment resulted in alteration of membrane permeability. In situ assessment of S3E3 in orange juice exhibited a significant reduction in the native bacteria population.

  8. Nanoemulsion of eucalyptus oil and its larvicidal activity against Culex quinquefasciatus.

    PubMed

    Sugumar, S; Clarke, S K; Nirmala, M J; Tyagi, B K; Mukherjee, A; Chandrasekaran, N

    2014-06-01

    Filariasis is a mosquito-borne disease that causes lymphedema and the main vector is Culex quinquefasciatus. A simple measure was taken to eradicate the vector using nanoemulsion. Eucalyptus oil nanoemulsion was formulated in various ratios comprising of eucalyptus oil, tween 80 and water by ultrasonication. The stability of nanoemulsion was observed over a period of time and 1:2 ratios of eucalyptus oil (6%) and surfactant (12%) was found to be stable. The formulated eucalyptus oil nanoemulsion was characterized by transmission electron microscopy and dynamic light scattering. The nanoemulsion droplets were found to have a Z-average diameter of 9.4 nm and were spherical in shape. The larvicidal activity of eucalyptus oil nanoemulsion and bulk emulsion was tested and compared. Our nanoemulsion showed higher activity when compared to bulk emulsion. The histopathology of larvae-treated and untreated nanoemulsion was analyzed. Furthermore, biochemical assays were carried out to examine the effect of nanoemulsion on biochemical characteristics of larvae. The treated larval homogenate showed decrease in total protein content and a significant reduction in the levels of acetylcholinesterase. The levels of acid and alkaline phosphatase also showed reduction as compared to control larval homogenate. PMID:24401169

  9. Phase Change Characteristics of a Nanoemulsion as a Latent Heat Storage Material

    NASA Astrophysics Data System (ADS)

    Fumoto, Koji; Sato, Noriaki; Kawaji, Masahiro; Kawanami, Tsuyoshi; Inamura, Takao

    2014-10-01

    The primary objective of this study was to investigate the fundamental phase change characteristics of a nanoemulsion using differential scanning calorimetry (DSC). Tetradecane, which has a slightly higher melting point than water, was utilized as the phase change material for the nanoemulsion. The melting point of the nanoemulsion, the melting peak temperature, and latent heat were examined in detail. Regarding the fundamental phase change characteristics of the nanoemulsion, it was found that its phase change characteristics were strongly affected by the temperature-scanning rate of the DSC. Moreover, it was confirmed that the phase change behavior does not change with repeated solidification and melting.

  10. Exotic Vegetable Oils for Cosmetic O/W Nanoemulsions: In Vivo Evaluation.

    PubMed

    Pereira, Tatiana A; Guerreiro, Carolina M; Maruno, Monica; Ferrari, Marcio; Rocha-Filho, Pedro Alves

    2016-01-01

    Oil-in-water nanoemulsions are stable systems with droplet sizes in the 20-200 nm range. The physicochemical properties of these systems may be influenced by the addition of additives. Thus, the influence of ethoxylated (EL) and acetylated lanolin (AL) addition on the droplet size, pH values, electrical conductivity and stability of nanoemulsions was investigated. Then, effect of nano-emulsions additives with EL (NE-EL) or AL (NE-AL) in hydration, oiliness and pH of the skin were evaluated. Nanoemulsion safety was evaluated through the observation of no undesirable effects after skin formulation application. Both additives caused changes in droplet size and electrical conductivity, but not in pH values. Nanoemulsions containing up to 6.0% ethoxylated lanolin and 2.0% acetylated lanolin remained stable after centrifugation tests. Higher concentrations of the additives made the nanoemulsions unstable. Stability tests showed that ethoxylated lanolin produced more stable nanoemulsions then acetylated lanolin and that the major instability phenomenon occurring in these systems is coalescence at elevated temperatures. Nanoemulsion-based lanolin derivatives increased skin hydration and oiliness and did not change cutaneous pH values. These formulations are non-toxic since they did not cause any irritation on the skin surface after nanoemulsion application, showing potential as carriers for pharmaceuticals and cosmetic applications. PMID:26927034

  11. Development of food-grade nanoemulsions and emulsions for delivery of omega-3 fatty acids: opportunities and obstacles in the food industry.

    PubMed

    Walker, Rebecca; Decker, Eric A; McClements, David Julian

    2015-01-01

    Consumption of biologically active amounts of omega-3 fatty acids is linked to improved human health, which has partly been attributed to their important role in brain development and cardiovascular health. Western diets are relatively low in omega-3 fatty acids and many consumers turn to supplements or functional foods to increase their intake of these healthy lipids. Fish oil is one of the most widely used sources of omega-3 fatty acid for supplementation and has greater health benefits than plant sources because of its higher concentration of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA). The incorporation of omega-3 fatty acids into foods and beverages is often challenging due to their low water-solubility, poor oxidative stability, and variable bioavailability. Nanoemulsions offer a promising way to incorporate omega-3 fatty acids into liquid food systems like beverages, dressing, sauces, and dips. Nanoemulsions are colloidal dispersions that contain small oil droplets (r<100 nm) that may be able to overcome many of the challenges of fortifying foods and beverages with omega-3 fatty acids. The composition and fabrication of nanoemulsions can be optimized to increase the chemical and physical stability of oil droplets, as well as to increase the bioavailability of omega-3 fatty acids.

  12. Social perception of facial resemblance in humans.

    PubMed

    DeBruine, Lisa M; Jones, Benedict C; Little, Anthony C; Perrett, David I

    2008-02-01

    Two lines of reasoning predict that highly social species will have mechanisms to influence behavior toward individuals depending on their degree of relatedness. First, inclusive fitness theory leads to the prediction that organisms will preferentially help closely related kin over more distantly related individuals. Second, evaluation of the relative costs and potential benefits of inbreeding suggests that the degree of kinship should also be considered when choosing a mate. In order to behaviorally discriminate between individuals with different levels of relatedness, organisms must be able to discriminate cues of kinship. Facial resemblance is one such potential cue in humans. Computer-graphic manipulation of face images has made it possible to experimentally test hypotheses about human kin recognition by facial phenotype matching. We review recent experimental evidence that humans respond to facial resemblance in ways consistent with inclusive fitness theory and considerations of the costs of inbreeding, namely by increasing prosocial behavior and positive attributions toward self-resembling images and selectively tempering attributions of attractiveness to other-sex faces in the context of a sexual relationship.

  13. Social perception of facial resemblance in humans.

    PubMed

    DeBruine, Lisa M; Jones, Benedict C; Little, Anthony C; Perrett, David I

    2008-02-01

    Two lines of reasoning predict that highly social species will have mechanisms to influence behavior toward individuals depending on their degree of relatedness. First, inclusive fitness theory leads to the prediction that organisms will preferentially help closely related kin over more distantly related individuals. Second, evaluation of the relative costs and potential benefits of inbreeding suggests that the degree of kinship should also be considered when choosing a mate. In order to behaviorally discriminate between individuals with different levels of relatedness, organisms must be able to discriminate cues of kinship. Facial resemblance is one such potential cue in humans. Computer-graphic manipulation of face images has made it possible to experimentally test hypotheses about human kin recognition by facial phenotype matching. We review recent experimental evidence that humans respond to facial resemblance in ways consistent with inclusive fitness theory and considerations of the costs of inbreeding, namely by increasing prosocial behavior and positive attributions toward self-resembling images and selectively tempering attributions of attractiveness to other-sex faces in the context of a sexual relationship. PMID:18157627

  14. Modification of palm kernel oil esters nanoemulsions with hydrocolloid gum for enhanced topical delivery of ibuprofen

    PubMed Central

    Salim, Norazlinaliza; Basri, Mahiran; Rahman, Mohd BA; Abdullah, Dzulkefly K; Basri, Hamidon

    2012-01-01

    Introduction During recent years, there has been growing interest in the use of nanoemulsion as a drug-carrier system for topical delivery. A nanoemulsion is a transparent mixture of oil, surfactant and water with a very low viscosity, usually the product of its high water content. The present study investigated the modification of nanoemulsions with different hydrocolloid gums, to enhanced drug delivery of ibuprofen. The in vitro characterization of the initial and modified nanoemulsions was also studied. Methods A palm kernel oil esters nanoemulsion was modified with different hydrocolloid gums for the topical delivery of ibuprofen. Three different hydrocolloids (gellan gum, xanthan gum, and carrageenan) were selected for use. Ternary phase diagrams were constructed using palm kernel oil esters as the oil, Tween 80 as the surfactant, and water. Nanoemulsions were prepared by phase inversion composition, and were gradually mixed with the freshly prepared hydrocolloids. The initial nanoemulsion and modified nanoemulsions were characterized. The abilities of the nanoemulsions to deliver ibuprofen were assessed in vitro, using a Franz diffusion cell fitted with rat skin. Results No significant changes were observed in droplet size (~16–20 nm) but a significant difference in polydispersity indexes were observed before and after the modification of nanoemulsions using gellan gum, carrageenan, and xanthan gum. The zeta potentials of the initial nanoemulsions (−11.0 mV) increased to −19.6 mV, −13.9 mV, and −41.9 mV, respectively. The abilities of both the initial nanoemulsion (T802) and the modified nanoemulsion to deliver ibuprofen through the skin were evaluated in vitro, using Franz diffusion cells fitted with rat skin. The in vitro permeation data showed that the modified nanoemulsion (Kp value of 55.4 × 10−3 cm · h−1) increased the permeability of ibuprofen 4.40 times over T802 (Kp value of 12.6 × 10−3 cm · h−1) (P < 0.05). Conclusion The

  15. Microemulsions and nanoemulsions: novel vehicles for whitening cosmeceuticals.

    PubMed

    Boonme, Prapaporn; Junyaprasert, Varaporn B; Suksawad, Nattiya; Songkro, Sarunyoo

    2009-08-01

    For Asian women, white skin is preferable. During the last decade, skin whitening products appear to be the largest and continually growing segment in skin-care market in Asia and have an impaction of economic worth. Skin whitening or lightening agents are as cosmetics which act as a drug-like benefit since melanin producing process of the skin is disturbed and can be classified as cosmeceuticals. To increase efficiency, novel vehicles are necessary for skin penetration enhancement of these agents. Microemulsions and nanoemulsions are one of useful nanocarriers for skin application in view of achieving efficiency of the active substances. Moreover, they can be formulated with ease for active ingredient incorporation, high stability and good appearance. In this review article, applications of well-known whitening or lightening agents were summarized. In addition, the use of microemulsions and nanoemulsions as novel vehicles for whitening products were discussed. PMID:20055083

  16. Familial resemblance for serum metabolite concentrations.

    PubMed

    Draisma, Harmen H M; Beekman, Marian; Pool, René; van Ommen, Gert-Jan B; Adamski, Jerzy; Prehn, Cornelia; Vaarhorst, Anika A M; de Craen, Anton J M; Willemsen, Gonneke; Slagboom, P Eline; Boomsma, Dorret I

    2013-10-01

    Metabolomics is the comprehensive study of metabolites, which are the substrates, intermediate, and end products of cellular metabolism. The heritability of the concentrations of circulating metabolites bears relevance for evaluating their suitability as biomarkers for disease. We report aspects of familial resemblance for the concentrations in human serum of more than 100 metabolites, measured using a targeted metabolomics platform. Age- and sex-corrected monozygotic twin correlations, midparent-offspring regression coefficients, and spouse correlations in subjects from two independent cohorts (Netherlands Twin Register and Leiden Longevity Study) were estimated for each metabolite. In the Netherlands Twin Register subjects, who were largely fasting, we found significant monozygotic twin correlations for 121 out of 123 metabolites. Heritability was confirmed by midparent-offspring regression. For most detected metabolites, the correlations between spouses were considerably lower than those between twins, indicating a contribution of genetic effects to familial resemblance. Remarkably high heritability was observed for free carnitine (monozygotic twin correlation 0.66), for the amino acids serine (monozygotic twin correlation 0.77) and threonine (monozygotic twin correlation 0.64), and for phosphatidylcholine acyl-alkyl C40:3 (monozygotic twin correlation 0.77). For octenoylcarnitine, a consistent point estimate of approximately 0.50 was found for the spouse correlations in the two cohorts as well as for the monozygotic twin correlation, suggesting that familiality for this metabolite is explained by shared environment. We conclude that for the majority of metabolites targeted by the used metabolomics platform, the familial resemblance of serum concentrations is largely genetic. Our results contribute to the knowledge of the heritability of fasting serum metabolite concentrations, which is relevant for biomarker research. PMID:23985338

  17. Development of a Larvicidal Nanoemulsion with Pterodon emarginatus Vogel Oil.

    PubMed

    Oliveira, Anna E M F M; Duarte, Jonatas L; Amado, Jesus R R; Cruz, Rodrigo A S; Rocha, Clarice F; Souto, Raimundo N P; Ferreira, Ricardo M A; Santos, Karen; da Conceição, Edemilson C; de Oliveira, Leandra A R; Kelecom, Alphonse; Fernandes, Caio P; Carvalho, José C T

    2016-01-01

    Pterodon emarginatus Vogel is a Brazilian species that belongs to the family Fabaceae, popularly known as sucupira. Its oil has several biological activities, including potent larvicidal property against Aedes aegypti. This insect is the vector of dengue, a tropical disease that has been considered a critical health problem in developing countries, such as Brazil. Most of dengue control methods involve larvicidal agents suspended or diluted in water and making active lipophilic natural products available is therefore considered a technological challenge. In this context, nanoemulsions appear as viable alternatives to solve this major problem. The present study describes the development of a novel nanoemulsion with larvicidal activity against A. aegypti along with the required Hydrophile Lipophile Balance determination of this oil. It was suggested that the mechanism of action might involve reversible inhibition of acetylcholinesterase and our results also suggest that the P. emarginatus nanoemulsion is not toxic for mammals. Thus, it contributes significantly to alternative integrative practices of dengue control, as well as to develop sucupira based nanoproducts for application in aqueous media.

  18. Development of a Larvicidal Nanoemulsion with Pterodon emarginatus Vogel Oil

    PubMed Central

    Oliveira, Anna E. M. F. M.; Duarte, Jonatas L.; Amado, Jesus R. R.; Cruz, Rodrigo A. S.; Rocha, Clarice F.; Souto, Raimundo N. P.; Ferreira, Ricardo M. A.; Santos, Karen; da Conceição, Edemilson C.; de Oliveira, Leandra A. R.; Kelecom, Alphonse; Fernandes, Caio P.; Carvalho, José C. T.

    2016-01-01

    Pterodon emarginatus Vogel is a Brazilian species that belongs to the family Fabaceae, popularly known as sucupira. Its oil has several biological activities, including potent larvicidal property against Aedes aegypti. This insect is the vector of dengue, a tropical disease that has been considered a critical health problem in developing countries, such as Brazil. Most of dengue control methods involve larvicidal agents suspended or diluted in water and making active lipophilic natural products available is therefore considered a technological challenge. In this context, nanoemulsions appear as viable alternatives to solve this major problem. The present study describes the development of a novel nanoemulsion with larvicidal activity against A. aegypti along with the required Hydrophile Lipophile Balance determination of this oil. It was suggested that the mechanism of action might involve reversible inhibition of acetylcholinesterase and our results also suggest that the P. emarginatus nanoemulsion is not toxic for mammals. Thus, it contributes significantly to alternative integrative practices of dengue control, as well as to develop sucupira based nanoproducts for application in aqueous media. PMID:26742099

  19. Study on Tetradecane Nanoemulsion for Thermal Energy Transportation and Storage

    NASA Astrophysics Data System (ADS)

    Fumoto, Koji; Kawaji, Masahiro; Kawanami, Tsuyoshi

    Phase change emulsion (PCE) is a novel fluid used for heat storage and transfer. It has the following characteristics: higher apparent specific heat and higher heat transfer ability in the phase-change temperature range as compared to the conventional single-phase heat transfer fluids. In particular, oil-in-water (O/W) emulsions are latent heat storage materials that have low melting points, thus offering attractive opportunities for heat transfer enhancement and thermal energy transportation and storage. In this paper, milky white oil-in-water emulsions have been formed using water, Tween 80, Span 80, and tetradecane by low-energy emulsification methods (e.g., the phase inversion temperature (PIT) method). The relations between the component ratios of the emulsions and both the particle diameters and the stability of the resulting emulsions have been determined by dynamic light scattering (DLS) and vibration viscometry. The results show that the apparent viscosity of the nanoemulsion is lower than that of an emulsion, which was prepared with the same mixing ratio of surfactant and concentration of phase change material. Moreover, the surfactant concentration is found to contribute to the stability of the phase change nanoemulsion. Results indicate that the phase change nanoemulsion is a promising material for thermal storage applications.

  20. Development of a Larvicidal Nanoemulsion with Pterodon emarginatus Vogel Oil.

    PubMed

    Oliveira, Anna E M F M; Duarte, Jonatas L; Amado, Jesus R R; Cruz, Rodrigo A S; Rocha, Clarice F; Souto, Raimundo N P; Ferreira, Ricardo M A; Santos, Karen; da Conceição, Edemilson C; de Oliveira, Leandra A R; Kelecom, Alphonse; Fernandes, Caio P; Carvalho, José C T

    2016-01-01

    Pterodon emarginatus Vogel is a Brazilian species that belongs to the family Fabaceae, popularly known as sucupira. Its oil has several biological activities, including potent larvicidal property against Aedes aegypti. This insect is the vector of dengue, a tropical disease that has been considered a critical health problem in developing countries, such as Brazil. Most of dengue control methods involve larvicidal agents suspended or diluted in water and making active lipophilic natural products available is therefore considered a technological challenge. In this context, nanoemulsions appear as viable alternatives to solve this major problem. The present study describes the development of a novel nanoemulsion with larvicidal activity against A. aegypti along with the required Hydrophile Lipophile Balance determination of this oil. It was suggested that the mechanism of action might involve reversible inhibition of acetylcholinesterase and our results also suggest that the P. emarginatus nanoemulsion is not toxic for mammals. Thus, it contributes significantly to alternative integrative practices of dengue control, as well as to develop sucupira based nanoproducts for application in aqueous media. PMID:26742099

  1. HIV-1 Superinfection Resembles Primary Infection

    PubMed Central

    Sheward, Daniel J.; Ntale, Roman; Garrett, Nigel J.; Woodman, Zenda L.; Abdool Karim, Salim S.; Williamson, Carolyn

    2015-01-01

    The relevance of superinfection as a model to identify correlates of protection against human immunodeficiency virus (HIV) depends on whether the superinfecting transmission resembles primary infection, which has not been established. Here, we characterize the genetic bottleneck in superinfected individuals for the first time. In all 3 cases, superinfection produced a spike in viral load and could be traced to a single, C-C chemokine receptor 5–tropic founder virus with shorter, less glycosylated variable regions than matched chronic viruses. These features are consistent with primary HIV transmission and provide support for the use of superinfection as a model to address correlates of protection against HIV. PMID:25754982

  2. Clotrimazole nanoemulsion for malaria chemotherapy. Part I: preformulation studies, formulation design and physicochemical evaluation.

    PubMed

    Borhade, Vivek; Pathak, Sulabha; Sharma, Shobhona; Patravale, Vandana

    2012-07-15

    Clotrimazole was formulated in nanoemulsion based system with the aim of improving its solubility and dissolution, which can further used for its preclinical evaluation. Clotrimazole nanoemulsion was prepared using spontaneous nanoemulsification method. Preformulation studies were preformed to evaluate drug-excipient compatibility, solution state pH stability and pH solubility profile. Solubility of clotrimazole in oils, surfactants and cosurfactants was determined to identify nanoemulsion components. Surfactants and cosurfactants were screened for their ability to emulsify selected oily phases. Phase diagrams were constructed to identify area of nanoemulsification. Influence of clotrimazole and pH of dilution medium on phase behavior were assessed. Drug-excipient chemical compatibility study facilitated to anticipate acid catalyzed degradation of clotrimazole. The pH of nanoemulsion was adjusted to 7.5, which could stabilize clotrimazole. Nanoemulsion composed of Capryol 90, Solutol HS 15 and Gelucire 44/14 enhanced solubility of clotrimazole up to 25mg/ml. The optimized clotrimazole nanoemulsion could withstand the extensive dilution and did not show any phase separation or drug precipitation. The nanoemulsion exhibited mean globule size <25 nm, which was not affected by pH of dilution medium. Dissolution profile of clotrimazole nanoemulsion in various media showed 100% drug release within 15 min irrespective of pH of medium. PMID:22227344

  3. Nanoemulsion-based gel formulations of COX-2 inhibitors for enhanced efficacy in inflammatory conditions

    NASA Astrophysics Data System (ADS)

    Lala, R. R.; Awari, N. G.

    2013-01-01

    In the present study, we have investigated the potential of a nanoemulsion (thermodynamically stable transparent dispersions of oil and water having a droplet size <200 nm) formulation for the topical delivery of COX-2 inhibitors using etoricoxib as a model drug. Various oil-in-water nanoemulsions were prepared by the spontaneous emulsification method. The nanoemulsion area was identified by constructing pseudo-ternary phase diagrams. The prepared nanoemulsions were subjected to thermodynamic stability testing. Those that passed these tests were characterized for viscosity, droplet size and differential scanning calorimetry. Topical permeation of etoricoxib through porcine abdominal skin was estimated using the Franz diffusion cell. The ex vivo skin permeation profile of optimized formulations was compared with that of etoricoxib conventional gel. A significant increase in permeability was observed in optimized nanoemulsion formulations consisting of 2 % w/w of etoricoxib, 20 % w/w of Triacetin, 38 % w/w of a surfactant mixture (Cremophor RH 40:Transcutol P), and 42 % w/w of water. The anti-inflammatory effects of this formulation on carrageenan-induced paw edema in rats showed a significant increase in the percent inhibition value (84.61 % with the nanoemulsion gel and 92.30 % with the nanoemulsion) as compared with the conventional gel (69.23 %) after 6 h when compared with etoricoxib conventional gel. These results suggest that nanoemulsions can serve as potential vehicles for improved transdermal delivery of anti-inflammatory agents such as etoricoxib.

  4. Nanoemulsion formulation of fisetin improves bioavailability and antitumour activity in mice.

    PubMed

    Ragelle, Héloïse; Crauste-Manciet, Sylvie; Seguin, Johanne; Brossard, Denis; Scherman, Daniel; Arnaud, Philippe; Chabot, Guy G

    2012-05-10

    The natural flavonoid fisetin (3,3',4',7-tetrahydroxyflavone) has shown antitumour activity but its administration is complicated by its low water solubility. Our aim was to incorporate fisetin into a nanoemulsion to improve its pharmacokinetics and therapeutic efficacy. Solubility and emulsification tests allowed to develop an optimal nanoemulsion composed of Miglyol 812N/Labrasol/Tween 80/Lipoid E80/water (10%/10%/2.5%/1.2%/76.3%). The nanoemulsion had an oil droplet diameter of 153 ± 2 nm, a negative zeta potential (-28.4 ± 0.6 mV) and a polydispersity index of 0.129. The nanoemulsion was stable at 4 °C for 30 days, but phase separation occurred at 20 °C. Pharmacokinetic studies in mice revealed that the fisetin nanoemulsion injected intravenously (13 mg/kg) showed no significant difference in systemic exposure compared to free fisetin. However, when the fisetin nanoemulsion was administered intraperitoneally, a 24-fold increase in fisetin relative bioavailability was noted, compared to free fisetin. Additionally, the antitumour activity of the fisetin nanoemulsion in Lewis lung carcinoma bearing mice occurred at lower doses (36.6 mg/kg) compared to free fisetin (223 mg/kg). In conclusion, we have developed a stable nanoemulsion of fisetin and have shown that it could improve its relative bioavailability and antitumour activity.

  5. Biodegradable polymer based encapsulation of neem oil nanoemulsion for controlled release of Aza-A.

    PubMed

    Jerobin, Jayakumar; Sureshkumar, R S; Anjali, C H; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2012-11-01

    Azadirachtin a biological compound found in neem have medicinal and pesticidal properties. The present work reports on the encapsulation of neem oil nanoemulsion using sodium alginate (Na-Alg) by cross linking with glutaraldehyde. Starch and polyethylene glycol (PEG) were used as coating agents for smooth surface of beads. The SEM images showed beads exhibited nearly spherical shape. Swelling of the polymeric beads reduced with coating which in turn decreased the rate of release of Aza-A. Starch coated encapsulation of neem oil nanoemulsion was found to be effective when compared to PEG coated encapsulation of neem oil nanoemulsion. The release rate of neem Aza-A from the beads into an aqueous environment was analyzed by UV-visible spectrophotometer (214 nm). The encapsulated neem oil nanoemulsion have the potential for controlled release of Aza-A. Neem oil nanoemulsion encapsulated beads coated with PEG was found to be toxic in lymphocyte cells.

  6. Development and Evaluation of Nanoemulsions Containing Phthalocyanines for Use in Photodynamic Cancer Therapy.

    PubMed

    Senna, Juliana P; Ricci-Júnior, Eduardo; Mansur, Claudia R E

    2015-06-01

    This work reports the development of oil in water (o/w) nanoemulsions containing poly(ethylene oxide)-poly(propylene oxide) block copolymer surfactant for the formulation of a delivery system for endovenous zinc and chloroaluminum phthalocyanines. A solubility study suggested clove oil and its combination with ethanol as the best candidates for the oil phase composition. The nanoemulsions were obtained using a high-pressure homogenizer and analyzed for droplet size to determine their short- and long-term stability. Formulations containing 7 and 10% oil phase and 12% surfactant presented higher stability and allowed the incorporation of a bigger amount of phthalocyanines in the formulation. Rheological analyses showed the prevailing Newtonian behavior of the nanoemulsions. Studies of toxicity and phototoxicity determined that the nanoemulsions produced were capable of inhibiting the growth of adenocarcinoma tumor cells. The nanoemulsions proved to be a good alternative for use in photodynamic therapy.

  7. Ultrasonic emulsification of food-grade nanoemulsion formulation and evaluation of its bactericidal activity.

    PubMed

    Ghosh, Vijayalakshmi; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2013-01-01

    Basil oil (Ocimum basilicum) nanoemulsion was formulated using non-ionic surfactant Tween80 and water by ultrasonic emulsification method. Process of nanoemulsion development was optimized for parameters such as surfactant concentration and emulsification time to achieve minimum droplet diameter with high physical stability. Surfactant concentration was found to have a negative correlation with droplet diameter, whereas emulsification time had a positive correlation with droplet diameter and also with intrinsic stability of the emulsion. Stable basil oil nanoemulsion with droplet diameter 29.3 nm was formulated by ultrasonic emulsification for 15 min. Formulated nanoemulsion was evaluated for antibacterial activity against Escherichia coli by kinetics of killing experiment. Fluorescence microscopy and FT-IR results showed that nanoemulsion treatment resulted alteration in permeability and surface features of bacterial cell membrane. PMID:22954686

  8. Biodegradable polymer based encapsulation of neem oil nanoemulsion for controlled release of Aza-A.

    PubMed

    Jerobin, Jayakumar; Sureshkumar, R S; Anjali, C H; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2012-11-01

    Azadirachtin a biological compound found in neem have medicinal and pesticidal properties. The present work reports on the encapsulation of neem oil nanoemulsion using sodium alginate (Na-Alg) by cross linking with glutaraldehyde. Starch and polyethylene glycol (PEG) were used as coating agents for smooth surface of beads. The SEM images showed beads exhibited nearly spherical shape. Swelling of the polymeric beads reduced with coating which in turn decreased the rate of release of Aza-A. Starch coated encapsulation of neem oil nanoemulsion was found to be effective when compared to PEG coated encapsulation of neem oil nanoemulsion. The release rate of neem Aza-A from the beads into an aqueous environment was analyzed by UV-visible spectrophotometer (214 nm). The encapsulated neem oil nanoemulsion have the potential for controlled release of Aza-A. Neem oil nanoemulsion encapsulated beads coated with PEG was found to be toxic in lymphocyte cells. PMID:22944443

  9. Development and Evaluation of Nanoemulsions Containing Phthalocyanines for Use in Photodynamic Cancer Therapy.

    PubMed

    Senna, Juliana P; Ricci-Júnior, Eduardo; Mansur, Claudia R E

    2015-06-01

    This work reports the development of oil in water (o/w) nanoemulsions containing poly(ethylene oxide)-poly(propylene oxide) block copolymer surfactant for the formulation of a delivery system for endovenous zinc and chloroaluminum phthalocyanines. A solubility study suggested clove oil and its combination with ethanol as the best candidates for the oil phase composition. The nanoemulsions were obtained using a high-pressure homogenizer and analyzed for droplet size to determine their short- and long-term stability. Formulations containing 7 and 10% oil phase and 12% surfactant presented higher stability and allowed the incorporation of a bigger amount of phthalocyanines in the formulation. Rheological analyses showed the prevailing Newtonian behavior of the nanoemulsions. Studies of toxicity and phototoxicity determined that the nanoemulsions produced were capable of inhibiting the growth of adenocarcinoma tumor cells. The nanoemulsions proved to be a good alternative for use in photodynamic therapy. PMID:26369031

  10. Formulation and in vitro evaluation of ketoprofen in palm oil esters nanoemulsion for topical delivery.

    PubMed

    Sakeena, M H F; Muthanna, F A; Ghassan, Z A; Kanakal, M M; Elrashid, S M; Munavvar, A S; Azmin, M N

    2010-01-01

    The aim of the present study is to formulate and investigate the potential of nanoemulsion formulation for topical delivery of ketoprofen. In this study, Palm Oil Esters (POEs) a newly introduced oil by Universiti Putra Malaysia researchers was chosen for the oil phase of the nanoemulsion, because the oil was reported to be a good vehicle for pharmaceutical use. Oil-in-water nanoemulsion was prepared by spontaneous emulsification method. The droplets size was studied by laser scattering spectroscopy (Nanophox) and Transmission Electron Microscopy (TEM). Franz diffusion cells were used, to determine the drug release and drug transferred through methyl acetate cellulose membrane (artificial membrane). The results of droplets size analysis shows the droplets are in the range of nanoemulsion which is below than 500 nm. The in vitro release profile shows a sufficient percentage of drugs released through the methyl acetate cellulose membrane. This initial study showed that the nanoemulsion formulated using POEs has great potential for topical delivery of ketoprofen.

  11. Effect of limonene on permeation enhancement of ketoprofen in palm oil esters nanoemulsion.

    PubMed

    Sakeena, M H F; Elrashid, S M; Muthanna, F A; Ghassan, Z A; Kanakal, M M; Laila, Lia; Munavvar, A S; Azmin, M N

    2010-01-01

    This study sets out to investigate the in vitro permeation of ketoprofen from the formulated nanoemulsions through excised rat skin. In vitro permeation of ketoprofen nanoemulsion through rat skin was evaluated in Franz diffusion cells and compared with marketed product (Fastum gel). Limonene which has been reported to be a good enhancer for ketoprofen was selected. Moreover the effects of limonene which was added to the nanoemulsion formulations at levels of 1%, 2%, 3% and on rat skin permeation of ketoprofen were also evaluated. The selected optimized formulation was further studied for skin irritation. Utilization of limonene as a penetration enhancer increased the permeation of ketoprofen from the formulated nanoemulsion with increasing concentrations of limonene. The results obtained showed that nanoemulsion with 3% limonene produced similar and comparable skin permeation of ketoprofen with marketed formulation and the skin irritation study on rats showed the optimized formulation prepared was safe.

  12. Antioxidant activity and bioaccessibility of size-different nanoemulsions for lycopene-enriched tomato extract.

    PubMed

    Ha, Thi Van Anh; Kim, Saehoon; Choi, Yeri; Kwak, Hae-Soo; Lee, Sung Je; Wen, Jingyuan; Oey, Indrawati; Ko, Sanghoon

    2015-07-01

    Lycopene nanoemulsions were prepared to protect the antioxidant activity and improve the bioaccessibility of lycopene-enriched tomato extract (containing 6% of lycopene) by an emulsification-evaporation method. Lycopene nanoemulsions, with droplet sizes between 100 and 200 nm, exhibited higher anti-radical efficiency and antioxidant activity, than did those smaller than 100 nm. Strong protectability of lycopene in droplets smaller than 100 nm was associated with relatively slower rates of DPPH and ABTS reactions. In vitro bioaccessibility values of lycopene-enriched tomato extract, lycopene nanoemulsions with droplets larger than 100 nm (approximately 150 nm on average), and lycopene nanoemulsions with droplets smaller than 100 nm (69 nm on average) were 0.01, 0.53, and 0.77, respectively. Interestingly, nanoemulsions with droplets smaller than 100 nm showed the highest in vitro bioaccessibility, which could be interpreted as evidence of nanoemulsification enhancing the in vitro bioaccessibility of lycopene. PMID:25704691

  13. Parasagittal solitary fibrous tumor resembling hemangiopericytoma.

    PubMed

    Shidoh, Satoka; Yoshida, Kazunari; Takahashi, Satoshi; Mikami, Shuji; Mukai, Makio; Kawase, Takeshi

    2010-04-01

    Solitary fibrous tumor (SFT) is a rare mesenchymal tumor in the central nervous system, and the clinical behavior of this tumor is similar to that of meningioma. We report the case of a Japanese woman with parasagittal SFT that resembled hemangiopericytoma (HPC). Histological examination revealed that the tumor was highly cellular, with cells containing oval- or spindle-shaped nuclei arranged in sheets or a pattern-less growth mode. Focal vascular proliferation was also observed. Some areas showed intercellular stroma containing remarkable eosinophilic collagens. Tumor cells showed a strong immunoreactivity for CD34 but were negative for S-100 protein and epithelial membrane antigen. MIB-1 labeling index of the tumor was 6.6%. Owing to the high cellularity, high MIB-1 labeling index, and focal vascular proliferation, it was difficult to distinguish this lesion from HPC. However, the tumor was finally diagnosed as SFT on the basis of the strong immunostaining for CD34 and absence of pericellular reticulin.

  14. Eugenol improves physical and chemical stabilities of nanoemulsions loaded with β-carotene.

    PubMed

    Guan, Yongguang; Wu, Jine; Zhong, Qixin

    2016-03-01

    Food-grade nanoemulsions are potential vehicles of labile lipophilic compounds such as β-carotene, but much work is needed to improve physical and chemical stabilities. The objective of this work was to study impacts of eugenol on physical and chemical stabilities of β-carotene-loaded nanoemulsions prepared with whey protein and lecithin. The combination of whey protein and lecithin resulted in stable nanoemulsions with eugenol added at 10% mass of soybean oil. Nanoemulsions, especially with eugenol, drastically reduced the degradation of β-carotene during ambient storage, heating at 60 and 80°C, and UV radiation at 254, 302, and 365nm. The droplet diameter of the nanoemulsion without eugenol increased from 153.6 to 227.3nm after 30-day ambient storage, contrasting with no significant changes of nanoemulsions with eugenol. Heating or UV radiation up to 8h did not significantly change the droplet diameter. Therefore, eugenol can be used to improve the stability of nanoemulsion delivery systems. PMID:26471619

  15. Stability studies of silymarin nanoemulsion containing Tween 80 as a surfactant

    PubMed Central

    Parveen, Rabea; Baboota, Sanjula; Ali, Javed; Ahuja, Alka; Ahmad, Sayeed

    2015-01-01

    Background: Silymarin, a flavonolignan from “milk thistle” (Silybum marianum) plant is used almost exclusively for hepatoprotection. Because of its low bioavailability, it was incorporated into a nanoemulsion formulation. The aim of the present study was to check the stability of silymarin nanoemulsion at different temperatures for 3 months. Materials and Methods: The oil-in-water based nanoemulsion formulation was prepared by titration method. Silymarin nanoemulsion was characterized by droplet size, viscosity, and refractive index. Droplet size, viscosity, and refractive index were determined every month. The shelf-life of silymarin nanoemulsion was determined by accelerated stability testing. Results: It was found that there was no significant change in the droplet size, viscosity, and refractive index at refrigerator and room temperature during the period of 3 months. The half-life of the optimized nanoemulsion formulation was found to be 4.74 years at room temperature. Conclusion: These results indicated that stability of silymarin can be enhanced in nanoemulsion formulation using Tween 80 as a surfactant. PMID:26681893

  16. Eugenol improves physical and chemical stabilities of nanoemulsions loaded with β-carotene.

    PubMed

    Guan, Yongguang; Wu, Jine; Zhong, Qixin

    2016-03-01

    Food-grade nanoemulsions are potential vehicles of labile lipophilic compounds such as β-carotene, but much work is needed to improve physical and chemical stabilities. The objective of this work was to study impacts of eugenol on physical and chemical stabilities of β-carotene-loaded nanoemulsions prepared with whey protein and lecithin. The combination of whey protein and lecithin resulted in stable nanoemulsions with eugenol added at 10% mass of soybean oil. Nanoemulsions, especially with eugenol, drastically reduced the degradation of β-carotene during ambient storage, heating at 60 and 80°C, and UV radiation at 254, 302, and 365nm. The droplet diameter of the nanoemulsion without eugenol increased from 153.6 to 227.3nm after 30-day ambient storage, contrasting with no significant changes of nanoemulsions with eugenol. Heating or UV radiation up to 8h did not significantly change the droplet diameter. Therefore, eugenol can be used to improve the stability of nanoemulsion delivery systems.

  17. Organogel-nanoemulsion containing nisin and D-limonene and its antimicrobial activity

    PubMed Central

    Bei, Weiya; Zhou, Yan; Xing, Xuya; Zahi, Mohamed Reda; Li, Yuan; Yuan, Qipeng; Liang, Hao

    2015-01-01

    The aim of this study was to investigate a novel delivery system containing D-limonene and nisin by food organogel-nanoemulsion and study its effect on the antimicrobial activity. Organogel-nanoemulsion containing with D-limonene and nisin or without nisin was prepared by a homogenization method. Factors that may affect the droplet size and stability of organogel-nanoemulsion such as pressure and surfactant to oil ratio (SOR) were studied. The average droplet size decreased with pressure, and the organogel-nanoemulsion could achieve good stability at low SOR. Positive effects and outstanding antimicrobial activities of organogel-nanoemulsion containing with D-limonene and nisin were confirmed by minimal inhibitory concentrations comparison, growth curves of bacteria, scanning electron microscopy and determination of cell constituents’ release. Furthermore, the organogel-nanoemulsion applied as food preservative in milk also shown excellent antimicrobial performance. Overall, the research described in the current article show that organogel-nanoemulsion containing with D-limonene and nisin may be an effective antimicrobial system for the production and preservation of food. PMID:26441935

  18. Two-color fluorescent (near-infrared and visible) triphasic perfluorocarbon nanoemulsions

    PubMed Central

    Patel, Sravan Kumar; Patrick, Michael J.; Pollock, John A.

    2013-01-01

    Abstract. Design and development of a new formulation as a unique assembly of distinct fluorescent reporters with nonoverlapping fluorescence spectra and a F19 magnetic resonance imaging agent into colloidally and optically stable triphasic nanoemulsion are reported. Specifically, a cyanine dye-perfluorocarbon (PFC) conjugate was introduced into the PFC phase of the nanoemulsion and a near-infrared dye was introduced into the hydrocarbon (HC) layer. To the best of our knowledge, this is the first report of a triphasic nanoemulsion system where each oil phase, HC, and PFC are fluorescently labeled and formulated into an optically and colloidally stable nanosystem. Having, each oil phase separately labeled by a fluorescent dye allows for improved correlation between in vivo imaging and histological data. Further, dual fluorescent labeling can improve intracellular tracking of the nanodroplets and help assess the fate of the nanoemulsion in biologically relevant media. The nanoemulsions were produced by high shear processing (microfluidization) and stabilized with biocompatible nonionic surfactants resulting in mono-modal size distribution with average droplet size less than 200 nm. Nanoemulsions demonstrate excellent colloidal stability and only moderate changes in the fluorescence signal for both dyes. Confocal fluorescence microscopy of macrophages exposed to nanoemulsions shows the presence of both fluorescence agents in the cytoplasm. PMID:23912666

  19. Cell Labeling for 19F MRI: New and Improved Approach to Perfluorocarbon Nanoemulsion Design

    PubMed Central

    Patel, Sravan K.; Williams, Jonathan; Janjic, Jelena M.

    2013-01-01

    This report describes novel perfluorocarbon (PFC) nanoemulsions designed to improve ex vivo cell labeling for 19F magnetic resonance imaging (MRI). 19F MRI is a powerful non-invasive technique for monitoring cells of the immune system in vivo, where cells are labeled ex vivo with PFC nanoemulsions in cell culture. The quality of 19F MRI is directly affected by the quality of ex vivo PFC cell labeling. When co-cultured with cells for longer periods of time, nanoemulsions tend to settle due to high specific weight of PFC oils (1.5–2.0 g/mL). This in turn can decrease efficacy of excess nanoemulsion removal and reliability of the cell labeling in vitro. To solve this problem, novel PFC nanoemulsions are reported which demonstrate lack of sedimentation and high stability under cell labeling conditions. They are monodisperse, have small droplet size (~130 nm) and low polydispersity (<0.15), show a single peak in the 19F nuclear magnetic resonance spectrum at −71.4 ppm and possess high fluorine content. The droplet size and polydispersity remained unchanged after 160 days of follow up at three temperatures (4, 25 and 37 °C). Further, stressors such as elevated temperature in the presence of cells, and centrifugation, did not affect the nanoemulsion droplet size and polydispersity. Detailed synthetic methodology and in vitro testing for these new PFC nanoemulsions is presented. PMID:25586263

  20. Organogel-nanoemulsion containing nisin and D-limonene and its antimicrobial activity.

    PubMed

    Bei, Weiya; Zhou, Yan; Xing, Xuya; Zahi, Mohamed Reda; Li, Yuan; Yuan, Qipeng; Liang, Hao

    2015-01-01

    The aim of this study was to investigate a novel delivery system containing D-limonene and nisin by food organogel-nanoemulsion and study its effect on the antimicrobial activity. Organogel-nanoemulsion containing with D-limonene and nisin or without nisin was prepared by a homogenization method. Factors that may affect the droplet size and stability of organogel-nanoemulsion such as pressure and surfactant to oil ratio (SOR) were studied. The average droplet size decreased with pressure, and the organogel-nanoemulsion could achieve good stability at low SOR. Positive effects and outstanding antimicrobial activities of organogel-nanoemulsion containing with D-limonene and nisin were confirmed by minimal inhibitory concentrations comparison, growth curves of bacteria, scanning electron microscopy and determination of cell constituents' release. Furthermore, the organogel-nanoemulsion applied as food preservative in milk also shown excellent antimicrobial performance. Overall, the research described in the current article show that organogel-nanoemulsion containing with D-limonene and nisin may be an effective antimicrobial system for the production and preservation of food.

  1. Formation and stabilization of nanoemulsions using biosurfactants: Rhamnolipids.

    PubMed

    Bai, Long; McClements, David Julian

    2016-10-01

    Nanoemulsions are used in the food, cosmetics, personal care and pharmaceutical industries to provide desirable optical, textural, stability, and delivery characteristics. In many industrial applications, it is desirable to formulate nanoemulsions using natural ingredients so as to develop label-friendly products. Rhamnolipids are biosurfactants isolated from certain microorganisms using fermentation processes. They are glycolipids that have a polar head consisting of rhamnose units and a non-polar tail consisting of a hydrocarbon chain. In this study, the interfacial characteristics of this natural surfactant at medium chain triglyceride (MCT) oil-water interfaces were characterized, and its ability to form nanoemulsions was compared to that of another natural surfactant (quillaja saponins). The influence of rhamnolipid concentration, homogenization pressure, and oil type on the mean droplet diameter of emulsions produced by microfluidization was determined. Rhamnolipids were highly effective at forming small droplets (d32<0.15μm) at low surfactant-to-oil ratios (SOR<1:10) for MCT oil. Rhamnolipids could also be used to form small droplets using long chain triglyceride oils, such as corn and fish oil. Rhamnolipid-coated droplets were stable to aggregation over a range of pH values (5-9), salt concentrations (<100mM NaCl) and temperatures (20-90°C). However, droplet aggregation was observed at highly acidic (pH 2-4) and high ionic strength (200-500mM NaCl) conditions. These effects were attributed to a reduction in electrostatic repulsion at low pH and high salt levels. Rhamnolipid-coated droplets had a high negative charge at neutral pH that decreased in magnitude with decreasing pH. These results indicate that rhamnolipids are effective natural surfactants that may be able to replace synthetic surfactants in certain commercial applications. PMID:27372634

  2. Body elimination attitude family resemblance in Kuwait.

    PubMed

    Al-Fayez, Ghenaim; Awadalla, Abdelwahid; Arikawa, Hiroko; Templer, Donald I; Hutton, Shane

    2009-12-01

    The purpose of the present study was to determine the family resemblance of attitude toward body elimination in Kuwaiti participants. This study was conceptualized in the context of the theories of moral development, importance of cleanliness in the Muslim religion, cross-cultural differences in personal hygiene practices, previous research reporting an association between family attitudes and body elimination attitude, and health implications. The 24-item Likert-type format Body Elimination Attitude Scale-Revised was administered to 277 Kuwaiti high school students and 437 of their parents. Females scored higher, indicating greater disgust, than the males. Moreover, sons' body elimination attitude correlated more strongly with fathers' attitude (r = .85) than with that of the mothers (r = .64). Daughters' attitude was similarly associated with the fathers' (r = .89) and the mothers' attitude (r = .86). The high correlations were discussed within the context of Kuwait having a collectivistic culture with authoritarian parenting style. The higher adolescent correlations, and in particular the boys' correlation with fathers than with mothers, was explained in terms of the more dominant role of the Muslim father in the family. Public health and future research implications were suggested. A theoretical formulation was advanced in which "ideal" body elimination attitude is relative rather than absolute, and is a function of one's life circumstances, one's occupation, one's culture and subculture, and the society that one lives in.

  3. Adrenal Cushing's syndrome may resemble eating disorders.

    PubMed

    Hatakeyama, Makiko; Nakagami, Taku; Yasui-Furukori, Norio

    2014-01-01

    We encountered a patient who presented extreme weight loss and received an eating disorder diagnosis that was later identified as adrenal Cushing's syndrome. A 32-year-old woman with a 2-year history of an eating disorder was admitted to our psychiatric ward due to dehydration, malnutrition and low weight. Her height and body weight were 152.1 cm and 29.8 kg, respectively (body mass index: 12.8). Her other symptoms included a depressed mood, decreased interest, retardation and suicidal ideation. Standard medical cares were prescribed to treat the depressive symptoms and eating disorder, but the depressive episode and low body weight of the patient persisted. Computed tomography of the abdomen revealed an unexpected left adrenal gland tumor. Cushing's syndrome was diagnosed based on several endocrinological examinations. After an enucleation of the left adrenal gland tumor, the patient began eating, and her body weight increased gradually. Her body weight increased to 42.0-47.0 kg (body mass index: 18.2-20.3). Her mental and physical conditions had stabilized. This case suggests that adrenal Cushing's syndrome may resemble eating disorders.

  4. Ultrasound assisted manufacturing of paraffin wax nanoemulsions: process optimization.

    PubMed

    Jadhav, A J; Holkar, C R; Karekar, S E; Pinjari, D V; Pandit, A B

    2015-03-01

    This work reports on the process optimization of ultrasound-assisted, paraffin wax in water nanoemulsions, stabilized by modified sodium dodecyl sulfate (SDS). This work focuses on the optimization of major emulsification process variables including sonication time, applied power and surfactant concentration. The effects of these variables were investigated on the basis of mean droplet diameter and stability of the prepared emulsion. It was found that the stable emulsion with droplet diameters about 160.9 nm could be formed with the surfactant concentration of 10 mg/ml and treated at 40% of applied power (power density: 0.61 W/ml) for 15 min. Scanning electron microscopy (SEM) was used to study the morphology of the emulsion droplets. The droplets were solid at room temperature, showing bright spots under polarized light and a spherical shape under SEM. The electrophoretic properties of emulsion droplets showed a negative zeta potential due to the adsorption of head sulfate groups of the SDS surfactant. For the sake of comparison, paraffin wax emulsion was prepared via emulsion inversion point method and was checked its intrinsic stability. Visually, it was found that the emulsion get separated/creamed within 30 min. while the emulsion prepared via ultrasonically is stable for more than 3 months. From this study, it was found that the ultrasound-assisted emulsification process could be successfully used for the preparation of stable paraffin wax nanoemulsions.

  5. Ultrasound assisted manufacturing of paraffin wax nanoemulsions: process optimization.

    PubMed

    Jadhav, A J; Holkar, C R; Karekar, S E; Pinjari, D V; Pandit, A B

    2015-03-01

    This work reports on the process optimization of ultrasound-assisted, paraffin wax in water nanoemulsions, stabilized by modified sodium dodecyl sulfate (SDS). This work focuses on the optimization of major emulsification process variables including sonication time, applied power and surfactant concentration. The effects of these variables were investigated on the basis of mean droplet diameter and stability of the prepared emulsion. It was found that the stable emulsion with droplet diameters about 160.9 nm could be formed with the surfactant concentration of 10 mg/ml and treated at 40% of applied power (power density: 0.61 W/ml) for 15 min. Scanning electron microscopy (SEM) was used to study the morphology of the emulsion droplets. The droplets were solid at room temperature, showing bright spots under polarized light and a spherical shape under SEM. The electrophoretic properties of emulsion droplets showed a negative zeta potential due to the adsorption of head sulfate groups of the SDS surfactant. For the sake of comparison, paraffin wax emulsion was prepared via emulsion inversion point method and was checked its intrinsic stability. Visually, it was found that the emulsion get separated/creamed within 30 min. while the emulsion prepared via ultrasonically is stable for more than 3 months. From this study, it was found that the ultrasound-assisted emulsification process could be successfully used for the preparation of stable paraffin wax nanoemulsions. PMID:25465097

  6. High carotenoid bioaccessibility through linseed oil nanoemulsions with enhanced physical and oxidative stability.

    PubMed

    Sotomayor-Gerding, Daniela; Oomah, B Dave; Acevedo, Francisca; Morales, Eduardo; Bustamante, Mariela; Shene, Carolina; Rubilar, Mónica

    2016-05-15

    Carotenoid (astaxanthin or lycopene) emulsions obtained by high pressure homogenization were investigated for their physical, oxidative and storage stability and biological fate on an in vitro digestion model of bioaccessibility. Emulsion stability evaluated at various processing environments (20-50°C, 2-10 pH, 0-500 mM NaCl, and 0-35 days storage at 25°C) depended on carotenoid and homogenization pressures (5, 10, 100 MPa). Trolox increased the oxidative stability of nanoemulsions (100 MPa) and acted synergistically with BHT in increasing the stability of lycopene nanoemulsion. Intestinal digestibility depended on homogenization pressures with the fastest release and lower amount of free fatty acids observed at 100 MPa. Carotenoid nanoemulsions (100 MPa) were partially (66%) digested and highly bioaccessible (>70%). Therefore, nanoemulsions provide an effective and stable system for efficient astaxanthin or lycopene delivery and bioavailability in foods, beverages, nutraceuticals and/or other agriproducts.

  7. Formation of flavor oil microemulsions, nanoemulsions and emulsions: influence of composition and preparation method.

    PubMed

    Rao, Jiajia; McClements, David Julian

    2011-05-11

    This study aimed to establish conditions where stable microemulsions, nanoemulsions or emulsions could be fabricated from a nonionic surfactant (Tween 80) and flavor oil (lemon oil). Different colloidal dispersions could be formed by simple heat treatment (90 °C, 30 min) depending on the surfactant-to-oil ratio (SOR): emulsions (r > 100 nm) at SOR < 1; nanoemulsions (r < 100 nm) at 1 < SOR < 2; microemulsions (r < 10 nm) at SOR > 2. Turbidity, electrical conductivity, shear rheology, and DSC measurements suggested there was a kinetic energy barrier in the oil-water-surfactant systems at ambient temperature that prevented them from forming metastable emulsion/nanoemulsion or thermodynamically stable microemulsion systems. High energy homogenization (high pressure or ultrasonic homogenizer) or low energy homogenization (heating) could be used to form emulsions or nanoemulsions at low or intermediate SOR values; whereas only heating was necessary to form stable microemulsions at high SOR values. PMID:21410259

  8. Effects of oil and drug concentrations on droplets size of palm oil esters (POEs) nanoemulsion.

    PubMed

    Sakeena, M H F; Elrashid, S M; Munavvar, A S; Azmin, M N

    2011-01-01

    Aim of the present work is to study the effects of oil and drug concentrations on droplets size of a nanoemulsion. Newly introduced oil, palm oil esters (POEs) by Universiti Putra Malaysia researchers was selected for the oil phase of the nanoemulsion, because the oil was reported to be a good vehicle for pharmaceutical use. Nanoemulsions were prepared with different concentrations of oil and drug and their effects on droplets size were studied by laser scattering spectroscopy (Nanophox). The results of droplets size analysis shows the droplets size increase with increasing concentration of oil and drug concentrations. It can be concluded from this study, that oil and drug concentrations have an effect on the droplets size of POEs nanoemulsion system.

  9. Inhibition of colon cancer cell growth by nanoemulsion carrying gold nanoparticles and lycopene

    PubMed Central

    Huang, Rwei-Fen S; Wei, Yi-Jun; Inbaraj, Baskaran Stephen; Chen, Bing-Huei

    2015-01-01

    Lycopene (LP), an important functional compound in tomatoes, and gold nanoparticles (AN), have received considerable attention as potential candidates for cancer therapy. However, the extreme instability and poor bioavailability of LP limits its in vivo application. This study intends to develop a nanoemulsion system incorporating both LP and AN, and to study the possible synergistic effects on the inhibition of the HT-29 colon cancer cell line. LP–nanogold nanoemulsion containing Tween 80 as an emulsifier was prepared, followed by characterization using transmission electron microscopy (TEM), dynamic light scattering (DLS) analysis, ultraviolet spectroscopy, and zeta potential analysis. The particle size as determined by TEM and DLS was 21.3±3.7 nm and 25.0±4.2 nm for nanoemulsion and 4.7±1.1 nm and 3.3±0.6 nm for AN, while the zeta potential of nanoemulsion and AN was −32.2±1.8 mV and −48.5±2.7 mV, respectively. Compared with the control treatment, both the combo (AN 10 ppm plus LP 12 μM) and nanoemulsion (AN 0.16 ppm plus LP 0.4 μM) treatments resulted in a five- and 15-fold rise in early apoptotic cells of HT-29, respectively. Also, the nanoemulsion significantly reduced the expressions of procaspases 8, 3, and 9, as well as PARP-1 and Bcl-2, while Bax expression was enhanced. A fivefold decline in the migration capability of HT-29 cells was observed for this nanoemulsion when compared to control, with the invasion-associated markers being significantly reversed through the upregulation of the epithelial marker E-cadherin and downregulation of Akt, nuclear factor kappa B, pro-matrix metalloproteinase (MMP)-2, and active MMP-9 expressions. The TEM images revealed that numerous nanoemulsion-filled vacuoles invaded cytosol and converged into the mitochondria, resulting in an abnormally elongated morphology with reduced cristae and matrix contents, demonstrating a possible passive targeting effect. The nanoemulsion containing vacuoles were engulfed

  10. Polymeric micelles and nanoemulsions as drug carriers: Therapeutic efficacy, toxicity, and drug resistance.

    PubMed

    Gupta, Roohi; Shea, Jill; Scafe, Courtney; Shurlygina, Anna; Rapoport, Natalya

    2015-08-28

    The manuscript reports the side-by-side comparison of therapeutic properties of polymeric micelles and nanoemulsions generated from micelles. The effect of the structure of a hydrophobic block of block copolymer on the therapeutic efficacy, tumor recurrence, and development of drug resistance was studied in pancreatic tumor bearing mice. Mice were treated with paclitaxel (PTX) loaded poly(ethylene oxide)-co-polylactide micelles or corresponding perfluorocarbon nanoemulsions. Two structures of the polylactide block differing in a physical state of micelle cores or corresponding nanodroplet shells were compared. Poly(ethylene oxide)-co-poly(d,l-lactide) (PEG-PDLA) formed micelles with elastic amorphous cores while poly(ethylene oxide)-co-poly(l-lactide) (PEG-PLLA) formed micelles with solid crystalline cores. Micelles and nanoemulsions stabilized with PEG-PDLA copolymer manifested higher therapeutic efficacy than those formed with PEG-PLLA copolymer studied earlier. Better performance of PEG-PDLA micelles and nanodroplets was attributed to the elastic physical state of micelle cores (or droplet shells) allowing adequate rate of drug release via drug diffusion and/or copolymer biodegradation. The biodegradation of PEG-PDLA stabilized nanoemulsions was monitored by the ultrasonography of nanodroplets injected directly into the tumor; the PEG-PDLA stabilized nanodroplets disappeared from the injection site within 48h. In contrast, nanodroplets stabilized with PEG-PLLA copolymer were preserved at the injection site for weeks and months indicating extremely slow biodegradation of solid PLLA blocks. Multiple injections of PTX-loaded PEG-PDLA micelles or nanoemulsions to pancreatic tumor bearing mice resulted in complete tumor resolution. Two of ten tumors treated with either PEG-PDLA micellar or nanoemulsion formulation recurred after the completion of treatment but proved sensitive to the second treatment cycle indicating that drug resistance has not been developed. This

  11. Influence of palmitoyl pentapeptide and Ceramide III B on the droplet size of nanoemulsion

    NASA Astrophysics Data System (ADS)

    Sondari, Dewi; Haryono, Agus; Harmami, Sri Budi; Randy, Ahmad

    2010-05-01

    The influence of the Palmitoyl Pentapeptide (PPp) and Ceramide IIIB (Cm III B) as active ingredients on the droplet size of nano-emulsion was studied using different kinds of oil (avocado oil, sweet almond oil, jojoba oil, mineral oil and squalene). The formation of nano-emulsions were prepared in water mixed non ionic surfactant/oils system using the spontaneous emulsification mechanism. The aqueous solution, which consist of water and Tween® 20 as a hydrophilic surfactant was mixed homogenously. The organic solution, which consist of oil and Span® 80 as a lipophilic surfactant was mixed homogenously in ethanol. Ethanol was used as a water miscible solvent, which can help the formation of nano-emulsion. The oil phase (containing the blend of surfactant Span® 80, ethanol, oil and active ingredient) and the aqueous phase (containing water and Tween® 20) were separately prepared at room temperatures. The oil phase was slowly added into aqueous phase under continuous mechanical agitation (18000 rpm). All samples were subsequently homogenized with Ultra-Turrax for 30 minutes. The characterizations of nano-emulsion were carried out using photo-microscope and particle size analyzer. Addition of active ingredients on the formation of nano-emulsion gave smallest droplet size compared without active ingredients addition on the formation of nano-emulsion. Squalene oil with Palmitoyl Pentapeptide (PPm) and Ceramide IIIB (Cm IIIB) gave smallest droplet size (184.0 nm) compared without Palmitoyl Pentapeptide and Ceramide IIIB (214.9 nm), however the droplets size of the emulsion prepared by the other oils still in the range of nano-emulsion (below 500 nm). The stability of nano-emulsion was observed using two methods. In one method, the stability of nano-emulsion was observed for three months at temperature of 5°C and 50°C, while in the other method, the stability nano-emulsion was observed by centrifuged at 12000 rpm for 30 minutes. Nanoemulsion with active ingredient

  12. Transdermal delivery of anticancer drug caffeine from water-in-oil nanoemulsions.

    PubMed

    Shakeel, Faiyaz; Ramadan, Wafa

    2010-01-01

    Recently caffeine has been investigated for the treatment of various types of cancers upon oral administration. There is also some evidence that dermally applied caffeine can protect the skin from skin cancer caused by sun exposure. Therefore nanoemulsion formulation of caffeine for transdermal drug delivery was developed and evaluated in the present investigation. Different w/o nanoemulsion formulations of caffeine were prepared by oil phase titration method. Thermodynamically stable nanoemulsions were characterized for morphology, droplet size, viscosity and refractive index. The in vitro skin permeation studies were performed on Franz diffusion cell using rat skin as permeation membrane. The in vitro skin permeation profile of optimized formulation was compared with aqueous solution of caffeine. Significant increase in permeability parameters was observed in nanoemulsion formulations (P<0.05) as compared to aqueous solution of caffeine. The steady-state flux (J(ss)) and permeability coefficient (K(p)) for optimized nanoemulsion formulation (C12) were found to be 147.55+/-8.21 microg/cm(2)/h and 1.475 x 10(-2)+/-0.031 x 10(-2)cm/h, respectively. Enhancement ratio (E(r)) was found to be 17.37 in optimized formulation C12 compared with other formulations. Overall these results suggested that w/o nanoemulsions are good carriers for transdermal delivery of caffeine.

  13. Highly efficient and lowly toxic docetaxel nanoemulsions for intravenous injection to animals.

    PubMed

    Li, Xin; Du, Lina; Wang, Chenyun; Liu, Yan; Mei, Xingguo; Jin, Yiguang

    2011-07-01

    Hypersensitivity many occur with commercial docetaxel injections containing Tween 80 and ethanol. An alternative formulation of docetaxel, an oil-in-water nanoemulsion was prepared using the high-pressure homogenization method. It was composed of medium-chain triglyceride, oleic acid, egg lecithin, and poloxamer. These ingredients are known as safe agents for intravenous (i.v.) injection. The nanoemulsion had a small size of 169 nm, and a high surface charge with the zeta potential of -33.9 mV. It maintained well stable even under high centrifugation. Acute toxicity of i.v. injection, erythrocyte hemolysis experiment, and rabbit ear vein irritation test showed no toxicity for the docetaxel nanoemulsion. The docetaxel nanoemulsion led to a larger apparent distribution volume and area under curve than the docetaxel injection after i.v. administration to rats. The histopathological test of tumor further demonstrated the highly anticancer efficiency of the docetaxel nanoemulsion. Thus, the nanoemulsion is a promising delivery system for docetaxel with highly anticancer efficiency and low toxicity. PMID:21812321

  14. Vitamin E-enriched nanoemulsions formed by emulsion phase inversion: factors influencing droplet size and stability.

    PubMed

    Mayer, Sinja; Weiss, Jochen; McClements, David Julian

    2013-07-15

    There is considerable interest in using nanoemulsions as delivery systems for lipophilic bioactive ingredients, such as oil-soluble vitamins. Nanoemulsions can be fabricated using either high-energy or low-energy methods, but the latter offer advantages in terms of low cost, higher energy efficiency, and simplicity of implementation. In this study, the emulsion phase inversion (EPI) method was used to produce food-grade nanoemulsions enriched with vitamin E acetate. The EPI method simply involves titrating water into a mixture containing oil and surfactant, which initially leads to the formation of a water-in-oil emulsion that then inverts into an oil-in-water emulsion. Oil composition, surfactant type, and surfactant-to-oil ratio (SOR) were all found to influence the particle size distribution of the systems produced. Nanoemulsions with a mean particle diameter of 40 nm could be produced at a final system composition of 2 wt% MCT, 8 wt%vitamin E acetate, and 20 wt% Tween 80. The EPI method was shown to be unsuitable for producing nanoemulsions from label-friendly surfactants, such as Quillaja saponin, whey protein, casein, and sucrose monoesters. The EPI method was more effective at producing nanoemulsions at high SOR than microfluidization, but much less effective at low SOR. PMID:23660020

  15. Multiplexed detection of various breast cancer cells by perfluorocarbon/quantum dot nanoemulsions conjugated with antibodies

    NASA Astrophysics Data System (ADS)

    Bae, Pan Kee; Chung, Bong Hyun

    2014-07-01

    The effective targeting of cancer cell surface antigens is an attractive approach in cancer diagnosis and therapy. Multifunctional nanoprobes with cell-targeting specificity are likely to find important applications in bioanalysis, biomedicine, and clinical diagnosis. In this study, we have fabricated biocompatible perfluorocan/quantum dot nanoemulsions as bimodal imaging nanoprobes for the targeting of breast cancer cells. Perfluorocarbon/quantum dot nanoemulsions conjugated with monoclonal antibodies, as a type of bimodal imaging nanoprobe based on 19 F-MR and optical imaging, have been synthesized and applied for targeted imaging of three different breast cancer cells (SKBR3, MCF-7, MDA-MB 468), respectively. We have shown that the cancer-detection capabilities of antibody-conjugated PFC/QDs nanoemulsions could be successfully applied to target of various breast cancer cells. These modified PFC/QDs nanoemulsions were shown to target the cancer cell surface receptors specially. Conjugation of ligands to nanoemulsions targeting over-expressed cell surface receptors is a promising approach for targeted imaging to tumor cells. We further propose that the PFC/QDs nanoemulsions could be used in targeted imaging of breast cancer cells.

  16. Anti-inflammatory and analgesic effects of ketoprofen in palm oil esters nanoemulsion.

    PubMed

    Sakeena, M H F; Yam, M F; Elrashid, S M; Munavvar, A S; Azmin, M N

    2010-01-01

    Ketoprofen is a potent non-steroidal anti-inflammatory drug has been used in the treatment of various kinds of pains, inflammation and arthritis. However, oral administration of ketoprofen produces serious gastrointestinal adverse effects. One of the promising methods to overcome these adverse effects is to administer the drug through the skin. The aim of the present work is to evaluate the anti-inflammatory and analgesic effects from topically applied ketoprofen entrapped palm oil esters (POEs) based nanoemulsion and to compare with market ketoprofen product, Fastum(®) gel. The novelty of this study is, use of POEs for the oil phase of nanoemulsion. The anti-inflammatory and analgesic studies were performed on rats by carrageenan-induced rat hind paw edema test and carrageenan-induced hyperalgesia pain threshold test to compare the ketoprofen entrapped POEs based nanoemulsion formulation and market formulation. Results indicated that there are no significant different between ketoprofen entrapped POEs nanoemulsion and market formulation in carrageenan-induced rat hind paw edema study and carrageenan-induced hyperalgesia pain threshold study. However, it shows a significant different between POEs nanoemulsion formulation and control group in these studies at p<0.05. From these results it was concluded that the developed nanoemulsion have great potential for topical application of ketoprofen.

  17. EGFR Targeted Theranostic Nanoemulsion For Image-Guided Ovarian Cancer Therapy

    PubMed Central

    Ganta, Srinivas; Singh, Amit; Kulkarni, Praveen; Keeler, Amanda W.; Piroyan, Aleksandr; Sawant, Rupa R.; Patel, Niravkumar R.; Davis, Barbara; Ferris, Craig; O’Neal, Sara; Zamboni, William; Amiji, Mansoor M.; Coleman, Timothy P.

    2015-01-01

    Purpose Platinum-based therapies are the first line treatments for most types of cancer including ovarian cancer. However, their use is associated with dose-limiting toxicities and resistance. We report initial translational studies of a theranostic nanoemulsion loaded with a cisplatin derivative, myrisplatin and pro-apoptotic agent, C6-ceramide. Methods The surface of the nanoemulsion is annotated with an endothelial growth factor receptor (EGFR) binding peptide to improve targeting ability and gadolinium to provide diagnostic capability for image-guided therapy of EGFR overexpressing ovarian cancers. A high shear microfludization process was employed to produce the formulation with particle size below 150 nm. Results Pharmacokinetic study showed a prolonged blood platinum and gadolinium levels with nanoemulsions in nu/nu mice. The theranostic nanoemulsions also exhibited less toxicity and enhanced the survival time of mice as compared to an equivalent cisplatin treatment. Conclusions Magnetic resonance imaging (MRI) studies indicate the theranostic nanoemulsions were effective contrast agents and could be used to track accumulation in a tumor. The MRI study additionally indicate that significantly more EGFR-targeted theranostic nanoemulsion accumulated in a tumor than non-targeted nanoemulsuion providing the feasibility of using a targeted theranostic agent in conjunction with MRI to image disease loci and quantify the disease progression. PMID:25732960

  18. Development of Food-Grade Curcumin Nanoemulsion and its Potential Application to Food Beverage System: Antioxidant Property and In Vitro Digestion.

    PubMed

    Joung, Hee Joung; Choi, Mi-Jung; Kim, Jun Tae; Park, Seok Hoon; Park, Hyun Jin; Shin, Gye Hwa

    2016-03-01

    Curcumin nanoemulsions (Cur-NEs) were developed with various surfactant concentrations by using high pressure homogenization and finally applied to the commercial milk system. Characterization of Cur-NEs was performed by measuring the droplet size and polydispersity index value at different Tween 20 concentrations. The morphology of the Cur-NEs was observed by confocal laser scanning microscopy and transmission electron microscopy. Antioxidant activity and in vitro digestion ability were tested using 2,2-diphenyl-1-picrylhydrazyl, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt, pH-stat method, and thiobarbituric acid reactive substances assays. Cur-NEs were found to be physically stable for 1 mo at room temperature. The surfactant concentration affects particle formation and droplet size. The mean droplet size decreased from 122 to 90 nm when surfactant concentration increased 3 times. Cur-NEs had shown an effective oxygen scavenging activity. Cur-NEs-fortified milk showed significantly lower lipid oxidation than control (unfortified) milk and milk containing curcumin-free nanoemulsions. These properties make Cur-NEs suitable systems for the beverage industry.

  19. Non-enzymatic glucose detection using magnetic nanoemulsions

    SciTech Connect

    Mahendran, V.; Philip, John

    2014-09-22

    We probe the optical properties and intermolecular interactions in magnetically responsive nanoemulsions in the presence of glucose. The equilibrium interdroplet distance between the emulsion droplets in an one-dimensional array increases by several nanometers in the presence of glucose because of intermolecular hydrogen bonding with sodium dodecyl sulphate molecules at the oil-water interface that gives rise to stretched lamellae-like structure. The observed large red shift in the diffracted Bragg peak (∼50–100 nm) and the linear response in the glucose concentration range of 0.25–25 mM offer a simple, fast, and cost effective non-enzymatic approach for glucose detection.

  20. Formation and stability of nanoemulsions with mixed ionic-nonionic surfactants.

    PubMed

    Wang, Lijuan; Tabor, Rico; Eastoe, Julian; Li, Xuefeng; Heenan, Richard K; Dong, Jinfeng

    2009-11-14

    A simple, low-energy two-step dilution process has been applied with binary mixtures of ionic-nonionic surfactants to prepare nanoemulsions. The systems consist of water/DDAB-C(12)E(5)/decane. Nanoemulsions were obtained by dilution of concentrates located in bicontinuous microemulsion or lamellar liquid crystal phase regions. The nanoemulsions generated were investigated both by contrast-variation small-angle neutron scattering (SANS) and dynamic light scattering (DLS). The SANS profiles show that C(12)E(5) nanodroplets suffer essentially no structural change on incorporation of the cationic DDAB surfactant, except for increased electrostatic repulsive interactions. Interestingly, SANS indicated that the preferred droplet sizes were hardly affected by the surfactant mixture composition (up to a DDAB molar ratio (m(DDAB)/(m(DDAB) + m(C(12)E(5))) of 0.40) and droplet volume fraction, phi, between 0.006 and 0.120. No notable changes in the structure or radius of nanoemulsion droplets were observed by SANS over the test period of 1 d, although the droplet number intensity decreased significantly in systems stabilized by C(12)E(5) only. However, the DLS sizing shows a marked increase with time, with higher droplet volume fractions giving rise to the largest changes. The discrepancy between apparent nanoemulsion droplet size determined by DLS and SANS data can be attributed to long-range droplet interactions occurring outside of the SANS sensitivity range. The combined SANS and DLS results suggest flocculation is the main mechanism of instability for these nanoemulsions. The flocculation rate is shown to be significantly retarded by addition of the charged DDAB, which may be due to enhanced electrostatic repulsive forces between droplets, leading to improved stability of the nanoemulsions.

  1. Ultrasound-Mediated Tumor Imaging and Nanotherapy using Drug Loaded, Block Copolymer Stabilized Perfluorocarbon Nanoemulsions

    PubMed Central

    Rapoport, Natalya; Nam, Kweon-Ho; Gupta, Roohi; Gao, Zhongao; Mohan, Praveena; Payne, Allison; Todd, Nick; Liu, Xin; Kim, Taeho; Shea, Jill; Scaife, Courtney; Parker, Dennis L.; Jeong, Eun-Kee; Kennedy, Anne M.

    2011-01-01

    Perfluorocarbon nanoemulsions can deliver lipophilic therapeutic agents to solid tumors and simultaneously provide for monitoring nanocarrier biodistribution via ultrasonography and/or 19F MRI. In the first generation of block copolymer stabilized perfluorocarbon nanoemulsions, perfluoropentane (PFP) was used as the droplet forming compound. Although manifesting excellent therapeutic and ultrasound imaging properties, PFP nanoemulsions were unstable at storage, difficult to handle, and underwent hard to control phenomenon of irreversible droplet-to-bubble transition upon injection. To solve the above problems, perfluoro-15-crown-5-ether (PFCE) was used as a core forming compound in the second generation of block copolymer stabilized perfluorocarbon nanoemulsions. PFCE nanodroplets manifest both ultrasound and fluorine (19F) MR contrast properties, which allows using multimodal imaging and 19F MR spectroscopy for monitoring nanodroplet pharmacokinetics and biodistribution. In the present paper, acoustic, imaging, and therapeutic properties of unloaded and paclitaxel (PTX) loaded PFCE nanoemulsions are reported. As manifested by the 19F MR spectroscopy, PFCE nanodroplets are long circulating, with about 50% of the injected dose remaining in circulation two hours after the systemic injection. Sonication with 1-MHz therapeutic ultrasound triggered reversible droplet-to-bubble transition in PFCE nanoemulsions. Microbubbles formed by acoustic vaporization of nanodroplets underwent stable cavitation. The nanodroplet size (200 nm to 350 nm depending on a type of the shell and conditions of emulsification) as well as long residence in circulation favored their passive accumulation in tumor tissue that was confirmed by ultrasonography. In the breast and pancreatic cancer animal models, ultrasound-mediated therapy with paclitaxel-loaded PFCE nanoemulsions showed excellent therapeutic properties characterized by tumor regression and suppression of metastasis. Anticipated

  2. Nanoemulsion strategy for olmesartan medoxomil improves oral absorption and extended antihypertensive activity in hypertensive rats.

    PubMed

    Gorain, Bapi; Choudhury, Hira; Kundu, Amit; Sarkar, Lipi; Karmakar, Sanmoy; Jaisankar, P; Pal, Tapan Kumar

    2014-03-01

    Olmesartan medoxomil (OM) is hydrolyzed to its active metabolite olmesartan by the action of aryl esterase to exert its antihypertensive actions by selectively blocking angiotensin II-AT1 receptor. Poor aqueous solubility and uncontrolled enzymatic conversion of OM to its poorly permeable olmesartan limits its oral bioavailability. The aim of the current study was to formulate a novel nanoemulsion of OM to improve its pharmacokinetics and therapeutic efficacy. The oil-in-water (o/w) nanoemulsion of OM was developed using lipoid purified soybean oil 700, sefsol 218 and solutol HS 15. We have characterized the nanoemulsions by considering their thermodynamic stability, morphology, droplet size, zeta potential and viscosity and in vitro drug release characteristics in fasting state simulated gastric fluid (pH 1.2) and intestinal fluid (pH 6.5). The thermodynamically stable nanoemulsions comprises of spherical nanometer sized droplets (<50 nm) with low polydispersity index showed enhanced permeability through the Caco-2 cell monolayer. The concentration of active olmesartan in rat plasma following oral absorption study was determined by our validated LC-MS/MS method. The result of the pharmacokinetic study showed 2.8-fold increased in area under the curve (AUC0-27) of olmesartan upon oral administration of OM nanoemulsion and sustained release profile. Subsequent, in vivo studies with nanoemulsion demonstrated better and prolonged control of experimentally induced hypertension with 3-fold reduction in conventional dose. By analysing the findings of the present investigations based on stability study, Caco-2 permeability, pharmacokinetic profile and pharmacodynamic evaluation indicated that the nanoemulsion of OM (OMF6) could significantly enhance the oral bioavailability of relatively insoluble OM contributing to improved clinical application.

  3. Nanoemulsion strategy for olmesartan medoxomil improves oral absorption and extended antihypertensive activity in hypertensive rats.

    PubMed

    Gorain, Bapi; Choudhury, Hira; Kundu, Amit; Sarkar, Lipi; Karmakar, Sanmoy; Jaisankar, P; Pal, Tapan Kumar

    2014-03-01

    Olmesartan medoxomil (OM) is hydrolyzed to its active metabolite olmesartan by the action of aryl esterase to exert its antihypertensive actions by selectively blocking angiotensin II-AT1 receptor. Poor aqueous solubility and uncontrolled enzymatic conversion of OM to its poorly permeable olmesartan limits its oral bioavailability. The aim of the current study was to formulate a novel nanoemulsion of OM to improve its pharmacokinetics and therapeutic efficacy. The oil-in-water (o/w) nanoemulsion of OM was developed using lipoid purified soybean oil 700, sefsol 218 and solutol HS 15. We have characterized the nanoemulsions by considering their thermodynamic stability, morphology, droplet size, zeta potential and viscosity and in vitro drug release characteristics in fasting state simulated gastric fluid (pH 1.2) and intestinal fluid (pH 6.5). The thermodynamically stable nanoemulsions comprises of spherical nanometer sized droplets (<50 nm) with low polydispersity index showed enhanced permeability through the Caco-2 cell monolayer. The concentration of active olmesartan in rat plasma following oral absorption study was determined by our validated LC-MS/MS method. The result of the pharmacokinetic study showed 2.8-fold increased in area under the curve (AUC0-27) of olmesartan upon oral administration of OM nanoemulsion and sustained release profile. Subsequent, in vivo studies with nanoemulsion demonstrated better and prolonged control of experimentally induced hypertension with 3-fold reduction in conventional dose. By analysing the findings of the present investigations based on stability study, Caco-2 permeability, pharmacokinetic profile and pharmacodynamic evaluation indicated that the nanoemulsion of OM (OMF6) could significantly enhance the oral bioavailability of relatively insoluble OM contributing to improved clinical application. PMID:24388859

  4. Formation and stability of nanoemulsions with mixed ionic-nonionic surfactants.

    PubMed

    Wang, Lijuan; Tabor, Rico; Eastoe, Julian; Li, Xuefeng; Heenan, Richard K; Dong, Jinfeng

    2009-11-14

    A simple, low-energy two-step dilution process has been applied with binary mixtures of ionic-nonionic surfactants to prepare nanoemulsions. The systems consist of water/DDAB-C(12)E(5)/decane. Nanoemulsions were obtained by dilution of concentrates located in bicontinuous microemulsion or lamellar liquid crystal phase regions. The nanoemulsions generated were investigated both by contrast-variation small-angle neutron scattering (SANS) and dynamic light scattering (DLS). The SANS profiles show that C(12)E(5) nanodroplets suffer essentially no structural change on incorporation of the cationic DDAB surfactant, except for increased electrostatic repulsive interactions. Interestingly, SANS indicated that the preferred droplet sizes were hardly affected by the surfactant mixture composition (up to a DDAB molar ratio (m(DDAB)/(m(DDAB) + m(C(12)E(5))) of 0.40) and droplet volume fraction, phi, between 0.006 and 0.120. No notable changes in the structure or radius of nanoemulsion droplets were observed by SANS over the test period of 1 d, although the droplet number intensity decreased significantly in systems stabilized by C(12)E(5) only. However, the DLS sizing shows a marked increase with time, with higher droplet volume fractions giving rise to the largest changes. The discrepancy between apparent nanoemulsion droplet size determined by DLS and SANS data can be attributed to long-range droplet interactions occurring outside of the SANS sensitivity range. The combined SANS and DLS results suggest flocculation is the main mechanism of instability for these nanoemulsions. The flocculation rate is shown to be significantly retarded by addition of the charged DDAB, which may be due to enhanced electrostatic repulsive forces between droplets, leading to improved stability of the nanoemulsions. PMID:19851556

  5. Cognitive Resemblance and Citation Relations in Chemical Engineering Publications.

    ERIC Educational Resources Information Center

    Peters, H. P. F.; And Others

    1995-01-01

    Describes an empirical study that measured word-profile similarities between citing and cited publications in the chemical engineering field. Highlights include cognitive resemblance and bibliographic coupling; data collection techniques; analysis of word-profile similarity; bibliographic coupled publications; mapping of cognitive resemblance; and…

  6. Layered nanoemulsions as mucoadhesive buccal systems for controlled delivery of oral cancer therapeutics.

    PubMed

    Gavin, Amy; Pham, Jimmy Th; Wang, Dawei; Brownlow, Bill; Elbayoumi, Tamer A

    2015-01-01

    Oral cavity and oropharyngeal cancers are considered the eighth most common cancer worldwide, with relatively poor prognosis (62% of patients surviving 5 years, after diagnosis). The aim of this study was to develop a proof-of-concept mucoadhesive lozenge/buccal tablet, as a potential platform for direct sustained delivery of therapeutic antimitotic nanomedicines. Our system would serve as an adjuvant therapy for oral cancer patients undergoing full-scale diagnostic and operative treatment plans. We utilized lipid-based nanocarriers, namely nanoemulsions (NEs), containing mixed-polyethoxylated emulsifiers and a tocopheryl moiety-enriched oil phase. Prototype NEs, loaded with the proapoptotic lipophilic drug genistein (Gen), were further processed into buccal tablet formulations. The chitosan polyelectrolyte solution overcoat rendered NE droplets cationic, by acting as a mucoadhesive interfacial NE layer. With approximate size of 110 nm, the positively charged chitosan-layered NE (+25 mV) vs negatively charged chitosan-free/primary aqueous NE (-28 mV) exhibited a controlled-release profile and effective mucoadhesion for liquid oral spray prototypes. When punch-pressed, porous NE-based buccal tablets were physically evaluated for hardness, friability, and swelling in addition to ex vivo tissue mucoadhesion force and retention time measurements. Chitosan-containing NE tablets were found equivalent to primary NE and placebo tablets in compression tests, yet significantly superior in all ex vivo adhesion and in vitro release assays (P≤0.05). Following biocompatibility screening of prototype chitosan-layered NEs, substantial anticancer activity of selected cationic Gen-loaded NE formulations, against two oropahryngeal carcinomas, was observed. The data strongly indicate the potential of such nanomucoadhesive systems as maintenance therapy for oral cancer patients awaiting surgical removal, or postresection of identified cancerous lesions. PMID:25759580

  7. Layered nanoemulsions as mucoadhesive buccal systems for controlled delivery of oral cancer therapeutics.

    PubMed

    Gavin, Amy; Pham, Jimmy Th; Wang, Dawei; Brownlow, Bill; Elbayoumi, Tamer A

    2015-01-01

    Oral cavity and oropharyngeal cancers are considered the eighth most common cancer worldwide, with relatively poor prognosis (62% of patients surviving 5 years, after diagnosis). The aim of this study was to develop a proof-of-concept mucoadhesive lozenge/buccal tablet, as a potential platform for direct sustained delivery of therapeutic antimitotic nanomedicines. Our system would serve as an adjuvant therapy for oral cancer patients undergoing full-scale diagnostic and operative treatment plans. We utilized lipid-based nanocarriers, namely nanoemulsions (NEs), containing mixed-polyethoxylated emulsifiers and a tocopheryl moiety-enriched oil phase. Prototype NEs, loaded with the proapoptotic lipophilic drug genistein (Gen), were further processed into buccal tablet formulations. The chitosan polyelectrolyte solution overcoat rendered NE droplets cationic, by acting as a mucoadhesive interfacial NE layer. With approximate size of 110 nm, the positively charged chitosan-layered NE (+25 mV) vs negatively charged chitosan-free/primary aqueous NE (-28 mV) exhibited a controlled-release profile and effective mucoadhesion for liquid oral spray prototypes. When punch-pressed, porous NE-based buccal tablets were physically evaluated for hardness, friability, and swelling in addition to ex vivo tissue mucoadhesion force and retention time measurements. Chitosan-containing NE tablets were found equivalent to primary NE and placebo tablets in compression tests, yet significantly superior in all ex vivo adhesion and in vitro release assays (P≤0.05). Following biocompatibility screening of prototype chitosan-layered NEs, substantial anticancer activity of selected cationic Gen-loaded NE formulations, against two oropahryngeal carcinomas, was observed. The data strongly indicate the potential of such nanomucoadhesive systems as maintenance therapy for oral cancer patients awaiting surgical removal, or postresection of identified cancerous lesions.

  8. Layered nanoemulsions as mucoadhesive buccal systems for controlled delivery of oral cancer therapeutics

    PubMed Central

    Gavin, Amy; Pham, Jimmy TH; Wang, Dawei; Brownlow, Bill; Elbayoumi, Tamer A

    2015-01-01

    Oral cavity and oropharyngeal cancers are considered the eighth most common cancer worldwide, with relatively poor prognosis (62% of patients surviving 5 years, after diagnosis). The aim of this study was to develop a proof-of-concept mucoadhesive lozenge/buccal tablet, as a potential platform for direct sustained delivery of therapeutic antimitotic nanomedicines. Our system would serve as an adjuvant therapy for oral cancer patients undergoing full-scale diagnostic and operative treatment plans. We utilized lipid-based nanocarriers, namely nanoemulsions (NEs), containing mixed-polyethoxylated emulsifiers and a tocopheryl moiety–enriched oil phase. Prototype NEs, loaded with the proapoptotic lipophilic drug genistein (Gen), were further processed into buccal tablet formulations. The chitosan polyelectrolyte solution overcoat rendered NE droplets cationic, by acting as a mucoadhesive interfacial NE layer. With approximate size of 110 nm, the positively charged chitosan-layered NE (+25 mV) vs negatively charged chitosan-free/primary aqueous NE (−28 mV) exhibited a controlled-release profile and effective mucoadhesion for liquid oral spray prototypes. When punch-pressed, porous NE-based buccal tablets were physically evaluated for hardness, friability, and swelling in addition to ex vivo tissue mucoadhesion force and retention time measurements. Chitosan-containing NE tablets were found equivalent to primary NE and placebo tablets in compression tests, yet significantly superior in all ex vivo adhesion and in vitro release assays (P≤0.05). Following biocompatibility screening of prototype chitosan-layered NEs, substantial anticancer activity of selected cationic Gen-loaded NE formulations, against two oropahryngeal carcinomas, was observed. The data strongly indicate the potential of such nanomucoadhesive systems as maintenance therapy for oral cancer patients awaiting surgical removal, or postresection of identified cancerous lesions. PMID:25759580

  9. Lipid-Based Nanocarriers for RNA Delivery

    PubMed Central

    Xue, Hui Yi; Guo, Pengbo; Wen, Wu-Cheng; Wong, Ho Lun

    2015-01-01

    RNA-interference (RNAi) agents such as small-interfering RNA (siRNA) and micro-RNA (miRNA) have strong potential as therapeutic agents for the treatment of a broad range of diseases such as malignancies, infections, autoimmune diseases and neurological diseases that are associated with undesirable gene expression. In recent years, several clinical trials of RNAi therapeutics especially siRNAs have been conducted with limited success so far. For systemic administration of these poorly permeable and easily degradable macromolecules, it is obvious that a safe and efficient delivery platform is highly desirable. Because of high biocompatibility, biodegradability and solid track record for clinical use, nanocarriers made of lipids and/or phospholipids have been commonly employed to facilitate RNA delivery. In this article, the key features of the major sub-classes of lipid-based nanocarriers, e.g. liposomes, lipid nanoparticles and lipid nanoemulsions, will be reviewed. Focus of the discussion is on the various challenges researchers face when developing lipid-based RNA nanocarriers, such as the toxicity of cationic lipids and issues related to PEGylated lipids, as well as the strategies employed in tackling these challenges. It is hoped that by understanding more about the pros and cons of these most frequently used RNA delivery systems, the pharmaceutical scientists, biomedical researchers and clinicians will be more successful in overcoming some of the obstacles that currently limit the clinical translation of RNAi therapy.

  10. Influence of surfactant charge on antimicrobial efficacy of surfactant-stabilized thyme oil nanoemulsions.

    PubMed

    Ziani, Khalid; Chang, Yuhua; McLandsborough, Lynne; McClements, David Julian

    2011-06-01

    Thyme oil-in-water nanoemulsions stabilized by a nonionic surfactant (Tween 80, T80) were prepared as potential antimicrobial delivery systems (pH 4). The nanoemulsions were highly unstable to droplet growth and phase separation, which was attributed to Ostwald ripening due to the relatively high water solubility of thyme oil. Ostwald ripening could be inhibited by incorporating ≥75% of corn oil (a hydrophobic material with a low water solubility) into the nanoemulsion droplets. The electrical characteristics of the droplets in the nanoemulsions were varied by incorporating ionic surfactants with different charges after homogenization: a cationic surfactant (lauric arginate, LAE) or an anionic surfactant (sodium dodecyl sulfate, SDS). The antifungal activity of nanoemulsions containing positive, negative, or neutral thymol droplets was then conducted against four strains of acid-resistant spoilage yeasts: Zygosaccharomyces bailli, Saccharomyces cerevisiae, Brettanomyces bruxellensis, and Brettanomyces naardenensis. The antifungal properties of the three surfactants (T80, LAE, SDS) were also tested in the absence of thymol droplets. Both ionic surfactants showed strong antifungal activity in the absence of thymol droplets, but no antimicrobial activity in their presence. This effect was attributed to partitioning of the antimicrobial surfactant molecules between the oil droplet and microbial surfaces, thereby reducing the effective concentration of active surfactants available to act as antimicrobials. This study shows oil droplets may decrease the efficacy of surfactant-based antimicrobials, which has important consequences for formulating effective antimicrobial agents for utilization in emulsion-based food and beverage products. PMID:21520914

  11. Skin intervention of fullerene-integrated nanoemulsion in structural and collagen regeneration against skin aging.

    PubMed

    Ngan, Cheng Loong; Basri, Mahiran; Tripathy, Minaketan; Abedi Karjiban, Roghayeh; Abdul-Malek, Emilia

    2015-04-01

    Despite the fact that intrinsic oxidative stress is inevitable, the extrinsic factor such as ultraviolet radiation enhances reactive oxygen species (ROS) generation resulting in premature skin aging. Nanoemulsion was loaded with fullerene, a strong free radical scavenger, and its efficacy to provide protection and regenerative effect against ROS-induced collagen breakdown in human skin was studied. Stable fullerene nanoemulsions were formulated using high shear homogenization and ultrasonic dispersion technique. An open trial was conducted using fullerene nanoemulsion on skin twice a day for 28 days. The mean collagen score significantly increased (P<0.05) from 36.53±4.39 to 48.69±5.46 with 33.29% increment at the end of the treatment. Biophysical characteristics of skin revealed that skin hydration was increased significantly (P<0.05) from 40.91±7.01 to 58.55±6.08 corneometric units (43.12% increment) and the water was able to contain within the stratum corneum without any increased in transepidermal water loss. In the in vitro safety evaluation, fullerene nanoemulsion showed no acute toxicity on 3T3 fibroblast cell line for 48h and no indication of potential dermal irritation. Hence, the fullerene nanoemulsion may assist in protecting collagen from breakdown with cosmeceutical benefit.

  12. Development of low-energy methods for preparing food Nano-emulsions.

    PubMed

    Miyanoshita, Michitaka; Hashida, Chitose; Ikeda, Shinya; Gohtani, Shoichi

    2011-01-01

    The aim of this work was to investigate the effect of sucrose on the phase behavior of vegetable oil/polyoxyethylene sorbitan monooleate (MOPS, Tween 80) and decaglycerol monolaurilester (DGML)/aqueous solution systems to establish low-energy emulsification methods for preparing nano-emulsions suitable for food uses. Phase diagrams were constructed to elucidate the optimal process for preparing the nano-emulsions. It was found that nano-emulsions were obtained when the composition was altered to either cross the sponge phase (L(3)) or lamellar phase (La) in the vegetable oil/MOPS/aqueous solution system or vegetable oil/DGML/aqueous solution system, respectively. The average droplet sizes in the former and latter emulsions were 0.203 µm and 0.165 µm, respectively. The addition of sucrose changed the hexagonal phase in the vegetable oil/MOPS/aqueous solution system into the sponge phase. As a result, the sponge region in the vegetable oil/MOPS/sucrose aqueous solution system occupied a larger area than that in the vegetable oil/MOPS/water system. In contrast, sucrose had no effect on the area of the La region in the vegetable oil/DGML/aqueous solution system. However, the addition of sucrose decreased the amount of emulsifier required to prepare nano-emulsions in both the vegetable oil/MOPS and DGML/aqueous solution systems. Sucrose was confirmed to facilitate the preparation of nano-emulsions in both systems.

  13. Physicochemical Characterization and Thermodynamic Studies of Nanoemulsion-Based Transdermal Delivery System for Fullerene

    PubMed Central

    Basri, Mahiran; Tripathy, Minaketan; Abdul-Malek, Emilia

    2014-01-01

    Fullerene nanoemulsions were formulated in palm kernel oil esters stabilized by low amount of mixed nonionic surfactants. Pseudoternary phase diagrams were established in the colloidal system of PKOEs/Tween 80 : Span 80/water incorporated with fullerene as antioxidant. Preformulation was subjected to combination of high and low energy emulsification methods and the physicochemical characteristics of fullerene nanoemulsions were analyzed using electroacoustic spectrometer. Oil-in-water (O/W) nanoemulsions with particle sizes in the range of 70–160 nm were formed. The rheological characteristics of colloidal systems exhibited shear thinning behavior which fitted well into the power law model. The effect of xanthan gum (0.2–1.0%, w/w) and beeswax (1–3%, w/w) in the estimation of thermodynamics was further studied. From the energetic parameters calculated for the viscous flow, a moderate energy barrier for transport process was observed. Thermodynamic study showed that the enthalpy was positive in all xanthan gum and beeswax concentrations indicating that the formation of nanoemulsions could be endothermic in nature. Fullerene nanoemulsions with 0.6% or higher xanthan gum content were found to be stable against creaming and flocculation when exposed to extreme environmental conditions. PMID:25165736

  14. Superior antibacterial activity of nanoemulsion of Thymus daenensis essential oil against E. coli.

    PubMed

    Moghimi, Roya; Ghaderi, Lida; Rafati, Hasan; Aliahmadi, Atousa; McClements, David Julian

    2016-03-01

    Natural preservatives are being extensively investigated for their potential industrial applications in foods and other products. In this work, an essential oil (Thymus daenensis) was formulated as a water-dispersible nanoemulsion (diameter=143nm) using high-intensity ultrasound. The antibacterial activity of the essential oil in both pure and nanoemulsion forms was measured against an important food-borne pathogen bacterium, Escherichia coli. Antibacterial activity was determined by measuring the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). The antibacterial activity of the essential oil against E. coli was enhanced considerably when it was converted into a nanoemulsion, which was attributed to easier access of the essential oils to the bacterial cells. The mechanism of antibacterial activity was investigated by measuring potassium, protein, and nucleic acid leakage from the cells, and electron microscopy. Evaluation of the kinetics of microbial deactivation showed that the nanoemulsion killed all the bacteria in about 5min, whereas only a 1-log reduction was observed for pure essential oil. The nanoemulsion appeared to amplify the antibacterial activity of essential oils against E. coli by increasing their ability to disrupt cell membrane integrity.

  15. Superior antibacterial activity of nanoemulsion of Thymus daenensis essential oil against E. coli.

    PubMed

    Moghimi, Roya; Ghaderi, Lida; Rafati, Hasan; Aliahmadi, Atousa; McClements, David Julian

    2016-03-01

    Natural preservatives are being extensively investigated for their potential industrial applications in foods and other products. In this work, an essential oil (Thymus daenensis) was formulated as a water-dispersible nanoemulsion (diameter=143nm) using high-intensity ultrasound. The antibacterial activity of the essential oil in both pure and nanoemulsion forms was measured against an important food-borne pathogen bacterium, Escherichia coli. Antibacterial activity was determined by measuring the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). The antibacterial activity of the essential oil against E. coli was enhanced considerably when it was converted into a nanoemulsion, which was attributed to easier access of the essential oils to the bacterial cells. The mechanism of antibacterial activity was investigated by measuring potassium, protein, and nucleic acid leakage from the cells, and electron microscopy. Evaluation of the kinetics of microbial deactivation showed that the nanoemulsion killed all the bacteria in about 5min, whereas only a 1-log reduction was observed for pure essential oil. The nanoemulsion appeared to amplify the antibacterial activity of essential oils against E. coli by increasing their ability to disrupt cell membrane integrity. PMID:26471573

  16. The Effect of Nanoemulsion as a Carrier of Hydrophilic Compound for Transdermal Delivery

    PubMed Central

    Lin, Yu-Hsuan; Huang, Yaw-Bin; Wu, Pao-Chu

    2014-01-01

    The purpose of the present study was to investigate the effect of nanoemulsions as a carrier vehicle of hydrophilic drug for transdermal delivery. The response surface methodology with a mixture design was used to evaluate the effect of ingredient levels of nanoemulsion formulations including cosurfactant (isopropyl alcohol, 20∼30%), surfactant (mixed of Brij 30 and Brij 35, 20∼30%), and distilled-water (34.5∼50.0%) on properties of the drug-loaded nanoemulsions including physicochemical characters and drug permeability through rat skin. The result showed that the hydrophilic drug in aqueous solution with or without penetration enhancer could not transport across rat skin after 12 h of application. Used nanoemulsions as carrier vehicle, the permeation rate of drug was significantly increased from 0 to 63.23 µg/cm2/h and the lag time was shortened from more than 12 h to about 2.7∼4.0 h. Moreover, the drug-loaded nanoemulsion formulation also showed physicochemical stability after 3 month storage at 25°C and 40°C. PMID:25068531

  17. Nanoemulsions as novel oral carriers of stiripentol: insights into the protective effect and absorption enhancement.

    PubMed

    Lu, Rong; Liu, Shan; Wang, Qilin; Li, Xia

    2015-01-01

    Oral administration remains a significant challenge in regards to drugs with serious solubility and stability issues. This article aimed to investigate the suitability of nanoemulsions as oral carriers of stiripentol (STP), an acid-labile drug, for enhancement of stability and bioavailability. STP-loaded nanoemulsions (STP-NEs) were prepared by using a solvent-diffusion/ultrasonication technique. STP-NEs were characterized in a variety of ways such as by particle size, entrapment efficiency, in vitro drug release, and transmission electron microscopy. A bioavailability study was performed in rats after oral administration of either STP-NEs, or commercial formulation (Diacomit). The resultant nanoemulsions were 146.6 nm in particle size with an entrapment efficiency of 99.47%. It was demonstrated that nanoemulsions significantly improved the biochemical stability and bioavailability of STP. The bioavailability of STP-NEs was up to 206.2% relative to Diacomit. Nanoemulsions fabricated from poly(ethylene glycol) monooleate/medium-chain triglycerides exhibited excellent performance in drug stabilization and absorption enhancement. The results suggest that STP-NEs are a promising means to solve the problems associated with stability and solubility of STP. PMID:26261418

  18. Antioxidant Effect of Nanoemulsions Containing Extract of Achyrocline satureioides (Lam) D.C.-Asteraceae.

    PubMed

    Zorzi, Giovanni Konat; Caregnato, Fernanda; Moreira, José Cláudio Fonseca; Teixeira, Helder Ferreira; Carvalho, Edison Luis Santana

    2016-08-01

    Ethanolic extracts of Achyrocline satureioides have pronounced antioxidant activity mainly due to the presence of the flavonoid quercetin. However, direct topical application of the extract is not possible due to the presence of high amounts of ethanol. In this sense, nanoemulsions arise as an alternative for topical formulation associating molecules with limited aqueous solubility. This article describes the development of topical nanoemulsions containing either A. satureioides extract or one of its most abundant flavonoid, quercetin. Nanoemulsions composed of octyldodecanol, egg lecithin, water and extract (NEE), or quercetin (NEQ) were prepared by spontaneous emulsification. This process led to monodisperse nanoemulsions presenting a mean droplet size of approximately 200-300 nm, negative zeta potential, and high association efficiency. A study of quercetin skin retention using porcine skin which was performed using a Franz diffusion cell revealed a higher accumulation of quercetin in skin for NEE when compared to NEQ. Finally, the antioxidant activity of formulations was measured by thiobarbituric acid-reactive species and the APPH model. A lower lipoperoxidation for the extract in respect to quercetin solution was observed. However, no difference between NEQ and NEE lipoperoxidation could be seen. The protection against lipoperoxidation by the formulations was also measured in the skin, where lower formation of reactive species was observed after treatment with NEE. In conclusion, this study shows the formulation effect on the physicochemical properties of nanoemulsions as well as on the skin retention and antioxidant activity of quercetin.

  19. Stearylamine-Containing Cationic Nanoemulsion as a Promising Carrier for Gene Delivery.

    PubMed

    Silva, André L; Marcelino, Henrique R; Verissimo, Lourena M; Araujo, Ivonete B; Agnez-Lima, Lucymara F; do Egito, Eryvaldo S T

    2016-02-01

    The drawbacks related to the use of viral vectors in gene therapy have been stimulated the research in non-viral strategies such as cationic nanoemulsions. The aim of this work was to develop a stearylamine-containing nanoemulsion for gene therapy purpose. The formulation was chosen from a Pseudo-Ternary Phase Diagram and had its long-term stability assessed by Dynamic Light Scattering and Phase Analysis Light Scattering during 180 days at 4 degrees C, 25 degrees C and 40 degrees C. Besides, studies of sterilization and scale up of the product were conducted. It was demonstrated that the proposed system was stable up to 180 days when stored at 4 degrees C and could be sterilized by a 0.22 microm filter pore without changes on its characteristics. The scale up was possible by adjusting the volume to the sonication time. Because the nanoemulsion presented a droplet size smaller than 200 nm and a zeta potential higher than 30 mV, this system was able to correctly complex the plasmid model PIRES2-EGFP, as confirmed by the agarosis gel electrophoresis assay. The nanoemulsion toxicity evaluated over lung fetus human cells (MRC-5) was dose-dependent. However, it does not appear to be a limiting factor for further experiments aiming gene transfection. As a conclusion, stearylamine-containing cationic nanoemulsions can be used for gene therapy, since it presents suitable characteristics, stability and possibility of sterilization. PMID:27433584

  20. Development and stability evaluation of olive oil nanoemulsion using sucrose monoester laurate

    NASA Astrophysics Data System (ADS)

    Eid, Ahmad M. M.; Baie, Saringat Haji; Arafat, Osama

    2012-11-01

    Nanoemulsion is a type of emulsion that consists of fine oil-in-water dispersions, with the droplets covering the size range of 20-200 nm. It can be achieved through emulsification process. One of the processes is through low energy emulsification method. Olive oil was chosen in this study due to its efficiency in treating skin problem. Olive oil nanophase gel (NPG) formulations were performed through various ratios of olive oil, sucrose laurate and glycerin. The particle sizes and stability of the prepared olive oil nanophase gel were evaluated and the optimal formulation was then selected for the development of olive oil nanoemulsion. This study proved that the composition of oil and surfactant play an important roles in influencing the nanophase gel droplet size. Nanophase gels containing olive oil in the concentration of 50 and 60 % show good stability at 4 °C and room temperature while it was less stable at 40 °C. Olive oil nanophase gels in the concentration of 50 % and 60 % with sucrose laurate 25 % in each formulation were good candidates to prepare nanoemulsion because they have the suitable droplets size and Polydispersing Index (PDI) when compared to other formulations. A mixture of NPG 50 % and water in the ratio of 40:60 and NPG 60 % and water in the ratio of 33.3:66.7 were used to produce nanoemulsions containing 20 % of oil with negative values of zeta potential (>60) which indicate the good stability of the nanoemulsions.

  1. Ketoprofen-loaded pomegranate seed oil nanoemulsion stabilized by pullulan: Selective antiglioma formulation for intravenous administration.

    PubMed

    Ferreira, Luana M; Cervi, Verônica F; Gehrcke, Mailine; da Silveira, Elita F; Azambuja, Juliana H; Braganhol, Elizandra; Sari, Marcel H M; Zborowski, Vanessa A; Nogueira, Cristina W; Cruz, Letícia

    2015-06-01

    This study aimed to prepare pomegranate seed oil nanoemulsions containing ketoprofen using pullulan as a polymeric stabilizer, and to evaluate antitumor activity against in vitro glioma cells. Formulations were prepared by the spontaneous emulsification method and different concentrations of pullulan were tested. Nanoemulsions presented adequate droplet size, polydispersity index, zeta potential, pH, ketoprofen content and encapsulation efficiency. Nanoemulsions were able to delay the photodegradation profile of ketoprofen under UVC radiation, regardless of the concentration of pullulan. In vitro release study indicates that nanoemulsions were able to release approximately 95.0% of ketoprofen in 5h. Free ketoprofen and formulations were considered hemocompatible at 1 μg/mL, in a hemolysis study, for intravenous administration. In addition, a formulation containing the highest concentration of pullulan was tested against C6 cell line and demonstrated significant activity, and did not reduce fibroblasts viability. Thus, pullulan can be considered an interesting excipient to prepare nanostructured systems and nanoemulsion formulations can be considered promising alternatives for the treatment of glioma.

  2. Comparison of modified starch and Quillaja saponins in the formation and stabilization of flavor nanoemulsions.

    PubMed

    Zhang, Jian; Bing, Lu; Reineccius, Gary A

    2016-02-01

    Modified starch (MS) and Quillaja saponins (QS) were compared to fabricate and stabilize orange oil nanoemulsions using microfluidization. Ester gum (EG) was incorporated in the oil phase at variable proportions (0-60%) as Ostwald ripening inhibitor and viscosity modifier. Optimal viscosity ratios of dispersed to continuous phase (ηd/ηc) were identified as 0.8-3.1 and 2.1-3.3 with MS and QS as emulsifier, respectively. QS was found superior to MS in fabricating nanoemulsion with smallest MDD of 69 nm and turbidity of 102 NTU at 0.05% of dispersed phase. With EG incorporated in the oil phase, QS stabilized nanoemulsions were stable during 2 weeks of storage at 23 °C; whereas MS stabilized nanoemulsions showed significant increases in MDD and turbidity. Zeta potential measurements showed QS imparted higher droplet charge (>-20 mV) than MS (<-5 mV) at pH 3.6 indicating MS stabilized nanoemulsions were destabilized by coalescence due to insufficient interfacial charge. PMID:26304319

  3. Optimization of ultrasonic emulsification conditions for the production of orange peel essential oil nanoemulsions.

    PubMed

    Hashtjin, Adel Mirmajidi; Abbasi, Soleiman

    2015-05-01

    The aim of the present study was to investigate the influence of emulsifying conditions on some physical and rheological properties of orange peel essential oil (OPEO) in water nanoemulsions. In this regard, using the response surface methodology, the influence of ultrasonication conditions including sonication amplitude (70-100 %), sonication time (90-150 s) and process temperature (5-45 °C) on the mean droplets diameter (Z-average value), polydispersity index (PDI), and viscosity of the OPEO nanoemulsions was evaluated. In addition, the flow behavior and stability of selected nanoemulsions was evaluated during storage (up to 3 months) at different temperatures (5, 25 and 45 °C). Based on the results of the optimization, the optimum conditions for producing OPEO nanoemulsions (Z-average value 18.16 nm) were determined as 94 % (sonication amplitude), 138 s (sonication time) and 37 °C (process temperature). Moreover, analysis of variance (ANOVA) showed high coefficients of determination values (R (2) > 0.95) for the response surface models of the energy input and Z-average. In addition, the flow behavior of produced nanoemulsions was Newtonian, and the effect of time and storage temperature as well as their interactions on the Z-average value was highly significant (P < 0.0001). PMID:25892765

  4. Pareidolia in Neuroendocrinology: A Pituitary Macroadenoma Resembling "Big Bird".

    PubMed

    de Herder, Wouter W

    2016-04-01

    The MRI picture of a pituitary macroadenoma with supra- and perisellar expansion resembled a famous character from a children's television series demonstrating that pareidolia is also observed in neuro-endocrinology and -radiology. PMID:26812692

  5. Pareidolia in Neuroendocrinology: A Pituitary Macroadenoma Resembling "Big Bird".

    PubMed

    de Herder, Wouter W

    2016-04-01

    The MRI picture of a pituitary macroadenoma with supra- and perisellar expansion resembled a famous character from a children's television series demonstrating that pareidolia is also observed in neuro-endocrinology and -radiology.

  6. Nanoemulsion of D-limonene in water system prepared by ultrasonic emulsification.

    PubMed

    Lu, Wen-Chien; Zhang, Ting-Jie; Huang, Da-Wei; Li, Po-Hsien

    2014-01-01

    D-Limonene is a component of essential oil extracted from citrus fruits. This component has shown chemopreventive and therapeutic activity against a wide variety of experimental tumors, but D-limonene is unstable and lose its lemon-like flavor under normal storage condition, and it is almost insoluble in water. Therefore, studying the formation of nanoemulsion in D-limonene in water system is probably a good method to prevent the oxidation degradation of D-limonene. For the purpose of our study, we used mixed surfactant to form D- limonene-in-water emulsion, and found the best formula for forming nanoemulsion droplets with specified hydrophilic-lipophilic balance (HLB) value and droplet size. The results demonstrated that nanoemulsion droplets formed at So ratio of 0.4 and applied power of 18 W for 120 s under mixed surfactant at HLB values 12 and had droplet size of 20-50 nm. PMID:25423744

  7. Argan oil nanoemulsions as new hydrophobic drug-loaded delivery system for transdermal application.

    PubMed

    Lococo, D; Mora-Huertas, C E; Fessi, H; Zaanoun, I; Elaissari, A

    2012-10-01

    This research work deals with the development of argan oil-based nanoemulsions as vehicle of hydrophobic drugs such as diclofenac used as model. Nanoemulsions of oil in water were prepared using the ultrasonication method in order to obtain submicron size colloidal dispersion. The size, zeta potential and encapsulation efficiency of the dispersions obtained were investigated. In addition, the ability of sorbitan ester derivatives to form nanovesicles (niosomes), which in turn were used for encapsulating drug in oily solutions forming stable nanoemulsions, was particularly examined. Thus, additional stabilizing agents were not required in the recipe and formulations using only sorbitan monolaurate, argan oil and water lead to attractive results. Their submicronic size (<250 nm), high negative zeta potential (between -40 and -50 mV) and drug-encapsulation efficiency (higher than 85%) allow predicting both a good physical stability and a good performance as drug carriers.

  8. Nanoemulsion of D-limonene in water system prepared by ultrasonic emulsification.

    PubMed

    Lu, Wen-Chien; Zhang, Ting-Jie; Huang, Da-Wei; Li, Po-Hsien

    2014-01-01

    D-Limonene is a component of essential oil extracted from citrus fruits. This component has shown chemopreventive and therapeutic activity against a wide variety of experimental tumors, but D-limonene is unstable and lose its lemon-like flavor under normal storage condition, and it is almost insoluble in water. Therefore, studying the formation of nanoemulsion in D-limonene in water system is probably a good method to prevent the oxidation degradation of D-limonene. For the purpose of our study, we used mixed surfactant to form D- limonene-in-water emulsion, and found the best formula for forming nanoemulsion droplets with specified hydrophilic-lipophilic balance (HLB) value and droplet size. The results demonstrated that nanoemulsion droplets formed at So ratio of 0.4 and applied power of 18 W for 120 s under mixed surfactant at HLB values 12 and had droplet size of 20-50 nm.

  9. Evaluation of a Nanoemulsion Formulation Strategy for Oral Bioavailability Enhancement of Danazol in Rats and Dogs

    PubMed Central

    Devalapally, Harikrishna; Silchenko, Svitlana; Zhou, Feng; McDade, Jessica; Goloverda, Galina; Owen, Albert; Hidalgo, Ismael J.

    2013-01-01

    The objective of this study was to determine whether nanoemulsion formulations constitute a viable strategy to improve the oral bioavailability of danazol, a compound whose poor aqueous solubility limits its oral bioavailability. Danazol-containing oil-in-water nanoemulsions (NE) with and without co-surfactants stearylamine (SA) and deoxycholic acid (DCA) were prepared and characterized. Nanoemulsion droplets size ranging from 238 to 344 nm and with surface charges of −24.8 mV (NE), −26.5 mV (NE-DCA), and +27.8 mV (NE-SA) were reproducibly obtained. Oral bioavailability of danazol in nanoemulsions was compared with other vehicles such as, PEG400, 1% methylcellulose in water (1% MC), Labrafil, and a Labrafil/Tween 80 (9:1) mixture, after intragastric administration to rats and after oral administration of NE-SA, a Labrafil solution, or a Danocrine® tablet to dogs. The absolute bioavailability of danazol was 0.6% (PEG400), 1.2% (1% MC), 6.0% (Labrafil), 7.5% (Labrafil/Tween80), 8.1% (NE-DCA), 14.8% (NE), and 17.4% (NE-SA) in rats, and 0.24% (Danocrine), 6.2% (Labrafil), and 58.7% (NE-SA) in dogs. Overall, danazol bioavailability in any nanoemulsion was higher than any other formulation. Danazol bioavailability from NE and NE-SA was 1.8 to 2.2-fold higher than NE-DCA nanoemulsion and could be due to significant difference in droplet size. PMID:23878097

  10. Preparation, Characterization and Stability Study of Dutasteride Loaded Nanoemulsion for Treatment of Benign Prostatic Hypertrophy

    PubMed Central

    Ali, Mohammad Sajid; Alam, Mohammad Sarfaraz; Alam, Nawazish; Siddiqui, Masoom Raza

    2014-01-01

    Benign prostatic hyperplasia (BPH)is the most common condition in aging men, associated with lower urinary tract symptoms. It is caused due to the augmented levels of the androgen dihydrotestosterone. Dutasteride, a 5α-Reductase inhibitor has been recommended for the treatment of BPH upon oral administration. However, long term oral administration of dutasteride may cause sexual problem in man. Therefore the main objective of this study was to develop transdermal patch having nanoemulsion gel of dutasteride in order to enhance physical and chemical stability and eliminate adverse effect of dutasteride. Optimized nanoemulsion was prepared by aqueous phase-titration method and characterized by droplet size, viscosity and refractive index. In-vitro skin permeation of dutasteride through rat abdominal skin was determined by the Franz diffusion cell.Significant increase in the steady state flux (Jss), permeability coefficient (Kp) and enhancement ratio (Er) was observed in optimized nanoemulsion formulation A1 (p < 0.05). The Er of optimized nanoemulsion A1 was found to be 1.52 times with respect to control which indicates transdermal delivery may be better approach for BPH. Stability studies were performed for the period of 3 months. It was found that droplet size, viscosity and refractive index were slightly increased at refrigerator and room temperature in 3 months period. However, the changes in these parameters were not statistically significant (p ≥ 0.05). The shelf-life of optimized nanoemulsion A1 was found to be 2.18 years at room temperature. These results indicated that both physical as well as chemical stability of dutasteride in nanoemulsion formulation. PMID:25587300

  11. Preparation, characterization and stability study of dutasteride loaded nanoemulsion for treatment of benign prostatic hypertrophy.

    PubMed

    Ali, Mohammad Sajid; Alam, Mohammad Sarfaraz; Alam, Nawazish; Siddiqui, Masoom Raza

    2014-01-01

    Benign prostatic hyperplasia (BPH)is the most common condition in aging men, associated with lower urinary tract symptoms. It is caused due to the augmented levels of the androgen dihydrotestosterone. Dutasteride, a 5α-Reductase inhibitor has been recommended for the treatment of BPH upon oral administration. However, long term oral administration of dutasteride may cause sexual problem in man. Therefore the main objective of this study was to develop transdermal patch having nanoemulsion gel of dutasteride in order to enhance physical and chemical stability and eliminate adverse effect of dutasteride. Optimized nanoemulsion was prepared by aqueous phase-titration method and characterized by droplet size, viscosity and refractive index. In-vitro skin permeation of dutasteride through rat abdominal skin was determined by the Franz diffusion cell.Significant increase in the steady state flux (J ss), permeability coefficient (K p) and enhancement ratio (E r) was observed in optimized nanoemulsion formulation A1 (p < 0.05). The Er of optimized nanoemulsion A1 was found to be 1.52 times with respect to control which indicates transdermal delivery may be better approach for BPH. Stability studies were performed for the period of 3 months. It was found that droplet size, viscosity and refractive index were slightly increased at refrigerator and room temperature in 3 months period. However, the changes in these parameters were not statistically significant (p ≥ 0.05). The shelf-life of optimized nanoemulsion A1 was found to be 2.18 years at room temperature. These results indicated that both physical as well as chemical stability of dutasteride in nanoemulsion formulation. PMID:25587300

  12. Ostwald Ripening Stability of Curcumin-Loaded MCT Nanoemulsion: Influence of Various Emulsifiers

    PubMed Central

    Kim, Sun-Hyung; Ji, Yeun-Sun; Lee, Eui-Seok; Hong, Soon-Taek

    2016-01-01

    Curcumin is a flavonoid found in the rhizome of the turmeric plant (Curcuma longa L.) and has recently attracted interest because it has numerous biological functions and therapeutic properties. In the present study, we attempted to incorporate curcumin into medium-chain triglyceride (MCT) nanoemulsions (0.15 wt% curcumin, 10 wt% MCT oil, and 10 wt% emulsifiers) with various emulsifiers [polyoxyethylene (20) sorbitan monolaurate (Tween-20), sorbitan monooleate (SM), and soy lecithin (SL)]. The physicochemical properties of the nanoemulsions including the Ostwald ripening stability were investigated. The initial droplet size was found to be 89.08 nm for the nanoemulsion with 10 wt% Tween-20 (control), and when Tween-20 was partially replaced with SM and SL, the size decreased: 73.43 nm with 4 wt% SM+6 wt% Tween-20 and 67.68 nm with 4 wt% SL+6 wt% Tween-20 (prepared at 15,000 psi). When the nanoemulsions were stored for 28 days at room temperature, the droplet size increased as the storage time increased. The largest increase was observed for the control nanoemulsion, followed by the 4 wt% SL+6 wt% Tween-20 and 4 wt% SM+6 wt% Tween-20 systems. The Turbiscan dispersion stability results strongly supported the relationship between droplet size and storage time. The time-dependent increase in droplet size was attributed to the Ostwald ripening phenomenon. Thus, the Ostwald ripening stability of curcumin-loaded MCT nanoemulsions with Tween-20 was considerably improved by partially replacing the Tween-20 with SM or SL. In addition, curcumin may have acted as an Ostwald ripening inhibitor. PMID:27752506

  13. Tunable stability of monodisperse secondary O/W nano-emulsions

    NASA Astrophysics Data System (ADS)

    Vecchione, R.; Ciotola, U.; Sagliano, A.; Bianchini, P.; Diaspro, A.; Netti, P. A.

    2014-07-01

    Stable and biodegradable oil in water (O/W) nano-emulsions can have a huge impact on a wide range of bio-applications, from food to cosmetics and pharmaceuticals. Emulsions, however, are immiscible systems unstable over time; polymer coatings are known to be helpful, but an effective procedure to stabilize monodisperse and biodegradable O/W nano-emulsions is yet to be designed. Here, we coat biodegradable O/W nano-emulsions with a molecular layer of biodegradable polyelectrolytes such as polysaccharides - like chitosan - and polypeptides - like polylysine - and effectively re-disperse and densify the polymer coating at high pressure, thus obtaining monodisperse and stable systems. In particular, focusing on chitosan, our tests show that it is possible to obtain unprecedented ultra-stable O/W secondary nano-emulsions (diameter sizes tunable from ~80 to 160 nm and polydispersion indices below 0.1) by combining this process with high concentrations of polymers. Depending on the polymer concentration, it is possible to control the level of coating that results in a tunable stability ranging from a few weeks to several months. The above range of concentrations has been investigated using a fluorescence-based approach with new insights into the coating evolution.Stable and biodegradable oil in water (O/W) nano-emulsions can have a huge impact on a wide range of bio-applications, from food to cosmetics and pharmaceuticals. Emulsions, however, are immiscible systems unstable over time; polymer coatings are known to be helpful, but an effective procedure to stabilize monodisperse and biodegradable O/W nano-emulsions is yet to be designed. Here, we coat biodegradable O/W nano-emulsions with a molecular layer of biodegradable polyelectrolytes such as polysaccharides - like chitosan - and polypeptides - like polylysine - and effectively re-disperse and densify the polymer coating at high pressure, thus obtaining monodisperse and stable systems. In particular, focusing on

  14. Irreversible shear-induced vitrification of droplets into elastic nanoemulsions by extreme rupturing

    SciTech Connect

    Wilking, James N.; Mason, Thomas G.

    2007-04-15

    Many materials weaken through fracturing when subjected to extreme stresses. By contrast, we show that breaking down repulsive bits of matter dispersed in a viscous liquid can cause a dramatic and irreversible increase in the dispersion's elasticity. Anionically stabilized microscale emulsions subjected to a history of high-pressure microfluidic flow can develop an unusually large elastic modulus as droplets are ruptured to the nanoscale, yielding 'nanonaise'. As the droplet size approaches the Debye screening length, the nanoemulsion vitrifies. Consequently, the onset of elasticity for disordered uniform nanoemulsions can occur at droplet volume fractions far below maximal random jamming of spheres.

  15. Nanoemulsion of ethanolic extracts of propolis and its antioxidant activity

    NASA Astrophysics Data System (ADS)

    Mauludin, R.; Primaviri, D. S.; Fidrianny, I.

    2015-09-01

    Propolis contains several antioxidant compounds which can be used in topical application to protect skin against free radical and prevent skin cancer and skin aging. Ethanolic extracts of propolis (EEP) provided the greatest antioxidant activity but has very small solubility in water thus was prepared in nanoemulsion (NE). EEP contains steroid/triterpenoid, flavonoid, and saponin. EEP had the value of DPPH scavenging activity 61.14% and IC50 0.41629 ppm. The best NE formulation consisted of 26.25% Kolliphor RH40; 8.75% glycerin; 5% rice bran oil; and 3% EEP. NE was transparent, had particle size of 23.72 nm and polydispersity index of 0.338. Based on TEM morphology, NE was almost spherical and has particle size below 50 nm. NE propolis revealed to be physically stable after stability test within 63 days at 25°C and passed 6 cycles of Freeze and Thaw test without separated. NE propolis reduced around 58% of free radical DPPH similar to antioxidant activity of the original extracts. Antioxidant activity of NE propolis is relatively stable after stored for 6 weeks. NE propolis was proven to be safe by primary irritation test with the value of primary irritation index (OECD) was 0.

  16. Eucalyptus oil nanoemulsion-impregnated chitosan film: antibacterial effects against a clinical pathogen, Staphylococcus aureus, in vitro.

    PubMed

    Sugumar, Saranya; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2015-01-01

    Eucalyptus oil (Eucalyptus globulus) nanoemulsion was formulated using low-and high-energy emulsification methods. Development of nanoemulsion was optimized for system parameters such as emulsifier type, emulsifier concentration, and emulsification methods to obtain a lower droplet size with greater stability. The minimized droplet diameter was achieved using the high-energy method of ultrasonication. Tween 80 was more effective in reducing droplet size and emulsion appearance when compared to Tween 20. Stable nanoemulsion was formulated with Tween 80 as a surfactant, and the particle size was found to be 9.4 nm (1:2 v/v). The eucalyptus oil nanoemulsion was impregnated into chitosan (1%) as a biopolymer in varying concentrations. Further, the film was characterized by moisture content, microscopic study, X-ray diffraction, and Fourier transform infrared spectroscopy. Also, the film with and without nanoemulsion was evaluated against Staphylococcus aureus. The nanoemulsion-impregnated chitosan film showed higher antibacterial activity than chitosan film. These results support the inclusion of nanoemulsion-impregnated chitosan film in wound management studies.

  17. Eucalyptus oil nanoemulsion-impregnated chitosan film: antibacterial effects against a clinical pathogen, Staphylococcus aureus, in vitro

    PubMed Central

    Sugumar, Saranya; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2015-01-01

    Eucalyptus oil (Eucalyptus globulus) nanoemulsion was formulated using low-and high-energy emulsification methods. Development of nanoemulsion was optimized for system parameters such as emulsifier type, emulsifier concentration, and emulsification methods to obtain a lower droplet size with greater stability. The minimized droplet diameter was achieved using the high-energy method of ultrasonication. Tween 80 was more effective in reducing droplet size and emulsion appearance when compared to Tween 20. Stable nanoemulsion was formulated with Tween 80 as a surfactant, and the particle size was found to be 9.4 nm (1:2 v/v). The eucalyptus oil nanoemulsion was impregnated into chitosan (1%) as a biopolymer in varying concentrations. Further, the film was characterized by moisture content, microscopic study, X-ray diffraction, and Fourier transform infrared spectroscopy. Also, the film with and without nanoemulsion was evaluated against Staphylococcus aureus. The nanoemulsion-impregnated chitosan film showed higher antibacterial activity than chitosan film. These results support the inclusion of nanoemulsion-impregnated chitosan film in wound management studies. PMID:26491308

  18. Multimodal Perfluorocarbon Nanoemulsions for 19F MRI, Ultrasonography, and Catalysis of MRgFUS-Mediated Drug Delivery

    NASA Astrophysics Data System (ADS)

    Rapoport, N.; Nam, K.-H.; Christensen, D. A.; Kennedy, A. M.; Parker, D. L.; Payne, A. H.; Todd, N.; Shea, J. E.; Scaife, C. L.

    2011-09-01

    Perfluorocarbon nanoemulsions can target lipophilic therapeutic agents to solid tumors and simultaneously provide for monitoring nanocarrier biodistribution via ultrasonography and/or 19F MRI. In the first generation of block copolymer stabilized perfluorocarbon nanoemulsions, perfluoropentane (PFP) was used as the droplet forming compound. Although manifesting excellent therapeutic and ultrasound imaging properties, PFP nanoemulsions were unstable at storage, difficult to handle, and underwent droplet-to-bubble transition upon injection that was hard to control. To solve the above problems, perfluoro-15-crown-5-ether (PFCE) was used as a core forming compound in the second generation of block copolymer stabilized perfluorocarbon nanoemulsions. In the present paper, acoustic, imaging, and therapeutic properties of unloaded and paclitaxel (PTX) loaded PFCE nanoemulsions are reported. The size of paclitaxel-loaded PFCE nanodroplets (300 nm to 500 nm depending on emulsification conditions) favors their passive accumulation in tumor tissue. PFCE nanodroplets manifest both ultrasound and 19F MR contrast properties, which allows the use of multimodal imaging to monitor nanodroplet biodistribution. Ultrasonography and 19F MRI produced consistent results on nanodroplet biodistribution. Sonication with 1-MHz therapeutic ultrasound triggered reversible droplet-to-bubble transition in PFCE nanoemulsions. Microbubbles formed by acoustic vaporization underwent stable cavitation. In a pilot study on ultrasound-mediated therapy of a large breast cancer tumor, paclitaxel-loaded PFCE nanoemulsions combined with 1-MHz ultrasound (MI≥1.75) showed excellent therapeutic properties. Anticipated mechanisms of the observed effects are discussed.

  19. Eucalyptus oil nanoemulsion-impregnated chitosan film: antibacterial effects against a clinical pathogen, Staphylococcus aureus, in vitro.

    PubMed

    Sugumar, Saranya; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2015-01-01

    Eucalyptus oil (Eucalyptus globulus) nanoemulsion was formulated using low-and high-energy emulsification methods. Development of nanoemulsion was optimized for system parameters such as emulsifier type, emulsifier concentration, and emulsification methods to obtain a lower droplet size with greater stability. The minimized droplet diameter was achieved using the high-energy method of ultrasonication. Tween 80 was more effective in reducing droplet size and emulsion appearance when compared to Tween 20. Stable nanoemulsion was formulated with Tween 80 as a surfactant, and the particle size was found to be 9.4 nm (1:2 v/v). The eucalyptus oil nanoemulsion was impregnated into chitosan (1%) as a biopolymer in varying concentrations. Further, the film was characterized by moisture content, microscopic study, X-ray diffraction, and Fourier transform infrared spectroscopy. Also, the film with and without nanoemulsion was evaluated against Staphylococcus aureus. The nanoemulsion-impregnated chitosan film showed higher antibacterial activity than chitosan film. These results support the inclusion of nanoemulsion-impregnated chitosan film in wound management studies. PMID:26491308

  20. Nanoemulsion as a carrier to improve the topical anti-inflammatory activity of stem bark extract of Rapanea ferruginea

    PubMed Central

    Dal Mas, Juarana; Zermiani, Tailyn; Thiesen, Liliani C; Silveira, Joana LM; da Silva, Kathryn ABS; de Souza, Márcia M; Malheiros, Angela; Bresolin, Tania MB; Lucinda-Silva, Ruth M

    2016-01-01

    The aim of this study was to develop nanoemulsion containing soft extract of stem bark of Rapanea ferruginea to improve the topical delivery and anti-inflammatory activity. The extract of R. ferruginea stem bark was incorporated into the oily phase of the nanoemulsion by the method of phase inversion at low energy. The developed nanoemulsion had an average droplet size of 47.88±8.20 nm and a polydispersibility index of 0.228. Uniformity of size, spherical shape of droplet, and absence of clusters were confirmed by transmission electronic microscopy. The zeta potential was −34.7±1.15 mV. The nanoemulsion showed a moderate degree of skin irritation in the agarose overlay assay in vitro. The content of the extract markers, myrsinoic acids A and B, was 54.10±0.08 and 53.03 μg/g in the formulation, respectively. The formulation demonstrated pseudoplastic and thixotropic rheological behavior. In vitro release of chemical markers was controlled by diffusion mechanism. An extract-loaded nanoemulsion showed a topical anti-inflammatory activity in a croton oil-induced edema ear model, with a decrease in tumor necrosis factor release and myeloperoxidase activity. The nanoemulsion was 160% more efficient than the conventional cream containing 0.13% of the extract. The nanoemulsion showed suitable properties as a carrier for topical use of R. ferruginea extract and the approach for improving the topical anti-inflammatory activity.

  1. Nanoemulsion as a carrier to improve the topical anti-inflammatory activity of stem bark extract of Rapanea ferruginea

    PubMed Central

    Dal Mas, Juarana; Zermiani, Tailyn; Thiesen, Liliani C; Silveira, Joana LM; da Silva, Kathryn ABS; de Souza, Márcia M; Malheiros, Angela; Bresolin, Tania MB; Lucinda-Silva, Ruth M

    2016-01-01

    The aim of this study was to develop nanoemulsion containing soft extract of stem bark of Rapanea ferruginea to improve the topical delivery and anti-inflammatory activity. The extract of R. ferruginea stem bark was incorporated into the oily phase of the nanoemulsion by the method of phase inversion at low energy. The developed nanoemulsion had an average droplet size of 47.88±8.20 nm and a polydispersibility index of 0.228. Uniformity of size, spherical shape of droplet, and absence of clusters were confirmed by transmission electronic microscopy. The zeta potential was −34.7±1.15 mV. The nanoemulsion showed a moderate degree of skin irritation in the agarose overlay assay in vitro. The content of the extract markers, myrsinoic acids A and B, was 54.10±0.08 and 53.03 μg/g in the formulation, respectively. The formulation demonstrated pseudoplastic and thixotropic rheological behavior. In vitro release of chemical markers was controlled by diffusion mechanism. An extract-loaded nanoemulsion showed a topical anti-inflammatory activity in a croton oil-induced edema ear model, with a decrease in tumor necrosis factor release and myeloperoxidase activity. The nanoemulsion was 160% more efficient than the conventional cream containing 0.13% of the extract. The nanoemulsion showed suitable properties as a carrier for topical use of R. ferruginea extract and the approach for improving the topical anti-inflammatory activity. PMID:27660442

  2. Evaluation of transdermal delivery of nanoemulsions in ex vivo porcine skin using two-photon microscopy and confocal laser-scanning microscopy

    NASA Astrophysics Data System (ADS)

    Choi, Sanghoon; Kim, Jin Woong; Lee, Yong Joong; Delmas, Thomas; Kim, Changhwan; Park, Soyeun; Lee, Ho

    2014-10-01

    This study experimentally evaluates the self-targeting ability of asiaticoside-loaded nanoemulsions compared with nontargeted nanoemulsions in ex vivo experiments with porcine skin samples. Homebuilt two-photon and confocal laser-scanning microscopes were employed to noninvasively examine the transdermal delivery of two distinct nanoemulsions. Prior to the application of nanoemulsions, we noninvasively observed the morphology of porcine skin using two-photon microscopy. We have successfully visualized the distributions of the targeted and nontargeted nanoemulsions absorbed into the porcine skin samples. Asiaticoside-loaded nanoemulsions showed an improved ex vivo transdermal delivery through the stratum corneum compared with nonloaded nanoemulsions. As a secondary measure, nanoemulsions-applied samples were sliced in the depth direction with a surgical knife in order to obtain the complete depth-direction distribution profile of Nile red fluorescence. XZ images demonstrated that asiaticoside-loaded nanoemulsion penetrated deeper into the skin compared with nontargeted nanoemulsions. The basal layer boundary is clearly visible in the case of the asiaticoside-loaded skin sample. These results reaffirm the feasibility of using self-targeting ligands to improve permeation through the skin barrier for cosmetics and topical drug applications.

  3. Intentions vs. resemblance: understanding pictures in typical development and autism.

    PubMed

    Hartley, Calum; Allen, Melissa L

    2014-04-01

    Research has debated whether children reflect on artists' intentions when comprehending pictures, or instead derive meaning entirely from resemblance. We explore these hypotheses by comparing how typically developing toddlers and low-functioning children with autism (a population impaired in intentional reasoning) interpret abstract pictures. In Experiment 1, both groups mapped familiar object names onto abstract pictures, however, they related the same representations to different 3-D referents. Toddlers linked abstract pictures with intended referents they did not resemble, while children with autism mapped picture-referent relations based on resemblance. Experiment 2 showed that toddlers do not rely upon linguistic cues to determine intended referential relations. Experiment 3 confirmed that the responding of children with autism was not due to perseveration or associative word learning, and also provided independent evidence of their intention-reading difficulties. We argue that typically developing children derive meaning from the social-communicative intentions underlying pictures when resemblance is an inadequate cue to meaning. By contrast, children with autism do not reflect on artists' intentions and simply relate pictures to whatever they happen to resemble.

  4. Analysis of anti-neoplastic drug in bacterial ghost matrix, w/o/w double nanoemulsion and w/o nanoemulsion by a validated 'green' liquid chromatographic method.

    PubMed

    Youssof, Abdullah M E; Salem-Bekhit, Mounir M; Shakeel, Faiyaz; Alanazi, Fars K; Haq, Nazrul

    2016-07-01

    The objective of the present investigation was to develop and validate a 'green' reversed phase high-performance liquid chromatography (RP-HPLC) method for rapid analysis of a cytotoxic drug 5-fluorouracil (5-FU) in bulk drug, marketed injection, water-in-oil (w/o) nanoemulsion, double water-in-oil-in-water (w/o/w) nanoemulsion and bacterial ghost (BG) matrix. The chromatography study was carried out at room temperature (25±1°C) using an HPLC system with the help of ultraviolet (UV)-visible detector. The chromatographic performance was achieved with a Nucleodur 150mm×4.6mm RP C8 column filled with 5µm filler as a static phase. The mobile phase consisted of ethyl acetate: methanol (7:3% v/v) which was delivered at a flow rate of 1.0mLmin(-1) and the drug was detected in UV mode at 254nm. The developed method was validated in terms of linearity (r(2)=0.998), accuracy (98.19-102.09%), precision (% RSD=0.58-1.17), robustness (% RSD=0.12-0.53) and sensitivity with satisfactory results. The efficiency of the method was demonstrated by the assay of the drug in marketed injection, w/o nanoemulsion, w/o/w nanoemulsion and BG with satisfactory results. The successful resolution of the drug along with its degradation products clearly established the stability-indicating nature of the proposed method. Overall, these results suggested that the proposed analytical method could be effectively applied to the routine analysis of 5-FU in bulk drug, various pharmaceutical dosage forms and BG.

  5. Analysis of anti-neoplastic drug in bacterial ghost matrix, w/o/w double nanoemulsion and w/o nanoemulsion by a validated 'green' liquid chromatographic method.

    PubMed

    Youssof, Abdullah M E; Salem-Bekhit, Mounir M; Shakeel, Faiyaz; Alanazi, Fars K; Haq, Nazrul

    2016-07-01

    The objective of the present investigation was to develop and validate a 'green' reversed phase high-performance liquid chromatography (RP-HPLC) method for rapid analysis of a cytotoxic drug 5-fluorouracil (5-FU) in bulk drug, marketed injection, water-in-oil (w/o) nanoemulsion, double water-in-oil-in-water (w/o/w) nanoemulsion and bacterial ghost (BG) matrix. The chromatography study was carried out at room temperature (25±1°C) using an HPLC system with the help of ultraviolet (UV)-visible detector. The chromatographic performance was achieved with a Nucleodur 150mm×4.6mm RP C8 column filled with 5µm filler as a static phase. The mobile phase consisted of ethyl acetate: methanol (7:3% v/v) which was delivered at a flow rate of 1.0mLmin(-1) and the drug was detected in UV mode at 254nm. The developed method was validated in terms of linearity (r(2)=0.998), accuracy (98.19-102.09%), precision (% RSD=0.58-1.17), robustness (% RSD=0.12-0.53) and sensitivity with satisfactory results. The efficiency of the method was demonstrated by the assay of the drug in marketed injection, w/o nanoemulsion, w/o/w nanoemulsion and BG with satisfactory results. The successful resolution of the drug along with its degradation products clearly established the stability-indicating nature of the proposed method. Overall, these results suggested that the proposed analytical method could be effectively applied to the routine analysis of 5-FU in bulk drug, various pharmaceutical dosage forms and BG. PMID:27154677

  6. Application of an oregano oil nanoemulsion to the control of foodborne bacteria on fresh lettuce.

    PubMed

    Bhargava, Kanika; Conti, Denise S; da Rocha, Sandro R P; Zhang, Yifan

    2015-05-01

    Although antimicrobial activities of plant essential oils are well documented, challenges remain as to their application in fresh produce due to the hydrophobic nature of essential oils. Oregano oil nanoemulsions were formulated with a food-grade emulsifier and evaluated for their efficacy in inactivating the growth of foodborne bacteria on fresh lettuce. Lettuce was artificially inoculated with Listeria monocytogenes, Salmonella Typhimurium and Escherichia coli O157:H7, followed by a one-minute dipping in oregano oil nanoemulsions (0.05% or 0.1%). Samples were stored at 4 °C and enumerated for bacteria at fixed intervals (0 h, 3 h, 24 h, and 72 h). Compared to control, 0.05% nanoemulsion showed an up to 3.44, 2.31, and 3.05 log CFU/g reductions in L. monocytogenes, S. Typhimurium, and E. coli O157:H7, respectively. Up to 3.57, 3.26, and 3.35 log CFU/g reductions were observed on the same bacteria by the 0.1% treatment. Scanning Electron Microscopy (SEM) demonstrated disrupted bacterial membranes due to the oregano oil treatment. The data suggest that applying oregano oil nanoemulsions to fresh produce may be an effective antimicrobial control strategy. PMID:25583339

  7. In Vitro Evaluation of Mucosa Permeation/Retention and Antiherpes Activity of Genistein from Cationic Nanoemulsions.

    PubMed

    Argenta, D F; Bidone, J; Misturini, F D; Koester, L S; Bassani, V L; Simbes, C M; Teixeira, H F

    2016-02-01

    In this report, we described the genistein distribution on excised porcine esophageal mucosa from cationic nanoemulsions, as well as the anti-HSV-1 activity against a viral strain resistant to acyclovir. Genistein-loaded cationic nanoemulsions were prepared by spontaneous emulsification. This procedure yielded monodisperse nanoemulsions exhibiting a mean droplet size of approximately 200-300 nm. Hydroxyethyl cellulose (HEC) was added at the end of the manufacturing process as a thickening agent (at 3%). Such formulations exhibit a non-Newtonian pseudoplastic behavior. The addition of HEC significantly reduces the genistein flux through excised porcine mucosa specimens as compared with values elicited by nanoemulsions before thickening. Furthermore, a significant increase of genistein retention in mucosa was observed as compared to the genistein propylene glycol solution, as illustrated by confocal fluorescence microscopy images. Formulations exhibited antiherpetic activity in vitro against HSV-1 (strain 29R). Taken together, these results suggest that these formulations have promising potential to be used topically for herpes infections. PMID:27433578

  8. The application of nanoemulsions with different orange oil concentrations to remediate crude oil-contaminated soil.

    PubMed

    Oliveira, Priscila F; Spinelli, Luciana S; Mansur, Claudia R E

    2012-05-01

    The petroleum industry stands out for causing significant environmental risks from contamination of the air, water and soil. The removal of organic pollutants from the environment poses a great technological challenge, making it increasingly necessary to develop efficient clean-up technologies. Surfactant solutions have been used to remediate soils and aquifers contaminated by hydrocarbons or crude oil derivatives. The aim of this study was to develop nanoemulsions and analyze their efficiency in extracting crude oil from a sand sample. The nanoemulsions were prepared by the phase inversion temperature (PIT) method. The oil phase consisted of orange oil and the nonionic surfactant ethoxylated lauryl ether (Ultrol L70) was used to stabilize the nanoemulsions. The surfactant concentrations were varied from 10 to 12 wt% and the oil phase from 5 to 20 wt%. The efficiency of extraction of oil from sand was assessed using the two nanoemulsions that presented the greatest stability (containing 5 wt% oil phase with 12 wt% surfactant and 20 wt% oil phase with 10 wt% surfactant). A 2(3) factorial experimental design with center point was used to evaluate and improve the soil washing process, varying the time, temperature and agitation speed of the system. The highest efficiencies were obtained at 45 degrees C.

  9. Physico-chemical characterization of nano-emulsions in cosmetic matrix enriched on omega-3

    PubMed Central

    2011-01-01

    Background Nano-emulsions, as non-equilibrium systems, present characteristics and properties which depend not only on composition but also on their method of preparation. To obtain better penetration, nanocosmeceuticals use nano-sized systems for the delivery of active ingredients to targeted cells. In this work, nano-emulsions composed of miglyol, rapeseed oil and salmon oil were developed as a cosmetic matrix. Measurements of different physico-chemical properties of nano-emulsions were taken according to size, electrophoretic mobility, conductivity, viscosity, turbidity, cristallization and melting point. The RHLB was calculated for each formulation in order to achieve maximum stability. Results Both tween 80 and soya lecithin were found to stabilize formulations. The results showed that rapeseed oil and miglyol are the predominant parameters for determining the expression of results concerning the characterization of emulsion. Based on the mixture design, we achieved the optimal point using the following formulation: 56.5% rapessed oil, 35.5% miglyol, and 8% salmon oil. We considered this formulation to be the best as a nanocosmeceutical product due to the small size, good turbidity, and average HLB. Conclusions This study demonstrates the influence of formulation on the physico-chemical properties of each nano-emulsion obtained by the mixture design. PMID:21936893

  10. Benefits of cetalkonium chloride cationic oil-in-water nanoemulsions for topical ophthalmic drug delivery

    PubMed Central

    Daull, Philippe; Lallemand, Frédéric; Garrigue, Jean-Sébastien

    2014-01-01

    Objectives Topical ocular administration is the most convenient route of administration of drugs for the treatment of eye diseases. However, the bioavailability of drugs following eye instillations of eye drops is very low. Over the past 20 years, extensive efforts have been put into research to improve drug bioavailability without compromising treatment compliance and patients' quality of life. Key findings One of the most efficient ways to improve drug bioavailability is to increase the precorneal residence time of the eye drop formulations. As a result, new eye drops, with bioadhesive properties, have been developed based on the cationic oil-in-water (o/w) nanoemulsion technology. These low viscosity eye drop nanoemulsions have improved precorneal residence time through the electrostatic interactions between the positively charged oil nanodroplets and the negatively charged ocular surface epithelium. Summary This review is the first to present the benefits of this new strategy used to improve ocular drug bioavailability. The roles of the cationic agent in the stabilization of a safe cationic o/w nanoemulsion have been discussed, as well as the unexpected benefits of the cationic o/w nanoemulsion for the protection and restoration of a healthy tear film and corneal epithelium. PMID:24001405

  11. Tunable stability of monodisperse secondary O/W nano-emulsions.

    PubMed

    Vecchione, R; Ciotola, U; Sagliano, A; Bianchini, P; Diaspro, A; Netti, P A

    2014-08-01

    Stable and biodegradable oil in water (O/W) nano-emulsions can have a huge impact on a wide range of bio-applications, from food to cosmetics and pharmaceuticals. Emulsions, however, are immiscible systems unstable over time; polymer coatings are known to be helpful, but an effective procedure to stabilize monodisperse and biodegradable O/W nano-emulsions is yet to be designed. Here, we coat biodegradable O/W nano-emulsions with a molecular layer of biodegradable polyelectrolytes such as polysaccharides--like chitosan--and polypeptides--like polylysine--and effectively re-disperse and densify the polymer coating at high pressure, thus obtaining monodisperse and stable systems. In particular, focusing on chitosan, our tests show that it is possible to obtain unprecedented ultra-stable O/W secondary nano-emulsions (diameter sizes tunable from ∼ 80 to 160 nm and polydispersion indices below 0.1) by combining this process with high concentrations of polymers. Depending on the polymer concentration, it is possible to control the level of coating that results in a tunable stability ranging from a few weeks to several months. The above range of concentrations has been investigated using a fluorescence-based approach with new insights into the coating evolution.

  12. Bactericidal action mechanism of negatively charged food grade clove oil nanoemulsions.

    PubMed

    Majeed, Hamid; Liu, Fei; Hategekimana, Joseph; Sharif, Hafiz Rizwan; Qi, Jing; Ali, Barkat; Bian, Yuan-Yuan; Ma, Jianguo; Yokoyama, Wallace; Zhong, Fang

    2016-04-15

    Clove oil (CO) anionic nanoemulsions were prepared with varying ratios of CO to canola oil (CA), emulsified and stabilized with purity gum ultra (PGU), a newly developed succinylated waxy maize starch. Interfacial tension measurements showed that CO acted as a co-surfactant and there was a gradual decrease in interfacial tension which favored the formation of small droplet sizes on homogenization until a critical limit (5:5% v/v CO:CA) was reached. Antimicrobial activity of the negatively charged CO nanoemulsion was determined against Gram positive GPB (Listeria monocytogenes and Staphylococcus aureus) and Gram negative GNB (Escherichia coli) bacterial strains using minimum inhibitory concentration (MIC) and a time kill dynamic method. Negatively charged PGU emulsified CO nanoemulsion showed prolonged antibacterial activities against Gram positive bacterial strains. We concluded that negatively charged CO nanoemulsion droplets self-assemble with GPB cell membrane, and facilitated interaction with cellular components of bacteria. Moreover, no electrostatic interaction existed between negatively charged droplets and the GPB membrane. PMID:26616926

  13. Bactericidal action mechanism of negatively charged food grade clove oil nanoemulsions.

    PubMed

    Majeed, Hamid; Liu, Fei; Hategekimana, Joseph; Sharif, Hafiz Rizwan; Qi, Jing; Ali, Barkat; Bian, Yuan-Yuan; Ma, Jianguo; Yokoyama, Wallace; Zhong, Fang

    2016-04-15

    Clove oil (CO) anionic nanoemulsions were prepared with varying ratios of CO to canola oil (CA), emulsified and stabilized with purity gum ultra (PGU), a newly developed succinylated waxy maize starch. Interfacial tension measurements showed that CO acted as a co-surfactant and there was a gradual decrease in interfacial tension which favored the formation of small droplet sizes on homogenization until a critical limit (5:5% v/v CO:CA) was reached. Antimicrobial activity of the negatively charged CO nanoemulsion was determined against Gram positive GPB (Listeria monocytogenes and Staphylococcus aureus) and Gram negative GNB (Escherichia coli) bacterial strains using minimum inhibitory concentration (MIC) and a time kill dynamic method. Negatively charged PGU emulsified CO nanoemulsion showed prolonged antibacterial activities against Gram positive bacterial strains. We concluded that negatively charged CO nanoemulsion droplets self-assemble with GPB cell membrane, and facilitated interaction with cellular components of bacteria. Moreover, no electrostatic interaction existed between negatively charged droplets and the GPB membrane.

  14. Skin permeation of D-limonene-based nanoemulsions as a transdermal carrier prepared by ultrasonic emulsification.

    PubMed

    Lu, Wen-Chien; Chiang, Been-Huang; Huang, Da-Wei; Li, Po-Hsien

    2014-03-01

    Nanoemulsions can be used for transporting pharmaceutical phytochemicals in skin-care products because of their stability and rapid permeation properties. However, droplet size may be a critical factor aiding permeation through skin and transdermal delivery efficiency. We prepared D-limonene nanoemulsions with various droplet sizes by ultrasonic emulsification using mixed surfactants of sorbitane trioleate and polyoxyethylene (20) oleyl ether under different hydrophilic-lipophilic balance (HLB) values. Droplet size decreased with increasing HLB value. With HLB 12, the droplet size was 23 nm, and the encapsulated ratio peaked at 92.3%. Transmission electron microscopy revealed spherical droplets and the gray parts were D-limonene precipitation incorporated in spherical droplets of the emulsion system. Franz diffusion cell was used to evaluate the permeation of D-limonene nanoemulsion through rat abdominal skin; the permeation rate depended on droplet size. The emulsion with the lowest droplet size (54 nm) achieved the maximum permeation rate. The concentration of D-limonene in the skin was 40.11 μL/cm(2) at the end of 360 min. Histopathology revealed no distinct voids or empty spaces in the epidermal region of permeated rat skin, so the D-limonene nanoemulsion may be a safe carrier for transdermal drug delivery.

  15. Optimization of curcumin nanoemulsion for intranasal delivery using design of experiment and its toxicity assessment.

    PubMed

    Sood, Sumeet; Jain, Kunal; Gowthamarajan, K

    2014-01-01

    The objective of the study was to optimize curcumin nanoemulsion for intranasal delivery using design of experiment. Box-Behnken design was constructed using oil, surfactant and co-surfactant concentration as independent variables and their affect on response y1 (globule size) and y2 (zeta potential) were studied. The ANOVA test identified the significant factors that affected the responses. For globule size, percentage of oil, surfactant and co-surfactant were identified as significant model terms whereas for zeta potential, oil and co-surfactant were found to be significant. Critical factors affecting the responses were identified using perturbation and contour plots. The derived polynomial equation and contour graph aid in predicting the values of selected independent variables for preparation of optimum nanoemulsion with desired properties. Further, 2(4) factorial design was used to study influence of chitosan on particle size and zeta potential. The formulations were subjected to in vitro cytotoxicity using SK-N-SH cell line and nasal ciliotoxicity studies. The developed formulations did not show any toxicity and were safe for intranasal delivery for brain targeting. In vitro diffusion studies revealed that nanoemulsions had a significantly higher release compared to drug solution. Ex vivo diffusion studies were carried out using sheep nasal mucosa fixed onto Franz diffusion cells. Mucoadhesive nanoemulsion showed higher flux and permeation across sheep nasal mucosa.

  16. Preparation and in vitro/ex vivo evaluation of nanoemulsion for transnasal delivery of paliperidone

    NASA Astrophysics Data System (ADS)

    Patel, Mrunali R.; Patel, Mitali H.; Patel, Rashmin B.

    2016-03-01

    Paliperidone was formulated in mucoadhesive nanoemulsion with the aim of improving its solubility and transnasal delivery, which can further utilized for its preclinical evaluation. Solubility of Paliperidone in oils, emulsifiers, co-emulsifiers was determined to identify nanoemulsion components. Emulsifier and co-emulsifiers were screened for their ability to emulsify selected oily phase. Phase diagrams were constructed to identify the area of nanoemulsification. Paliperidone nanoemulsion was formulated using spontaneous nanoemulsification method. The three nanoemulsions (PMNE4, PMNE5, and PMNE6) containing 5.71-6.80 % oleic acid as an oily phase, 47.62-51.63 % labrasol and plurol oleique CC 497 as emulsifier mixture (1:1), 42.86-45.58 % (wt/wt) aqueous phase having a suitable optical transparency of 98.33-99.33 %, globule size of 28.8-43.2 nm and polydispersity of 0.129-0.152 were selected for the incorporation of mucoadhesive polymer. The PMNE6 showed highest flux (5.072 ± 0.13 µg/cm2/min) with enhancement ratio of 1.1 as compared to Paliperidone solution (PS). The diffusion co-efficient of PMNE6 was significantly higher than PMNE5, PMNE4 and PS and followed higuchi model. The formulation was found to be free from nasal cilio toxicity. All formulations were found to be stable for 6 months at room temperature.

  17. Near infrared light absorption in magnetic nanoemulsion under external magnetic field

    NASA Astrophysics Data System (ADS)

    Brojabasi, Surajit; Mahendran, V.; Lahiri, B. B.; Philip, John

    2014-07-01

    We study the magnetic field dependent near infrared photon absorption behavior in a magnetically polarizable oil-in-water emulsion of droplet radius ~110 nm. The absorption of near infrared photons in magnetic nanoemulsion is found to be dependent on the volume fraction and applied magnetic field, which is attributed to the variation in the Mie absorption efficiency during the structural transitions of nanoemulsion droplets in dispersion. Also, the absorption linearly increases with incident near infrared photon energy up to certain external magnetic field. The imaginary part of the refractive index (k1) of magnetic nanoemulsion obtained from the near infrared absorption profile in the Rayleigh regime is found to vary with external magnetic field and the sample volume fraction (ϕ). The measured k1 follows a power law increment with sample volume fraction (k1~ϕ, where p is the exponent). The exponent (p) decreases with external magnetic field implying that the structural transition of nanoemulsion droplets increases k1. After a critical magnetic field (beyond Rayleigh regime), field induced absorption of near infrared photons decreases because of the increase in the aspect ratio of the chain like aggregates and interchain spacing which in turn reduces the Mie absorption efficiency.

  18. Application of an oregano oil nanoemulsion to the control of foodborne bacteria on fresh lettuce.

    PubMed

    Bhargava, Kanika; Conti, Denise S; da Rocha, Sandro R P; Zhang, Yifan

    2015-05-01

    Although antimicrobial activities of plant essential oils are well documented, challenges remain as to their application in fresh produce due to the hydrophobic nature of essential oils. Oregano oil nanoemulsions were formulated with a food-grade emulsifier and evaluated for their efficacy in inactivating the growth of foodborne bacteria on fresh lettuce. Lettuce was artificially inoculated with Listeria monocytogenes, Salmonella Typhimurium and Escherichia coli O157:H7, followed by a one-minute dipping in oregano oil nanoemulsions (0.05% or 0.1%). Samples were stored at 4 °C and enumerated for bacteria at fixed intervals (0 h, 3 h, 24 h, and 72 h). Compared to control, 0.05% nanoemulsion showed an up to 3.44, 2.31, and 3.05 log CFU/g reductions in L. monocytogenes, S. Typhimurium, and E. coli O157:H7, respectively. Up to 3.57, 3.26, and 3.35 log CFU/g reductions were observed on the same bacteria by the 0.1% treatment. Scanning Electron Microscopy (SEM) demonstrated disrupted bacterial membranes due to the oregano oil treatment. The data suggest that applying oregano oil nanoemulsions to fresh produce may be an effective antimicrobial control strategy.

  19. Eugenol oil nanoemulsion: antifungal activity against Fusarium oxysporum f. sp. vasinfectum and phytotoxicity on cottonseeds

    NASA Astrophysics Data System (ADS)

    Abd-Elsalam, Kamel A.; Khokhlov, Alexei R.

    2015-02-01

    The current research deals with the formulation and characterization of bio-based oil-in-water nanoemulsion. The formulated eugenol oil nanoemulsion was characterized by dynamic light scattering, stability test, transmission electron microscopy and thin layer chromatography. The nanoemulsion droplets were found to have a Z-average diameter of 80 nm and TEM study reveals the spherical shape of eugenol oil nanoemulsion (EON). The size of the nanoemulsion was found to be physically stable up to more than 1-month when it was kept at room temperature (25 °C). The TEM micrograph showed that the EON was spherical in shape and moderately mono or di-dispersed and was in the range of 50-110 nm. Three concentrations of the nanoformulation were used to evalute the anti-fusarium activity both in vitro and in vivo experiments. SDS-PAGE results of total protein from the Fusarium oxysporum f. sp. vasinfectum (FOV) isolate before and after treatment with eugenol oil nanoemulsion indicate that the content of extra cellular soluble small molecular proteins decreased significantly in EON-treated fungus. Light micrographs of mycelia and spores treated with EON showed the disruption of the fungal structures. The analysis of variance (ANOVA) for Fusarium wilt incidence indicated highly significant ( p = 0.000) effects of concentration, genotype, and their interaction. The difference in wilt incidence between concentrations and control was not the same for each genotype, that is, the genotypes responded differently to concentrations. Effects of three EON concentration on germination percentage, and radicle length, were determined in the laboratory. One very interesting finding in the current study is that cotton genotypes was the most important factors in determining wilt incidence as it accounted for 93.18 % of the explained (model) variation. In vitro experiments were conducted to evaluate the potential phytotoxic effect of three EON concentrations. Concentration, genotype and

  20. Ultrathin cellulose nanosheet membranes for superfast separation of oil-in-water nanoemulsions

    NASA Astrophysics Data System (ADS)

    Zhou, Ke; Zhang, Qiu Gen; Li, Hong Mei; Guo, Nan Nan; Zhu, Ai Mei; Liu, Qing Lin

    2014-08-01

    Oily wastewater is generated in diverse industrial processes, and its treatment has become crucial due to increasing environmental concerns. Herein, novel ultrathin nanoporous membranes of cellulose nanosheets have been fabricated for separation of oil-in-water nanoemulsions. The fabrication approach is facile and environmentally friendly, in which cellulose nanosheets are prepared by freeze-extraction of a very dilute cellulose solution. The as-prepared membranes have a cellulose nanosheet layer with a cut-off of 10-12 nm and a controllable thickness of 80-220 nm. They allow ultrafast water permeation and exhibit excellent size-selective separation properties. A 112 nm-thick membrane has a water flux of 1620 l m-2 h-1 bar-1 and a ferritin rejection of 92.5%. These membranes have been applied to remove oil from its aqueous nanoemulsions successfully, and they show an ultrafast and effective separation of oil-in-water nanoemulsions. The newly developed ultrathin cellulose membranes have a wide application in oily wastewater treatment, separation and purification of nanomaterials.Oily wastewater is generated in diverse industrial processes, and its treatment has become crucial due to increasing environmental concerns. Herein, novel ultrathin nanoporous membranes of cellulose nanosheets have been fabricated for separation of oil-in-water nanoemulsions. The fabrication approach is facile and environmentally friendly, in which cellulose nanosheets are prepared by freeze-extraction of a very dilute cellulose solution. The as-prepared membranes have a cellulose nanosheet layer with a cut-off of 10-12 nm and a controllable thickness of 80-220 nm. They allow ultrafast water permeation and exhibit excellent size-selective separation properties. A 112 nm-thick membrane has a water flux of 1620 l m-2 h-1 bar-1 and a ferritin rejection of 92.5%. These membranes have been applied to remove oil from its aqueous nanoemulsions successfully, and they show an ultrafast and effective

  1. Optimization of Ibuprofen Delivery through Rat Skin from Traditional and Novel Nanoemulsion Formulations

    PubMed Central

    Sharif Makhmalzadeh, Behzad; Torabi, Shiva; Azarpanah, Armita

    2012-01-01

    The topical delivery of non-steroidal anti-inflammatory drugs (NSAIDS) such as Ibuprofen has been explored as a potential method of avoiding the first pass effects and the gastric irritation, which may occur when used orally. Ibuprofen is formulated into many topical preparations to reduce the adverse effects and simultaneously avoid the hepatic first-pass metabolism as well. However, it is difficult to obtain an effective concentration through topical delivery of Ibuprofen due to its low skin permeability. The aim of this study was to develop two types of nanoemulsions formulations and focused on the screening of Ibuprofen-loaded nanoemulsions and evaluating the influence of these types of nanoemulsions on the skin permeability of the drug. In both nanoemulsion formulations, oil was similar, but the surfactant and co-surfactant were different. The effect of independent variables on skin permeability parameters was evaluated using full factorial design. Results demonstrate that novel formulations were more effective as skin enhancer than traditional formulation. In case of the novel formulation, any increase in percentage of surfactant and co-surfactant had increasing effect on flux (Jss). On the other hand, the proportion of surfactant/co-surfactant (S/C) demonstrated reverse correlation with Jss. While, in traditional formulations, direct correlation was found between both variables, and Jss. Comparison between two types of nanoemulsion formulations revealed that, novel formulations were more effective as topical Ibuprofen carrier in contrast to traditional type due to lower amounts of surfactant and co-surfactant and less irritating effect. PMID:25317184

  2. Formulation development and optimization of palm kernel oil esters-based nanoemulsions containing sodium diclofenac

    PubMed Central

    Rezaee, Malahat; Basri, Mahiran; Rahman, Raja Noor Zaliha Raja Abdul; Salleh, Abu Bakar; Chaibakhsh, Naz; Karjiban, Roghayeh Abedi

    2014-01-01

    Response surface methodology was employed to study the effect of formulation composition variables, water content (60%–80%, w/w) and oil and surfactant (O/S) ratio (0.17–1.33), as well as high-shear emulsification conditions, mixing rate (300–3,000 rpm) and mixing time (5–30 minutes) on the properties of sodium diclofenac-loaded palm kernel oil esters-nanoemulsions. The two response variables were droplet size and viscosity. Optimization of the conditions according to the four variables was performed for preparation of the nanoemulsions with the minimum values of particle size and viscosity. The results showed that the experimental data could be sufficiently fitted into a third-order polynomial model with multiple regression coefficients (R2) of 0.938 and 0.994 for the particle size and viscosity, respectively. Water content, O/S ratio and mixing time, quadrics of all independent variables, interaction between O/S ratio and mixing rate and between mixing time and rate, as well as cubic term of water content had a significant effect (P<0.05) on the particle size of nanoemulsions. The linear effect of all independent variables, quadrics of water content and O/S ratio, interaction of water content and O/S ratio, as well as cubic term of water content and O/S ratio had significant effects (P<0.05) on the viscosity of all nanoemulsions. The optimum conditions for preparation of sodium diclofenac nanoemulsions were predicted to be: 71.36% water content; 0.69 O/S ratio; 950 rpm mixing rate, and 5 minute mixing time. The optimized formulation showed good storage stability in different temperatures. PMID:24531324

  3. Allergic Contact Dermatitis to Benzoyl Peroxide Resembling Impetigo.

    PubMed

    Kim, Changhyun; Craiglow, Brittany G; Watsky, Kalman L; Antaya, Richard J

    2015-01-01

    A 17-year-old boy presented with recurring severe dermatitis of the face of 5-months duration that resembled impetigo. He had been treated with several courses of antibiotics without improvement. Biopsy showed changes consistent with allergic contact dermatitis and patch testing later revealed sensitization to benzoyl peroxide, which the patient had been using for the treatment of acne vulgaris. PMID:25782705

  4. Allergic Contact Dermatitis to Benzoyl Peroxide Resembling Impetigo.

    PubMed

    Kim, Changhyun; Craiglow, Brittany G; Watsky, Kalman L; Antaya, Richard J

    2015-01-01

    A 17-year-old boy presented with recurring severe dermatitis of the face of 5-months duration that resembled impetigo. He had been treated with several courses of antibiotics without improvement. Biopsy showed changes consistent with allergic contact dermatitis and patch testing later revealed sensitization to benzoyl peroxide, which the patient had been using for the treatment of acne vulgaris.

  5. Encapsulation of ω-3 fatty acids in nanoemulsion-based delivery systems fabricated from natural emulsifiers: Sunflower phospholipids.

    PubMed

    Komaiko, Jennifer; Sastrosubroto, Ashtri; McClements, David Julian

    2016-07-15

    Nanoemulsions have considerable potential for encapsulating and delivering ω-3 fatty acids, but they are typically fabricated from synthetic surfactants. This study shows that fish oil-in-water nanoemulsions can be formed from sunflower phospholipids, which have advantages for food applications because they have low allergenicity and do not come from genetically modified organisms. Nanoemulsions containing small droplets (d<150 nm) could be produced using microfluidization, by optimizing phospholipid type and concentration, with the smallest droplets being formed at high phosphatidylcholine levels and at surfactant-to-oil ratios exceeding unity. The physical stability of the nanoemulsions was mainly attributed to electrostatic repulsion, with droplet aggregation occurring at low pH values (low charge magnitude) and at high ionic strengths (electrostatic screening). These results suggest that sunflower phospholipids may be a viable natural emulsifier to deliver ω-3 fatty acids into food and beverage products.

  6. Encapsulation of ω-3 fatty acids in nanoemulsion-based delivery systems fabricated from natural emulsifiers: Sunflower phospholipids.

    PubMed

    Komaiko, Jennifer; Sastrosubroto, Ashtri; McClements, David Julian

    2016-07-15

    Nanoemulsions have considerable potential for encapsulating and delivering ω-3 fatty acids, but they are typically fabricated from synthetic surfactants. This study shows that fish oil-in-water nanoemulsions can be formed from sunflower phospholipids, which have advantages for food applications because they have low allergenicity and do not come from genetically modified organisms. Nanoemulsions containing small droplets (d<150 nm) could be produced using microfluidization, by optimizing phospholipid type and concentration, with the smallest droplets being formed at high phosphatidylcholine levels and at surfactant-to-oil ratios exceeding unity. The physical stability of the nanoemulsions was mainly attributed to electrostatic repulsion, with droplet aggregation occurring at low pH values (low charge magnitude) and at high ionic strengths (electrostatic screening). These results suggest that sunflower phospholipids may be a viable natural emulsifier to deliver ω-3 fatty acids into food and beverage products. PMID:26948622

  7. Vitamin E loaded resveratrol nanoemulsion for brain targeting for the treatment of Parkinson’s disease by reducing oxidative stress

    NASA Astrophysics Data System (ADS)

    Pangeni, Rudra; Sharma, Shrestha; Mustafa, Gulam; Ali, Javed; Baboota, Sanjula

    2014-12-01

    Resveratrol, a potent natural antioxidant, possesses a wide range of pharmacological activities, but its oral bioavailability is very low due to its extensive hepatic and presystemic metabolism. The aim of the present study was to formulate a kinetically stable nanoemulsion (o/w) using vitamin E:sefsol (1:1) as the oil phase, Tween 80 as the surfactant and Transcutol P as the co-surfactant for the better management of Parkinson’s disease. The nanoemulsion was prepared by a spontaneous emulsification method, followed by high-pressure homogenization. Ternary phase diagrams were constructed to locate the area of nanoemulsion. The prepared formulations were studied for globule size, zeta potential, refractive index, viscosity, surface morphology and in vitro and ex vivo release. The homogenized formulation, which contained 150 mg ml-1 of resveratrol, showed spherical globules with an average globule diameter of 102 ± 1.46 nm, a least poly dispersity index of 0.158 ± 0.02 and optimal zeta potential values of -35 ± 0.02. The cumulative percentage drug release for the pre-homogenized resveratrol suspension, pre-homogenized nanoemulsion and post-homogenized nanoemulsion were 24.18 ± 2.30%, 54.32 ± 0.95% and 88.57 ± 1.92%, respectively, after 24 h. The ex vivo release also showed the cumulative percentage drug release of 85.48 ± 1.34% at 24 h. The antioxidant activity determined by using a DPPH assay showed high scavenging efficiency for the optimized formulation. Pharmacokinetic studies showed the higher concentration of the drug in the brain (brain/blood ratio: 2.86 ± 0.70) following intranasal administration of the optimized nanoemulsion. Histopathological studies showed decreased degenerative changes in the resveratrol nanoemulsion administered groups. The levels of GSH and SOD were significantly higher, and the level of MDA was significantly lower in the resveratrol nanoemulsion treated group.

  8. Nanotoxicology applied to solid lipid nanoparticles and nanostructured lipid carriers - a systematic review of in vitro data.

    PubMed

    Doktorovova, Slavomira; Souto, Eliana B; Silva, Amélia M

    2014-05-01

    Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were developed as alternative to other colloidal carriers. They were designed to overcome lipid nanoemulsions and liposomes in stability and ability to control the release of an encapsulated substance, and at the same time to be better tolerated than polymeric nanoparticles. Since the patenting of SLN discovery, large amount of data became available on the behaviour of these systems in vitro. SLN/NLC have many prerequisites to be a well tolerated carrier - the currently available data seem to confirm it, but there are also some contradictory results. In this review, we collected the available data from cytotoxicity, oxidative stress and hemocompatibility studies in vitro and analysed their outcomes. We also provide a summary of the available data in a form of reference table. PMID:24530885

  9. Thermal Degradation and Isomerization of β-Carotene in Oil-in-Water Nanoemulsions Supplemented with Natural Antioxidants.

    PubMed

    Yi, Jiang; Fan, Yuting; Yokoyama, Wallace; Zhang, Yuzhu; Zhao, Liqing

    2016-03-01

    The goal of this study was to see the impact on the retention and isomerization of encapsulated β-carotene (BC) in nanoemulsions fortified with natural antioxidants (α-tocopherol (AT) and l-ascorbic acid (AA)). The physical stability of nanoemulsion, oxidative stability, and isomerization of all-trans-β-carotene (BC) in oil-in-water (O/W) nanoemulsions were determined in the presence or absence of natural antioxidants at 25 and 50 °C at certain intervals of time by high-performance liquid chromatography (HPLC). Sodium caseinate was used as the emulsifier, and corn oil (CO) was more protective than medium-chain triglycerides (MCT) and used for isomerization studies. Mean diameters of control (without antioxidants) and AA- and AT-fortified particles were similar. Mean particle diameter of nanoemulsions increased from 10 to 25 nm at 25 °C and from 40 to 50 nm at 50 °C during 30 days of storage. The isomerization from all-trans-BC to cis-BC isomers was inhibited by antioxidants. The isomerization rates were in the following order: 13-cis-BC > 15-cis-BC > 9-cis-BC. AT had better antioxidant activities than AA in inhibiting BC degradation in O/W nanoemulsions. The results indicated that BC encapsulated in nanoemulsions supplemented with antioxidants could significantly improve BC's chemical stability.

  10. Analgesic Efficacy and Safety of DALDA Peptide Analog Delivery to the Brain using Oil-in-Water Nanoemulsion Formulation

    PubMed Central

    Shah, Lipa; Kulkarni, Praveen; Ferris, Craig; Amiji, Mansoor M.

    2014-01-01

    Purpose The main objective of this study was to develop and evaluate therapeutic efficacy and safety following systemic delivery of a peptide analgesic into the CNS using an oil-in-water nanoemulsion system. Methods We have formulated a safe and effective, omega-3 rich polyunsaturated fatty acid containing oil-in-water nanoemulsion formulation, for encapsulating and delivering chemically-modified DALDA, a potent mu-opioid peptide analogue, to the CNS. Another challenge with CNS delivery is the lack of a non-invasive bioanalytical technique to confirm CNS uptake and therapeutic efficacy. Using blood oxygen-level dependent (BOLD) functional magenetic resonance imaging (fMRI), we provide quantitative evidence of nanoemulsion-based delivery and analgesic activity of DALDA analogue in capsaicin-induced awake rat model of pain. Results Nanoemulsion formulation effectively encapsulated the modified analgesic peptide and demonstrated efficacy in the capsaicin- pain induced functional magnetic resonance imaging model in rodents. Preliminary safety evaluations show that the nanoemulsion system was well tolerated and did not cause any acute negative effects. Conclusions Overall, these results show tremendous opportunity for the development of modified peptide analgesic-encapsulated nanoemulsion formulations for CNS delivery and therapeutic efficacy. PMID:24792826

  11. Thermal Degradation and Isomerization of β-Carotene in Oil-in-Water Nanoemulsions Supplemented with Natural Antioxidants.

    PubMed

    Yi, Jiang; Fan, Yuting; Yokoyama, Wallace; Zhang, Yuzhu; Zhao, Liqing

    2016-03-01

    The goal of this study was to see the impact on the retention and isomerization of encapsulated β-carotene (BC) in nanoemulsions fortified with natural antioxidants (α-tocopherol (AT) and l-ascorbic acid (AA)). The physical stability of nanoemulsion, oxidative stability, and isomerization of all-trans-β-carotene (BC) in oil-in-water (O/W) nanoemulsions were determined in the presence or absence of natural antioxidants at 25 and 50 °C at certain intervals of time by high-performance liquid chromatography (HPLC). Sodium caseinate was used as the emulsifier, and corn oil (CO) was more protective than medium-chain triglycerides (MCT) and used for isomerization studies. Mean diameters of control (without antioxidants) and AA- and AT-fortified particles were similar. Mean particle diameter of nanoemulsions increased from 10 to 25 nm at 25 °C and from 40 to 50 nm at 50 °C during 30 days of storage. The isomerization from all-trans-BC to cis-BC isomers was inhibited by antioxidants. The isomerization rates were in the following order: 13-cis-BC > 15-cis-BC > 9-cis-BC. AT had better antioxidant activities than AA in inhibiting BC degradation in O/W nanoemulsions. The results indicated that BC encapsulated in nanoemulsions supplemented with antioxidants could significantly improve BC's chemical stability. PMID:26881704

  12. Formation and stability of oil-in-water nanoemulsions containing rice bran oil: in vitro and in vivo assessments

    PubMed Central

    2011-01-01

    Background Nanoemulsions have practical application in a multitude of commercial areas, such as the chemical, pharmaceutical and cosmetic industries. Cosmetic industries use rice bran oil in sunscreen formulations, anti ageing products and in treatments for skin diseases. The aim of this study was to create rice bran oil nanoemulsions using low energy emulsification methods and to evaluate their physical stability, irritation potential and moisturising activity on volunteers with normal and diseased skin types. Results The nanoemulsion developed by this phase diagram method was composed of 10% rice bran oil, 10% surfactants sorbitan oleate/PEG-30 castor oil, 0.05% antioxidant and 0.50% preservatives formulated in distilled water. The nanoemulsion was stable over the time course of this study. In vitro assays showed that this formulation has a low irritation potential, and when applied to human skin during in vivo studies, the nanoemulsion improved the skin's moisture and maintained normal skin pH values. Conclusion The results of irritation potential studies and in vivo assessments indicate that this nanoemulsion has potential to be a useful tool to treat skin diseases, such as atopic dermatitis and psoriasis. PMID:21952107

  13. Physicochemical properties of whey protein, lactoferrin and Tween 20 stabilised nanoemulsions: Effect of temperature, pH and salt.

    PubMed

    Teo, Anges; Goh, Kelvin K T; Wen, Jingyuan; Oey, Indrawati; Ko, Sanghoon; Kwak, Hae-Soo; Lee, Sung Je

    2016-04-15

    Oil-in-water nanoemulsions were prepared by emulsification and solvent evaporation using whey protein isolate (WPI), lactoferrin and Tween 20 as emulsifiers. Protein-stabilised nanoemulsions showed a decrease in particle size with increasing protein concentration from 0.25% to 1% (w/w) level with Z-average diameter between 70 and 90 nm. However, larger droplets were produced by Tween 20 (120-450 nm) especially at concentration above 0.75% (w/w). The stability of nanoemulsions to temperature (30-90°C), pH (2-10) and ionic strength (0-500 mM NaCl or 0-90 mM CaCl2) was also tested. Tween 20 nanoemulsions were unstable to heat treatment at 90°C for 15 min. WPI-stabilised nanoemulsions exhibited droplet aggregation near the isoelectric point at pH 4.5 and 5 and they were also unstable at salt concentration above 30 mM CaCl2. These results indicated that stable nanoemulsions can be prepared by careful selection of emulsifiers. PMID:26616953

  14. Physicochemical properties of whey protein, lactoferrin and Tween 20 stabilised nanoemulsions: Effect of temperature, pH and salt.

    PubMed

    Teo, Anges; Goh, Kelvin K T; Wen, Jingyuan; Oey, Indrawati; Ko, Sanghoon; Kwak, Hae-Soo; Lee, Sung Je

    2016-04-15

    Oil-in-water nanoemulsions were prepared by emulsification and solvent evaporation using whey protein isolate (WPI), lactoferrin and Tween 20 as emulsifiers. Protein-stabilised nanoemulsions showed a decrease in particle size with increasing protein concentration from 0.25% to 1% (w/w) level with Z-average diameter between 70 and 90 nm. However, larger droplets were produced by Tween 20 (120-450 nm) especially at concentration above 0.75% (w/w). The stability of nanoemulsions to temperature (30-90°C), pH (2-10) and ionic strength (0-500 mM NaCl or 0-90 mM CaCl2) was also tested. Tween 20 nanoemulsions were unstable to heat treatment at 90°C for 15 min. WPI-stabilised nanoemulsions exhibited droplet aggregation near the isoelectric point at pH 4.5 and 5 and they were also unstable at salt concentration above 30 mM CaCl2. These results indicated that stable nanoemulsions can be prepared by careful selection of emulsifiers.

  15. Association efficiency of three ionic forms of oxytetracycline to cationic and anionic oil-in-water nanoemulsions analyzed by diafiltration.

    PubMed

    Orellana, Sandra L; Torres-Gallegos, Cesar; Araya-Hermosilla, Rodrigo; Oyarzun-Ampuero, Felipe; Moreno-Villoslada, Ignacio

    2015-03-01

    The association efficiency of oxytetracycline (OTC) to pharmaceutical available, ionic oil-in-water nanoemulsions is studied. Theoretical mathematical developments allowed us to differentiate by diafiltration (DF) between thermodynamically and kinetically controlled binding of the drug to the nanoemulsions, and relate these important magnitudes to the association efficiency. The nanoemulsions have been prepared by the solvent displacement technique in the presence of cationic and anionic surfactants. The resulting nanoemulsions were stable at 4°C and 25°C for 60 days, have a size of ∼ 200 nm, showing polydispersity indexes ranging between 0.11 and 0.23, and present zeta potentials ranging between -90 and +60 mV, depending on the charge of the surfactants used. The zeta potential of the nanoemulsions influenced the interaction with OTC, having three ionic forms at different pH, namely, cationic, zwitterionic, and anionic. DF proved to be a powerful tool for the quantification of the drug association efficiency, achieving values up to 84%. Furthermore, this technique allowed obtaining different values of the drug fractions reversibly bound (11%-57%) and irreversibly bound (10%-40%) to the nanoemulsions depending on the surfactants used and pH. These findings may be useful for the development of new drug delivery systems, and as routine assays in academia and pharmaceutical industries.

  16. Delivery of lipophilic bioactives: assembly, disassembly, and reassembly of lipid nanoparticles.

    PubMed

    Yao, Mingfei; Xiao, Hang; McClements, David Julian

    2014-01-01

    The oral bioavailability of lipophilic bioactive molecules can be greatly increased by encapsulating them within engineered lipid nanoparticles (ELNs), such as micelles, microemulsions, nanoemulsions, or solid lipid nanoparticles (SLNs). After ingestion, these ELNs are disassembled in the gastrointestinal tract (GIT) and then reassembled into biological lipid nanoparticles (mixed micelles) in the small intestine. These mixed micelles solubilize and transport lipophilic bioactive components to the epithelial cells. The mixed micelles are then disassembled and reassembled into yet another form of biological lipid nanoparticle [chylomicrons (CMs)] within the enterocyte cells. The CMs carry the bioactive components into the systemic (blood) circulation via the lymphatic system, thereby avoiding first-pass metabolism. This article provides an overview of the various physicochemical and physiological processes responsible for the assembly and disassembly of lipid nanoparticles outside and inside the GIT. This knowledge can be used to design food-grade delivery systems to improve the oral bioavailability of encapsulated lipophilic bioactive components. PMID:24328432

  17. Recent Techniques and Patents on Solid Lipid Nanoparticles as Novel Carrier for Drug Delivery.

    PubMed

    Khatak, Sunil; Dureja, Harish

    2015-01-01

    The various approaches have been utilized in the treatment of a variety of diseases by applying drug delivery system such as polymeric nanoparticles, self-emulsifying delivery systems, liposomes, microemulsions and micellar solutions. Recently, solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs) and lipid-drug conjugates (LDCs) have been exploited as a carrier of lipophilic and hydrophilic/amphiphilic substances for invasive and non-invasive routes of delivery. SLNs are colloidal drug carrier system and are like nanoemulsion, however, the lipid content in SLNs is solid in nature. These novel type of lipid nanoparticles with solid matrix offers to develop new prototype therapeutics in drug delivery, which could be used for controlled release, drug targeting, gene therapy, physical and chemical stability and site-specific drug delivery and thereby attracted the research groups worldwide. This manuscript overviews the recent patents, advantages, formulation techniques, stability aspects and applications of SLNs. PMID:27009132

  18. Carbonaceous objects resembling nannobacteria in the Allende meteorite

    NASA Astrophysics Data System (ADS)

    Folk, Robert L.; Lynch, F. Leo

    1998-07-01

    The carbon in Allende consists of balls ranging form 30 to 150 nm in diameter.Most are spheres, but some ovoid to worm- like forms occur. Grape-like clumps and rosary-like chains are the most dramatic mimics of terrestrial bacterial colonies. We propose that the carbon balls in Allende represent roasted corpses of nanobacteria because of their resemblance to nanobacteria on earth.

  19. In Vitro Study on Antihypertensive and Antihypercholesterolemic Effects of a Curcumin Nanoemulsion.

    PubMed

    Rachmawati, Heni; Soraya, Irene Surya; Kurniati, Neng Fisheri; Rahma, Annisa

    2016-01-01

    Atherosclerosis and hypertension can potentially progess into dangerous cardiovascular diseases such as myocardial infarction and stroke. Statins are widely used to lower cholesterol levels while antihypertensive agents such as captopril are widely prescribed to treat high blood pressure. Curcumin, a phenolic compound isolated from Curcuma domestica, has been proven effective for a broad spectrum of diseases, including hypertension and hypercholesterolemia. Therefore, curcumin is quite promising as an alternative therapeutic compound. Our previous studies have proven a significant increase in physical properties, bioavailability, and stability of curcumin when encapsulated in a nanoemulsion. The purpose of this study was to assess the ability of the nanoemulsion in enhancing curcumin activity as a antihypertensive and antihypercholesterolemic agent. The formulation and preparation method of the curcumin nanoemulsion have been developed in our previous study. Physical characterization was performed, including measurement of droplet size, polidispersity index, zeta potential, entrapment efficiency, and loading capacity. Antihypertensive activity of curcumin was evaluated by determining Angiotensin Converting Enzyme (ACE) inhibition in vitro. A substrate for ACE, hippuryl-L-histidyl-L-leucine was allowed to react with ACE, resulting in hippuric acid formation as the product. The degree of ACE inhibition by curcumin was represented by the amount of hippuric acid formed. Antihypercholesterolemic activity of curcumin was studied using the HMG-CoA reductase assay equipped with a 96-well UV plate. This assay was based on the spectrophotometric measurement of the decrease in absorbance which represents the oxidation of NADPH by the catalytic subunit of 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) in the presence of the substrate HMG-CoA. Curcumin is known to have no significant difference in inhibiting ACE compared to Captopril, but when it was incorporated in the self

  20. In Vitro Study on Antihypertensive and Antihypercholesterolemic Effects of a Curcumin Nanoemulsion

    PubMed Central

    Rachmawati, Heni; Soraya, Irene Surya; Kurniati, Neng Fisheri; Rahma, Annisa

    2016-01-01

    Atherosclerosis and hypertension can potentially progess into dangerous cardiovascular diseases such as myocardial infarction and stroke. Statins are widely used to lower cholesterol levels while antihypertensive agents such as captopril are widely prescribed to treat high blood pressure. Curcumin, a phenolic compound isolated from Curcuma domestica, has been proven effective for a broad spectrum of diseases, including hypertension and hypercholesterolemia. Therefore, curcumin is quite promising as an alternative therapeutic compound. Our previous studies have proven a significant increase in physical properties, bioavailability, and stability of curcumin when encapsulated in a nanoemulsion. The purpose of this study was to assess the ability of the nanoemulsion in enhancing curcumin activity as a antihypertensive and antihypercholesterolemic agent. The formulation and preparation method of the curcumin nanoemulsion have been developed in our previous study. Physical characterization was performed, including measurement of droplet size, polidispersity index, zeta potential, entrapment efficiency, and loading capacity. Antihypertensive activity of curcumin was evaluated by determining Angiotensin Converting Enzyme (ACE) inhibition in vitro. A substrate for ACE, hippuryl-L-histidyl-L-leucine was allowed to react with ACE, resulting in hippuric acid formation as the product. The degree of ACE inhibition by curcumin was represented by the amount of hippuric acid formed. Antihypercholesterolemic activity of curcumin was studied using the HMG-CoA reductase assay equipped with a 96-well UV plate. This assay was based on the spectrophotometric measurement of the decrease in absorbance which represents the oxidation of NADPH by the catalytic subunit of 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) in the presence of the substrate HMG-CoA. Curcumin is known to have no significant difference in inhibiting ACE compared to Captopril, but when it was incorporated in the self

  1. Familial resemblance of blood pressure and body weight.

    PubMed

    André, J L; Deschamps, J P; Gueguen, R

    1986-01-01

    Familial resemblance of blood pressure (BP) was studied in 545 families of which 370 included natural children, 24 adopted children and 151 both natural and adopted children. Mean values of four automatic BP measurements (Dinamap 845) were converted into age (adult) or height (children) and sex adjusted scores. BP was compared between parents and randomly chosen index children. A significant resemblance of BP was observed between natural children and their parents: r = 0.24 for systolic BP, r = 0.29 for diastolic BP, (n = 272 p greater than 0.05). BP of adopted children did not resemble that of their foster parents except for a significant correlation to BP of the adopting mothers (n = 46). Weight, heart rate, age and time of common life shared did not influence the results. The relative contribution of genetic and common environmental factors to BP correlation between family members could not be evaluated in this study. BP of children whose parents have high BP should be monitored regularly.

  2. Lipid nanoparticles for dermal drug delivery.

    PubMed

    Kakadia, Pratibha G; Conway, Barbara R

    2015-01-01

    Lipid based drug delivery systems have been widely studied and reported over the past decade and offer a useful alternative to other colloidal drug delivery systems. Skin is a popular route of drug delivery for locally and systemically acting drugs and nanoparticles are reported as a potential formulation strategy for dermal delivery. Although the skin acts as a natural physical barrier against penetration of foreign materials, including particulates, opportunities exist for the delivery of therapeutic nanoparticles, especially in diseased and damaged skin and via appendageal routes such as the openings of hair follicles. The extent and ability of nanoparticles to penetrate into the underlying viable tissue is still the subject of debate although recent studies have identified the follicular route as the most likely route of entry; this influences the potential applications of these dosage forms as a drug delivery strategy. This paper reviews present state of art of lipid-based nanocarriers focussing on solid lipid nanoparticles, nanostructured lipid carriers and nanoemulsions, their production methods, potential advantages and applications in dermal drug delivery. PMID:25925115

  3. Evaluation of short cycles of ultrasound application in nanoemulsions to obtain nanocapsules.

    PubMed

    Carneiro, Simone Pinto; Cruz, Ricardo Machado; dos Santos, Orlando David Henrique

    2015-11-01

    Ultrasound is widely used in several chemical reactions and other process, including production of nanocapsules by in situ polymerization. In this work, the main objective was to evaluate the impacts and viability of successive ultrasound application in nanoemulsions to obtain nanocapsules. Initiator potassium persulfate (KPS) concentration, number of ultrasound cycles and reaction time influences on polymerization efficiency and droplet size were evaluated. This work revealed the successful in situ production of nanocapsules using successive shorts cycles of ultrasound. Number of cycles was the only parameter that not exerted significant influence in polymerization yield. Particle size decay was observed in all nanoemulsions after the first ultrasound application, the same was not observed in further cycles. Gravimetric assessment showed remarkable increase of monomer conversion, indicating that once started polymerization continued at least until 28 days after ultrasound application. Concluding, ultrasound short cycles can be used with no harm to formulation, if carefully performed and, furthermore is a potential cost-effective route for polymerization reactions.

  4. Ultrasonic emulsification of parenteral valproic acid-loaded nanoemulsion with response surface methodology and evaluation of its stability.

    PubMed

    Tan, Suk Fei; Masoumi, Hamid Reza Fard; Karjiban, Roghayeh Abedi; Stanslas, Johnson; Kirby, Brian P; Basri, Mahiran; Basri, Hamidon Bin

    2016-03-01

    Response surface methodology (RSM) was used to optimize the formulation of a nanoemulsion for central delivery following parenteral administration. A mixture of medium-chain triglyceride (MCT) and safflower seed oil (SSO) was determined as a sole phase from the emulsification properties. Similarly, a natural surfactant (lecithin) and non-ionic surfactant (Tween 80) (ratio 1:2) were used in the formulation. A central composite design (CCD) with three-factor at five-levels was used to optimize the processing method of high energy ultrasonicator. Effects of pre-sonication ultrasonic intensity (A), sonication time (B), and temperature (C) were studied on the preparation of nanoemulsion loaded with valproic acid. Influence of the aforementioned specifically the effects of the ultrasonic processing parameters on droplet size and polydispersity index were investigated. From the analysis, it was found that the interaction between ultrasonic intensity and sonication time was the most influential factor on the droplet size of nanoemulsion formulated. Ultrasonic intensity (A) significantly affects the polydispersity index value. With this optimization method, a favorable droplet size of a nanoemulsion with reasonable polydispersity index was able to be formulated within a short sonication time. A valproic acid loaded nanoemulsion can be obtained with 60% power intensity for 15 min at 60 °C. Droplet size of 43.21±0.11 nm with polydispersity index of 0.211 were produced. The drug content was then increased to 1.5%. Stability study of nanoemulsion containing 1.5% of valproic acid had a good stability as there are no significant changes in physicochemical aspects such as droplet size and polydispersity index. With the characteristisation study of pH, viscosity, transmission electron microscope (TEM) and stability assessment study the formulated nanoemulsion has the potential to penetrate blood-brain barrier in the treatment of epilepsy.

  5. Ultrasonic emulsification of parenteral valproic acid-loaded nanoemulsion with response surface methodology and evaluation of its stability.

    PubMed

    Tan, Suk Fei; Masoumi, Hamid Reza Fard; Karjiban, Roghayeh Abedi; Stanslas, Johnson; Kirby, Brian P; Basri, Mahiran; Basri, Hamidon Bin

    2016-03-01

    Response surface methodology (RSM) was used to optimize the formulation of a nanoemulsion for central delivery following parenteral administration. A mixture of medium-chain triglyceride (MCT) and safflower seed oil (SSO) was determined as a sole phase from the emulsification properties. Similarly, a natural surfactant (lecithin) and non-ionic surfactant (Tween 80) (ratio 1:2) were used in the formulation. A central composite design (CCD) with three-factor at five-levels was used to optimize the processing method of high energy ultrasonicator. Effects of pre-sonication ultrasonic intensity (A), sonication time (B), and temperature (C) were studied on the preparation of nanoemulsion loaded with valproic acid. Influence of the aforementioned specifically the effects of the ultrasonic processing parameters on droplet size and polydispersity index were investigated. From the analysis, it was found that the interaction between ultrasonic intensity and sonication time was the most influential factor on the droplet size of nanoemulsion formulated. Ultrasonic intensity (A) significantly affects the polydispersity index value. With this optimization method, a favorable droplet size of a nanoemulsion with reasonable polydispersity index was able to be formulated within a short sonication time. A valproic acid loaded nanoemulsion can be obtained with 60% power intensity for 15 min at 60 °C. Droplet size of 43.21±0.11 nm with polydispersity index of 0.211 were produced. The drug content was then increased to 1.5%. Stability study of nanoemulsion containing 1.5% of valproic acid had a good stability as there are no significant changes in physicochemical aspects such as droplet size and polydispersity index. With the characteristisation study of pH, viscosity, transmission electron microscope (TEM) and stability assessment study the formulated nanoemulsion has the potential to penetrate blood-brain barrier in the treatment of epilepsy. PMID:26585010

  6. Immunoadjuvant Chemotherapy of Visceral Leishmaniasis in Hamsters Using Amphotericin B-Encapsulated Nanoemulsion Template-Based Chitosan Nanocapsules

    PubMed Central

    Asthana, Shalini; Jaiswal, Anil K.; Gupta, Pramod K.; Pawar, Vivek K.; Dube, Anuradha

    2013-01-01

    The accessible treatment options for life-threatening neglected visceral leishmaniasis (VL) disease have problems with efficacy, stability, adverse effects, and cost, making treatment a complex issue. Here we formulated nanometric amphotericin B (AmB)-encapsulated chitosan nanocapsules (CNC-AmB) using a polymer deposition technique mediated by nanoemulsion template fabrication. CNC-AmB exhibited good steric stability in vitro, where the chitosan content was found to be efficient at preventing destabilization in the presence of protein and Ca2+. A toxicity study on the model cell line J774A and erythrocytes revealed that CNC-AmB was less toxic than commercialized AmB formulations such as Fungizone and AmBisome. The results of in vitro (macrophage-amastigote system; 50% inhibitory concentration [IC50], 0.19 ± 0.04 μg AmB/ml) and in vivo (Leishmania donovani-infected hamsters; 86.1% ± 2.08% parasite inhibition) experiments in conjunction with effective internalization by macrophages illustrated the efficacy of CNC-AmB at augmenting antileishmanial properties. Quantitative mRNA analysis by real-time PCR (RT-PCR) showed that the improved effect was synergized with the upregulation of tumor necrosis factor alpha (TNF-α), interleukin-12 (IL-12), and inducible nitric oxide synthase and with the downregulation of transforming growth factor β (TGF-β), IL-10, and IL-4. These research findings suggest that a cost-effective CNC-AmB immunoadjuvant chemotherapeutic delivery system could be a viable alternative to the current high-cost commercial lipid-based formulations. PMID:23357762

  7. Antimicrobial Activity of Nanoemulsion in Combination with Cetylpyridinium Chloride in Multidrug-Resistant Acinetobacter baumannii

    PubMed Central

    Hwang, Yoon Y.; Ramalingam, Karthikeyan; Bienek, Diane R.; Lee, Valerie; You, Tao

    2013-01-01

    Acinetobacter baumannii has emerged as a serious problematic pathogen due to the ever-increasing presence of antibiotic resistance, demonstrating a need for novel, broad-spectrum antimicrobial therapeutic options. Antimicrobial nanoemulsions are emulsified mixtures of detergent, oil, and water (droplet size, 100 to 800 nm) which have broad antimicrobial activity against bacteria, enveloped viruses, and fungi. Here, we screened the antimicrobial activities of five nanoemulsion preparations against four Acinetobacter baumannii isolates to identify the most suitable preparation for further evaluation. Among them, N5, which contains 10% (vol/vol) Triton X-100, 25% (vol/vol) soybean oil, and 1% (wt/vol) cetylpyridinium chloride (CPC), showed the best efficacy against A. baumannii in both its planktonic and biofilm forms and was selected for further study. Our data demonstrate that, while the killing of planktonic forms of A. baumannii was due to the 1% CPC component of our nanoemulsions, the breakdown of biofilms was achieved via the emulsified oil and detergent fractions. Furthermore, we documented the effect of ethanol and NaCl in combination with N5 on planktonic A. baumannii. In killing curves of N5 combined with other agents (ethanol or NaCl), a synergistic effect of a ≥2-log decrease in CFU/ml was observed. The antibiofilm activity of N5 was confirmed via a cell proliferation test and scanning electron microscopy. The effects of exposure to severe environmental conditions, which simulates the field conditions in Iraq and Afghanistan, were evaluated, and this exposure did not affect the overall antimicrobial activity of N5. These studies lay a solid foundation for the utilization of nanoemulsions against the antibiotic-resistant forms of A. baumannii. PMID:23669390

  8. Monitoring the Stability of Perfluorocarbon Nanoemulsions by Cryo-TEM Image Analysis and Dynamic Light Scattering

    PubMed Central

    Grapentin, Christoph; Barnert, Sabine; Schubert, Rolf

    2015-01-01

    Perfluorocarbon nanoemulsions (PFC-NE) are disperse systems consisting of nanoscale liquid perfluorocarbon droplets stabilized by an emulsifier, usually phospholipids. Perfluorocarbons are chemically inert and non-toxic substances that are exhaled after in vivo administration. The manufacture of PFC-NE can be done in large scales by means of high pressure homogenization or microfluidization. Originally investigated as oxygen carriers for cases of severe blood loss, their application nowadays is more focused on using them as marker agents in 19F Magnetic Resonance Imaging (19F MRI). 19F is scarce in organisms and thus PFC-NE are a promising tool for highly specific and non-invasive imaging of inflammation via 19F MRI. Neutrophils, monocytes and macrophages phagocytize PFC-NE and subsequently migrate to inflamed tissues. This technique has proven feasibility in numerous disease models in mice, rabbits and mini pigs. The translation to clinical trials in human needs the development of a stable nanoemulsion whose droplet size is well characterized over a long storage time. Usually dynamic light scattering (DLS) is applied as the standard method for determining particle sizes in the nanometer range. Our study uses a second method, analysis of transmission electron microscopy images of cryo-fixed samples (Cryo-TEM), to evaluate stability of PFC-NE in comparison to DLS. Four nanoemulsions of different composition are observed for one year. The results indicate that DLS alone cannot reveal the changes in particle size, but can even mislead to a positive estimation of stability. The combination with Cryo-TEM images gives more insight in the particulate evolution, both techniques supporting one another. The study is one further step in the development of analytical tools for the evaluation of a clinically applicable perfluorooctylbromide nanoemulsion. PMID:26098661

  9. Carisoprodol withdrawal syndrome resembling neuroleptic malignant syndrome: Diagnostic dilemma

    PubMed Central

    Paul, Gunchan; Parshotam, Gautam L; Garg, Rajneesh

    2016-01-01

    Soma (Carisoprodol) is N-isopropyl-2 methyl-2-propyl-1,3-propanediol dicarbamate; a commonly prescribed, centrally acting skeletal muscle relaxant. Neuroleptic malignant syndrome (NMS) is a potentially life-threatening adverse effect of antipsychotic agents. Although diagnostic criteria for NMS have been established, it should be recognized that atypical presentations occur and more flexible diagnostic criteria than currently mandated, may be warranted. We wish to report a postoperative case of bilateral knee replacement who presented with carisoprodol (Soma) withdrawal resembling NMS that was a diagnostic dilemma. Subsequently, it was successfully treated with oral baclofen in absence of sodium dantrolene. PMID:27625493

  10. Carisoprodol withdrawal syndrome resembling neuroleptic malignant syndrome: Diagnostic dilemma.

    PubMed

    Paul, Gunchan; Parshotam, Gautam L; Garg, Rajneesh

    2016-01-01

    Soma (Carisoprodol) is N-isopropyl-2 methyl-2-propyl-1,3-propanediol dicarbamate; a commonly prescribed, centrally acting skeletal muscle relaxant. Neuroleptic malignant syndrome (NMS) is a potentially life-threatening adverse effect of antipsychotic agents. Although diagnostic criteria for NMS have been established, it should be recognized that atypical presentations occur and more flexible diagnostic criteria than currently mandated, may be warranted. We wish to report a postoperative case of bilateral knee replacement who presented with carisoprodol (Soma) withdrawal resembling NMS that was a diagnostic dilemma. Subsequently, it was successfully treated with oral baclofen in absence of sodium dantrolene. PMID:27625493

  11. In vitro effects of Eucalyptus staigeriana nanoemulsion on Haemonchus contortus and toxicity in rodents.

    PubMed

    Ribeiro, Wesley Lyeverton Correia; Camurça-Vasconcelos, Ana Lourdes Fernandes; Macedo, Iara Tersia Freitas; dos Santos, Jessica Maria Leite; de Araújo-Filho, José Vilemar; Ribeiro, Juliana de Carvalho; Pereira, Vanessa de Abreu; Viana, Daniel de Araújo; de Paula, Haroldo Cesar Beserra; Bevilaqua, Claudia Maria Leal

    2015-09-15

    Strategies for controlling gastrointestinal nematodes have been developed based on the use of numerous alternative methods, including the use of phytotherapy. New formulations of essential oils with anthelmintic activity have been proposed as a means to optimize their biological effects. Thus, the objective of this study was to formulate a nanoemulsion to optimize the nematicide effect of Eucalyptus staigeriana essential oil (EsEO). Initially, physico-chemical analyses were performed to verify the stability of the E. staigeriana nanoemulsion (EsNano). In vitro tests were conducted to evaluate the ovicidal and larvicidal activities of both EsNano and EsEO against Haemonchus contortus, and toxicology tests were then performed on rodents. The EsEO content in the nanoemulsion was 36.4% (v/v), and the mean particle size was 274.3 nm. EsNano and EsEO inhibited larval hatching by 99% and 96.3% at 1 and 2mg/ml concentrations, respectively, and inhibited larval development by 96.3% and 97.3% at 8 mg/ml concentrations. The acute toxicity test revealed that the EsNano and EsEO doses required to kill 50% of the mice (LD50) were 1,603.9 and 3,495.9 mg/ml, respectively. EsNano did not alter the hematological parameters in the rats after treatment.

  12. Intranasal nanoemulsion-based inactivated respiratory syncytial virus vaccines protect against viral challenge in cotton rats

    PubMed Central

    O'Konek, Jessica J; Makidon, Paul E; Landers, Jeffrey J; Cao, Zhengyi; Malinczak, Carrie-Anne; Pannu, Jessie; Sun, Jennifer; Bitko, Vira; Ciotti, Susan; Hamouda, Tarek; Wojcinski, Zbigniew W; Lukacs, Nicholas W; Fattom, Ali; Baker, James R

    2015-01-01

    Respiratory Syncytial Virus is a leading cause of bronchiolitis and pneumonia in infants, the elderly and individuals with compromised immune systems. Despite decades of research, there is currently no available vaccine for RSV. Our group has previously demonstrated that intranasal immunization of mice with RSV inactivated by and adjuvanted with W805EC nanoemulsion elicits robust humoral and cellular immune responses, resulting in protection against RSV infection. This protection was achieved without the induction of airway hyper-reactivity or a Th2-skewed immune response. The cotton rat Sigmodon hispidus has been used for years as an excellent small animal model of RSV disease. Thus, we extended these rodent studies to the more permissive cotton rat model. Intranasal immunization of the nanoemulsion-adjuvanted RSV vaccines induced high antibody titers and a robust Th1-skewed cellular response. Importantly, vaccination provided sterilizing cross-protective immunity against a heterologous RSV challenge and did not induce marked or severe histological effects or eosinophilia in the lung after viral challenge. Overall, these data demonstrate that nanoemulsion-formulated whole RSV vaccines are both safe and effective for immunization in multiple animal models. PMID:26307915

  13. Inactivation of Salmonella on Sprouting Seeds Using a Spontaneous Carvacrol Nanoemulsion Acidified with Organic Acids.

    PubMed

    Landry, Kyle S; Komaiko, Jennifer; Wong, Dana E; Xu, Ting; McClements, David Julian; McLandsborough, Lynne

    2016-07-01

    Over the past decade, demand has increased for natural, minimally processed produce, including sprout-based products. Sanitization with 20,000 ppm of calcium hypochlorite is currently recommended for all sprouting seeds before germination to limit sprout-related foodborne outbreaks. A potentially promising disinfectant as an alternative to calcium hypochlorite is acidified spontaneous essential oil nanoemulsions. In this study, the efficacy of an acidified carvacrol nanoemulsion was tested against mung beans and broccoli seeds artificially contaminated with a Salmonella enterica Enteritidis cocktail (ATCC BAA-709, ATCC BAA-711, and ATCC BAA-1045). Treatments were performed by soaking inoculated seeds in acidified (50 mM acetic or levulinic acid) carvacrol nanoemulsions (4,000 or 8,000 ppm) for 30 or 60 min. After treatment, the number of surviving cells was determined via plate counts and/or the most probable number (MPN) approach. Treatment for 30 min successfully reduced Salmonella Enteritidis by 4 log CFU/g on mung beans (from an initial contamination level of 4.2 to 4.6 log CFU/g) and by 2 log CFU/g on broccoli seeds (from an initial contamination level of 2.4 to 2.6 log CFU/g) to below our detection limit (≤3 MPN/g). Treated seeds were sprouted and tested for the presence of pathogens and sprout yield. The final sprout product had no detectable pathogens, and total sprout yield was not influenced by any treatment.

  14. Paramagnetic fluorinated nanoemulsions for sensitive cellular fluorine-19 magnetic resonance imaging.

    PubMed

    Kislukhin, Alexander A; Xu, Hongyan; Adams, Stephen R; Narsinh, Kazim H; Tsien, Roger Y; Ahrens, Eric T

    2016-06-01

    Fluorine-19 magnetic resonance imaging ((19)F MRI) probes enable quantitative in vivo detection of cell therapies and inflammatory cells. Here, we describe the formulation of perfluorocarbon-based nanoemulsions with improved sensitivity for cellular MRI. Reduction of the (19)F spin-lattice relaxation time (T1) enables rapid imaging and an improved signal-to-noise ratio, thereby improving cell detection sensitivity. We synthesized metal-binding β-diketones conjugated to linear perfluoropolyether (PFPE), formulated these fluorinated ligands as aqueous nanoemulsions, and then metallated them with various transition and lanthanide ions in the fluorous phase. Iron(III) tris-β-diketonate ('FETRIS') nanoemulsions with PFPE have low cytotoxicity (<20%) and superior MRI properties. Moreover, the (19)F T1 can readily be reduced by an order of magnitude and tuned by stoichiometric modulation of the iron concentration. The resulting (19)F MRI detection sensitivity is enhanced by three- to fivefold over previously used tracers at 11.7 T, and is predicted to increase by at least eightfold at the clinical field strength of 3 T. PMID:26974409

  15. Paramagnetic fluorinated nanoemulsions for sensitive cellular fluorine-19 magnetic resonance imaging

    NASA Astrophysics Data System (ADS)

    Kislukhin, Alexander A.; Xu, Hongyan; Adams, Stephen R.; Narsinh, Kazim H.; Tsien, Roger Y.; Ahrens, Eric T.

    2016-06-01

    Fluorine-19 magnetic resonance imaging (19F MRI) probes enable quantitative in vivo detection of cell therapies and inflammatory cells. Here, we describe the formulation of perfluorocarbon-based nanoemulsions with improved sensitivity for cellular MRI. Reduction of the 19F spin-lattice relaxation time (T1) enables rapid imaging and an improved signal-to-noise ratio, thereby improving cell detection sensitivity. We synthesized metal-binding β-diketones conjugated to linear perfluoropolyether (PFPE), formulated these fluorinated ligands as aqueous nanoemulsions, and then metallated them with various transition and lanthanide ions in the fluorous phase. Iron(III) tris-β-diketonate (`FETRIS’) nanoemulsions with PFPE have low cytotoxicity (<20%) and superior MRI properties. Moreover, the 19F T1 can readily be reduced by an order of magnitude and tuned by stoichiometric modulation of the iron concentration. The resulting 19F MRI detection sensitivity is enhanced by three- to fivefold over previously used tracers at 11.7 T, and is predicted to increase by at least eightfold at the clinical field strength of 3 T.

  16. Synergistic Skin Penetration Enhancer and Nanoemulsion Formulations Promote the Human Epidermal Permeation of Caffeine and Naproxen.

    PubMed

    Abd, Eman; Namjoshi, Sarika; Mohammed, Yousuf H; Roberts, Michael S; Grice, Jeffrey E

    2016-01-01

    We examined the extent of skin permeation enhancement of the hydrophilic drug caffeine and lipophilic drug naproxen applied in nanoemulsions incorporating skin penetration enhancers. Infinite doses of fully characterized oil-in-water nanoemulsions containing the skin penetration enhancers oleic acid or eucalyptol as oil phases and caffeine (3%) or naproxen (2%) were applied to human epidermal membranes in Franz diffusion cells, along with aqueous control solutions. Caffeine and naproxen fluxes were determined over 8 h. Solute solubility in the formulations and in the stratum corneum (SC), as well as the uptake of product components into the SC were measured. The nanoemulsions significantly enhanced the skin penetration of caffeine and naproxen, compared to aqueous control solutions. Caffeine maximum flux enhancement was associated with a synergistic increase in both caffeine SC solubility and skin diffusivity, whereas a formulation-increased solubility in the SC was the dominant determinant for increased naproxen fluxes. Enhancements in SC solubility were related to the uptake of the formulation excipients containing the active compounds into the SC. Enhanced skin penetration in these systems is largely driven by uptake of formulation excipients containing the active compounds into the SC with impacts on SC solubility and diffusivity.

  17. Fabrication of polymeric nanocapsules from curcumin-loaded nanoemulsion templates by self-assembly.

    PubMed

    Abbas, Shabbar; Karangwa, Eric; Bashari, Mohanad; Hayat, Khizar; Hong, Xiao; Sharif, Hafiz Rizwan; Zhang, Xiaoming

    2015-03-01

    In this study, biodegradable polymeric nanocapsules were prepared by sequential deposition of food-grade polyelectrolytes through the self-assembling process onto the oil (medium chain triglycerides) droplets enriched with curcumin (lipophilic bioactive compound). Optimum conditions were used to prepare ultrasound-assisted nanoemulsions stabilized by octenyl-succinic-anhydride (OSA)-modified starch. Negatively charged droplets (-39.4 ± 1.84 mV) of these nanoemulsions, having a diameter of 142.7 ± 0.85 nm were used as templates for the fabrication of nanocapsules. Concentrations of layer-forming cationic (chitosan) and anionic (carboxymethylcellulose) biopolymers were optimized based on the mean droplet/particle diameter (MDD/MPD), polydispersity index (PDI) and net charge on the droplets/capsules. Prepared core-shell structures or nanocapsules, having MPD of 159.85 ± 0.92 nm, were characterized by laser diffraction (DLS), ζ-potential (ZP), atomic force microscopy (AFM), transmission electron microscopy (TEM) and confocal laser scanning microscopy (CLSM). Furthermore, physical stability of curcumin-loaded nanocapsules in suspension was determined and compared at different storage temperatures. This study may provide information regarding the formation of ultrasound-assisted polymeric nanocapsules from the nanoemulsion templates which could be helpful in the development of delivery systems for lipophilic food bioactives. PMID:25453208

  18. Nonlinear acoustic enhancement in photoacoustic imaging with wideband absorptive nanoemulsion beads

    NASA Astrophysics Data System (ADS)

    Wei, Chen-wei; Lombardo, Michael; Xia, Jinjun; Pelivanov, Ivan; Perez, Camilo; Larson-Smith, Kjersta; Matula, Thomas J.; Pozzo, Danilo; O'Donnell, Matthew

    2014-03-01

    A nanoemulsion contrast agent with a perfluorohexane core and optically absorptive gold nanospheres (GNSs) assembled on the surface, is presented to improve the specificity of photoacoustic (PA) molecular imaging in differentiating targeted cells or aberrant regions from heterogeneous background signals. Compared to distributed GNSs, clustered GNSs at the emulsion oil-water interface produce a red-shifted and broadened absorption spectrum, exhibiting fairly high absorption in the near-infrared region commonly used for deep tissue imaging. Above a certain laser irradiation fluence threshold, a phase transition creating a microbubble in the emulsion core leads to more than 10 times stronger PA signals compared with conventional thermal-expansion-induced PA signals. These signals are also strongly non-linear, as verified by a differential scheme using recorded PA images at different laser fluences. Assuming a linear relation between laser fluence and the PA signal amplitude, differential processing results in nearly perfect suppression of linear sources, but retains a significant residue for the non-linear nanoemulsion with more than 35 dB enhancement. This result demonstrates that contrast specificity can be improved using the nanoemulsion as a targeting agent in PA molecular imaging by suppressing all background signals related to a linear PA response. Furthermore, combined with a system providing simultaneous laser/ultrasound excitation, cavitation-generated bubbles have the potential to be a highly specific contrast agent for ultrasound molecular imaging and harmonic imaging, as well as a targeted means for noninvasive ultrasound-based therapies.

  19. Cationic Nanoemulsions as a Gene Delivery System: Proof of Concept in the Mucopolysaccharidosis I Murine Model.

    PubMed

    Fraga, Michelle; de Carvalho, Talita Giacomet; Diel, Dirnete da Silva; Kretzmann Filho, Nélson Alexandre; Teixeira, Helder Ferreira; Matte, Ursula

    2015-01-01

    Mucopolysaccharidosis I (MPS I) is an autosomal recessive lysosomal storage disease due to deficient a-L-iduronidase (IDUA) activity. It results in the accumulation of the glycosaminoglycans (GAGs) heparan and dermatan sulfate and leads to several clinical manifestations. This study describes the use of cationic nanoemulsions as a non-viral carrier for the plasmid named pIDUA, which has the gene that encodes for the IDUA enzyme. Cationic nanoemulsions, composed by a medium chain triglycerides oil core stabilized by DOTAP, DOPE and DSPE-PEG, were prepared by high pressure homogeneization. pIDUA was complexed with nanoemulsions in the end of manufacturing process. Physicochemical properties of complexes were influenced by the charge ratio used. From a charge ratio of +2/-, it was observed a total complexation of pIDUA with formulation as well as a protection of plasmid against DNAse I digestion. In vitro assay in fibroblasts of one MPS I patient presented greater and significant trasfection efficiency for pIDUA complexed to formulation in the +4/- charge ratio. This formulation was administered via the tail vein and the portal vein. Animals were compared to untreated MPS I mice. Transfection efficiency was measured as IDUA enzyme activity. After intravenous administration, IDUA activity was significantly higher in lungs and liver. The set of results shows the formulation obtained at the +4/- charge ratio as a promising non-viral gene delivery system, once showed increased enzyme activity both in vitro and in vivo. PMID:26328445

  20. Effects of nisin on the antimicrobial activity of d-limonene and its nanoemulsion.

    PubMed

    Zhang, Zijie; Vriesekoop, Frank; Yuan, Qipeng; Liang, Hao

    2014-05-01

    d-Limonene has been considered to be a safer alternative compared to synthetic antimicrobial food additives. However, its hydrophobic and oxidative nature has limited its application in foods. The purpose of this research was to study effects of nisin on the antimicrobial activity of d-limonene and its nanoemulsion and develop a novel antimicrobial delivery system by combining the positive effect of these two antibacterial agents at the same time. By the checkerboard method, both the synergistic and additive effects of d-limonene and nisin were found against four selected food-related microorganisms. Then, d-limonene nanoemulsion with or without nisin was prepared by catastrophic phase inversion method, which has shown good droplet size and stability. The positive effects and outstanding antimicrobial activity of d-limonene nanoemulsion with nisin were confirmed by MICs comparison, scanning electron microscopy and determination of cell constituents released. Overall, the research described in the current article would be helpful in developing a more effective antimicrobial system for the production and preservation of foods.

  1. Controlled and targeted tumor chemotherapy by ultrasound-activated nanoemulsions/microbubbles

    PubMed Central

    Rapoport, Natalya Y.; Kennedy, Anne M.; Shea, Jill E.; Scaife, Courtney L.; Nam, Kweon-Ho

    2009-01-01

    The paper reports the results of nanotherapy of ovarian, breast, and pancreatic cancerous tumors by paclitaxel-loaded nanoemulsions that convert into microbubbles locally in tumor tissue under the action of tumor-directed therapeutic ultrasound. Tumor accumulation of nanoemulsions was confirmed by ultrasound imaging. Dramatic regression of ovarian, breast, and orthotopic pancreatic tumors was observed in tumor therapy through systemic injections of drug-loaded nanoemulsions combined with therapeutic ultrasound, signifying efficient ultrasound-triggered drug release from tumor-accumulated nanodroplets. The mechanism of drug release in the process of droplet-to-bubble conversion is discussed. No therapeutic effect from the nanodroplet/ultrasound combination was observed without the drug, indicating that therapeutic effect was caused by the ultrasound-enhanced chemotherapeutic action of the tumor-targeted drug, rather than the mechanical or thermal action of ultrasound itself. Tumor recurrence was observed after the completion of the first treatment round; a second treatment round with the same regimen proved less effective, suggesting that drug resistant cells were either developed or selected during the first treatment round. PMID:19477208

  2. In vitro effects of Eucalyptus staigeriana nanoemulsion on Haemonchus contortus and toxicity in rodents.

    PubMed

    Ribeiro, Wesley Lyeverton Correia; Camurça-Vasconcelos, Ana Lourdes Fernandes; Macedo, Iara Tersia Freitas; dos Santos, Jessica Maria Leite; de Araújo-Filho, José Vilemar; Ribeiro, Juliana de Carvalho; Pereira, Vanessa de Abreu; Viana, Daniel de Araújo; de Paula, Haroldo Cesar Beserra; Bevilaqua, Claudia Maria Leal

    2015-09-15

    Strategies for controlling gastrointestinal nematodes have been developed based on the use of numerous alternative methods, including the use of phytotherapy. New formulations of essential oils with anthelmintic activity have been proposed as a means to optimize their biological effects. Thus, the objective of this study was to formulate a nanoemulsion to optimize the nematicide effect of Eucalyptus staigeriana essential oil (EsEO). Initially, physico-chemical analyses were performed to verify the stability of the E. staigeriana nanoemulsion (EsNano). In vitro tests were conducted to evaluate the ovicidal and larvicidal activities of both EsNano and EsEO against Haemonchus contortus, and toxicology tests were then performed on rodents. The EsEO content in the nanoemulsion was 36.4% (v/v), and the mean particle size was 274.3 nm. EsNano and EsEO inhibited larval hatching by 99% and 96.3% at 1 and 2mg/ml concentrations, respectively, and inhibited larval development by 96.3% and 97.3% at 8 mg/ml concentrations. The acute toxicity test revealed that the EsNano and EsEO doses required to kill 50% of the mice (LD50) were 1,603.9 and 3,495.9 mg/ml, respectively. EsNano did not alter the hematological parameters in the rats after treatment. PMID:26233731

  3. Synergistic Skin Penetration Enhancer and Nanoemulsion Formulations Promote the Human Epidermal Permeation of Caffeine and Naproxen.

    PubMed

    Abd, Eman; Namjoshi, Sarika; Mohammed, Yousuf H; Roberts, Michael S; Grice, Jeffrey E

    2016-01-01

    We examined the extent of skin permeation enhancement of the hydrophilic drug caffeine and lipophilic drug naproxen applied in nanoemulsions incorporating skin penetration enhancers. Infinite doses of fully characterized oil-in-water nanoemulsions containing the skin penetration enhancers oleic acid or eucalyptol as oil phases and caffeine (3%) or naproxen (2%) were applied to human epidermal membranes in Franz diffusion cells, along with aqueous control solutions. Caffeine and naproxen fluxes were determined over 8 h. Solute solubility in the formulations and in the stratum corneum (SC), as well as the uptake of product components into the SC were measured. The nanoemulsions significantly enhanced the skin penetration of caffeine and naproxen, compared to aqueous control solutions. Caffeine maximum flux enhancement was associated with a synergistic increase in both caffeine SC solubility and skin diffusivity, whereas a formulation-increased solubility in the SC was the dominant determinant for increased naproxen fluxes. Enhancements in SC solubility were related to the uptake of the formulation excipients containing the active compounds into the SC. Enhanced skin penetration in these systems is largely driven by uptake of formulation excipients containing the active compounds into the SC with impacts on SC solubility and diffusivity. PMID:26554868

  4. Intranasal nanoemulsion-based inactivated respiratory syncytial virus vaccines protect against viral challenge in cotton rats.

    PubMed

    O'Konek, Jessica J; Makidon, Paul E; Landers, Jeffrey J; Cao, Zhengyi; Malinczak, Carrie-Anne; Pannu, Jessie; Sun, Jennifer; Bitko, Vira; Ciotti, Susan; Hamouda, Tarek; Wojcinski, Zbigniew W; Lukacs, Nicholas W; Fattom, Ali; Baker, James R

    2015-01-01

    Respiratory Syncytial Virus is a leading cause of bronchiolitis and pneumonia in infants, the elderly and individuals with compromised immune systems. Despite decades of research, there is currently no available vaccine for RSV. Our group has previously demonstrated that intranasal immunization of mice with RSV inactivated by and adjuvanted with W805EC nanoemulsion elicits robust humoral and cellular immune responses, resulting in protection against RSV infection. This protection was achieved without the induction of airway hyper-reactivity or a Th2-skewed immune response. The cotton rat Sigmodon hispidus has been used for years as an excellent small animal model of RSV disease. Thus, we extended these rodent studies to the more permissive cotton rat model. Intranasal immunization of the nanoemulsion-adjuvanted RSV vaccines induced high antibody titers and a robust Th1-skewed cellular response. Importantly, vaccination provided sterilizing cross-protective immunity against a heterologous RSV challenge and did not induce marked or severe histological effects or eosinophilia in the lung after viral challenge. Overall, these data demonstrate that nanoemulsion-formulated whole RSV vaccines are both safe and effective for immunization in multiple animal models. PMID:26307915

  5. Stable nanoemulsions prepared via interfacial solidification of amphiphilic polyether-polyester block copolymers.

    PubMed

    Kim, Trang Huyen Le; Jun, Hwiseok; Kim, Jee Seon; Nam, Yoon Sung

    2015-04-01

    Oil-in-water (O/W) emulsions are generally stabilized by water-soluble surfactants, which anchor to the surface of oil droplets dispersed in an aqueous solution. Our recent work introduced a new approach to stabilize nanoemulsions through the formation of a semi-solid interphase at the O/W interface using a water-insoluble amphiphilic block copolymer, methoxy poly(ethylene glycol)-block-poly(ɛ-caprolactone). However, the approach is not applicable to relatively non-polar oils due to the quick precipitation of the hydrophobic PCL block within the oil phase. Here we report on successful stabilization of non-polar liquid paraffin nanoemulsions using an amphiphilic copolymers having a new hydrophobic block comprising ɛ-caprolactone and L-lactide. The new block copolymer was reorganized at the O/W interface of liquid paraffin, generating stable nano-sized emulsions via the formation of a robust semi-solid polymeric barrier. The prepared nanoemulsions show excellent dispersion stability even under a high level of mechanical stresses during freeze/thaw cycles.

  6. Inactivation of Salmonella on Sprouting Seeds Using a Spontaneous Carvacrol Nanoemulsion Acidified with Organic Acids.

    PubMed

    Landry, Kyle S; Komaiko, Jennifer; Wong, Dana E; Xu, Ting; McClements, David Julian; McLandsborough, Lynne

    2016-07-01

    Over the past decade, demand has increased for natural, minimally processed produce, including sprout-based products. Sanitization with 20,000 ppm of calcium hypochlorite is currently recommended for all sprouting seeds before germination to limit sprout-related foodborne outbreaks. A potentially promising disinfectant as an alternative to calcium hypochlorite is acidified spontaneous essential oil nanoemulsions. In this study, the efficacy of an acidified carvacrol nanoemulsion was tested against mung beans and broccoli seeds artificially contaminated with a Salmonella enterica Enteritidis cocktail (ATCC BAA-709, ATCC BAA-711, and ATCC BAA-1045). Treatments were performed by soaking inoculated seeds in acidified (50 mM acetic or levulinic acid) carvacrol nanoemulsions (4,000 or 8,000 ppm) for 30 or 60 min. After treatment, the number of surviving cells was determined via plate counts and/or the most probable number (MPN) approach. Treatment for 30 min successfully reduced Salmonella Enteritidis by 4 log CFU/g on mung beans (from an initial contamination level of 4.2 to 4.6 log CFU/g) and by 2 log CFU/g on broccoli seeds (from an initial contamination level of 2.4 to 2.6 log CFU/g) to below our detection limit (≤3 MPN/g). Treated seeds were sprouted and tested for the presence of pathogens and sprout yield. The final sprout product had no detectable pathogens, and total sprout yield was not influenced by any treatment. PMID:27357030

  7. Anti-cariogenic effect of a cetylpyridinium chloride-containing nanoemulsion

    PubMed Central

    Lee, Valerie A.; Karthikeyan, Ramalingam; Rawls, H. Ralph; Amaechi, Bennett T.

    2010-01-01

    Objectives The aim of this pilot study was to investigate the anticaries activity of a nanoemulsion composed of soybean oil, water, Triton X-100 and cetylpyridinium chloride. Methods Tooth blocks (3 mm length × 3 mm width × 2 mm thickness) were cut from smooth surfaces of selected molar teeth using a water-cooled diamond wire saw. The blocks were randomly assigned to three experimental groups, (A) nanoemulsion, (B) 0.12% chlorhexidine gluconate, and (C) no treatment. The formation of dental caries in human tooth enamel was tested using a continuous flow dual-organism (Streptococcus mutans and Lactobacillus casei), biofilm model, which acts as an artificial mouth and simulates the biological and physiological activities observed within the oral environment. Experimental groups A and B were treated with their respective solutions once daily for 30 seconds on each occasion, while group C received no treatment. 10% sucrose was supplied every 6 hours for 6 minutes to simulate meals and pH cycling. The experiment lasted for 5 days, and the tooth blocks were harvested and processed for demineralization assessment using transverse microradiography (TMR). Results For both lesion depth and mineral loss, statistical analysis indicated that Emulsion was significantly lower than Control and Chlorhexidine, and Chlorhexidine was significantly lower than Control. Conclusions We conclude that cetylpyridinium-containing nanoemulsions appear to present a feasible means of preventing the occurrence of early caries. PMID:20600554

  8. Stable nanoemulsions prepared via interfacial solidification of amphiphilic polyether-polyester block copolymers.

    PubMed

    Kim, Trang Huyen Le; Jun, Hwiseok; Kim, Jee Seon; Nam, Yoon Sung

    2015-04-01

    Oil-in-water (O/W) emulsions are generally stabilized by water-soluble surfactants, which anchor to the surface of oil droplets dispersed in an aqueous solution. Our recent work introduced a new approach to stabilize nanoemulsions through the formation of a semi-solid interphase at the O/W interface using a water-insoluble amphiphilic block copolymer, methoxy poly(ethylene glycol)-block-poly(ɛ-caprolactone). However, the approach is not applicable to relatively non-polar oils due to the quick precipitation of the hydrophobic PCL block within the oil phase. Here we report on successful stabilization of non-polar liquid paraffin nanoemulsions using an amphiphilic copolymers having a new hydrophobic block comprising ɛ-caprolactone and L-lactide. The new block copolymer was reorganized at the O/W interface of liquid paraffin, generating stable nano-sized emulsions via the formation of a robust semi-solid polymeric barrier. The prepared nanoemulsions show excellent dispersion stability even under a high level of mechanical stresses during freeze/thaw cycles. PMID:25585162

  9. Acoustic Droplet Vaporization, Cavitation, and Therapeutic Properties of Copolymer-Stabilized Perfluorocarbon Nanoemulsions

    SciTech Connect

    Nam, Kweon-Ho; Christensen, Douglas A.; Rapoport, Natalya; Kennedy, Anne M.

    2009-04-14

    Acoustic and therapeutic properties of Doxorubicin (DOX) and paclitaxel (PTX)-loaded perfluorocarbon nanoemulsions have been investigated in a mouse model of ovarian cancer. The nanoemulsions were stabilized by two biodegradable amphiphilic block copolymers that differed in the structure of the hydrophobic block. Acoustic droplet vaporization (ADV) and cavitation parameters were measured as a function of ultrasound frequency, pressure, duty cycles, and temperature. The optimal parameters that induced ADV and inertial cavitation of the formed microbubbles were used in vivo in the experiments on the ultrasound-mediated chemotherapy of ovarian cancer. A combination tumor treatment by intravenous injections of drug-loaded perfluoropentane nanoemulsions and tumor-directed 1-MHz ultrasound resulted in a dramatic decrease of ovarian or breast carcinoma tumor volume and sometimes complete tumor resolution. However, tumors often recurred three to six weeks after the treatment indicating that some cancer cells survived the treatment. The recurrent tumors proved more aggressive and resistant to the repeated therapy than initial tumors suggesting selection for the resistant cells during the first treatment.

  10. Improved absorption and in vivo kinetic characteristics of nanoemulsions containing evodiamine–phospholipid nanocomplex

    PubMed Central

    Hu, Jiangbo; Chen, Dilong; Jiang, Rong; Tan, Qunyou; Zhu, Biyue; Zhang, Jingqing

    2014-01-01

    Purpose The purpose of this study was to assess the improved absorption and in vivo kinetic characteristics of a novel water-in-oil nanoemulsion containing evodiamine–phospholipid nanocomplex (NEEPN) when administered orally. Methods NEEPN was fabricated by loading an evodiamine–phospholipid nanocomplex into a water-in-oil nanoemulsive system. The gastrointestinal absorption of NEEPN was investigated using an in situ perfusion method. The modified in vivo kinetic characteristics of evodiamine (EDA) in NEEPN were also evaluated. Results Compared with EDA or conventional nanoemulsions containing EDA instead of evodiamine–phospholipid complex, NEEPN with its favorable in vivo kinetic characteristics clearly enhanced the gastrointestinal absorption and oral bioavailability of EDA; for example, the relative bioavailability of NEEPN to free EDA was calculated to be 630.35%, and the effective permeability of NEEPN in the colon was 8.64-fold that of EDA. Conclusion NEEPN markedly improved the oral bioavailability of EDA, which was probably due to its increased gastrointestinal absorption. NEEPN also increased efficacy and reduced adverse effects for oral delivery of EDA. Such finding demonstrates great clinical significance as an ideal drug delivery system demands high efficacy and no adverse effects. PMID:25258531

  11. Bio-based nanoemulsion formulation, characterization and antibacterial activity against food-borne pathogens.

    PubMed

    Sugumar, Saranya; Nirmala, Joyce; Ghosh, Vijayalakshmi; Anjali, Haridasan; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2013-08-01

    The current study deals with the formulation and characterization of bio-based oil in water nanoemulsion and its potential antibacterial activity. A typical v/v% of eucalyptus oil (16.66%), Tween 80 (16.66%), and water (68.68%) was prepared by ultrasonication method. The mean droplet size was 17.1 nm as confirmed by dynamic light scattering. Different concentrations of the formulation ranging from undiluted to 10-, 100-, and 1000-fold dilutions were used to check the antibacterial activity in three different microorganisms, namely, Bacillus cereus, Staphylococcus aureus (Gram-positive), and Escherichia coli (Gram-negative). All three species showed a 100% bactericidal at the 10-fold dilution of the nanoemulsion formulation in the following order: B. cereus at 0th min, S. aureus at 15 min and E. coli at 1 h, respectively. A 10-fold dilution of the nanoemulsion showed that, the cytoplasmic content leakage from the bacterial species was high for S. aureus when compared to B. cereus and E. coli as determined by UV-Vis spectroscopic method. Fluorescence microscopic technique further confirmed this study.

  12. Effects of nisin on the antimicrobial activity of d-limonene and its nanoemulsion.

    PubMed

    Zhang, Zijie; Vriesekoop, Frank; Yuan, Qipeng; Liang, Hao

    2014-05-01

    d-Limonene has been considered to be a safer alternative compared to synthetic antimicrobial food additives. However, its hydrophobic and oxidative nature has limited its application in foods. The purpose of this research was to study effects of nisin on the antimicrobial activity of d-limonene and its nanoemulsion and develop a novel antimicrobial delivery system by combining the positive effect of these two antibacterial agents at the same time. By the checkerboard method, both the synergistic and additive effects of d-limonene and nisin were found against four selected food-related microorganisms. Then, d-limonene nanoemulsion with or without nisin was prepared by catastrophic phase inversion method, which has shown good droplet size and stability. The positive effects and outstanding antimicrobial activity of d-limonene nanoemulsion with nisin were confirmed by MICs comparison, scanning electron microscopy and determination of cell constituents released. Overall, the research described in the current article would be helpful in developing a more effective antimicrobial system for the production and preservation of foods. PMID:24360455

  13. Vitamin E derivative-based multifunctional nanoemulsions for overcoming multidrug resistance in cancer.

    PubMed

    Zheng, Nannan; Gao, Yanan; Ji, Hongyu; Wu, Linhua; Qi, Xuejing; Liu, Xiaona; Tang, Jingling

    2016-08-01

    The multidrug resistance (MDR), including intrinsic and acquired multidrug resistance, is a major problem in tumor chemotherapy. Here, we proposed a strategy for modulating intrinsic and/or acquired multidrug resistance by altering the levels of Bax and Bcl-2 expression and inhibiting the transport function of P-gp, increasing the intracellular concentration of its substrate anticancer drugs. Vitamin E derivative-based nanoemulsions containing paclitaxel (MNEs-PTX) were fabricated in this study, and in vitro anticancer efficacy of the nanoemulsion system was evaluated in the paclitaxel-resistant human ovarian carcinoma cell line A2780/Taxol. The MNEs-PTX exhibited a remarkably enhanced antiproliferation effect on A2780/Taxol cells than free paclitaxel (PTX) (p < 0.01). Compared with that in the Taxol group, MNEs-PTX further decreased mitochondrial potential. Vitamin E derivative-based multifunctional nanoemulsion (MNEs) obviously increased intracellular accumulation of rhodamine 123 (P-gp substrate). Overexpression of Bcl-2 is generally associated with tumor drug resistance, we found that MNEs could reduce Bcl-2 protein level and increase Bax protein level. Taken together, our findings suggest that anticancer drugs associated with MNEs could play a role in the development of MDR in cancers. PMID:26710274

  14. Ritodrine-induced pustular eruptions distinctly resembling impetigo herpetiformis.

    PubMed

    Kuwabara, Yoshimitsu; Sato, Atsuki; Abe, Hiroko; Abe, Sumino; Kawai, Naoki; Takeshita, Toshiyuki

    2011-01-01

    A 27-year-old nulligravida woman without a history of dermatosis was hospitalized for threatened preterm labor at 29 weeks' gestation; therefore, continuous infusion of ritodrine hydrochloride was started. At 31 weeks' gestation, erythematous plaques appeared and spread over the body surface; therefore, a topical steroid preparation was applied. At 32 weeks' gestation, the eruptions developed into irregular annular areas of erythema with multiple pustules accompanied by severe itching, and oral prednisolone treatment was started. Bacterial cultures of the pustules were negative, and a crural cutaneous biopsy revealed Kogoj's spongiform pustules. Based on the clinicopathological findings, the most likely diagnosis was impetigo herpetiformis, which causes cutaneous symptoms closely resembling pustular psoriasis in pregnant females without a history of psoriasis. To rule out ritodrine-induced pustular eruptions, the ritodrine infusion was stopped and treatment with an MgSO(4) preparation was started at 33 weeks' 3 days' gestation; however, the uterine contractions could not be suppressed. Because of the patient's highly edematous, severely painful feet, a cesarean section was performed the same day. Within several days of delivery, the eruptions began to resolve, and no recurrence was observed after treatment with oral prednisolone was stopped 31 days after delivery. On the basis of a positive patch test for ritodrine, we diagnosed pustular drug eruptions caused by ritodrine hydrochloride. Although ritodrine-induced pathognomonic cutaneous eruptions are rare, we would like to emphasize that ritodrine can cause drug-induced pustular eruptions distinctly resembling life-threatening impetigo herpetiformis.

  15. [Osteoid osteoma of the wrist joint resembling tenosynovitis].

    PubMed

    Volpin, Gershon; Shtarker, Haim; Oliver, Simon; Katznelson, Alexander; Stahl, Shalom

    2006-12-01

    Osteoid osteoma of bones of the wrist joint is a relatively rare lesion. This article presents a series of three patients, one with osteoid osteoma of the styloid process of the radius and two with osteoid osteoma of the capitate bone. All of them had clinical symptoms resembling those of stenosing tenosynovitis of the wrist joint. X-rays, tomography and bone scan revealed the characteristic findings of osteoid osteoma. Histological examination confirmed the diagnosis. Treatment consisted of "en bloc" excision of these tumors. Following surgery patients were asymptomatic and had normal mobility of the affected wrist. In the first patient this has been maintained for the succeeding 27 years. It is suggested that in any case of persistent unexplained pain of the wrist or clinical symptoms resembling those of tenosynovitis, osteoid osteoma of the styloid process of the radius or of the carpal bones should also be included in the differential diagnosis. The recommended treatment of osteoid osteoma is "en bloc" excision of this tumour in the affected bone, resulting in complete relief of pain and absence of functional disturbances. PMID:17220026

  16. Ritodrine-induced pustular eruptions distinctly resembling impetigo herpetiformis.

    PubMed

    Kuwabara, Yoshimitsu; Sato, Atsuki; Abe, Hiroko; Abe, Sumino; Kawai, Naoki; Takeshita, Toshiyuki

    2011-01-01

    A 27-year-old nulligravida woman without a history of dermatosis was hospitalized for threatened preterm labor at 29 weeks' gestation; therefore, continuous infusion of ritodrine hydrochloride was started. At 31 weeks' gestation, erythematous plaques appeared and spread over the body surface; therefore, a topical steroid preparation was applied. At 32 weeks' gestation, the eruptions developed into irregular annular areas of erythema with multiple pustules accompanied by severe itching, and oral prednisolone treatment was started. Bacterial cultures of the pustules were negative, and a crural cutaneous biopsy revealed Kogoj's spongiform pustules. Based on the clinicopathological findings, the most likely diagnosis was impetigo herpetiformis, which causes cutaneous symptoms closely resembling pustular psoriasis in pregnant females without a history of psoriasis. To rule out ritodrine-induced pustular eruptions, the ritodrine infusion was stopped and treatment with an MgSO(4) preparation was started at 33 weeks' 3 days' gestation; however, the uterine contractions could not be suppressed. Because of the patient's highly edematous, severely painful feet, a cesarean section was performed the same day. Within several days of delivery, the eruptions began to resolve, and no recurrence was observed after treatment with oral prednisolone was stopped 31 days after delivery. On the basis of a positive patch test for ritodrine, we diagnosed pustular drug eruptions caused by ritodrine hydrochloride. Although ritodrine-induced pathognomonic cutaneous eruptions are rare, we would like to emphasize that ritodrine can cause drug-induced pustular eruptions distinctly resembling life-threatening impetigo herpetiformis. PMID:22041881

  17. Design and formulation of nanoemulsions using 2-(poly(hexafluoropropylene oxide)) perfluoropropyl benzene in combination with linear perfluoro(polyethylene glycol dimethyl ether)

    PubMed Central

    Mountain, Gregory A.; Jelier, Benson J.; Bagia, Christina; Friesen, Chadron M.; Janjic, Jelena M.

    2014-01-01

    This is the first report where PFPAE aromatic conjugates and perfluoro(polyethylene glycol dimethyl ether) are combined and formulated as nanoemulsions with droplet size below 100 nm. A perfluoropolyalkylether (PFPAE) aromatic conjugate, 2-(poly(hexafluoropropylene oxide)) perfluoropropyl benzene, was used as fluorophilic-hydrophilic diblock (FLD) aimed at stabilizing perfluoro(polyethylene glycol dimethyl ether) nanoemulsions. Its effects on colloidal behaviors in triphasic (organic/fluorous/aqueous) nanoemulsions were studied. The addition of FLD construct to fluorous phase led to decrease in PFPAE nanoemulsion droplet size to as low as 85 nm. Prepared nanoemulsions showed high colloidal stability. Our results suggest that these materials represent viable novel approach to fluorous colloid systems design with potential for biomedical and synthetic applications. PMID:24976645

  18. Ultrasonic emulsification of eucalyptus oil nanoemulsion: antibacterial activity against Staphylococcus aureus and wound healing activity in Wistar rats.

    PubMed

    Sugumar, Saranya; Ghosh, Vijayalakshmi; Nirmala, M Joyce; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2014-05-01

    The plant derived essential oil nanoemulsion was prepared using a mixture of components containing eucalyptus oil as organic phase, water as continuous phase, and non ionic surfactant, Tween 80, as emulsifier at a particular proportion of 1:1 v/v%. The ultrasonication was applied for varied processing time from 0 to 30 min to study the effect of time on the formation of nanoemulsion and physical stability of formulation by this method. The transparency and stability of emulsion was enhanced when the sonication time was increased compared to hand blender emulsion. The most stable nanoemulsion was obtained in 30 min sonication having the mean droplet diameter of 3.8 nm. The antibacterial studies of nanoemulsion against Staphylococcus aureus by time kill analysis showed complete loss of viability within 15 min of interaction. Observations from scanning electron microscopy of treated bacterial cells confirmed the membrane damage compared to control bacteria. Furthermore, the wound healing potential and skin irritation activity of the formulated nanoemulsion in Wistar rats, suggested non-irritant and higher wound contraction rate with respect to control and neomycin treated rats. These results proposed that the formulated system could be favourable for topical application in pharmaceutical industries.

  19. Formulation of saponin stabilized nanoemulsion by ultrasonic method and its role to protect the degradation of quercitin from UV light.

    PubMed

    Kaur, Khushwinder; Kumar, Raj; Mehta, S K

    2016-07-01

    The objective of the present study was to prepare quercitin (QT) loaded o/w nanoemulsion using food grade surfactants (saponin and tween 80). The prepared nanoemulsion) was stable up to 30 days. The average particle size of the nanoemulsion was 52 ± 10 nm. The formation of saponin stabilized nanoemulsion was confirmed by transmission electron microscopy. Quercitin (QT) trapped nanoemulsion showed higher stability on exposure to UV light (254 nm) as compared to water/ethanol system. The degradation rate was found to decrease from 9 ± 1%, 11 ± 1% at pH 7.4, 8.0 respectively as compared to 42 ± 2% in water/ethanol system. Attempt was also made to study the interaction of QT with two different bile salts (sodium cholate and sodium taurocholate). The free radical scavenging activity of DPPH quercitin and curcumin was compared in NEm media. The obtained IC50 value of quercitin, curcumin and ascorbic acid are 28.88 ± 1, 45.53 ± 2 and 51.51 ± 2 μM respectively. The values of binding constant for sodium cholate (NaC) and sodium taurocholate (NaTC) are 2.66 × 10(5) and 2.72 × 10(4) M(-1) respectively. Sodium cholate (NaC) was found to show strong interaction towards quercitin (QT) due to more electron density on oxygen atom of carboxylate ion. PMID:26964921

  20. Ultrasonic emulsification of eucalyptus oil nanoemulsion: antibacterial activity against Staphylococcus aureus and wound healing activity in Wistar rats.

    PubMed

    Sugumar, Saranya; Ghosh, Vijayalakshmi; Nirmala, M Joyce; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2014-05-01

    The plant derived essential oil nanoemulsion was prepared using a mixture of components containing eucalyptus oil as organic phase, water as continuous phase, and non ionic surfactant, Tween 80, as emulsifier at a particular proportion of 1:1 v/v%. The ultrasonication was applied for varied processing time from 0 to 30 min to study the effect of time on the formation of nanoemulsion and physical stability of formulation by this method. The transparency and stability of emulsion was enhanced when the sonication time was increased compared to hand blender emulsion. The most stable nanoemulsion was obtained in 30 min sonication having the mean droplet diameter of 3.8 nm. The antibacterial studies of nanoemulsion against Staphylococcus aureus by time kill analysis showed complete loss of viability within 15 min of interaction. Observations from scanning electron microscopy of treated bacterial cells confirmed the membrane damage compared to control bacteria. Furthermore, the wound healing potential and skin irritation activity of the formulated nanoemulsion in Wistar rats, suggested non-irritant and higher wound contraction rate with respect to control and neomycin treated rats. These results proposed that the formulated system could be favourable for topical application in pharmaceutical industries. PMID:24262758

  1. Formation and stability of D-limonene organogel-based nanoemulsion prepared by a high-pressure homogenizer.

    PubMed

    Zahi, Mohamed Reda; Wan, Pingyu; Liang, Hao; Yuan, Qipeng

    2014-12-31

    D-limonene organogel-based nanoemulsion was prepared by high-pressure homogenization technology. The organogelator type had a major role on the formation of the formulations, in which stearic acid has given nanoemulsions with the smallest droplet size. The surfactant type and concentration also had an appreciable effect on droplet formation, with Tween 80 giving a mean droplet diameter (d ≈ 112 nm) among a range of non-ionic surfactants (Tween 20, 40, 60, 80, and 85). In addition, high-pressure homogenization conditions played a key role in the nanoemulsion preparation. The stability of d-limonene organogel-based nanoemulsion was also investigated under two different temperatures (4 and 28 °C) through 2 weeks of storage. Results showed a good stability of the formulations, which is maybe due to the incorporation of D-limonene into the organogel prior to homogenization. This study may have a valuable contribution for the design and use of organogel-based nanoemulsion as a delivery system in food.

  2. Development and in vitro evaluation of a nanoemulsion for transcutaneous delivery

    PubMed Central

    Ledet, Grace; Pamujula, Sarala; Walker, Valencia; Simon, Shana; Graves, Richard; Mandal, Tarun K.

    2013-01-01

    Objective The purpose of this study is to develop a nanoemulsion formulation for its use as a transcutaneous vaccine delivery system. Materials and methods With bovine albumin-fluorescein isothiocyanate conjugate (FITC-BSA) as a vaccine model, formulations were selected with the construction of pseudo-ternary phase diagrams and a short-term stability study. The size of the emulsion droplets was furthered optimized with high-pressure homogenization. The optimized formulation was evaluated for its skin permeation efficiency. In vitro skin permeation studies were conducted with shaved BALB/c mice skin samples with a Franz diffusion cell system. Different drug concentrations were compared, and the effect of the nanoemulsion excipients on the permeation of the FITC-BSA was also studied. Results The optimum homogenization regime was determined to be five passes at 20 000 psi, with no evidence of protein degradation during processing. With these conditions, the particle diameter was 85.2 nm ± 15.5 nm with a polydispersity index of 0.186 ± 0.026 and viscosity of 14.6 cP ± 1.2 cP. The optimized formulation proved stable for 1 year at 4 °C. In vitro skin diffusion studies show that the optimized formulation improves the permeation of FITC-BSA through skin with an enhancement ratio of 4.2 compared to a neat control solution. Finally, a comparison of the skin permeation of the nanoemulsion versus only the surfactant excipients resulted in a steady state flux of 23.44 μg/cm2/h for the nanoemulsion as opposed to 6.10 μg/cm2/h for the emulsifiers. Conclusion A novel nanoemulsion with optimized physical characteristics and superior skin permeation compared to control solution was manufactured. The formulation proposed in this study has the flexibility for the incorporation of a variety of active ingredients and warrants further development as a transcutaneous vaccine delivery vehicle. PMID:23600657

  3. Characteristics of spontaneously formed nanoemulsions in octane/AOT/brine systems.

    PubMed

    Kini, Gautam C; Biswal, Sibani Lisa; Wong, Michael S; Miller, Clarence A

    2012-11-01

    Nanoemulsions were formed spontaneously by diluting water-in-oil (W/O) or brine-in-oil (B/O) microemulsions of a hydrocarbon (octane), anionic surfactant (Aerosol-OT or AOT) and water or NaCl brine in varying levels of excess brine. The water-continuous nanoemulsions were characterized by interfacial tension, dynamic light scattering, electrophoresis, optical microscopy and phase-behavior studies. The mechanism of emulsification was local supersaturation and resulting nucleation of oil during inversion. For nanoemulsions formed at low salinities with Winsor I phase behavior, octane drops grew from initial diameters of 150-250 nm to 480-1000 nm over 24h, depending on salinity. Growth was caused by mass transfer but seemed to approach the asymptotic stage of Ostwald ripening described by the Lifshitz-Slyozov-Wagner (LSW) theory only for dilution with salt-free water. Near the higher cross-over salinity (Winsor III), the nanoemulsions showed much slower growth with droplet size consistently remaining below 200 nm over 24h and reaching 250 nm after 1 week. Birefringence indicated the presence of liquid crystal for these conditions, which could have contributed to the slow growth rate. At even higher salinity levels in the Winsor II domain, W/O/W multiple emulsions having drops greater than 1 μm in diameter were consistently recorded for the first 5-7h, after which size decreased to values below 1 μm. The number and size of internal water droplets in multiple emulsion drops was found to decrease over time, suggesting coalescence of internal droplets with the continuous water phase and mass transfer of water from internal droplets to continuous phase as possible mechanisms of the observed drop shrinkage. Electrophoresis studies showed the nanoemulsions to be highly negatively charged (zeta potentials of -60 mV to -120 mV). The high charge on octane droplets helped assure stability to flocculation and coalescence, thereby allowing mass transfer to control growth in the

  4. Characteristics of spontaneously formed nanoemulsions in octane/AOT/brine systems.

    PubMed

    Kini, Gautam C; Biswal, Sibani Lisa; Wong, Michael S; Miller, Clarence A

    2012-11-01

    Nanoemulsions were formed spontaneously by diluting water-in-oil (W/O) or brine-in-oil (B/O) microemulsions of a hydrocarbon (octane), anionic surfactant (Aerosol-OT or AOT) and water or NaCl brine in varying levels of excess brine. The water-continuous nanoemulsions were characterized by interfacial tension, dynamic light scattering, electrophoresis, optical microscopy and phase-behavior studies. The mechanism of emulsification was local supersaturation and resulting nucleation of oil during inversion. For nanoemulsions formed at low salinities with Winsor I phase behavior, octane drops grew from initial diameters of 150-250 nm to 480-1000 nm over 24h, depending on salinity. Growth was caused by mass transfer but seemed to approach the asymptotic stage of Ostwald ripening described by the Lifshitz-Slyozov-Wagner (LSW) theory only for dilution with salt-free water. Near the higher cross-over salinity (Winsor III), the nanoemulsions showed much slower growth with droplet size consistently remaining below 200 nm over 24h and reaching 250 nm after 1 week. Birefringence indicated the presence of liquid crystal for these conditions, which could have contributed to the slow growth rate. At even higher salinity levels in the Winsor II domain, W/O/W multiple emulsions having drops greater than 1 μm in diameter were consistently recorded for the first 5-7h, after which size decreased to values below 1 μm. The number and size of internal water droplets in multiple emulsion drops was found to decrease over time, suggesting coalescence of internal droplets with the continuous water phase and mass transfer of water from internal droplets to continuous phase as possible mechanisms of the observed drop shrinkage. Electrophoresis studies showed the nanoemulsions to be highly negatively charged (zeta potentials of -60 mV to -120 mV). The high charge on octane droplets helped assure stability to flocculation and coalescence, thereby allowing mass transfer to control growth in the

  5. Uterine tumors resembling ovarian sex cord tumors: an update.

    PubMed

    Czernobilsky, Bernard

    2008-04-01

    Tumors of the uterus resembling ovarian sex cord tumors were reported by Clement and Scully in 1976 and were divided in 2 groups: group 1, endometrial stromal tumors, and group 2, mural uterine tumors-both with elements resembling ovarian sex cord tumors. In the former, the sex cord component constitutes a minor portion of an endometrial stromal neoplasm, whereas in the latter, it is the predominant or exclusive component of a uterine wall lesion composed of a variety of mesenchymal elements. An origin from endometrial stromal cells, adenomyosis, stromal myosis, endometriosis, or multipotential cells within the myometrium was postulated in both groups of tumors. In group 1 tumors, the prognosis depends on the type, grade, and stage of the underlying stromal neoplasm. Group 2 tumors seemed to be benign, although because of the occasional recurrence of these tumors, they should be considered of low-grade malignant potential. In recent years, the histological features in group 2 were found to be much more varied than those in group 1 and consisted among others of retiform areas, glomeruloid structures, and Leydig-like cells. In group 1 tumors, the sex cord elements remained limited to cords, trabeculae, nests, and tubules. Eventually, the abbreviation ESTSCLE, or endometrial stromal tumors with sex cord-like elements, was given to group 1 tumors, whereas UTROSCT, or uterine tumor resembling ovarian sex cord tumor, was used for group 2 tumors. The most significant information in recently conducted studies concerns the immunophenotype of these lesions especially of UTROSCT. Out of the plethora of the immunohistochemical stains, a panel of 4 including calretinin, inhibin, CD99, and Melan A has emerged which seemed to be the most characteristic sex cord markers. Positivity for calretinin and at least for 1 of the other above-mentioned markers may thus confirm the diagnosis of UTROSCT. Endometrial stromal tumors with sex cord-like elements, on the other hand, usually

  6. The family resemblance metaphor: some unfinished business of interpretive inquiry.

    PubMed

    Miller, S I; Fredericks, M

    2000-07-01

    The rapidly expanding discipline of interpretive inquiry, especially in its narrative analysis form, has not been fully cognizant of certain crucial epistemological and methodological assumptions that form the ultimate basis of its purpose. Even after abandoning traditional positivist views, the related disciplines within the human sciences that are engaged in interpretive inquiry have still not discovered the core implicit assumptions that militate against a full acceptance of this form of inquiry. This article outlines the locus of these implicit assumptions and then argues that the legitimacy of these enterprises must be grounded in a well-known but heretofore undiscovered perspective, namely, Wittgenstein's notion of a family resemblance. It is argued that this metaphoric phrase is the key to unlocking the real and unique nature of narrative analysis. PMID:11010071

  7. Muscular dystrophy in a dog resembling human becker muscular dystrophy.

    PubMed

    Baroncelli, A B; Abellonio, F; Pagano, T B; Esposito, I; Peirone, B; Papparella, S; Paciello, O

    2014-05-01

    A 3-year-old, male Labrador retriever dog was presented with clinical signs of progressive exercise intolerance, bilateral elbow extension, rigidity of the forelimbs, hindlimb flexion and kyphosis. Microscopical examination of muscle tissue showed marked variability in myofibre size, replacement of muscle with mature adipose tissue and degeneration/regeneration of muscle fibres, consistent with muscular dystrophy. Immunohistochemical examination for dystrophin showed markedly reduced labelling with monoclonal antibodies specific for the rod domain and the carboxy-terminal of dystrophin, while expression of β-sarcoglycan, γ-sarcoglycan and β-dystroglycan was normal. Immunoblotting revealed a truncated dystrophin protein of approximately 135 kDa. These findings supported a diagnosis of congenital canine muscular dystrophy resembling Becker muscular dystrophy in man.

  8. Curcuminoids-loaded lipid nanoparticles: novel approach towards malaria treatment.

    PubMed

    Nayak, Aditya P; Tiyaboonchai, Waree; Patankar, Swati; Madhusudhan, Basavaraj; Souto, Eliana B

    2010-11-01

    In the present work, curcuminoids-loaded lipid nanoparticles for parenteral administration were successfully prepared by a nanoemulsion technique employing high-speed homogenizer and ultrasonic probe. For the production of nanoparticles, trimyristin, tristerin and glyceryl monostearate were selected as solid lipids and medium chain triglyceride (MCT) as liquid lipid. Scanning electron microscopy (SEM) revealed the spherical nature of the particles with sizes ranging between 120 and 250 nm measured by photon correlation spectroscopy (PCS). The zeta potential of the particles ranged between -28 and -45 mV depending on the nature of the lipid matrix produced, which also influenced the entrapment efficiency (EE) and drug loading capacity (LC) found to be in the range of 80-94% and 1.62-3.27%, respectively. The LC increased reciprocally on increasing the amount of MCT as confirmed by differential scanning calorimetry (DSC). DSC analyses revealed that increasing imperfections within the lipid matrix allowed for increasing encapsulation parameters. Nanoparticles were further sterilized by filtration process which was found to be superior over autoclaving in preventing thermal degradation of thermo-sensitive curcuminoids. The in vivo pharmacodynamic activity revealed 2-fold increase in antimalarial activity of curcuminoids entrapped in lipid nanoparticles when compared to free curcuminoids at the tested dosage level.

  9. Design, Synthesis, and Characterization of Folate-Targeted Platinum-Loaded Theranostic Nanoemulsions for Therapy and Imaging of Ovarian Cancer.

    PubMed

    Patel, Niravkumar R; Piroyan, Aleksandr; Nack, Abbegial H; Galati, Corin A; McHugh, Mackenzi; Orosz, Samantha; Keeler, Amanda W; O'Neal, Sara; Zamboni, William C; Davis, Barbara; Coleman, Timothy P

    2016-06-01

    Platinum (Pt) based chemotherapy is widely used to treat many types of cancer. Pt therapy faces challenges such as dose limiting toxicities, cumulative side effects, and multidrug resistance. Nanoemulsions (NEs) have tremendous potential in overcoming these challenges as they can be designed to improve circulation time, limit non-disease tissue uptake, and enhance tumor uptake by surface modification. We designed novel synthesis of three difattyacid platins, dimyrisplatin, dipalmiplatin, and distearyplatin, suitable for encapsulation in the oil core of an NE. The dimyrisplatin, dipalmiplatin, and distearyplatin were synthesized, characterized, and loaded into the oil core of our NEs, NMI-350, NMI-351, and NMI-352 respectively. Sequestration of the difattyacid platins was accomplished through high energy microfluidization. To target the NE, FA-PEG3400-DSPE was incorporated into the surface during microfluidization. The FA-NEs selectively bind the folate receptor α (FR-α) and utilize receptor mediated endocytosis to deliver Pt past cell surface resistance mechanisms. FR-α is overexpressed in a number of oncological conditions including ovarian cancer. The difattyacid platins, lipidated Gd-DTPA, and lipidated folate were characterized by nuclear magnetic resonance (NMR), mass spectrometry (MS), and elemental analysis. NEs were synthesized using high shear microfluidization process and characterized for size, zeta-potential, and loading efficiency. In vitro cytotoxicity was determined using KB-WT (Pt-sensitive) and KBCR-1000 (Pt-resistant) cancer cells and measured by MTT assay. Pharmacokinetic profiles were studied in CD-1 mice. NEs loaded with difattyacid platins are highly stable and had size distribution in the range of ∼120 to 150 nm with low PDI. Cytotoxicity data indicates the longer the fatty acid chains, the less potent the NEs. The inclusion of C6-ceramide, an apoptosis enhancer, and surface functionalization with folate molecules significantly increased

  10. Design, Synthesis, and Characterization of Folate-Targeted Platinum-Loaded Theranostic Nanoemulsions for Therapy and Imaging of Ovarian Cancer.

    PubMed

    Patel, Niravkumar R; Piroyan, Aleksandr; Nack, Abbegial H; Galati, Corin A; McHugh, Mackenzi; Orosz, Samantha; Keeler, Amanda W; O'Neal, Sara; Zamboni, William C; Davis, Barbara; Coleman, Timothy P

    2016-06-01

    Platinum (Pt) based chemotherapy is widely used to treat many types of cancer. Pt therapy faces challenges such as dose limiting toxicities, cumulative side effects, and multidrug resistance. Nanoemulsions (NEs) have tremendous potential in overcoming these challenges as they can be designed to improve circulation time, limit non-disease tissue uptake, and enhance tumor uptake by surface modification. We designed novel synthesis of three difattyacid platins, dimyrisplatin, dipalmiplatin, and distearyplatin, suitable for encapsulation in the oil core of an NE. The dimyrisplatin, dipalmiplatin, and distearyplatin were synthesized, characterized, and loaded into the oil core of our NEs, NMI-350, NMI-351, and NMI-352 respectively. Sequestration of the difattyacid platins was accomplished through high energy microfluidization. To target the NE, FA-PEG3400-DSPE was incorporated into the surface during microfluidization. The FA-NEs selectively bind the folate receptor α (FR-α) and utilize receptor mediated endocytosis to deliver Pt past cell surface resistance mechanisms. FR-α is overexpressed in a number of oncological conditions including ovarian cancer. The difattyacid platins, lipidated Gd-DTPA, and lipidated folate were characterized by nuclear magnetic resonance (NMR), mass spectrometry (MS), and elemental analysis. NEs were synthesized using high shear microfluidization process and characterized for size, zeta-potential, and loading efficiency. In vitro cytotoxicity was determined using KB-WT (Pt-sensitive) and KBCR-1000 (Pt-resistant) cancer cells and measured by MTT assay. Pharmacokinetic profiles were studied in CD-1 mice. NEs loaded with difattyacid platins are highly stable and had size distribution in the range of ∼120 to 150 nm with low PDI. Cytotoxicity data indicates the longer the fatty acid chains, the less potent the NEs. The inclusion of C6-ceramide, an apoptosis enhancer, and surface functionalization with folate molecules significantly increased

  11. Ex vivo uranium decontamination efficiency on wounded skin and in vitro skin toxicity of a calixarene-loaded nanoemulsion.

    PubMed

    Grives, Sophie; Phan, Guillaume; Morat, Guillaume; Suhard, David; Rebiere, Francois; Fattal, Elias

    2015-06-01

    The present work aims at studying the decontamination efficacy of a calixarene-loaded nanoemulsion on two ex vivo wounded skin models mimicking superficial stings or cuts contaminated with uranium, and on a third model using excoriation. The decontaminating formulation was compared with the currently used radio-decontaminating soapy water (Trait rouge®) treatment. Moreover, to assess skin damage potentially induced by the undiluted nanoemulsion, in vitro toxicity studies were conducted on an in vitro reconstructed human epidermis, coupled with three different toxicity tests [3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyl tetrazolium bromide, lactate dehydrogenase, and interleukin-1-α]. This work demonstrated not only a significant decontamination activity of the calixarene nanoemulsion on wounded skin, ranging from 92% to 94% of the applied uranium solution according to the ex vivo model used, but also the absence of side effects of this promising treatment.

  12. Induction of systemic and mucosal immunity against methicillin-resistant Staphylococcus aureus infection by a novel nanoemulsion adjuvant vaccine

    PubMed Central

    Sun, HongWu; Wei, Chao; Liu, BaoShuai; Jing, HaiMing; Feng, Qiang; Tong, YaNan; Yang, Yun; Yang, LiuYang; Zuo, QianFei; Zhang, Yi; Zou, QuanMing; Zeng, Hao

    2015-01-01

    The Gram-positive bacterial pathogen methicillin-resistant Staphylococcus aureus (MRSA) can cause infections in the bloodstream, endocardial tissue, respiratory tract, culture-confirmed skin, or soft tissue. There are currently no effective vaccines, and none are expected to become available in the near future. An effective vaccine capable of eliciting both systemic and mucosal immune responses is also urgently needed. Here, we reported a novel oil-in-water nanoemulsion adjuvant vaccine containing an MRSA recombination protein antigen, Cremophor EL-35® as a surfactant, and propylene glycol as a co-surfactant. This nanoemulsion vaccine, whose average diameter was 31.34±0.49 nm, demonstrated good protein structure integrity, protein specificity, and good stability at room temperature for 1 year. The intramuscular systemic and nasal mucosal immune responses demonstrated that this nanoemulsion vaccine could improve the specific immune responses of immunoglobulin (Ig)G and related subclasses, such as IgG1, IgG2a, and IgG2b, as well as IgA, in the serum after Balb/c mice intramuscular immunization and C57 mice nasal immunization. Furthermore, this nanoemulsion vaccine also markedly enhanced the interferon-γ and interleukin-17A cytokine cell immune response, improved the survival ratio, and reduced bacterial colonization. Taken together, our results show that this novel nanoemulsion vaccine has great potential and is a robust generator of an effective intramuscular systemic and nasal mucosal immune response without the need for an additional adjuvant. Thus, the present study serves as a sound scientific foundation for future strategies in the development of this novel nanoemulsion adjuvant vaccine to enhance both the intramuscular systemic and nasal mucosal immune responses. PMID:26664118

  13. Enhancement of Anti-Dermatitis Potential of Clobetasol Propionate by DHA [Docosahexaenoic Acid] Rich Algal Oil Nanoemulsion Gel

    PubMed Central

    Sarfaraz Alam, Mohammad; Ali, Mohammad Sajid; Zakir, Foziyah; Alam, Nawazish; Intakhab Alam, Mohammad; Ahmad, Faruque; Siddiqui, Masoom Raza; Ali, Mohammad Daud; Ansari, Mohammad Salahuddin; Ahmad, Sarfaraz; Ali, Maksood

    2016-01-01

    The aim of the present study was to investigate the potential of nanoemulsion formulation for topical delivery of Clobetasol propionate (CP) using algal oil (containing omega-3 fatty acids) as the oil phase. CP has anti-inflammatory, immunomodulatory and antiproliferative activities. However, its clinical use is restricted to some extent due to its poor permeability across the skin. Algal oil was used as the oil phase and was also exploited for its anti-inflammatory effect along with CP in the treatment of inflammation associated with dermatitis. Nanoemulsion formulations were prepared by aqueous phase titration method, using algal oil, tween 20, PEG 200 and water as the oil phase, surfactant, co-surfactant and aqueous phase respectively. Furthermore, different formulations were subjected to evaluate for ex-vivo permeation and in-vivo anti-inflammatory, irritation and contact dermatitis studies. The optimized nanoemulsion was converted into hydrogel-thickened nanoemulsion system (HTN) using carbopol 971 and had a viscosity of 97.57 ± 0.04 PaS. The optimized formulation had small average diameter (120 nm) with zeta potential of -37.01 mV which indicated good long-term stability. In-vivo anti-inflammatory activity indicated 84.55% and 41.04% inhibition of inflammation for drug loaded and placebo formulations respectively. The assessment of skin permeation was done by DSC and histopathology studies which indicated changes in the structure of epidermal membrane of skin. Contact dermatitis reveals that the higher NTPDase activity in the treatment with the CP-loaded nanoemulsion could be related to the higher anti-inflammatory effect in comparison with placebo nanoemulsion gel. PMID:27610146

  14. Induction of systemic and mucosal immunity against methicillin-resistant Staphylococcus aureus infection by a novel nanoemulsion adjuvant vaccine.

    PubMed

    Sun, HongWu; Wei, Chao; Liu, BaoShuai; Jing, HaiMing; Feng, Qiang; Tong, YaNan; Yang, Yun; Yang, LiuYang; Zuo, QianFei; Zhang, Yi; Zou, QuanMing; Zeng, Hao

    2015-01-01

    The Gram-positive bacterial pathogen methicillin-resistant Staphylococcus aureus (MRSA) can cause infections in the bloodstream, endocardial tissue, respiratory tract, culture-confirmed skin, or soft tissue. There are currently no effective vaccines, and none are expected to become available in the near future. An effective vaccine capable of eliciting both systemic and mucosal immune responses is also urgently needed. Here, we reported a novel oil-in-water nanoemulsion adjuvant vaccine containing an MRSA recombination protein antigen, Cremophor EL-35(®) as a surfactant, and propylene glycol as a co-surfactant. This nanoemulsion vaccine, whose average diameter was 31.34±0.49 nm, demonstrated good protein structure integrity, protein specificity, and good stability at room temperature for 1 year. The intramuscular systemic and nasal mucosal immune responses demonstrated that this nanoemulsion vaccine could improve the specific immune responses of immunoglobulin (Ig)G and related subclasses, such as IgG1, IgG2a, and IgG2b, as well as IgA, in the serum after Balb/c mice intramuscular immunization and C57 mice nasal immunization. Furthermore, this nanoemulsion vaccine also markedly enhanced the interferon-γ and interleukin-17A cytokine cell immune response, improved the survival ratio, and reduced bacterial colonization. Taken together, our results show that this novel nanoemulsion vaccine has great potential and is a robust generator of an effective intramuscular systemic and nasal mucosal immune response without the need for an additional adjuvant. Thus, the present study serves as a sound scientific foundation for future strategies in the development of this novel nanoemulsion adjuvant vaccine to enhance both the intramuscular systemic and nasal mucosal immune responses.

  15. Induction of systemic and mucosal immunity against methicillin-resistant Staphylococcus aureus infection by a novel nanoemulsion adjuvant vaccine.

    PubMed

    Sun, HongWu; Wei, Chao; Liu, BaoShuai; Jing, HaiMing; Feng, Qiang; Tong, YaNan; Yang, Yun; Yang, LiuYang; Zuo, QianFei; Zhang, Yi; Zou, QuanMing; Zeng, Hao

    2015-01-01

    The Gram-positive bacterial pathogen methicillin-resistant Staphylococcus aureus (MRSA) can cause infections in the bloodstream, endocardial tissue, respiratory tract, culture-confirmed skin, or soft tissue. There are currently no effective vaccines, and none are expected to become available in the near future. An effective vaccine capable of eliciting both systemic and mucosal immune responses is also urgently needed. Here, we reported a novel oil-in-water nanoemulsion adjuvant vaccine containing an MRSA recombination protein antigen, Cremophor EL-35(®) as a surfactant, and propylene glycol as a co-surfactant. This nanoemulsion vaccine, whose average diameter was 31.34±0.49 nm, demonstrated good protein structure integrity, protein specificity, and good stability at room temperature for 1 year. The intramuscular systemic and nasal mucosal immune responses demonstrated that this nanoemulsion vaccine could improve the specific immune responses of immunoglobulin (Ig)G and related subclasses, such as IgG1, IgG2a, and IgG2b, as well as IgA, in the serum after Balb/c mice intramuscular immunization and C57 mice nasal immunization. Furthermore, this nanoemulsion vaccine also markedly enhanced the interferon-γ and interleukin-17A cytokine cell immune response, improved the survival ratio, and reduced bacterial colonization. Taken together, our results show that this novel nanoemulsion vaccine has great potential and is a robust generator of an effective intramuscular systemic and nasal mucosal immune response without the need for an additional adjuvant. Thus, the present study serves as a sound scientific foundation for future strategies in the development of this novel nanoemulsion adjuvant vaccine to enhance both the intramuscular systemic and nasal mucosal immune responses. PMID:26664118

  16. Design and in vitro evaluation of biocompatible dexamethasone-loaded nanoparticle dispersions, obtained from nano-emulsions, for inhalatory therapy.

    PubMed

    Fornaguera, Cristina; Llinàs, Meritxell; Solans, Conxita; Calderó, Gabriela

    2015-01-01

    Polymeric nanoparticle dispersions containing dexamethasone (DXM) have been prepared from O/W nano-emulsions of the water/polysorbate 80/[4 wt% poly(lactide-co-glycolide) acid+0.18 wt% DXM in ethyl acetate] system by a low-energy method at 25°C. Nano-emulsions were formed at O/S ratios between 45/55 and 72/25 and water contents above 70 wt% by the phase inversion composition (PIC) method. The mean hydrodynamic diameter of nano-emulsions with a constant water content of 90 wt% and O/S ratios from 50/50 to 70/30 was below 350 nm as assessed by dynamic light scattering. The nanoparticles obtained from these nano-emulsions (by solvent evaporation) showed mean diameters of around 130 nm, as determined by transmission electron microscopy image analysis. Therapeutic concentrations of DXM were encapsulated in the nano-emulsions prior to nanoparticle preparation. DXM entrapment efficiency of the nanoparticle dispersion (above 74 wt%) decreased at increasing O/S ratios of the precursor nano-emulsion while DXM loading, which was around 10 mg/100 mL, showed the reverse tendency. DXM release from nanoparticle dispersions was about an order of magnitude slower than from an aqueous solution. In vitro studies performed in a lung carcinoma cell line and in vitro haemolysis studies performed in red blood cells revealed a dose-dependent toxicity and haemolytic response, respectively. The as-prepared nanoparticle dispersions were non-toxic up to a concentration of 40 μg/mL and non-haemolytic up to a concentration of 1 mg/mL. After purification, nanoparticle dispersions were non-toxic up to a concentration of 90 μg/mL. These results allow concluding that these polymeric nanoparticle dispersions are good candidates for inhalatory therapy.

  17. Enhancement of Anti-Dermatitis Potential of Clobetasol Propionate by DHA [Docosahexaenoic Acid] Rich Algal Oil Nanoemulsion Gel.

    PubMed

    Sarfaraz Alam, Mohammad; Ali, Mohammad Sajid; Zakir, Foziyah; Alam, Nawazish; Intakhab Alam, Mohammad; Ahmad, Faruque; Siddiqui, Masoom Raza; Ali, Mohammad Daud; Ansari, Mohammad Salahuddin; Ahmad, Sarfaraz; Ali, Maksood

    2016-01-01

    The aim of the present study was to investigate the potential of nanoemulsion formulation for topical delivery of Clobetasol propionate (CP) using algal oil (containing omega-3 fatty acids) as the oil phase. CP has anti-inflammatory, immunomodulatory and antiproliferative activities. However, its clinical use is restricted to some extent due to its poor permeability across the skin. Algal oil was used as the oil phase and was also exploited for its anti-inflammatory effect along with CP in the treatment of inflammation associated with dermatitis. Nanoemulsion formulations were prepared by aqueous phase titration method, using algal oil, tween 20, PEG 200 and water as the oil phase, surfactant, co-surfactant and aqueous phase respectively. Furthermore, different formulations were subjected to evaluate for ex-vivo permeation and in-vivo anti-inflammatory, irritation and contact dermatitis studies. The optimized nanoemulsion was converted into hydrogel-thickened nanoemulsion system (HTN) using carbopol 971 and had a viscosity of 97.57 ± 0.04 PaS. The optimized formulation had small average diameter (120 nm) with zeta potential of -37.01 mV which indicated good long-term stability. In-vivo anti-inflammatory activity indicated 84.55% and 41.04% inhibition of inflammation for drug loaded and placebo formulations respectively. The assessment of skin permeation was done by DSC and histopathology studies which indicated changes in the structure of epidermal membrane of skin. Contact dermatitis reveals that the higher NTPDase activity in the treatment with the CP-loaded nanoemulsion could be related to the higher anti-inflammatory effect in comparison with placebo nanoemulsion gel. PMID:27610146

  18. Enhancement of Anti-Dermatitis Potential of Clobetasol Propionate by DHA [Docosahexaenoic Acid] Rich Algal Oil Nanoemulsion Gel

    PubMed Central

    Sarfaraz Alam, Mohammad; Ali, Mohammad Sajid; Zakir, Foziyah; Alam, Nawazish; Intakhab Alam, Mohammad; Ahmad, Faruque; Siddiqui, Masoom Raza; Ali, Mohammad Daud; Ansari, Mohammad Salahuddin; Ahmad, Sarfaraz; Ali, Maksood

    2016-01-01

    The aim of the present study was to investigate the potential of nanoemulsion formulation for topical delivery of Clobetasol propionate (CP) using algal oil (containing omega-3 fatty acids) as the oil phase. CP has anti-inflammatory, immunomodulatory and antiproliferative activities. However, its clinical use is restricted to some extent due to its poor permeability across the skin. Algal oil was used as the oil phase and was also exploited for its anti-inflammatory effect along with CP in the treatment of inflammation associated with dermatitis. Nanoemulsion formulations were prepared by aqueous phase titration method, using algal oil, tween 20, PEG 200 and water as the oil phase, surfactant, co-surfactant and aqueous phase respectively. Furthermore, different formulations were subjected to evaluate for ex-vivo permeation and in-vivo anti-inflammatory, irritation and contact dermatitis studies. The optimized nanoemulsion was converted into hydrogel-thickened nanoemulsion system (HTN) using carbopol 971 and had a viscosity of 97.57 ± 0.04 PaS. The optimized formulation had small average diameter (120 nm) with zeta potential of -37.01 mV which indicated good long-term stability. In-vivo anti-inflammatory activity indicated 84.55% and 41.04% inhibition of inflammation for drug loaded and placebo formulations respectively. The assessment of skin permeation was done by DSC and histopathology studies which indicated changes in the structure of epidermal membrane of skin. Contact dermatitis reveals that the higher NTPDase activity in the treatment with the CP-loaded nanoemulsion could be related to the higher anti-inflammatory effect in comparison with placebo nanoemulsion gel.

  19. Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs.

    PubMed

    Cerpnjak, Katja; Zvonar, Alenka; Gašperlin, Mirjana; Vrečer, Franc

    2013-12-01

    Low oral bioavailability as a consequence of low water solubility of drugs is a growing challenge to the development of new pharmaceutical products. One of the most popular approaches of oral bioavailability and solubility enhancement is the utilization of lipid-based drug delivery systems. Their use in product development is growing due to the versatility of pharmaceutical lipid excipients and drug formulations, and their compatibility with liquid, semi-solid, and solid dosage forms. Lipid formulations, such as self-emulsifying (SEDDS), self-microemulsifying SMEDDS) and self- -nanoemulsifying drug delivery systems (SNEDDS) were explored in many studies as an efficient approach for improving the bioavailability and dissolution rate of poorly water-soluble drugs. One of the greatest advantages of incorporating poorly soluble drugs into such formulations is their spontaneous emulsification and formation of an emulsion, microemulsion or nanoemulsion in aqueous media. This review article focuses on the following topics. First, it presents a classification overview of lipid-based drug delivery systems and mechanisms involved in improving the solubility and bioavailability of poorly water-soluble drugs. Second, the article reviews components of lipid-based drug delivery systems for oral use with their characteristics. Third, it brings a detailed description of SEDDS, SMEDDS and SNEDDS, which are very often misused in literature, with special emphasis on the comparison between microemulsions and nanoemulsions. PMID:24451070

  20. Food protein-stabilized nanoemulsions as potential delivery systems for poorly water-soluble drugs: preparation, in vitro characterization, and pharmacokinetics in rats

    PubMed Central

    He, Wei; Tan, Yanan; Tian, Zhiqiang; Chen, Lingyun; Hu, Fuqiang; Wu, Wei

    2011-01-01

    Nanoemulsions stabilized by traditional emulsifiers raise toxicological concerns for long-term treatment. The present work investigates the potential of food proteins as safer stabilizers for nanoemulsions to deliver hydrophobic drugs. Nanoemulsions stabilized by food proteins (soybean protein isolate, whey protein isolate, β-lactoglobulin) were prepared by high-pressure homogenization. The toxicity of the nanoemulsions was tested in Caco-2 cells using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide viability assay. In vivo absorption in rats was also evaluated. Food protein-stabilized nanoemulsions, with small particle size and good size distribution, exhibited better stability and biocompatibility compared with nanoemulsions stabilized by traditional emulsifiers. Moreover, β-lactoglobulin had a better emulsifying capacity and biocompatibility than the other two food proteins. The pancreatic degradation of the proteins accelerated drug release. It is concluded that an oil/water nanoemulsion system with good biocompatibility can be prepared by using food proteins as emulsifiers, allowing better and more rapid absorption of lipophilic drugs. PMID:21468355

  1. Musculoskeletal Hydatid Cysts Resembling Tumors: A Report of Five Cases.

    PubMed

    Toğral, Güray; Arıkan, Şefik M; Ekiz, Timur; Kekeç, Ahmet F; Ekşioğlu, Mehmet F

    2016-05-01

    Although challenges in treatment of musculoskeletal hydatid cysts (HC) lesions have been documented, data regarding the musculoskeletal HC lesions resembling tumor is scarce. This paper presented 5 patients (3 males, 2 females) with a mean age of 41.6 years with tumor-like lesions of HC. Three of them had left ilium and acetabulum involvement, one involved left femur, and one involved left thigh muscle compartments. Pain was the main symptom and was seen in all patients. Clinical examination, radiologic evaluation, and histologic analysis were performed for diagnosis. Patients were treated through different surgical options, including simple debridement, bone cement filling with or without internal fixation, hip arthrodesis, reconstruction using hemipelvic replantation with femoral prosthesis and distal femur endoprosthetic replacement. After surgery, the operation region was washed by 20% hypertonic saline, and debridement was performed carefully without contamination. All patients received albendazole treatment. Cases were followed up 1 to 9 years for the recurrence. Walking difficulty and pain were the main symptoms during the follow-up. One patient was symptom-free. A reoccurrence in the perioperative soft tissue was detected in only one patient and control visits with antihelmintic treatment were recommended. We would like to emphasize that HC should be kept in mind for the differential diagnosis of the cystic or tumoral lesions of the musculoskeletal system, particularly in the endemic regions. Prompt diagnosis is of paramount importance for preventing destruction and complications. PMID:27384735

  2. CYTOPLASMIC INCLUSIONS RESEMBLING NUCLEOLI IN SYMPATHETIC NEURONS OF ADULT RATS

    PubMed Central

    Grillo, Mary A.

    1970-01-01

    A distinctive cytoplasmic inclusion consisting of a convoluted network of electron-opaque strands embedded in a less dense matrix was identified in the neurons, but not in the supporting cells, of rat sympathetic ganglia. This ball-like structure, designated "nematosome," measures ∼ 0.9 µ and lacks a limiting membrane. Its strands (diameter = 400–600 A) appear to be made of an entanglement of tightly packed filaments and particles ∼ 25–50 A thick. Cytochemical studies carried out with the light microscope suggest the presence of nonhistone proteins and some RNA. Usually only one such structure is present in a cell, and it appears to occur in most ganglion cells. Although they can be seen anywhere in the cell body, nematosomes are typically located in the perinuclear cytoplasm, where they are often associated with smooth-surfaced and coated vesicles. In fine structure and stainability, they bear a resemblance to the fibrous component of the nucleolus. Subsynaptic formations, which are a special feature of some of the synapses in sympathetic ganglia, appear similar to the threadlike elements in the nematosomes. The possibility that these three structures—nucleolus, nematosome, and subsynaptic formation—may be interrelated in origin and function is discussed. PMID:5458990

  3. A neural network dynamics that resembles protein evolution

    NASA Astrophysics Data System (ADS)

    Ferrán, Edgardo A.; Ferrara, Pascual

    1992-06-01

    We use neutral networks to classify proteins according to their sequence similarities. A network composed by 7 × 7 neurons, was trained with the Kohonen unsupervised learning algorithm using, as inputs, matrix patterns derived from the bipeptide composition of cytochrome c proteins belonging to 76 different species. As a result of the training, the network self-organized the activation of its neurons into topologically ordered maps, wherein phylogenetically related sequences were positioned close to each other. The evolution of the topological map during learning, in a representative computational experiment, roughly resembles the way in which one species evolves into several others. For instance, sequences corresponding to vertebrates, initially grouped together into one neuron, were placed in a contiguous zone of the final neural map, with sequences of fishes, amphibia, reptiles, birds and mammals associated to different neurons. Some apparent wrong classifications are due to the fact that some proteins have a greater degree of sequence identity than the one expected by phylogenetics. In the final neural map, each synaptic vector may be considered as the pattern corresponding to the ancestor of all the proteins that are attached to that neuron. Although it may be also tempting to link real time with learning epochs and to use this relationship to calibrate the molecular evolutionary clock, this is not correct because the evolutionary time schedule obtained with the neural network depends highly on the discrete way in which the winner neighborhood is decreased during learning.

  4. On the resemblance of synapse formation and CNS myelination.

    PubMed

    Almeida, R G; Lyons, D A

    2014-09-12

    The myelination of axons in the central nervous system (CNS) is essential for nervous system formation, function and health. CNS myelination continues well into adulthood, but not all axons become myelinated. Unlike the peripheral nervous system, where we know of numerous axon-glial signals required for myelination, we have a poor understanding of the nature or identity of such molecules that regulate which axons are myelinated in the CNS. Recent studies have started to elucidate cell behavior during myelination in vivo and indicate that the choice of which axons are myelinated is made prior to myelin sheath generation. Here we propose that interactions between axons and the exploratory processes of oligodendrocyte precursor cells (OPCs) lead to myelination and may be similar to those between dendrites and axons that prefigure and lead to synapse formation. Indeed axons and OPCs form synapses with striking resemblance to those of neurons, suggesting a similar mode of formation. We discuss families of molecules with specific functions at different stages of synapse formation and address studies that implicate the same factors during axon-OPC synapse formation and myelination. We also address the possibility that the function of such synapses might directly regulate the myelinating behavior of oligodendrocyte processes in vivo. In the future it may be of benefit to consider these similarities when taking a candidate-based approach to dissect mechanisms of CNS myelination.

  5. Dimethyl silicone dry nanoemulsion inhalations: Formulation study and anti-acute lung injury effect.

    PubMed

    Zhu, Lifei; Li, Miao; Dong, Junxing; Jin, Yiguang

    2015-08-01

    Acute lung injury (ALI) is a severe disease, leading to death if not treated quickly. An emergency medicine is necessary for ALI therapy. Dimethyl silicone (DMS) is an effective agent to defoam the bubbles in the lung induced by ALI. However, DMS aerosols, a marketed formulation of DMS, affect environments and will be limited in the future. Here we firstly report a dry nanoemulsion inhalation for pulmonary delivery. Novel DMS dry nanoemulsion inhalations (DSNIs) were developed in this study. The optimal formulation of stable and homogenous DMS nanoemulsions (DSNs) was composed of Cremophor RH40/PEG 400/DMS (4:4:2, w/w/w) and water. The DSNs showed the tiny size of 19.8 nm, the zeta potential of -9.66 mV, and the low polydispersity index (PDI) of 0.37. The type of DSNs was identified as oil-in-water. The DSNs were added with mannitol followed by freeze-drying to obtain the DSNIs that were loose white powders, showed good fluidity, and were capable of rapid reconstitution to DSNs. The DSNs could adhere on the surfaces of lyophilized mannitol crystals. The aerodynamic diameter of DSNIs was 4.82 μm, suitable for pulmonary inhalation. The in vitro defoaming rate of DSNIs was 1.25 ml/s, much faster than those of the blank DSNIs, DMS, and DMS aerosols. The DSNIs showed significantly higher anti-ALI effect on the ALI rat models than the blank DSNIs and the DMS aerosols according to lung appearances, histological sections, and lung wet weight/dry weight ratios. The DSNIs are effective anti-ALI nanomedicines. The novel DMS formulation is a promising replacement of DMS aerosols.

  6. Topical Nanoemulsion Therapy Reduces Bacterial Wound Infection and Inflammation Following Burn Injury

    PubMed Central

    Hemmila, Mark R.; Mattar, Aladdein; Taddonio, Michael A.; Arbabi, Saman; Hamouda, Tarek; Ward, Peter A.; Wang, Stewart C.; Baker, James R.

    2010-01-01

    Background Nanoemulsions are broadly antimicrobial oil-in-water emulsions containing nanometer-sized droplets stabilized with surfactants. We hypothesize that topical application of a nanoemulsion compound (NB-201) can attenuate burn wound infection. In addition to reducing infection, nanoemulsion therapy may modulate dermal inflammatory signaling and thereby lessen inflammation following thermal injury. Methods Male Sprague-Dawley rats underwent a 20% total body surface area (TBSA) scald burn to create a partial thickness burn injury. Animals were resuscitated with Ringer’s lactate and the wound covered with an occlusive dressing. Eight hours after injury, the burn wound was inoculated with 1×106 CFU of Pseudomonas aeruginosa. NB-201, NB-201 placebo, 5% mafenide acetate solution or 0.9% saline (control) was applied onto the wound at 16 and 24 hrs following burn injury. Skin was harvested 32 hrs post-burn for quantitative wound culture and determination of inflammatory mediators in tissue homogenates. Results NB-201 reduced mean bacterial growth in the burn wound by a thousand fold, with only 11% animals having P. aeruginosa counts greater than 105 CFU/g tissue versus 91% in the control group (p<0.0001). Treatment with NB-201 attenuated neutrophil sequestration in the treatment group as measured by myeloperoxidase assay and by histology. It also, significantly reduced levels of pro-inflammatory cytokines (IL-1β and IL-6) and the degree of hair follicle cell apoptosis in skin when compared to saline-treated controls. Conclusions Topical NB-201 substantially reduced bacterial growth in a partial thickness burn model. This reduction in the level of wound infection was associated with an attenuation of the local dermal inflammatory response and diminished neutrophil sequestration. NB-201 represents a novel potent antimicrobial and antiinflammatory treatment for use in burn wounds. PMID:20189619

  7. Preparation and Thermal Properties of Fatty Alcohol/Surfactant/Oil/Water Nanoemulsions and Their Cosmetic Applications.

    PubMed

    Okamoto, Toru; Tomomasa, Satoshi; Nakajima, Hideo

    2016-01-01

    Physicochemical properties of oil-in-water (O/W) emulsions containing fatty alcohols and surfactants have been investigated with the aim of developing new formulations that are less viscous and more transparent than conventional milky lotions, as well as for providing greater skin-improving effects. O/W-based creams can be converted to low viscosity milky lotions following their emulsification with a homogenizer at temperatures greater than the transition temperatures of their molecular assemblies (α-gel). The stability of the O/W emulsions evaluated in the current study increased as the transition temperatures of the molecular assemblies formed from their fatty alcohol and surfactant constituents increased. A decrease in the emulsion droplet size led to the formation of a new formulation, which was transparent in appearance and showed a very low viscosity. The absence of a molecular assembly (α-gel) formed by the fatty alcohol and surfactant molecules in the aqueous phase allowed for the formation of a stable transparent and low viscosity nanoemulsion. Furthermore, this decrease in droplet size led to an increase in the interfacial area of the emulsion droplets, with almost all of the fatty alcohol and surfactant molecules being adsorbed on the surfaces of the emulsion droplets. This was found to be important for preparing a stable transparent formulation. Notably, this new formulation exhibited high occlusivity, which was equivalent to that of an ordinary cosmetic milky lotion, and consequently provided high skin hydration. The nanoemulsion was destroyed following its application to the skin, which led to the release of the fatty alcohol and surfactant molecules from the surface of the nanoemulsion into the aqueous phase. These results therefore suggest that the fatty alcohol and surfactant molecules organized the molecular assembly (α-gel) and allowed for the reconstruction of the network structure.

  8. Plum coatings of lemongrass oil-incorporating carnauba wax-based nanoemulsion.

    PubMed

    Kim, In-Hah; Lee, Hanna; Kim, Jung Eun; Song, Kyung Bin; Lee, Youn Suk; Chung, Dae Sung; Min, Sea C

    2013-10-01

    Nanoemulsions containing lemongrass oil (LO) were developed for coating plums and the effects of the nanoemulsion coatings on the microbial safety and physicochemical storage qualities of plums during storage at 4 and 25 °C were investigated. The emulsions used for coating were produced by mixing a carnauba wax-based solution (18%, w/w) with LO at various concentrations (0.5% to 4.0%, w/w) using dynamic high pressure processing at 172 MPa. The coatings were evaluated for their ability to inhibit the growth of Salmonella Typhimurium and Escherichia coli O157:H7 and their ability to preserve various physicochemical qualities of plums. Uniform and continuous coatings on plums, formed with stable emulsions, initially inhibited S. Typhimurium and E. coli O157:H7 by 0.2 to 2.8 and 0.8 to 2.7 log CFU/g, respectively, depending on the concentration of LO and the sequence of coating. The coatings did not significantly alter the flavor, fracturability, or glossiness of the plums. The antimicrobial effects of the coatings against S. Typhimurium and E. coli O157:H7 were demonstrated during storage at 4 and 25 °C. The coatings reduced weight loss and ethylene production by approximately 2 to 3 and 1.4 to 4.0 fold, respectively, and also retarded the changes in lightness and the concentration of phenolic compounds in plums during storage. The firmness of coated plums was generally higher than uncoated plums when stored at 4 °C and plum respiration rates were reduced during storage. Coatings containing nanoemulsions of LO have the potential to inhibit Salmonella and E. coli O157:H7 contamination of plums and may extend plum shelf life. PMID:24024904

  9. Inertial cavitation in theranostic nanoemulsions with simultaneous pulsed laser and low frequency ultrasound excitation

    NASA Astrophysics Data System (ADS)

    Arnal, Bastien; Wei, Chen-Wei; Xia, Jinjun; Pelivanov, Ivan M.; Lombardo, Michael; Perez, Camilo; Matula, Thomas J.; Pozzo, Danilo; O'Donnell, Matthew

    2014-03-01

    Ultrasound-induced inertial cavitation is a mechanical process used for site-localized therapies such as non-invasive surgery. Initiating cavitation in tissue requires very high intensity focused ultrasound (HIFU) and low-frequencies. Hence, some applications like thrombolysis require targeted contrast agents to reduce peak intensities and the potential for secondary effects. A new type of theranostic nanoemulsion has been developed as a combined ultrasound (US)/photoacoustic(PA) agent for molecular imaging and therapy. It includes a nanoscale emulsion core encapsulated with a layer of gold nanospheres at the water/ oil interface. Its optical absorption exhibits a spectrum broadened up to 1100 nm, opening the possibility that 1064 nm light can excite cavitation nuclei. If optically-excited nuclei are produced at the same time that a low-frequency US wave is at peak negative pressure, then highly localized therapies based on acoustic cavitation may be enabled at very low US pressures. We have demonstrated this concept using a low-cost, low energy, portable 1064 nm fiber laser in conjunction with a 1.24 MHz US transducer for simultaneous laser/US excitation of nanoemulsions. Active cavitation detection from backscattered signals indicated that cavitation can be initiated at very low acoustic pressures (less than 1 MPa) when laser excitation coincides with the rarefaction phase of the acoustic wave, and that no cavitation is produced when light is delivered during the compressive phase. US can sustain cavitation activity during long acoustic bursts and stimulate diffusion of the emulsion, thus increasing treatment speed. An in vitro clot model has been used to demonstrate combined US and laser excitation of the nanoemulsion for efficient thrombolysis.

  10. Plum coatings of lemongrass oil-incorporating carnauba wax-based nanoemulsion.

    PubMed

    Kim, In-Hah; Lee, Hanna; Kim, Jung Eun; Song, Kyung Bin; Lee, Youn Suk; Chung, Dae Sung; Min, Sea C

    2013-10-01

    Nanoemulsions containing lemongrass oil (LO) were developed for coating plums and the effects of the nanoemulsion coatings on the microbial safety and physicochemical storage qualities of plums during storage at 4 and 25 °C were investigated. The emulsions used for coating were produced by mixing a carnauba wax-based solution (18%, w/w) with LO at various concentrations (0.5% to 4.0%, w/w) using dynamic high pressure processing at 172 MPa. The coatings were evaluated for their ability to inhibit the growth of Salmonella Typhimurium and Escherichia coli O157:H7 and their ability to preserve various physicochemical qualities of plums. Uniform and continuous coatings on plums, formed with stable emulsions, initially inhibited S. Typhimurium and E. coli O157:H7 by 0.2 to 2.8 and 0.8 to 2.7 log CFU/g, respectively, depending on the concentration of LO and the sequence of coating. The coatings did not significantly alter the flavor, fracturability, or glossiness of the plums. The antimicrobial effects of the coatings against S. Typhimurium and E. coli O157:H7 were demonstrated during storage at 4 and 25 °C. The coatings reduced weight loss and ethylene production by approximately 2 to 3 and 1.4 to 4.0 fold, respectively, and also retarded the changes in lightness and the concentration of phenolic compounds in plums during storage. The firmness of coated plums was generally higher than uncoated plums when stored at 4 °C and plum respiration rates were reduced during storage. Coatings containing nanoemulsions of LO have the potential to inhibit Salmonella and E. coli O157:H7 contamination of plums and may extend plum shelf life.

  11. Preparation and Thermal Properties of Fatty Alcohol/Surfactant/Oil/Water Nanoemulsions and Their Cosmetic Applications.

    PubMed

    Okamoto, Toru; Tomomasa, Satoshi; Nakajima, Hideo

    2016-01-01

    Physicochemical properties of oil-in-water (O/W) emulsions containing fatty alcohols and surfactants have been investigated with the aim of developing new formulations that are less viscous and more transparent than conventional milky lotions, as well as for providing greater skin-improving effects. O/W-based creams can be converted to low viscosity milky lotions following their emulsification with a homogenizer at temperatures greater than the transition temperatures of their molecular assemblies (α-gel). The stability of the O/W emulsions evaluated in the current study increased as the transition temperatures of the molecular assemblies formed from their fatty alcohol and surfactant constituents increased. A decrease in the emulsion droplet size led to the formation of a new formulation, which was transparent in appearance and showed a very low viscosity. The absence of a molecular assembly (α-gel) formed by the fatty alcohol and surfactant molecules in the aqueous phase allowed for the formation of a stable transparent and low viscosity nanoemulsion. Furthermore, this decrease in droplet size led to an increase in the interfacial area of the emulsion droplets, with almost all of the fatty alcohol and surfactant molecules being adsorbed on the surfaces of the emulsion droplets. This was found to be important for preparing a stable transparent formulation. Notably, this new formulation exhibited high occlusivity, which was equivalent to that of an ordinary cosmetic milky lotion, and consequently provided high skin hydration. The nanoemulsion was destroyed following its application to the skin, which led to the release of the fatty alcohol and surfactant molecules from the surface of the nanoemulsion into the aqueous phase. These results therefore suggest that the fatty alcohol and surfactant molecules organized the molecular assembly (α-gel) and allowed for the reconstruction of the network structure. PMID:26743668

  12. Bio-active nanoemulsions enriched with gold nanoparticle, marigold extracts and lipoic acid: In vitro investigations.

    PubMed

    Guler, Emine; Barlas, F Baris; Yavuz, Murat; Demir, Bilal; Gumus, Z Pinar; Baspinar, Yucel; Coskunol, Hakan; Timur, Suna

    2014-09-01

    A novel and efficient approach for the preparation of enriched herbal formulations was described and their potential applications including wound healing and antioxidant activity (cell based and cell free) were investigated via in vitro cell culture studies. Nigella sativa oil was enriched with Calendula officinalis extract and lipoic acid capped gold nanoparticles (AuNP-LA) using nanoemulsion systems. The combination of these bio-active compounds was used to design oil in water (O/W) and water in oil (W/O) emulsions. The resulted emulsions were characterized by particle size measurements. The phenolic content of each nanoemulsion was examined by using both colorimetric assay and chromatographic analyses. Two different methods containing cell free chemical assay (1-diphenyl-2-picrylhydrazyl method) and cell based antioxidant activity test were used to evaluate the antioxidant capacities. In order to investigate the bio-activities of the herbal formulations, in vitro cell culture experiments, including cytotoxicity, scratch assay, antioxidant activity and cell proliferation were carried out using Vero cell line as a model cell line. Furthermore, to monitor localization of the nanoemulsions after application of the cell culture, the cell images were monitored via fluorescence microscope after FITC labeling. All data confirmed that the enriched N. sativa formulations exhibited better antioxidant and wound healing activity than N. sativa emulsion without any enrichment. In conclusion, the incorporation of AuNP-LA and C. officinalis extract into the N. sativa emulsions significantly increased the bio-activities. The present work may support further studies about using the other bio-active agents for the enrichment of herbal preparations to strengthen their activities.

  13. Bio-active nanoemulsions enriched with gold nanoparticle, marigold extracts and lipoic acid: In vitro investigations.

    PubMed

    Guler, Emine; Barlas, F Baris; Yavuz, Murat; Demir, Bilal; Gumus, Z Pinar; Baspinar, Yucel; Coskunol, Hakan; Timur, Suna

    2014-09-01

    A novel and efficient approach for the preparation of enriched herbal formulations was described and their potential applications including wound healing and antioxidant activity (cell based and cell free) were investigated via in vitro cell culture studies. Nigella sativa oil was enriched with Calendula officinalis extract and lipoic acid capped gold nanoparticles (AuNP-LA) using nanoemulsion systems. The combination of these bio-active compounds was used to design oil in water (O/W) and water in oil (W/O) emulsions. The resulted emulsions were characterized by particle size measurements. The phenolic content of each nanoemulsion was examined by using both colorimetric assay and chromatographic analyses. Two different methods containing cell free chemical assay (1-diphenyl-2-picrylhydrazyl method) and cell based antioxidant activity test were used to evaluate the antioxidant capacities. In order to investigate the bio-activities of the herbal formulations, in vitro cell culture experiments, including cytotoxicity, scratch assay, antioxidant activity and cell proliferation were carried out using Vero cell line as a model cell line. Furthermore, to monitor localization of the nanoemulsions after application of the cell culture, the cell images were monitored via fluorescence microscope after FITC labeling. All data confirmed that the enriched N. sativa formulations exhibited better antioxidant and wound healing activity than N. sativa emulsion without any enrichment. In conclusion, the incorporation of AuNP-LA and C. officinalis extract into the N. sativa emulsions significantly increased the bio-activities. The present work may support further studies about using the other bio-active agents for the enrichment of herbal preparations to strengthen their activities. PMID:25009101

  14. Preparation, characterization, and evaluation of antitumor effect of Brucea javanica oil cationic nanoemulsions.

    PubMed

    Liu, Ting-Ting; Mu, Li-Qiu; Dai, Wei; Wang, Chuan-Bang; Liu, Xin-Yi; Xiang, Da-Xiong

    2016-01-01

    The purpose of this study was to prepare Brucea javanica oil cationic nanoemulsions (BJO-CN) with BJO as drug as well as oil phase and chitosan as cationic inducer, to explore the practical suitability of using cationic nanoemulsions for oral delivery of mixed oil, and to test its bioavailability and antitumor effect. BJO-CN was prepared by chitosan solution stirring method and then characterized physicochemically. The obtained BJO-CN had a spherical morphology with a positive zeta potential of 18.9 mV and an average particle size of 42.36 nm, showing high colloidal stability. The drug loading of BJO-CN was 91.83 mg·mL(-1), determined by high-performance liquid chromatography with precolumn derivatization. Pharmacokinetic studies revealed that, compared with BJO emulsion (BJO-E) (the dosage of BJO-CN and BJO-E was equal to 505 mg·kg(-1), calculated by oleic acid), BJO-CN exhibited a significant increase in the area under the plasma drug concentration-time curve over the period of 24 hours and relative bioavailability was 1.6-fold. Furthermore, the antitumor effect of BJO-CN in the orthotopic mouse model of lung cancer was evaluated by recording the median survival time and the weight of lung tissue with tumor, hematoxylin and eosin staining, and immunohistochemical technique. Results of anticancer experiments illustrated that, even though the administrated dosage in the BJO-CN group was half of that in the BJO-E group, BJO-CN exhibited similar antitumor effect to BJO-E. Moreover, BJO-CN had good synergistic effect in combination therapy with vinorelbine. These results suggested that cationic nanoemulsions are an effective and promising delivery system to enhance the oral bioavailability and anticancer effect of BJO. PMID:27330293

  15. Preparation, characterization, and evaluation of antitumor effect of Brucea javanica oil cationic nanoemulsions

    PubMed Central

    Liu, Ting-ting; Mu, Li-Qiu; Dai, Wei; Wang, Chuan-bang; Liu, Xin-Yi; Xiang, Da-Xiong

    2016-01-01

    The purpose of this study was to prepare Brucea javanica oil cationic nanoemulsions (BJO-CN) with BJO as drug as well as oil phase and chitosan as cationic inducer, to explore the practical suitability of using cationic nanoemulsions for oral delivery of mixed oil, and to test its bioavailability and antitumor effect. BJO-CN was prepared by chitosan solution stirring method and then characterized physicochemically. The obtained BJO-CN had a spherical morphology with a positive zeta potential of 18.9 mV and an average particle size of 42.36 nm, showing high colloidal stability. The drug loading of BJO-CN was 91.83 mg·mL−1, determined by high-performance liquid chromatography with precolumn derivatization. Pharmacokinetic studies revealed that, compared with BJO emulsion (BJO-E) (the dosage of BJO-CN and BJO-E was equal to 505 mg·kg−1, calculated by oleic acid), BJO-CN exhibited a significant increase in the area under the plasma drug concentration–time curve over the period of 24 hours and relative bioavailability was 1.6-fold. Furthermore, the antitumor effect of BJO-CN in the orthotopic mouse model of lung cancer was evaluated by recording the median survival time and the weight of lung tissue with tumor, hematoxylin and eosin staining, and immunohistochemical technique. Results of anticancer experiments illustrated that, even though the administrated dosage in the BJO-CN group was half of that in the BJO-E group, BJO-CN exhibited similar antitumor effect to BJO-E. Moreover, BJO-CN had good synergistic effect in combination therapy with vinorelbine. These results suggested that cationic nanoemulsions are an effective and promising delivery system to enhance the oral bioavailability and anticancer effect of BJO. PMID:27330293

  16. Skin photoprotection improvement: synergistic interaction between lipid nanoparticles and organic UV filters.

    PubMed

    Nikolić, S; Keck, C M; Anselmi, C; Müller, R H

    2011-07-29

    A photoprotective formulation was developed with an increased sunprotection factor (SPF), compared to a conventional nanoemulsion, but having the same concentration of three molecular sunscreens, namely ethylhexyl triazone, bis-ethylhexyloxyphenol methoxyphenyl triazine, and ethylhexyl methoxycinnamate. The sunscreen mixture was incorporated into nanostructured lipid carriers (NLCs). The ability of nine different solid lipids to yield stable aqueous NLC suspensions was assessed. After the production by hot high pressure homogenization, the NLC were analyzed in terms of particle size, physical state, particle shape, ultraviolet absorbance and stability. The particle size for all NLC was around 200 nm after production. The NLC suspension with carnauba wax had superior UV absorbance, NLC from bees wax showed similar efficiency as the reference emulsion. The NLC formulations were incorporated into hydrogel formulations and the in vitro SPF was measured. This study demonstrated that approximately 45% higher SPF values could be obtained when the organic UV filters were incorporated into carnauba wax NLC, in comparison to the reference nanoemulsion and bees wax NLC. The data showed that the synergistic effect of NLC and incorporated sunscreens depends not only on the solid state of the lipid but also on its type. PMID:21600969

  17. Skin photoprotection improvement: synergistic interaction between lipid nanoparticles and organic UV filters.

    PubMed

    Nikolić, S; Keck, C M; Anselmi, C; Müller, R H

    2011-07-29

    A photoprotective formulation was developed with an increased sunprotection factor (SPF), compared to a conventional nanoemulsion, but having the same concentration of three molecular sunscreens, namely ethylhexyl triazone, bis-ethylhexyloxyphenol methoxyphenyl triazine, and ethylhexyl methoxycinnamate. The sunscreen mixture was incorporated into nanostructured lipid carriers (NLCs). The ability of nine different solid lipids to yield stable aqueous NLC suspensions was assessed. After the production by hot high pressure homogenization, the NLC were analyzed in terms of particle size, physical state, particle shape, ultraviolet absorbance and stability. The particle size for all NLC was around 200 nm after production. The NLC suspension with carnauba wax had superior UV absorbance, NLC from bees wax showed similar efficiency as the reference emulsion. The NLC formulations were incorporated into hydrogel formulations and the in vitro SPF was measured. This study demonstrated that approximately 45% higher SPF values could be obtained when the organic UV filters were incorporated into carnauba wax NLC, in comparison to the reference nanoemulsion and bees wax NLC. The data showed that the synergistic effect of NLC and incorporated sunscreens depends not only on the solid state of the lipid but also on its type.

  18. Gait analysis in a mouse model resembling Leigh disease.

    PubMed

    de Haas, Ria; Russel, Frans G; Smeitink, Jan A

    2016-01-01

    Leigh disease (LD) is one of the clinical phenotypes of mitochondrial OXPHOS disorders and also known as sub-acute necrotizing encephalomyelopathy. The disease has an incidence of 1 in 77,000 live births. Symptoms typically begin early in life and prognosis for LD patients is poor. Currently, no clinically effective treatments are available. Suitable animal and cellular models are necessary for the understanding of the neuropathology and the development of successful new therapeutic strategies. In this study we used the Ndufs4 knockout (Ndufs4(-/-)) mouse, a model of mitochondrial complex I deficiency. Ndusf4(-/-) mice exhibit progressive neurodegeneration, which closely resemble the human LD phenotype. When dissecting behavioral abnormalities in animal models it is of great importance to apply translational tools that are clinically relevant. To distinguish gait abnormalities in patients, simple walking tests can be assessed, but in animals this is not easy. This study is the first to demonstrate automated CatWalk gait analysis in the Ndufs4(-/-) mouse model. Marked differences were noted between Ndufs4(-/-) and control mice in dynamic, static, coordination and support parameters. Variation of walking speed was significantly increased in Ndufs4(-/-) mice, suggesting hampered and uncoordinated gait. Furthermore, decreased regularity index, increased base of support and changes in support were noted in the Ndufs4(-/-) mice. Here, we report the ability of the CatWalk system to sensitively assess gait abnormalities in Ndufs4(-/-) mice. This objective gait analysis can be of great value for intervention and drug efficacy studies in animal models for mitochondrial disease.

  19. Ventricular Tachycardia and Resembling Acute Coronary Syndrome During Pheochromocytoma Crisis

    PubMed Central

    Li, Shi-jun; Wang, Tao; Wang, Lin; Pang, Zhan-qi; Ma, Ben; Li, Ya-wen; Yang, Jian; Dong, He

    2016-01-01

    Abstract Pheochromocytomas are neuroendocrine tumors, and its cardiac involvement may include transient myocardial dysfunction, acute coronary syndrome (ACS), and even ventricular arrhythmias. A patient was referred for evaluation of stuttering chest pain, and his electrocardiogram showed T-wave inversion over leads V1 to V4. Coronary angiography showed 90% stenosis in the mid-left anterior descending coronary artery (LAD), which was stented. Five days later, the patient had ventricular tachycardia, and severe hypertension, remarkable blood pressure fluctuation between 224/76 and 70/50 mm Hg. The patient felt abdominal pain and his abdominal ultrasound showed suspicious right adrenal gland tumor. Enhanced computed tomography of adrenal gland conformed that there was a tumor in right adrenal gland accompanied by an upset level of aldosterone. The tumor was removed by laparoscope, and the pathological examination showed pheochromocytoma. After the surgery, the blood pressure turned normal gradually. There was no T-wave inversion in lead V1-V4. Our case illustrates a rare pheochromocytoma presentation with a VT and resembling ACS. In our case, the serious stenosis in the mid of LAD could be explained by worsen the clinical course of myocardial ischemia or severe coronary vasospasm by the excessive amounts of catecholamines released from the tumor. Coronary vasospasm was possible because he had no classic coronary risk factors (e.g. family history and smoking habit, essential hypertension, hyperglycemia and abnormal serum lipoprotein, high body mass index). Thus, pheochromocytoma was missed until he revealed the association of his symptoms with abdominalgia. As phaeochromocytomas that present with cardiovascular complications can be fatal, it is necessary to screen for the disease when patients present with symptoms indicating catecholamine excess. PMID:27057898

  20. Enhancement of encapsulation efficiency of nanoemulsion-containing aripiprazole for the treatment of schizophrenia using mixture experimental design.

    PubMed

    Masoumi, Hamid Reza Fard; Basri, Mahiran; Samiun, Wan Sarah; Izadiyan, Zahra; Lim, Chaw Jiang

    2015-01-01

    Aripiprazole is considered as a third-generation antipsychotic drug with excellent therapeutic efficacy in controlling schizophrenia symptoms and was the first atypical anti-psychotic agent to be approved by the US Food and Drug Administration. Formulation of nanoemulsion-containing aripiprazole was carried out using high shear and high pressure homogenizers. Mixture experimental design was selected to optimize the composition of nanoemulsion. A very small droplet size of emulsion can provide an effective encapsulation for delivery system in the body. The effects of palm kernel oil ester (3-6 wt%), lecithin (2-3 wt%), Tween 80 (0.5-1 wt%), glycerol (1.5-3 wt%), and water (87-93 wt%) on the droplet size of aripiprazole nanoemulsions were investigated. The mathematical model showed that the optimum formulation for preparation of aripiprazole nanoemulsion having the desirable criteria was 3.00% of palm kernel oil ester, 2.00% of lecithin, 1.00% of Tween 80, 2.25% of glycerol, and 91.75% of water. Under optimum formulation, the corresponding predicted response value for droplet size was 64.24 nm, which showed an excellent agreement with the actual value (62.23 nm) with residual standard error <3.2%.

  1. Effect of salts on the phase behavior and the stability of nanoemulsions with rapeseed oil and an extended surfactant.

    PubMed

    Klaus, Angelika; Tiddy, Gordon J T; Solans, Conxita; Harrar, Agnes; Touraud, Didier; Kunz, Werner

    2012-06-01

    For many decades, the solubilization of long-chain triglycerides in water has been a challenge. A new class of amphiphiles has been created to overcome this solubilization problem. The so-called "extended" surfactants contain a hydrophilic-lipophilic linker to reduce the contrast between the surfactant-water and surfactant-oil interfaces. In the present contribution, the effects of different anions and cations on the phase behavior of a mixture containing an extended surfactant (X-AES), a hydrotrope (sodium xylene sulfonate, SXS), water, and rapeseed oil were determined as a function of temperature. Nanoemulsions were obtained and characterized by conductivity measurements, light scattering, and optical microscopy. All salting-out salts show a transition from a clear region (O/W nanoemulsion), to a lamellar liquid crystalline phase region, a clear phase (bicontinuous L(3)), and again to a lamellar liquid crystalline phase region with increasing temperature. For the phase diagrams with NaSCN and Na(2)SO(4), only one clear region (O/W nanoemulsion) was observed, which turns into a lamellar phase region at elevated temperatures. Furthermore, the stability of the nanoemulsions was investigated by time-dependent measurements: the visual observation of phase separation, droplet size by dynamic light scattering (DLS), and optical microscopy. The mechanism of the different phase transitions is also discussed. PMID:22537241

  2. Antiherpes Activity and Skin/Mucosa Distribution of Flavonoids from Achyrocline satureioides Extract Incorporated into Topical Nanoemulsions.

    PubMed

    Bidone, Juliana; Argenta, Débora Fretes; Kratz, Jadel; Pettenuzzo, Letícia Ferreira; Horn, Ana Paula; Koester, Letícia Scherer; Bassani, Valquíria Linck; Simões, Claudia Maria Oliveira; Teixeira, Helder Ferreira

    2015-01-01

    This study investigated the inhibitory effects of Achyrocline satureioides extract (ASE) incorporated into a topical nanoemulsion on Herpes Simplex Virus type 1 (HSV-1/KOS strain) replication, as well as the distribution of the main ASE flavonoids (quercetin, luteolin, and 3-O-methylquercetin) in porcine skin and mucosa. The ASE-loaded nanoemulsion showed more pronounced effects against HSV-1 replication when compared to the ASE or pure quercetin, as determined by the viral plaque number reduction assay. All flavonoids were detected in the skin epidermis (2.2 µg/cm(2)) and the mucosa upper layers (3.0 µg/cm(2)) from ASE-loaded nanoemulsion until 8 h after topical application. A higher amount of flavonoids was detected when these tissues were impaired, especially in deeper mucosa layers (up to 7-fold). Flavonoids were detected in the receptor fluid only when the mucosa was injured. Such results were supported by confocal microscopy images. Overall, these findings suggest that the tested ASE-loaded nanoemulsion has potential to be used topically for herpes infections.

  3. Antiherpes Activity and Skin/Mucosa Distribution of Flavonoids from Achyrocline satureioides Extract Incorporated into Topical Nanoemulsions

    PubMed Central

    Bidone, Juliana; Argenta, Débora Fretes; Kratz, Jadel; Pettenuzzo, Letícia Ferreira; Horn, Ana Paula; Koester, Letícia Scherer; Bassani, Valquíria Linck; Simões, Claudia Maria Oliveira; Teixeira, Helder Ferreira

    2015-01-01

    This study investigated the inhibitory effects of Achyrocline satureioides extract (ASE) incorporated into a topical nanoemulsion on Herpes Simplex Virus type 1 (HSV-1/KOS strain) replication, as well as the distribution of the main ASE flavonoids (quercetin, luteolin, and 3-O-methylquercetin) in porcine skin and mucosa. The ASE-loaded nanoemulsion showed more pronounced effects against HSV-1 replication when compared to the ASE or pure quercetin, as determined by the viral plaque number reduction assay. All flavonoids were detected in the skin epidermis (2.2 µg/cm2) and the mucosa upper layers (3.0 µg/cm2) from ASE-loaded nanoemulsion until 8 h after topical application. A higher amount of flavonoids was detected when these tissues were impaired, especially in deeper mucosa layers (up to 7-fold). Flavonoids were detected in the receptor fluid only when the mucosa was injured. Such results were supported by confocal microscopy images. Overall, these findings suggest that the tested ASE-loaded nanoemulsion has potential to be used topically for herpes infections. PMID:26101767

  4. Antiherpes Activity and Skin/Mucosa Distribution of Flavonoids from Achyrocline satureioides Extract Incorporated into Topical Nanoemulsions.

    PubMed

    Bidone, Juliana; Argenta, Débora Fretes; Kratz, Jadel; Pettenuzzo, Letícia Ferreira; Horn, Ana Paula; Koester, Letícia Scherer; Bassani, Valquíria Linck; Simões, Claudia Maria Oliveira; Teixeira, Helder Ferreira

    2015-01-01

    This study investigated the inhibitory effects of Achyrocline satureioides extract (ASE) incorporated into a topical nanoemulsion on Herpes Simplex Virus type 1 (HSV-1/KOS strain) replication, as well as the distribution of the main ASE flavonoids (quercetin, luteolin, and 3-O-methylquercetin) in porcine skin and mucosa. The ASE-loaded nanoemulsion showed more pronounced effects against HSV-1 replication when compared to the ASE or pure quercetin, as determined by the viral plaque number reduction assay. All flavonoids were detected in the skin epidermis (2.2 µg/cm(2)) and the mucosa upper layers (3.0 µg/cm(2)) from ASE-loaded nanoemulsion until 8 h after topical application. A higher amount of flavonoids was detected when these tissues were impaired, especially in deeper mucosa layers (up to 7-fold). Flavonoids were detected in the receptor fluid only when the mucosa was injured. Such results were supported by confocal microscopy images. Overall, these findings suggest that the tested ASE-loaded nanoemulsion has potential to be used topically for herpes infections. PMID:26101767

  5. Hydrogels Containing Nanocapsules and Nanoemulsions of Tea Tree Oil Provide Antiedematogenic Effect and Improved Skin Wound Healing.

    PubMed

    Flores, Fernanda C; De Lima, Julia A; Da Silva, Cássia R; Benvegnú, Dalila; Ferreira, Juliano; Burger, Marilise E; Beck, Ruy C R; Rolim, Clarice M B; Rocha, Maria Isabel U M; Da Veiga, Marcelo L; Da Silva, Cristiane de B

    2015-01-01

    In previous works, we developed nanocapsules and nanoemulsions containing the tea tree oil. The aim of this work was to prepare and characterize hydrogels containing these nanocarriers, and to evaluate their in vivo efficacy in protecting skin damage induced by UVB and cutaneous wound healing. Hydrogels were prepared using Carbopol Ultrez and their physicochemical characteristics were evaluated: macroscopic analysis, pH, spreadability and rheological properties. The in vivo antiedematogenic effect was evaluated by ear thickness measurement after UVB-irradiation. In order to evaluate healing action of hydrogels, we investigated the regression of the cutaneous lesion in rats. Hydrogels showed homogeneous aspect and pH values between 5.6-5.8 and a non-Newtonian behavior. The presence of nanocapsules and nanoemulsions in hydrogels did not change their spreadability profile. The inclusion of tea tree oil in the nanocapsules and nanoemulsions allowed reducing the edema induced by UVB exposure. Hydrogel containing nanocapsules presented a higher reduction of the wound area compared to the hydrogel containing nanoemulsions and hydrogel containing allantoin. This study shows the feasibility of obtained dermatological formulations containing the tea tree oil associated in nanostructured systems. These formulations represent a promising approach to topical treatment of inflammatory disorders and wound healing.

  6. Comparison of process parameter optimization using different designs in nanoemulsion-based formulation for transdermal delivery of fullerene.

    PubMed

    Ngan, Cheng Loong; Basri, Mahiran; Lye, Fui Fang; Fard Masoumi, Hamid Reza; Tripathy, Minaketan; Karjiban, Roghayeh Abedi; Abdul-Malek, Emilia

    2014-01-01

    This research aims to formulate and to optimize a nanoemulsion-based formulation containing fullerene, an antioxidant, stabilized by a low amount of mixed surfactants using high shear and the ultrasonic emulsification method for transdermal delivery. Process parameters optimization of fullerene nanoemulsions was done by employing response surface methodology, which involved statistical multivariate analysis. Optimization of independent variables was investigated using experimental design based on Box-Behnken design and central composite rotatable design. An investigation on the effect of the homogenization rate (4,000-5,000 rpm), sonication amplitude (20%-60%), and sonication time (30-150 seconds) on the particle size, ζ-potential, and viscosity of the colloidal systems was conducted. Under the optimum conditions, the central composite rotatable design model suggested the response variables for particle size, ζ-potential, and viscosity of the fullerene nanoemulsion were 152.5 nm, -52.6 mV, and 44.6 pascal seconds, respectively. In contrast, the Box-Behnken design model proposed that preparation under the optimum condition would produce nanoemulsion with particle size, ζ-potential, and viscosity of 148.5 nm, -55.2 mV, and 39.9 pascal seconds, respectively. The suggested process parameters to obtain optimum formulation by both models yielded actual response values similar to the predicted values with residual standard error of <2%. The optimum formulation showed more elastic and solid-like characteristics due to the existence of a large linear viscoelastic region. PMID:25258528

  7. Hydrogels Containing Nanocapsules and Nanoemulsions of Tea Tree Oil Provide Antiedematogenic Effect and Improved Skin Wound Healing.

    PubMed

    Flores, Fernanda C; De Lima, Julia A; Da Silva, Cássia R; Benvegnú, Dalila; Ferreira, Juliano; Burger, Marilise E; Beck, Ruy C R; Rolim, Clarice M B; Rocha, Maria Isabel U M; Da Veiga, Marcelo L; Da Silva, Cristiane de B

    2015-01-01

    In previous works, we developed nanocapsules and nanoemulsions containing the tea tree oil. The aim of this work was to prepare and characterize hydrogels containing these nanocarriers, and to evaluate their in vivo efficacy in protecting skin damage induced by UVB and cutaneous wound healing. Hydrogels were prepared using Carbopol Ultrez and their physicochemical characteristics were evaluated: macroscopic analysis, pH, spreadability and rheological properties. The in vivo antiedematogenic effect was evaluated by ear thickness measurement after UVB-irradiation. In order to evaluate healing action of hydrogels, we investigated the regression of the cutaneous lesion in rats. Hydrogels showed homogeneous aspect and pH values between 5.6-5.8 and a non-Newtonian behavior. The presence of nanocapsules and nanoemulsions in hydrogels did not change their spreadability profile. The inclusion of tea tree oil in the nanocapsules and nanoemulsions allowed reducing the edema induced by UVB exposure. Hydrogel containing nanocapsules presented a higher reduction of the wound area compared to the hydrogel containing nanoemulsions and hydrogel containing allantoin. This study shows the feasibility of obtained dermatological formulations containing the tea tree oil associated in nanostructured systems. These formulations represent a promising approach to topical treatment of inflammatory disorders and wound healing. PMID:26328444

  8. Enhancement of encapsulation efficiency of nanoemulsion-containing aripiprazole for the treatment of schizophrenia using mixture experimental design

    PubMed Central

    Fard Masoumi, Hamid Reza; Basri, Mahiran; Sarah Samiun, Wan; Izadiyan, Zahra; Lim, Chaw Jiang

    2015-01-01

    Aripiprazole is considered as a third-generation antipsychotic drug with excellent therapeutic efficacy in controlling schizophrenia symptoms and was the first atypical anti-psychotic agent to be approved by the US Food and Drug Administration. Formulation of nanoemulsion-containing aripiprazole was carried out using high shear and high pressure homogenizers. Mixture experimental design was selected to optimize the composition of nanoemulsion. A very small droplet size of emulsion can provide an effective encapsulation for delivery system in the body. The effects of palm kernel oil ester (3–6 wt%), lecithin (2–3 wt%), Tween 80 (0.5–1 wt%), glycerol (1.5–3 wt%), and water (87–93 wt%) on the droplet size of aripiprazole nanoemulsions were investigated. The mathematical model showed that the optimum formulation for preparation of aripiprazole nanoemulsion having the desirable criteria was 3.00% of palm kernel oil ester, 2.00% of lecithin, 1.00% of Tween 80, 2.25% of glycerol, and 91.75% of water. Under optimum formulation, the corresponding predicted response value for droplet size was 64.24 nm, which showed an excellent agreement with the actual value (62.23 nm) with residual standard error <3.2%. PMID:26508853

  9. A new nano-engineered hierarchical membrane for concurrent removal of surfactant and oil from oil-in-water nanoemulsion

    NASA Astrophysics Data System (ADS)

    Qin, Detao; Liu, Zhaoyang; Bai, Hongwei; Sun, Darren Delai; Song, Xiaoxiao

    2016-04-01

    Surfactant stabilized oil-in-water nanoemulsions pose a severe threat to both the environment and human health. Recent development of membrane filtration technology has enabled efficient oil removal from oil/water nanoemulsion, however, the concurrent removal of surfactant and oil remains unsolved because the existing filtration membranes still suffer from low surfactant removal rate and serious surfactant-induced fouling issue. In this study, to realize the concurrent removal of surfactant and oil from nanoemulsion, a novel hierarchically-structured membrane is designed with a nanostructured selective layer on top of a microstructured support layer. The physical and chemical properties of the overall membrane, including wettability, surface roughness, electric charge, thickness and structures, are delicately tailored through a nano-engineered fabrication process, that is, graphene oxide (GO) nanosheet assisted phase inversion coupled with surface functionalization. Compared with the membrane fabricated by conventional phase inversion, this novel membrane has four times higher water flux, significantly higher rejections of both oil (~99.9%) and surfactant (as high as 93.5%), and two thirds lower fouling ratio when treating surfactant stabilized oil-in-water nanoemulsion. Due to its excellent performances and facile fabrication process, this nano-engineered membrane is expected to have wide practical applications in the oil/water separation fields of environmental protection and water purification.

  10. Physicochemical stability and in vitro bioaccessibility of ß-carotene nanoemulsions stabilized with whey protein-dextran conjugates

    Technology Transfer Automated Retrieval System (TEKTRAN)

    In this study, ß-carotene (BC)-loaded nanoemulsions encapsulated with native whey protein isolate (WPI) and WPI-dextran (DT, 5 kDa, 20 kDa, and 70 kDa) conjugates were prepared and the effects of glycosylation with various molecular weight DTs on the physicochemical property, lipolysis, and BC bioac...

  11. A new nano-engineered hierarchical membrane for concurrent removal of surfactant and oil from oil-in-water nanoemulsion.

    PubMed

    Qin, Detao; Liu, Zhaoyang; Bai, Hongwei; Sun, Darren Delai; Song, Xiaoxiao

    2016-01-01

    Surfactant stabilized oil-in-water nanoemulsions pose a severe threat to both the environment and human health. Recent development of membrane filtration technology has enabled efficient oil removal from oil/water nanoemulsion, however, the concurrent removal of surfactant and oil remains unsolved because the existing filtration membranes still suffer from low surfactant removal rate and serious surfactant-induced fouling issue. In this study, to realize the concurrent removal of surfactant and oil from nanoemulsion, a novel hierarchically-structured membrane is designed with a nanostructured selective layer on top of a microstructured support layer. The physical and chemical properties of the overall membrane, including wettability, surface roughness, electric charge, thickness and structures, are delicately tailored through a nano-engineered fabrication process, that is, graphene oxide (GO) nanosheet assisted phase inversion coupled with surface functionalization. Compared with the membrane fabricated by conventional phase inversion, this novel membrane has four times higher water flux, significantly higher rejections of both oil (~99.9%) and surfactant (as high as 93.5%), and two thirds lower fouling ratio when treating surfactant stabilized oil-in-water nanoemulsion. Due to its excellent performances and facile fabrication process, this nano-engineered membrane is expected to have wide practical applications in the oil/water separation fields of environmental protection and water purification. PMID:27087362

  12. A new nano-engineered hierarchical membrane for concurrent removal of surfactant and oil from oil-in-water nanoemulsion

    PubMed Central

    Qin, Detao; Liu, Zhaoyang; Bai, Hongwei; Sun, Darren Delai; Song, Xiaoxiao

    2016-01-01

    Surfactant stabilized oil-in-water nanoemulsions pose a severe threat to both the environment and human health. Recent development of membrane filtration technology has enabled efficient oil removal from oil/water nanoemulsion, however, the concurrent removal of surfactant and oil remains unsolved because the existing filtration membranes still suffer from low surfactant removal rate and serious surfactant-induced fouling issue. In this study, to realize the concurrent removal of surfactant and oil from nanoemulsion, a novel hierarchically-structured membrane is designed with a nanostructured selective layer on top of a microstructured support layer. The physical and chemical properties of the overall membrane, including wettability, surface roughness, electric charge, thickness and structures, are delicately tailored through a nano-engineered fabrication process, that is, graphene oxide (GO) nanosheet assisted phase inversion coupled with surface functionalization. Compared with the membrane fabricated by conventional phase inversion, this novel membrane has four times higher water flux, significantly higher rejections of both oil (~99.9%) and surfactant (as high as 93.5%), and two thirds lower fouling ratio when treating surfactant stabilized oil-in-water nanoemulsion. Due to its excellent performances and facile fabrication process, this nano-engineered membrane is expected to have wide practical applications in the oil/water separation fields of environmental protection and water purification. PMID:27087362

  13. Influence of the phase behavior on the properties of ionic nanoemulsions prepared by the phase inversion composition method.

    PubMed

    Maestro, Alicia; Solè, Isabel; González, Carmen; Solans, Conxita; Gutiérrez, José M

    2008-11-15

    The low-energy emulsification method phase inversion composition (PIC) was used to prepare O/W nanoemulsions in the W/oleylammonium chloride-oleylamine-C12E10/hexadecane ionic system, where the oleylammonium acted as a cationic surfactant. The results obtained, in terms of phase diagrams and emulsion characteristics, were compared with those obtained in the system W/potassium oleate-oleic acid-C12E10/hexadecane [I. Solè, A. Maestro, C. González, C. Solans, J.M. Gutiérrez, Langmuir 22 (2006) 8326], in which the oleate acted as an anionic surfactant. This study was done in order to extend the application range of the ionic nanoemulsions, not only in anionic systems but also in cationic ones, and in order to deep further into the nanoemulsion formation mechanism. The results show again that to obtain small droplet-sized nanoemulsions it is necessary to cross a direct cubic liquid crystal phase along the emulsification path, and it is also crucial to remain in this phase enough time and to use a proper mixing rate to incorporate all the oil into the liquid crystal. Then, when nanoemulsion forms, the oil is already intimately mixed with all the components, and the nanoemulsification is easier. Structural studies made with both cationic and anionic systems confirmed that the size of the "micelles" that form the cubic phase is the same or slightly smaller than the size of the nanoemulsion droplets obtained, depending on the emulsification path, which seems to point out that the nanoemulsions are formed in both cases by a dilution process of this cubic phase. When further watery solution is added to the cubic liquid crystal, these micelles separate, disrupting the cubic structure, and a small fraction of the surfactant migrates to the water. Moreover, due to the change in pH, the spontaneous curvature increases. Then, the phases in equilibrium are an oil-in-water microemulsion (W(m)) and the oil in excess. However, through this emulsification method, the surfactants can

  14. Cavitation-enhanced MR-guided focused ultrasound ablation of rabbit tumors in vivo using phase shift nanoemulsions

    PubMed Central

    Kopechek, Jonathan A; Park, Eun-Joo; Zhang, Yong-Zhi; Vykhodtseva, Natalia I; McDannold, Nathan J; Porter, Tyrone M

    2014-01-01

    Advanced tumors are often inoperable due to their size and proximity to critical vascular structures. High intensity focused ultrasound (HIFU) has been developed to non-invasively thermally ablate inoperable solid tumors. However, the clinical feasibility of HIFU ablation therapy has been limited by the long treatment times (on the order of hours) and high acoustic intensities required. Studies have shown that inertial cavitation can enhance HIFU-mediated heating by generating broadband acoustic emissions that increase tissue absorption and accelerate HIFU-induced heating. Unfortunately, initiating inertial cavitation in tumors requires high intensities and can be unpredictable. To address this need, phase-shift nanoemulsions (PSNE) have been developed. PSNE consist of lipid-coated liquid perfluorocarbon droplets that are less than 200 nm in diameter, thereby allowing passive accumulation in tumors through leaky tumor vasculature. PSNE can be vaporized into microbubbles in tumors in order to nucleate cavitation activity and enhance HIFU-mediated heating. In this study, MR-guided HIFU treatments were performed on intramuscular rabbit VX2 tumors in vivo to assess the effect of vaporized PSNE on acoustic cavitation and HIFU-mediated heating. HIFU pulses were delivered for 30 seconds using a 1.5 MHz, MR-compatible transducer, and cavitation emissions were recorded with a 650-kHz ring hydrophone while temperature was monitored using MR thermometry. Cavitation emissions were significantly higher (P<0.05) after PSNE injection and this was well correlated with enhanced HIFU-mediated heating in tumors. The peak temperature rise induced by sonication was significantly higher (P<0.05) after PSNE injection. For example, the mean percent change in temperature achieved at 5.2 W of acoustic power was 46 ± 22% with PSNE injection. The results indicate that PSNE nucleates cavitation which correlates with enhanced HIFU-mediated heating in tumors. This suggests that PSNE could

  15. Facial Resemblance to Emotions: Group Differences, Impression Effects, and Race Stereotypes

    PubMed Central

    Zebrowitz, Leslie A.; Kikuchi, Masako; Fellous, Jean-Marc

    2013-01-01

    The authors used connectionist modeling to extend previous research on emotion overgeneralization effects. Study 1 demonstrated that neutral expression male faces objectively resemble angry expressions more than female faces do, female faces objectively resemble surprise expressions more than male faces do, White faces objectively resemble angry expressions more than Black or Korean faces do, and Black faces objectively resemble happy and surprise expressions more than White faces do. Study 2 demonstrated that objective resemblance to emotion expressions influences trait impressions even when statistically controlling possible confounding influences of attractiveness and babyfaceness. It further demonstrated that emotion overgeneralization is moderated by face race and that racial differences in emotion resemblance contribute to White perceivers’ stereotypes of Blacks and Asians. These results suggest that intergroup relations may be strained not only by cultural stereotypes but also by adaptive responses to emotion expressions that are overgeneralized to groups whose faces subtly resemble particular emotions. PMID:20085393

  16. Facial resemblance to emotions: group differences, impression effects, and race stereotypes.

    PubMed

    Zebrowitz, Leslie A; Kikuchi, Masako; Fellous, Jean-Marc

    2010-02-01

    The authors used connectionist modeling to extend previous research on emotion overgeneralization effects. Study 1 demonstrated that neutral expression male faces objectively resemble angry expressions more than female faces do, female faces objectively resemble surprise expressions more than male faces do, White faces objectively resemble angry expressions more than Black or Korean faces do, and Black faces objectively resemble happy and surprise expressions more than White faces do. Study 2 demonstrated that objective resemblance to emotion expressions influences trait impressions even when statistically controlling possible confounding influences of attractiveness and babyfaceness. It further demonstrated that emotion overgeneralization is moderated by face race and that racial differences in emotion resemblance contribute to White perceivers' stereotypes of Blacks and Asians. These results suggest that intergroup relations may be strained not only by cultural stereotypes but also by adaptive responses to emotion expressions that are overgeneralized to groups whose faces subtly resemble particular emotions.

  17. Development of Organogel-Derived Capsaicin Nanoemulsion with Improved Bioaccessibility and Reduced Gastric Mucosa Irritation.

    PubMed

    Lu, Muwen; Cao, Yong; Ho, Chi-Tang; Huang, Qingrong

    2016-06-15

    Capsaicin (CAP) is the major active component in chili peppers with health-promoting benefits. However, the low bioavailability and irritating quality of CAP greatly limit its applications in functional foods. The objective of this study was to develop a food-grade nanoemulsion to increase the dissolution and bioaccessibility of CAP and to alleviate its irritating effects. To achieve this goal, CAP was first dissolved in medium-chain triacylglycerol (MCT), followed by the addition of sucrose stearate S-370 as organogelator to develop CAP-loaded organogel. The oil-in-water (O/W) emulsion was formed using organogel as the oil phase and Tween 80 as the emulsifier. After ultrasonication treatment, droplet sizes of emulsion were decreased to 168 nm with enhanced dissolution rate and bioaccessibility. In vivo study further confirmed the reduced rat gastric mucosa irritation caused by CAP. The organogel-derived nanoemulsion was proved to be an effective delivery system for CAP-based functional food products. PMID:27170269

  18. Development of Organogel-Derived Capsaicin Nanoemulsion with Improved Bioaccessibility and Reduced Gastric Mucosa Irritation.

    PubMed

    Lu, Muwen; Cao, Yong; Ho, Chi-Tang; Huang, Qingrong

    2016-06-15

    Capsaicin (CAP) is the major active component in chili peppers with health-promoting benefits. However, the low bioavailability and irritating quality of CAP greatly limit its applications in functional foods. The objective of this study was to develop a food-grade nanoemulsion to increase the dissolution and bioaccessibility of CAP and to alleviate its irritating effects. To achieve this goal, CAP was first dissolved in medium-chain triacylglycerol (MCT), followed by the addition of sucrose stearate S-370 as organogelator to develop CAP-loaded organogel. The oil-in-water (O/W) emulsion was formed using organogel as the oil phase and Tween 80 as the emulsifier. After ultrasonication treatment, droplet sizes of emulsion were decreased to 168 nm with enhanced dissolution rate and bioaccessibility. In vivo study further confirmed the reduced rat gastric mucosa irritation caused by CAP. The organogel-derived nanoemulsion was proved to be an effective delivery system for CAP-based functional food products.

  19. Hydrogel-thickened nanoemulsion system for topical delivery of lipophilic drugs.

    PubMed

    Mou, Dongsheng; Chen, Huabing; Du, Danrong; Mao, Chengwen; Wan, Jiangling; Xu, Huibi; Yang, Xiangliang

    2008-04-01

    In this work, a hydrogel-thickened nanoemulsion system (HTN) with powerful permeation ability, good stability and suitable viscosity was investigated for topical delivery of active molecules. HTN was prepared to deliver an oily mixture of 5% camphor, 5% menthol and 5% methyl salicylate for topical therapy of arthritis, minor joint and muscle pain using soybean oil as the oil phase, soybean lecithin, Tween 80 and poloxamer 407 as the surfactants, propylene glycol as the cosurfactant, carbomer 940 as a thickening agent. The HTN system was found to combine the o/w microstructure of nanoemulsion with the gel network of hydrogel and had a suitable viscosity of 133.2PaS. The system had small average diameters and good long-term stability. The abilities of HTN to deliver the high amounts of camphor, menthol and methyl salicylate were evaluated using the in vitro permeation studies. The permeation rates of camphor, menthol and methyl salicylate from the optimal HTN formulation were 138.0+/-6.5, 63.6+/-3.3, 53.8+/-3.2 microg cm(-2) h(-1) and showed the significant advantages over the control gel. The HTN with good stability and powerful permeation enhancing ability and suitable viscosity might be a promising prospective carrier for topical delivery of lipophilic drugs. PMID:18215479

  20. A potential tocopherol acetate loaded palm oil esters-in-water nanoemulsions for nanocosmeceuticals

    PubMed Central

    2010-01-01

    Background Cosmeceuticals are cosmetic-pharmaceutical hybrids intended to enhance health and beauty of the skin. Nanocosmeceuticals use nano-sized system for the delivery of active ingredients to the targeted cells for better penetration. In this work, nanoemulsion from palm oil esters was developed as a delivery system to produce nanocosmeceuticals. The stability of the resulting formulation was tested using various methods. In addition, the effect of components i.e. Vitamin E and Pluronic F-68 on the formulation was also studied. Results Both vitamin E and Pluronic F-68 were found to co-emulsify and co-stabilized the formulations. The best formulation was found to be the one having the composition of 10% Palm Oil Esters (POEs), 10% vitamin E, 24% Tween 80, 2.4% Pluronic F-68 and 53.6% deionised water. Those compositions are considered to be the best as a nanocosmeceutical product due to the small particle size (94.21 nm), low occurrence of Ostwald ripening and stable at different storing temperatures (5, 25 and 45°C) for four weeks. Conclusions Palm oil esters-in-water nanoemulsions loaded with vitamin E was successfully formulated and has the potential for the use as nanocosmeceuticals. PMID:20178581

  1. Mesophase and size manipulation of itraconazole liquid crystalline nanoparticles produced via quasi nanoemulsion precipitation.

    PubMed

    Mugheirbi, Naila A; Tajber, Lidia

    2015-10-01

    The fabrication of drug nanoparticles (NPs) with process-mediated tunable properties and performances continues to grow rapidly during the last decades. This study investigates the synthesis and phase tuning of nanoparticulate itraconazole (ITR) mesophases using quasi nanoemulsion precipitation from acetone/water systems to seek out an alternative pathway to the nucleation-based NP formation. ITR liquid crystalline (LC) phases were formed and nematic-smectic mesomorphism was achieved via controlling solvent:antisolvent temperature difference (ΔTS:AS). The use of ΔTS:AS=49.5°C was associated with a nematic assembly, while intercalated smectic A layering was observed at ΔTS:AS=0°C, with both phases confined in the nanospheres at room temperature. The quasi emulsion system has not been investigated at the nanoscale to date and in contrary to the microscale, quasi nanoemulsion was observed over the solvent:antisolvent viscosity ratios of 1:7-1:1.4. Poly(acrylic acid) in the solvent phase exhibited a concentration dependent interaction when ITR formed NPs. This nanodroplet-based approach enabled the preparation of a stable ITR nanodispersion using Poloxamer 407 at 80°C, which was unachievable before using precipitation via nucleation. Findings of this work lay groundwork in terms of rationalised molecular assembly as a tool in designing pharmaceutical LC NPs with tailored properties.

  2. Homogeneous percolation versus arrested phase separation in attractively-driven nanoemulsion colloidal gels.

    PubMed

    Helgeson, Matthew E; Gao, Yongxiang; Moran, Shannon E; Lee, Jinkee; Godfrin, Michael; Tripathi, Anubhav; Bose, Arijit; Doyle, Patrick S

    2014-05-01

    We elucidate mechanisms for colloidal gelation of attractive nanoemulsions depending on the volume fraction (ϕ) of the colloid. Combining detailed neutron scattering, cryo-transmission electron microscopy and rheological measurements, we demonstrate that gelation proceeds by either of two distinct pathways. For ϕ sufficiently lower than 0.23, gels exhibit homogeneous fractal microstructure, with a broad gel transition resulting from the formation and subsequent percolation of droplet-droplet clusters. In these cases, the gel point measured by rheology corresponds precisely to arrest of the fractal microstructure, and the nonlinear rheology of the gel is characterized by a single yielding process. By contrast, gelation for ϕ sufficiently higher than 0.23 is characterized by an abrupt transition from dispersed droplets to dense clusters with significant long-range correlations well-described by a model for phase separation. The latter phenomenon manifests itself as micron-scale "pores" within the droplet network, and the nonlinear rheology is characterized by a broad yielding transition. Our studies reinforce the similarity of nanoemulsions to solid particulates, and identify important qualitative differences between the microstructure and viscoelastic properties of colloidal gels formed by homogeneous percolation and those formed by phase separation.

  3. Quantification and evaluation of thymoquinone loaded mucoadhesive nanoemulsion for treatment of cerebral ischemia.

    PubMed

    Ahmad, Niyaz; Ahmad, Rizwan; Alam, Md Aftab; Samim, Mohd; Iqbal, Zeenat; Ahmad, Farhan Jalees

    2016-07-01

    Stroke is an important cause of deaths worldwide, resulting in an irreversible deterioration of the central nervous system. Finally, production of more free radicals. Therefore, Thymoquinone is having antioxidant property and reported to have a potential role in the amelioration of cerebral ischemia but due to low solubility and poor absorption; they exhibit low serum and tissue levels. Present work aims to prepare nanoemulsions in order enhance the bioavailability of drug and hence evaluate the drug targeting in brain via non-invasive nasal route administration. Thymoquinone Mucoadhesive Nanoemulsion (TMNE) was prepared by ionic gelation method; characterized for particles size, entrapment efficiency, zeta potential, and ex vivo permeation study. Optimized TMNE ended up with a mean globule size 94.8±6.61nm; zeta potential -13.5±1.01mV; drug content 99.86±0.35% and viscosity 110±12cp. Ultra Performance Liquid Chromatography-Photodiode Array (UPLC-PDA) based bioanalytical method was developed and validated for pharmacokinetics, biodistribution, brain-targeting efficiency (628.5786±44.79%) and brain drug-targeting potential (89.97±2.94%) studies via post intranasal administration which revealed enhanced bioavailability of TQ in brain as compared to intravenous administration. Improved neurobehavioural activity (locomotor and grip strength) was observed in middle cerebral artery occlusion induced cerebral ischemic rats after i.n. administration of TMNE. PMID:26976069

  4. Formulation Optimization of a Palm-Based Nanoemulsion System Containing Levodopa

    PubMed Central

    Zainol, Syafinaz; Basri, Mahiran; Basri, Hamidon Bin; Shamsuddin, Ahmad Fuad; Abdul-Gani, Siti Salwa; Karjiban, Roghayeh Abedi; Abdul-Malek, Emilia

    2012-01-01

    Response surface methodology (RSM) was utilized to investigate the influence of the main emulsion composition; mixture of palm and medium-chain triglyceride (MCT) oil (6%–12% w/w), lecithin (1%–3% w/w), and Cremophor EL (0.5%–1.5% w/w) as well as the preparation method; addition rate (2–20 mL/min), on the physicochemical properties of palm-based nanoemulsions. The response variables were the three main emulsion properties; particle size, zeta potential and polydispersity index. Optimization of the four independent variables was carried out to obtain an optimum level palm-based nanoemulsion with desirable characteristics. The response surface analysis showed that the variation in the three responses could be depicted as a quadratic function of the main composition of the emulsion and the preparation method. The experimental data could be fitted sufficiently well into a second-order polynomial model. The optimized formulation was stable for six months at 4 °C. PMID:23202937

  5. Nanoemulsions containing a synthetic chalcone as an alternative for treating cutaneous leshmaniasis: optimization using a full factorial design

    PubMed Central

    de Mattos, Cristiane Bastos; Argenta, Débora Fretes; Melchiades, Gabriela de Lima; Sechini Cordeiro, Marlon Norberto; Tonini, Maiko Luis; Moraes, Milene Hoehr; Weber, Tanara Beatriz; Roman, Silvane Souza; Nunes, Ricardo José; Teixeira, Helder Ferreira; Steindel, Mário; Koester, Letícia Scherer

    2015-01-01

    Nanoemulsions are drug delivery systems that may increase the penetration of lipophilic compounds through the skin, enhancing their topical effect. Chalcones are compounds of low water solubility that have been described as promising molecules for the treatment of cutaneous leishmaniasis (CL). In this context, the aim of this work was to optimize the development of a nanoemulsion containing a synthetic chalcone for CL treatment using a 22 full factorial design. The formulations were prepared by spontaneous emulsification and the experimental design studied the influence of two independent variables (type of surfactant – soybean lecithin or sorbitan monooleate and type of co-surfactants – polysorbate 20 or polysorbate 80) on the physicochemical characteristics of the nanoemulsions, as well as on the skin permeation/retention of the synthetic chalcone in porcine skin. In order to evaluate the stability of the systems, the antileishmanial assay was performed against Leishmania amazonensis 24 hours and 60 days after the preparation of the nanoemulsions. The formulation composed of soybean lecithin and polysorbate 20 presented suitable physicochemical characteristics (droplet size 171.9 nm; polydispersity index 0.14; zeta potential −39.43 mV; pH 5.16; and viscosity 2.00 cP), drug content (91.09%) and the highest retention in dermis (3.03 µg·g−1) – the main response of interest – confirmed by confocal microscopy. This formulation also presented better stability of leishmanicidal activity in vitro against L. amazonensis amastigote forms (half maximal inhibitory concentration value 0.32±0.05 µM), which confirmed the potential of the nanoemulsion soybean lecithin and polysorbate 20 for CL treatment. PMID:26366075

  6. Inhibition of lung cancer cells A549 and H460 by curcuminoid extracts and nanoemulsions prepared from Curcuma longa Linnaeus.

    PubMed

    Chang, Hong-Bin; Chen, Bing-Huei

    2015-01-01

    The objectives of this study were to explore the inhibition mechanism of lung cancer cells A549 and H460 by curcuminoid extracts and nanoemulsions prepared from Curcuma longa Linnaeus. In addition, human bronchus epithelial cell line BEAS-2B (normal cell) was selected for comparison. A high-performance liquid chromatography (HPLC) method was developed to separate and quantify the various curcuminoids in C. longa extract, including curcumin (1,714.5 μg/mL), demethoxycurcumin (1,147.4 μg/mL), and bisdemethoxycurcumin (190.2 μg/mL). A high-stability nanoemulsion composed of Tween 80, water, and curcuminoid extract was prepared, with mean particle size being 12.6 nm. The cell cycle was retarded at G2/M for both the curcuminoid extract and nanoemulsion treatments; however, the inhibition pathway may be different. H460 cells were more susceptible to apoptosis than A549 cells for both curcuminoid extract and nanoemulsion treatments. Growth of BEAS-2B remained unaffected for both the curcuminoid extract and nanoemulsion treatments, with a concentration range from 1 to 4 μg/mL. Also, the activities of caspase-3, caspase-8, and caspase-9 followed a dose-dependent increase for both A549 and H460 cells for both the treatments, accompanied by a dose-dependent increase in cytochrome C expression and a dose-dependent decrease in CDK1 expression. Interestingly, a dose-dependent increase in cyclin B expression was shown for A549 cells for both the treatments, while a reversed trend was found for H460 cells. Both mitochondria and death receptor pathways may be responsible for apoptosis of both A549 and H460 cells.

  7. Inhibition of lung cancer cells A549 and H460 by curcuminoid extracts and nanoemulsions prepared from Curcuma longa Linnaeus

    PubMed Central

    Chang, Hong-Bin; Chen, Bing-Huei

    2015-01-01

    The objectives of this study were to explore the inhibition mechanism of lung cancer cells A549 and H460 by curcuminoid extracts and nanoemulsions prepared from Curcuma longa Linnaeus. In addition, human bronchus epithelial cell line BEAS-2B (normal cell) was selected for comparison. A high-performance liquid chromatography (HPLC) method was developed to separate and quantify the various curcuminoids in C. longa extract, including curcumin (1,714.5 μg/mL), demethoxycurcumin (1,147.4 μg/mL), and bisdemethoxycurcumin (190.2 μg/mL). A high-stability nanoemulsion composed of Tween 80, water, and curcuminoid extract was prepared, with mean particle size being 12.6 nm. The cell cycle was retarded at G2/M for both the curcuminoid extract and nanoemulsion treatments; however, the inhibition pathway may be different. H460 cells were more susceptible to apoptosis than A549 cells for both curcuminoid extract and nanoemulsion treatments. Growth of BEAS-2B remained unaffected for both the curcuminoid extract and nanoemulsion treatments, with a concentration range from 1 to 4 μg/mL. Also, the activities of caspase-3, caspase-8, and caspase-9 followed a dose-dependent increase for both A549 and H460 cells for both the treatments, accompanied by a dose-dependent increase in cytochrome C expression and a dose-dependent decrease in CDK1 expression. Interestingly, a dose-dependent increase in cyclin B expression was shown for A549 cells for both the treatments, while a reversed trend was found for H460 cells. Both mitochondria and death receptor pathways may be responsible for apoptosis of both A549 and H460 cells. PMID:26345201

  8. PLGA nanoparticles from nano-emulsion templating as imaging agents: Versatile technology to obtain nanoparticles loaded with fluorescent dyes.

    PubMed

    Fornaguera, C; Feiner-Gracia, N; Calderó, G; García-Celma, M J; Solans, C

    2016-11-01

    The interest in polymeric nanoparticles as imaging systems for biomedical applications has increased notably in the last decades. In this work, PLGA nanoparticles, prepared from nano-emulsion templating, have been used to prepare novel fluorescent imaging agents. Two model fluorescent dyes were chosen and dissolved in the oil phase of the nano-emulsions together with PLGA. Nano-emulsions were prepared by the phase inversion composition (PIC) low-energy method. Fluorescent dye-loaded nanoparticles were obtained by solvent evaporation of nano-emulsion templates. PLGA nanoparticles loaded with the fluorescent dyes showed hydrodynamic radii lower than 40nm; markedly lower than those reported in previous studies. The small nanoparticle size was attributed to the nano-emulsification strategy used. PLGA nanoparticles showed negative surface charge and enough stability to be used for biomedical imaging purposes. Encapsulation efficiencies were higher than 99%, which was also attributed to the nano-emulsification approach as well as to the low solubility of the dyes in the aqueous component. Release kinetics of both fluorescent dyes from the nanoparticle dispersions was pH-independent and sustained. These results indicate that the dyes could remain encapsulated enough time to reach any organ and that the decrease of the pH produced during cell internalization by the endocytic route would not affect their release. Therefore, it can be assumed that these nanoparticles are appropriate as systemic imaging agents. In addition, in vitro toxicity tests showed that nanoparticles are non-cytotoxic. Consequently, it can be concluded that the preparation of PLGA nanoparticles from nano-emulsion templating represents a very versatile technology that enables obtaining biocompatible, biodegradable and safe imaging agents suitable for biomedical purposes.

  9. Preparation of artificial plasma membrane mimicking vesicles with lipid asymmetry.

    PubMed

    Lin, Qingqing; London, Erwin

    2014-01-01

    Lipid asymmetry, the difference in lipid distribution across the lipid bilayer, is one of the most important features of eukaryotic cellular membranes. However, commonly used model membrane vesicles cannot provide control of lipid distribution between inner and outer leaflets. We recently developed methods to prepare asymmetric model membrane vesicles, but facile incorporation of a highly controlled level of cholesterol was not possible. In this study, using hydroxypropyl-α-cyclodextrin based lipid exchange, a simple method was devised to prepare large unilamellar model membrane vesicles that closely resemble mammalian plasma membranes in terms of their lipid composition and asymmetry (sphingomyelin (SM) and/or phosphatidylcholine (PC) outside/phosphatidylethanolamine (PE) and phosphatidylserine (PS) inside), and in which cholesterol content can be readily varied between 0 and 50 mol%. We call these model membranes "artificial plasma membrane mimicking" ("PMm") vesicles. Asymmetry was confirmed by both chemical labeling and measurement of the amount of externally-exposed anionic lipid. These vesicles should be superior and more realistic model membranes for studies of lipid-lipid and lipid-protein interaction in a lipid environment that resembles that of mammalian plasma membranes.

  10. Pomegranate seed oil nanoemulsions improve the photostability and in vivo antinociceptive effect of a non-steroidal anti-inflammatory drug.

    PubMed

    Ferreira, Luana Mota; Sari, Marcel Henrique Marcondes; Cervi, Verônica Ferrari; Gehrcke, Mailine; Barbieri, Allanna Valentini; Zborowski, Vanessa Angonesi; Beck, Ruy Carlos Ruver; Nogueira, Cristina Wayne; Cruz, Letícia

    2016-08-01

    The combination of pomegranate seed oil and ketoprofen in nanoemulsions aiming to improve the antinociceptive effect was evaluated according to the writhing test and Complete Freud's Adjuvant induced paw inflammation in mice. The formulations showed adequate characteristics and improved ketoprofen's photostability against UVC radiation exposure. The dialysis bag technique showed that 100% of the drug was released from the nanoemulsions after 3h and the oil amount had no influence on the releasing. Furthermore, time- and dose-response curves were obtained to determine the antinociceptive effect of the formulations. In the post-test, the nanoemulsion containing ketoprofen significantly reduced abdominal constrictions in time-response curve, showing effect up to 12h while the free ketoprofen showed effect up to 3h. In addition, the blank nanoemulsion presented a reduction of abdominal constriction up to 1h of pre-treatment. Regarding the dose-response curve, the free ketoprofen presents effect at 0.5mg/Kg dose and nanoemulsion at 1.0mg/Kg dose. Time- and dose-response curves were performed to determine the antinociceptive effect in inflammatory pain. After the evaluation of mechanical allodynia testing at the Von Frey Hair, the free ketoprofen showed effect up to 6h while nanoemulsions presented effect up to 10h. Moreover, acute toxicity was performed with ALT and AST activity evaluations and urea levels. After 7 days of treatment, no toxic effects for nanoemulsions were found. In conclusion, ketoprofen-loaded pomegranate seed oil nanoemulsions presented adequate characteristics and a high antinociceptive activity in the animal models tested.

  11. Pomegranate seed oil nanoemulsions improve the photostability and in vivo antinociceptive effect of a non-steroidal anti-inflammatory drug.

    PubMed

    Ferreira, Luana Mota; Sari, Marcel Henrique Marcondes; Cervi, Verônica Ferrari; Gehrcke, Mailine; Barbieri, Allanna Valentini; Zborowski, Vanessa Angonesi; Beck, Ruy Carlos Ruver; Nogueira, Cristina Wayne; Cruz, Letícia

    2016-08-01

    The combination of pomegranate seed oil and ketoprofen in nanoemulsions aiming to improve the antinociceptive effect was evaluated according to the writhing test and Complete Freud's Adjuvant induced paw inflammation in mice. The formulations showed adequate characteristics and improved ketoprofen's photostability against UVC radiation exposure. The dialysis bag technique showed that 100% of the drug was released from the nanoemulsions after 3h and the oil amount had no influence on the releasing. Furthermore, time- and dose-response curves were obtained to determine the antinociceptive effect of the formulations. In the post-test, the nanoemulsion containing ketoprofen significantly reduced abdominal constrictions in time-response curve, showing effect up to 12h while the free ketoprofen showed effect up to 3h. In addition, the blank nanoemulsion presented a reduction of abdominal constriction up to 1h of pre-treatment. Regarding the dose-response curve, the free ketoprofen presents effect at 0.5mg/Kg dose and nanoemulsion at 1.0mg/Kg dose. Time- and dose-response curves were performed to determine the antinociceptive effect in inflammatory pain. After the evaluation of mechanical allodynia testing at the Von Frey Hair, the free ketoprofen showed effect up to 6h while nanoemulsions presented effect up to 10h. Moreover, acute toxicity was performed with ALT and AST activity evaluations and urea levels. After 7 days of treatment, no toxic effects for nanoemulsions were found. In conclusion, ketoprofen-loaded pomegranate seed oil nanoemulsions presented adequate characteristics and a high antinociceptive activity in the animal models tested. PMID:27088191

  12. Biodistribution of X-ray iodinated contrast agent in nano-emulsions is controlled by the chemical nature of the oily core.

    PubMed

    Attia, Mohamed F; Anton, Nicolas; Chiper, Manuela; Akasov, Roman; Anton, Halina; Messaddeq, Nadia; Fournel, Sylvie; Klymchenko, Andrey S; Mély, Yves; Vandamme, Thierry F

    2014-10-28

    In this study, we investigated the role of the chemical nature of the oil droplet core of nano-emulsions used as contrast agents for X-ray imaging on their pharmacokinetics and biodistribution. To this end, we formulated PEGylated nano-emulsions with two iodinated oils (i.e., iodinated monoglyceride and iodinated castor oil) and compared them with another iodinated nano-emulsion based on iodinated vitamin E. By using dynamic light scattering and transmission electron microscopy, the three iodinated nano-emulsions were found to exhibit comparable morphologies, size, and surface composition. Furthermore, they were shown to be endowed with very high iodine concentration, which leads to stronger X-ray attenuation properties as compared to the commercial iodinated nano-emulsion Fenestra VC. The three nano-emulsions were i.v. administered in mice and monitored by microcomputed tomography (micro-CT). They showed high contrast enhancement in blood with similar half-life around 6 h but very different accumulation sites. While iodinated monoglycerides exhibited low accumulation in liver and spleen, high accumulation in spleen was observed for iodinated castor oil and in liver for vitamin E. These data clearly highlighted the important role of the oil composition of the nano-emulsion core to obtain strong X-ray contrast enhancement in specific targets such as liver, spleen, or only blood. These differences in biodistribution were partly attributed to differences in the uptake of the nanodroplets by the macrophages in vitro. Another key feature of these nano-emulsions is their long half-elimination time (several weeks), which offers sufficient retention for micro-CT imaging. This work paves the way for the design of nanoparticulate contrast agents for X-ray imaging of selected organs.

  13. Combined effect of a nanoemulsion of D-limonene and nisin on Listeria monocytogenes growth and viability in culture media and foods.

    PubMed

    Maté, Javier; Periago, Paula M; Palop, Alfredo

    2016-03-01

    The present work evaluated the antibacterial effect of nanoemulsions from natural compounds d-limonene and nisin against Listeria monocytogenes in tryptic soy broth growth medium, chicken broth, and vegetable cream. Experiments were performed by means of optical density growth curves and studies of viability in culture media and foods. Stability of nanoemulsions was evaluated by a Mastersizer 2000 equipment. Results showed greater effectiveness when applying D-limonene in form of nanoemulsion than when applying it directly, and when using both compounds together, both directly and in the form of nanoemulsion. Concentration of L. monocytogenes decreased at least in three log cycles in all the culture media and foods used within the first 90 min after the addition of the natural antimicrobials combined in form of nanoemulsion. Moreover, the growth of L. monocytogenes was inhibited with the combination of antimicrobials in the four weeks that the experiment lasted. Nanoemulsion technology would solve present problems of solubility and stability of oily antimicrobials in the food industry.

  14. Solid lipid nanoparticles: promising therapeutic nanocarriers for drug delivery.

    PubMed

    Thukral, Dipti Kakkar; Dumoga, Shweta; Mishra, Anil K

    2014-01-01

    Development of colloidal delivery systems has opened new avenues/frontiers for improving drug delivery. Solid lipid nanoparticles have come up as the latest development in the arena of lipid based colloidal delivery systems after nanoemulsion and liposomes ever since their introduction in the early 1990s. In this review, the authors have made efforts to bring forth the essential and practically relevant aspects of SLNs. This review gives an overview of the preparation methods of solid lipid nanoparticles while mainly focussing on their biological applications including their projected applications in drug delivery. This review critically examines the influential factors governing the formation of SLNs and then discussing in detail the several techniques being utilized for their characterization. This review discusses the drug loading and drug release aspects of SLNs as these are useful biocompatible carriers of lipophilic and to a certain extent hydrophilic drugs. An updated list of drugs encapsulated into various lipids to prepare SLN formulations has been provided. Other relevant aspects pertaining to the clinical use of SLN formulations like their sterilization and storage stability have also been explained. A unique facet of this review is the discussion on the challenging issues of in vivo applications and recent progresses in overcoming these challenges which follows in the end. PMID:25469779

  15. Nanoemulsion-templated polylelectrolyte multifunctional nanocapsules for DNA entrapment and bioimaging.

    PubMed

    Bazylińska, Urszula; Saczko, Jolanta

    2016-01-01

    The emerging field of bionanotechnology aims at advancing colloidal and biomedical research via introduction of multifunctional nanoparticle-based containers intended for both gene therapy and bioimaging. In the present contribution we entrapped the model genetic material (herring testes DNA) in the newly-designed non-viral vectors, i.e., multifunctional nanocapsules obtained by layer-by-layer (LbL) adsorption of DNA and oppositely charged polysaccharide-based chitosan (CHIT) on the nanoemulsion core, loaded by IR-780 indocyanine (used as the fluorescent marker) and stabilized by gemini-type ammonium salts: N,N,N',N'-tetramethyl-N,N'-di(dodecyl)-ethylenediammonium bromide, d(DDA)PBr and N,N,N',N'-tetramethyl-N,N'-di(dodecyl)-butylenediammonium d(DDA)BBr. Ternary phase diagrams of the surfactant-oil-water systems were determined by titration method. Then, the stability of the nanoemulsions obtained with IR-780 solubilized in the oleic acid (OA) or isopropyl myristate (IPM) phase was evaluated by backscattering (BS) profiles and ζ-potential measurements. In the next step, CHIT and DNA layers were subsequently deposited on the kinetically stable nanoemulsion cores. The IR-780-loaded nanocarriers covered by (DNA/CHIT)4 bilayers shown the high ζ-potential value (about +43mV provided by Doppler electrophoresis), the size <120nm and the spherical shape as analyzed by dynamic light scattering (DLS), atomic force microscopy (AFM) and scanning electron microscopy (SEM). Finally, the long-lasting nanosystems were subjected to in vitro biological studies on human cancer cell lines - doxorubicin-sensitive breast (MCF-7/WT), epithelial lung adenocarcinoma (A549) and skin melanoma (MEWO). Biological response of the cell culture was expressed as cytotoxic activity evaluated by MTT-based proliferation assay as well as bioimaging of intracellular localization of IR-780 molecules loaded in the multilayer DNA-deposited nanocontainers - provided by confocal laser scanning microscopy

  16. Facial resemblance increases the attractiveness of same-sex faces more than other-sex faces.

    PubMed Central

    DeBruine, Lisa M.

    2004-01-01

    Our reactions to facial self-resemblance could reflect either specialized responses to cues of kinship or by-products of the general perceptual mechanisms of face encoding and mere exposure. The adaptive hypothesis predicts differences in reactions to self-resemblance in mating and prosocial contexts, while the by-product hypothesis does not. Using face images that were digitally transformed to resemble participants, I showed that the effects of resemblance on attractiveness judgements depended on both the sex of the judge and the sex of the face being judged: facial resemblance increased attractiveness judgements of same-sex faces more than other-sex faces, despite the use of identical procedures to manipulate resemblance. A control experiment indicated these effects were caused neither by lower resemblance of other-sex faces than same-sex faces, nor by an increased perception of averageness or familiarity of same-sex faces due to prototyping or mere exposure affecting only same-sex faces. The differential impact of self-resemblance on our perception of same-sex and other-sex faces supports the hypothesis that humans use facial resemblance as a cue of kinship. PMID:15451700

  17. Pyknoachondrogenesis: an association of skeletal defects resembling achondrogenesis with generalized bone sclerosis. A new condition?

    PubMed

    Camera, G; Giordano, F; Mastroiacovo, P

    1986-10-01

    A stillborn male with skeletal anomalies resembling achondrogenesis with remarkably sclerotic bones is reported. The term "Pyknoachondrogenesis" is suggested for this hitherto undescribed condition. PMID:3791681

  18. Sono-photoacoustic imaging of gold nanoemulsions: Part II. Real time imaging

    PubMed Central

    Arnal, Bastien; Wei, Chen-Wei; Perez, Camilo; Nguyen, Thu-Mai; Lombardo, Michael; Pelivanov, Ivan; Pozzo, Lilo D.; O’Donnell, Matthew

    2015-01-01

    Photoacoustic (PA) imaging using exogenous agents can be limited by degraded specificity due to strong background signals. This paper introduces a technique called sono-photoacoustics (SPA) applied to perfluorohexane nanodroplets coated with gold nanospheres. Pulsed laser and ultrasound (US) excitations are applied simultaneously to the contrast agent to induce a phase-transition ultimately creating a transient microbubble. The US field present during the phase transition combined with the large thermal expansion of the bubble leads to 20–30 dB signal enhancement. Aqueous solutions and phantoms with very low concentrations of this agent were probed using pulsed laser radiation at diagnostic exposures and a conventional US array used both for excitation and imaging. Contrast specificity of the agent was demonstrated with a coherent differential scheme to suppress US and linear PA background signals. SPA shows great potential for molecular imaging with ultrasensitive detection of targeted gold coated nanoemulsions and cavitation-assisted theranostic approaches. PMID:25893170

  19. New Edible Bionanocomposite Prepared by Pectin and Clove Essential Oil Nanoemulsions.

    PubMed

    Sasaki, Ronaldo S; Mattoso, Luiz H C; de Moura, Márcia Regina

    2016-06-01

    Nanocomposites are being extremely investigated to provide packaging with interesting characteristics for packages. Because of essential oils' natural occurrence and antibacterial activity, they are considered as an alternative for synthetic additives in the food industry. In this paper, we studied an edible bionanocomposite film made up of pectin and clove essential oil nanoemulsion for application as edible package. Mechanical properties, water vapor permeability (WVP), and antibacterial activity were analyzed. From mechanical and WVP analyses, we noticed an interesting improvement in film properties. In the antibacterial activity test, disk diffusion was used to assess the inhibition zones of Escherichia coli and Staphylococcus aureus. With these results, we concluded that the most interesting results were promoted by smaller nanodroplets (diameter of approximately 142 nm).

  20. Thermodynamic signature of secondary nano-emulsion formation by isothermal titration calorimetry.

    PubMed

    Fotticchia, Iolanda; Fotticchia, Teresa; Mattia, Carlo Andrea; Netti, Paolo Antonio; Vecchione, Raffaele; Giancola, Concetta

    2014-12-01

    The stabilization of oil in water nano-emulsions by means of a polymer coating is extremely important; it prolongs the shelf life of the product and makes it suitable for a variety of applications ranging from nutraceutics to cosmetics and pharmaceutics. To date, an effective methodology to assess the best formulations in terms of thermodynamic stability has yet to be designed. Here, we perform a complete physicochemical characterization based on isothermal titration calorimetry (ITC) compared to conventional dynamic light scattering (DLS) to identify polymer concentration domains that are thermodynamically stable and to define the degree of stability through thermodynamic functions depending upon any relevant parameter affecting the stability itself, such as type of polymer coating, droplet distance, etc. For instance, the method was proven by measuring the energetics in the case of two different biopolymers, chitosan and poly-L-lysine, and for different concentrations of the emulsion coated with poly-L-lysine.

  1. Shear Induced Rupturing of Nanoemulsion Droplets in Dilute and Concentrated Surfactant Solutions

    NASA Astrophysics Data System (ADS)

    Graves, S.

    2005-03-01

    We use high-pressure microfluidic injection to rupture silicone oil-in-water droplets repeatedly down to diameters below 100 nm, thereby creating ``nanoemulsions.'' These droplets are stabilized against coalescence by the surfactant sodium dodecyl sulfate (SDS). We systematically increase the SDS concentration, C, from 8 to 1000 mM, and we find a decrease in the droplet radius that follows a power law form:˜C^-α, where α= 1/3, over several decades in C down to an average radius of = 18 nm. The larger droplet radius at small C may be due to reduced coverage of the deformed droplet surfaces by the surfactant, thereby facilitating shear-induced coalescence. Our observed decrease in the droplet radius deviates from the classical prediction that the radius is inversely proportional to the viscosity of the continuous phase.

  2. Sono-photoacoustic imaging of gold nanoemulsions: Part I. Exposure thresholds

    PubMed Central

    Arnal, Bastien; Perez, Camilo; Wei, Chen-Wei; Xia, Jinjun; Lombardo, Michael; Pelivanov, Ivan; Matula, Thomas J.; Pozzo, Lilo D.; O’Donnell, Matthew

    2015-01-01

    Integrating high contrast bubbles from ultrasound imaging with plasmonic absorbers from photoacoustic imaging is investigated. Nanoemulsion beads coated with gold nanopsheres (NEB-GNS) are excited with simultaneous light (transient heat at the GNS's) and ultrasound (rarefactional pressure) resulting in a phase transition achievable under different scenarios, enhancing laser-induced acoustic signals and enabling specific detection of nanoprobes at lower concentration. An automated platform allowed dual parameter scans of both pressure and laser fluence while recording broadband acoustic signals. Two types of NEB-GNS and individual GNS were investigated and showed the great potential of this technique to enhance photoacoustic/acoustic signals. The NEB-GNS size distribution influences vaporization thresholds which can be reached at both permissible ultrasound and light exposures at deep penetration and at low concentrations of targets. This technique, called sono-photoacoustics, has great potential for targeted molecular imaging and therapy using compact nanoprobes with potentially high-penetrability into tissue. PMID:25893169

  3. Nonlinear contrast enhancement in photoacoustic molecular imaging with gold nanosphere encapsulated nanoemulsions

    SciTech Connect

    Wei, Chen-wei; Lombardo, Michael; Larson-Smith, Kjersta; Perez, Camilo; Xia, Jinjun; Matula, Thomas; Pozzo, Danilo; O'Donnell, Matthew; Pelivanov, Ivan

    2014-01-20

    A composite contrast agent, a nanoemulsion bead with assembled gold nanospheres at the interface, is proposed to improve the specific contrast of photoacoustic molecular imaging. A phase transition in the bead's core is induced by absorption of a nanosecond laser pulse with a fairly low laser fluence (∼3.5 mJ/cm{sup 2}), creating a transient microbubble through dramatically enhanced thermal expansion. This generates nonlinear photoacoustic signals with more than 10 times larger amplitude compared to that of a linear agent with the same optical absorption. By applying a differential scheme similar to ultrasound pulse inversion, more than 40 dB contrast enhancement is demonstrated with suppression of background signals.

  4. New Edible Bionanocomposite Prepared by Pectin and Clove Essential Oil Nanoemulsions.

    PubMed

    Sasaki, Ronaldo S; Mattoso, Luiz H C; de Moura, Márcia Regina

    2016-06-01

    Nanocomposites are being extremely investigated to provide packaging with interesting characteristics for packages. Because of essential oils' natural occurrence and antibacterial activity, they are considered as an alternative for synthetic additives in the food industry. In this paper, we studied an edible bionanocomposite film made up of pectin and clove essential oil nanoemulsion for application as edible package. Mechanical properties, water vapor permeability (WVP), and antibacterial activity were analyzed. From mechanical and WVP analyses, we noticed an interesting improvement in film properties. In the antibacterial activity test, disk diffusion was used to assess the inhibition zones of Escherichia coli and Staphylococcus aureus. With these results, we concluded that the most interesting results were promoted by smaller nanodroplets (diameter of approximately 142 nm). PMID:27427749

  5. Separating Oil-Water Nanoemulsions using Flux-Enhanced Hierarchical Membranes

    PubMed Central

    Solomon, Brian R.; Hyder, Md. Nasim; Varanasi, Kripa K.

    2014-01-01

    Membranes that separate oil-water mixtures based on contrasting wetting properties have recently received significant attention. Separation of nanoemulsions, i.e. oil-water mixtures containing sub-micron droplets, still remains a key challenge. Tradeoffs between geometric constraints, high breakthrough pressure for selectivity, high flux, and mechanical durability make it challenging to design effective membranes. In this paper, we fabricate a hierarchical membrane by the phase inversion process that consists of a nanoporous separation skin layer supported by an integrated microporous layer. We demonstrate the separation of water-in-oil emulsions well below 1 μm in size. In addition, we tune the parameters of the hierarchical membrane fabrication to control the skin layer thickness and increase the total flux by a factor of four. These simple yet robust hierarchical membranes with engineered wetting characteristics show promise for large-scale, efficient separation systems. PMID:24980852

  6. Nanoemulsion-based intranasal drug delivery system of saquinavir mesylate for brain targeting.

    PubMed

    Mahajan, Hitendra S; Mahajan, Milind S; Nerkar, Pankaj P; Agrawal, Anshuman

    2014-03-01

    The central nervous system (CNS) is an immunological privileged sanctuary site-providing reservoir for HIV-1 virus. Current anti-HIV drugs, although effective in reducing plasma viral levels, cannot eradicate the virus completely from the body. The low permeability of anti-HIV drugs across the blood-brain barrier (BBB) leads to insufficient delivery. Therefore, developing a novel approaches enhancing the CNS delivery of anti-HIV drugs are required for the treatment of neuro-AIDS. The aim of this study was to develop intranasal nanoemulsion (NE) for enhanced bioavailability and CNS targeting of saquinavir mesylate (SQVM). SQVM is a protease inhibitor which is a poorly soluble drug widely used as antiretroviral drug, with oral bioavailability is about 4%. The spontaneous emulsification method was used to prepare drug-loaded o/w nanoemulsion, which was characterized by droplet size, zeta potential, pH, drug content. Moreover, ex-vivo permeation studies were performed using sheep nasal mucosa. The optimized NE showed a significant increase in drug permeation rate compared to the plain drug suspension (PDS). Cilia toxicity study on sheep nasal mucosa showed no significant adverse effect of SQVM-loaded NE. Results of in vivo biodistribution studies show higher drug concentration in brain after intranasal administration of NE than intravenous delivered PDS. The higher percentage of drug targeting efficiency (% DTE) and nose-to-brain drug direct transport percentage (% DTP) for optimized NE indicated effective CNS targeting of SQVM via intranasal route. Gamma scintigraphy imaging of the rat brain conclusively demonstrated transport of drug in the CNS at larger extent after intranasal administration as NE.

  7. Lipid nanotechnology.

    PubMed

    Mashaghi, Samaneh; Jadidi, Tayebeh; Koenderink, Gijsje; Mashaghi, Alireza

    2013-01-01

    Nanotechnology is a multidisciplinary field that covers a vast and diverse array of devices and machines derived from engineering, physics, materials science, chemistry and biology. These devices have found applications in biomedical sciences, such as targeted drug delivery, bio-imaging, sensing and diagnosis of pathologies at early stages. In these applications, nano-devices typically interface with the plasma membrane of cells. On the other hand, naturally occurring nanostructures in biology have been a source of inspiration for new nanotechnological designs and hybrid nanostructures made of biological and non-biological, organic and inorganic building blocks. Lipids, with their amphiphilicity, diversity of head and tail chemistry, and antifouling properties that block nonspecific binding to lipid-coated surfaces, provide a powerful toolbox for nanotechnology. This review discusses the progress in the emerging field of lipid nanotechnology. PMID:23429269

  8. Lipid Nanotechnology

    PubMed Central

    Mashaghi, Samaneh; Jadidi, Tayebeh; Koenderink, Gijsje; Mashaghi, Alireza

    2013-01-01

    Nanotechnology is a multidisciplinary field that covers a vast and diverse array of devices and machines derived from engineering, physics, materials science, chemistry and biology. These devices have found applications in biomedical sciences, such as targeted drug delivery, bio-imaging, sensing and diagnosis of pathologies at early stages. In these applications, nano-devices typically interface with the plasma membrane of cells. On the other hand, naturally occurring nanostructures in biology have been a source of inspiration for new nanotechnological designs and hybrid nanostructures made of biological and non-biological, organic and inorganic building blocks. Lipids, with their amphiphilicity, diversity of head and tail chemistry, and antifouling properties that block nonspecific binding to lipid-coated surfaces, provide a powerful toolbox for nanotechnology. This review discusses the progress in the emerging field of lipid nanotechnology. PMID:23429269

  9. Protective role of free and quercetin-loaded nanoemulsion against damage induced by intracerebral haemorrhage in rats

    NASA Astrophysics Data System (ADS)

    Galho, A. R.; Cordeiro, M. F.; Ribeiro, S. A.; Marques, M. S.; Antunes, M. F. D.; Luz, D. C.; Hädrich, G.; Muccillo-Baisch, A. L.; Barros, D. M.; Lima, J. V.; Dora, C. L.; Horn, A. P.

    2016-04-01

    Intracerebral haemorrhage (ICH) is a worldwide public health problem. Experimental studies have shown that oxidative stress plays an important role in the pathogenesis of ICH and could represent a target for its treatment. However, the blood-brain barrier is an obstacle to be overcome, as it hampers the administration of compounds to the central nervous system. In this study, we compared the effects of a quercetin-loaded nanoemulsion (QU-N) with the free form of the drug (QU-SP) in a collagenase-induced ICH rat model. Quercetin (QU) is a polyphenol that has an antioxidant effect in vitro, but due to its high lipophilicity, it has low bioavailability in vivo. In this study, animals submitted or not to ICH were treated with a single intraperitoneal QU dose (free or nanoemulsion) of 30 mg kg-1. Motor assessment was evaluated by the open field, foot fault and beam walking behavioural tests. 72 h after surgery the haematoma size was evaluated and biochemical measurements were performed. Animals treated with QU-N had a significant improvement in the beam walking and open field tests. Also, QU-N was able to reduce the size of the haematoma, preserving the activity of glutathione S-transferase (GST), increasing GSH content, and the total antioxidant capacity. QU-SP recovered locomotor activity and increased the GSH content and the total antioxidant capacity. Thus, it can be observed that QU presented antioxidant activity in both formulations, but the incorporation into nanoemulsions increased its antioxidant effect, which was reflected in the improvement of the motor skills and in the haematoma size decrement. These results suggest that the nanoemulsion containing QU developed in this study could be promising for future studies on treatments for ICH.

  10. Intranasal delivery of paroxetine nanoemulsion via the olfactory region for the management of depression: formulation, behavioural and biochemical estimation

    NASA Astrophysics Data System (ADS)

    Pandey, Yogendra Raj; Kumar, Shobhit; Gupta, Bijay Kumar; Ali, Javed; Baboota, Sanjula

    2016-01-01

    Paroxetine is a selective serotonin reuptake inhibitor (SSRI) and is used for the treatment of depression and anxiety problems, but suffers from the drawback of poor oral bioavailability (less than 50%) due to its extensive first pass metabolism. The objective of the present study was to develop a paroxetine loaded nanoemulsion (o/w type) for direct nose-to-brain delivery. Nanoemulsions were prepared by the spontaneous emulsification technique using Capmul MCM, Solutol HS 15 and propylene glycol as oil phase, surfactant and co-surfactant, respectively, for delivery of drug directly to the brain through the nasal route for better management of depression. Formulations were studied for droplet size, polydispersity index (PDI), percentage transmittance, refractive index, viscosity, zeta potential, surface morphology and in vitro permeation study. TEM images of optimized formulation showed spherical droplets with a mean diameter of 58.47 ± 3.02 nm, PDI of 0.339 ± 0.007 and zeta potential values of -33 mV. The formulation showed good results for transmittance (100.60 ± 0.577%), refractive index (1.412 ± 0.003) and viscosity (40.85 ± 6.40 cP). Permeation studies revealed a 2.57-fold enhancement in permeation as compared to the paroxetine suspension. Behavioural studies such as the forced swimming test and locomotor activity test were done on Wistar rats to study the antidepressant effect of the optimized formulation. Treatment of depressed rats with paroxetine nanoemulsion (administered intranasally) significantly improved the behavioural activities in comparison to paroxetine suspension (orally administered). Biochemical estimation results revealed that the prepared nanoemulsion was effective in enhancing the depressed levels of glutathione and decreasing the elevated levels of TBARS.

  11. Comparison of process parameter optimization using different designs in nanoemulsion-based formulation for transdermal delivery of fullerene

    PubMed Central

    Ngan, Cheng Loong; Basri, Mahiran; Lye, Fui Fang; Fard Masoumi, Hamid Reza; Tripathy, Minaketan; Karjiban, Roghayeh Abedi; Abdul-Malek, Emilia

    2014-01-01

    This research aims to formulate and to optimize a nanoemulsion-based formulation containing fullerene, an antioxidant, stabilized by a low amount of mixed surfactants using high shear and the ultrasonic emulsification method for transdermal delivery. Process parameters optimization of fullerene nanoemulsions was done by employing response surface methodology, which involved statistical multivariate analysis. Optimization of independent variables was investigated using experimental design based on Box–Behnken design and central composite rotatable design. An investigation on the effect of the homogenization rate (4,000–5,000 rpm), sonication amplitude (20%–60%), and sonication time (30–150 seconds) on the particle size, ζ-potential, and viscosity of the colloidal systems was conducted. Under the optimum conditions, the central composite rotatable design model suggested the response variables for particle size, ζ-potential, and viscosity of the fullerene nanoemulsion were 152.5 nm, −52.6 mV, and 44.6 pascal seconds, respectively. In contrast, the Box–Behnken design model proposed that preparation under the optimum condition would produce nanoemulsion with particle size, ζ-potential, and viscosity of 148.5 nm, −55.2 mV, and 39.9 pascal seconds, respectively. The suggested process parameters to obtain optimum formulation by both models yielded actual response values similar to the predicted values with residual standard error of <2%. The optimum formulation showed more elastic and solid-like characteristics due to the existence of a large linear viscoelastic region. PMID:25258528

  12. Antimicrobial Nanoemulsion Formulation with Improved Penetration of Foliar Spray through Citrus Leaf Cuticles to Control Citrus Huanglongbing

    PubMed Central

    Yang, Chuanyu; Powell, Charles A.; Duan, Yongping; Shatters, Robert; Zhang, Muqing

    2015-01-01

    Huanglongbing (HLB) is the most serious disease affecting the citrus industry worldwide to date. The causal agent, Candidatus Liberibacter asiaticus (Las), resides in citrus phloem, which makes it difficult to effectively treat with chemical compounds. In this study, a transcuticular nanoemulsion formulation was developed to enhance the permeation of an effective antimicrobial compound (ampicillin; Amp) against HLB disease through the citrus cuticle into the phloem via a foliar spray. The results demonstrated that efficiency of cuticle isolation using an enzymatic method (pectinase and cellulase) was dependent on the citrus cultivar and Las-infection, and it was more difficult to isolate cuticles from valencia orange (Citrus sinensis) and HLB-symptomatic leaves. Of eight adjuvants tested, Brij 35 provided the greatest increase in permeability of the HLB-affected cuticle with a 3.33-fold enhancement of cuticular permeability over water control. An in vitro assay using Bacillus subtilis showed that nanoemulsion formulations containing Amp (droplets size = 5.26 ± 0.04 nm and 94 ± 1.48 nm) coupled with Brij 35 resulted in greater inhibitory zone diameters (5.75 mm and 6.66 mm) compared to those of Brij 35 (4.34 mm) and Amp solution (2.83 mm) alone. Furthermore, the nanoemulsion formulations eliminated Las bacteria in HLB-affected citrus in planta more efficiently than controls. Our study shows that a water in oil (W/O) nanoemulsion formulation may provide a useful model for the effective delivery of chemical compounds into citrus phloem via a foliar spray for controlling citrus HLB. PMID:26207823

  13. Protective role of free and quercetin-loaded nanoemulsion against damage induced by intracerebral haemorrhage in rats.

    PubMed

    Galho, A R; Cordeiro, M F; Ribeiro, S A; Marques, M S; Antunes, M F D; Luz, D C; Hädrich, G; Muccillo-Baisch, A L; Barros, D M; Lima, J V; Dora, C L; Horn, A P

    2016-04-29

    Intracerebral haemorrhage (ICH) is a worldwide public health problem. Experimental studies have shown that oxidative stress plays an important role in the pathogenesis of ICH and could represent a target for its treatment. However, the blood-brain barrier is an obstacle to be overcome, as it hampers the administration of compounds to the central nervous system. In this study, we compared the effects of a quercetin-loaded nanoemulsion (QU-N) with the free form of the drug (QU-SP) in a collagenase-induced ICH rat model. Quercetin (QU) is a polyphenol that has an antioxidant effect in vitro, but due to its high lipophilicity, it has low bioavailability in vivo. In this study, animals submitted or not to ICH were treated with a single intraperitoneal QU dose (free or nanoemulsion) of 30 mg kg(-1). Motor assessment was evaluated by the open field, foot fault and beam walking behavioural tests. 72 h after surgery the haematoma size was evaluated and biochemical measurements were performed. Animals treated with QU-N had a significant improvement in the beam walking and open field tests. Also, QU-N was able to reduce the size of the haematoma, preserving the activity of glutathione S-transferase (GST), increasing GSH content, and the total antioxidant capacity. QU-SP recovered locomotor activity and increased the GSH content and the total antioxidant capacity. Thus, it can be observed that QU presented antioxidant activity in both formulations, but the incorporation into nanoemulsions increased its antioxidant effect, which was reflected in the improvement of the motor skills and in the haematoma size decrement. These results suggest that the nanoemulsion containing QU developed in this study could be promising for future studies on treatments for ICH. PMID:26965041

  14. Antimicrobial Nanoemulsion Formulation with Improved Penetration of Foliar Spray through Citrus Leaf Cuticles to Control Citrus Huanglongbing.

    PubMed

    Yang, Chuanyu; Powell, Charles A; Duan, Yongping; Shatters, Robert; Zhang, Muqing

    2015-01-01

    Huanglongbing (HLB) is the most serious disease affecting the citrus industry worldwide to date. The causal agent, Candidatus Liberibacter asiaticus (Las), resides in citrus phloem, which makes it difficult to effectively treat with chemical compounds. In this study, a transcuticular nanoemulsion formulation was developed to enhance the permeation of an effective antimicrobial compound (ampicillin; Amp) against HLB disease through the citrus cuticle into the phloem via a foliar spray. The results demonstrated that efficiency of cuticle isolation using an enzymatic method (pectinase and cellulase) was dependent on the citrus cultivar and Las-infection, and it was more difficult to isolate cuticles from valencia orange (Citrus sinensis) and HLB-symptomatic leaves. Of eight adjuvants tested, Brij 35 provided the greatest increase in permeability of the HLB-affected cuticle with a 3.33-fold enhancement of cuticular permeability over water control. An in vitro assay using Bacillus subtilis showed that nanoemulsion formulations containing Amp (droplets size = 5.26 ± 0.04 nm and 94 ± 1.48 nm) coupled with Brij 35 resulted in greater inhibitory zone diameters (5.75 mm and 6.66 mm) compared to those of Brij 35 (4.34 mm) and Amp solution (2.83 mm) alone. Furthermore, the nanoemulsion formulations eliminated Las bacteria in HLB-affected citrus in planta more efficiently than controls. Our study shows that a water in oil (W/O) nanoemulsion formulation may provide a useful model for the effective delivery of chemical compounds into citrus phloem via a foliar spray for controlling citrus HLB. PMID:26207823

  15. Antimicrobial Nanoemulsion Formulation with Improved Penetration of Foliar Spray through Citrus Leaf Cuticles to Control Citrus Huanglongbing.

    PubMed

    Yang, Chuanyu; Powell, Charles A; Duan, Yongping; Shatters, Robert; Zhang, Muqing

    2015-01-01

    Huanglongbing (HLB) is the most serious disease affecting the citrus industry worldwide to date. The causal agent, Candidatus Liberibacter asiaticus (Las), resides in citrus phloem, which makes it difficult to effectively treat with chemical compounds. In this study, a transcuticular nanoemulsion formulation was developed to enhance the permeation of an effective antimicrobial compound (ampicillin; Amp) against HLB disease through the citrus cuticle into the phloem via a foliar spray. The results demonstrated that efficiency of cuticle isolation using an enzymatic method (pectinase and cellulase) was dependent on the citrus cultivar and Las-infection, and it was more difficult to isolate cuticles from valencia orange (Citrus sinensis) and HLB-symptomatic leaves. Of eight adjuvants tested, Brij 35 provided the greatest increase in permeability of the HLB-affected cuticle with a 3.33-fold enhancement of cuticular permeability over water control. An in vitro assay using Bacillus subtilis showed that nanoemulsion formulations containing Amp (droplets size = 5.26 ± 0.04 nm and 94 ± 1.48 nm) coupled with Brij 35 resulted in greater inhibitory zone diameters (5.75 mm and 6.66 mm) compared to those of Brij 35 (4.34 mm) and Amp solution (2.83 mm) alone. Furthermore, the nanoemulsion formulations eliminated Las bacteria in HLB-affected citrus in planta more efficiently than controls. Our study shows that a water in oil (W/O) nanoemulsion formulation may provide a useful model for the effective delivery of chemical compounds into citrus phloem via a foliar spray for controlling citrus HLB.

  16. Implicit trustworthiness ratings of self-resembling faces activate brain centers involved in reward.

    PubMed

    Platek, Steven M; Krill, Austen L; Wilson, Benjamin

    2009-01-01

    On the basis of Hamilton's (Hamilton, W. D. (1964). The genetical evolution of social behavior I, II. Journal of Theoretical Biology, 7, 17-52) theory of inclusive fitness, self-facial resemblance is hypothesized as a mechanism for self-referent phenotypic matching by which humans can detect kin. To understand the mechanisms underlying pro-sociality toward self-resembling faces, we investigated the neural correlates of implicit trustworthiness ratings for self-resembling faces. Here we show that idiosyncratic trustworthiness ratings of self-resembling faces predict brain activation in the ventral inferior, middle and medial frontal gyri, substrates involved in reward processing. These findings demonstrate that neural reward centers are implicated in evaluating implicit pro-social behaviors toward self-resembling faces. These findings suggest that humans have evolved to use neurocomputational architecture dedicated to face processing and reward evaluation for the differentiation of kin, which drives implicit idiosyncratic affectively regulated social interactions.

  17. Study of stability and thermodynamic properties of water-in-diesel nanoemulsion fuels with nano-Al additive

    NASA Astrophysics Data System (ADS)

    Mehta, Rakhi N.; More, Utkarsh; Malek, Naved; Chakraborty, Mousumi; Parikh, Parimal A.

    2015-11-01

    The present work addresses the formation of water-in-diesel (W/D) nanoemulsion by blending different percentages of water along with nano-Al additive in various propositions to enhance the combustion characteristics. The roles of various surfactants such as Sorbitan monooleate (Span 80), Triton X-100, Tetradecyltrimethylammonium bromide, and newly synthesized and characterized dicationic surfactants were discussed based upon their ability to stabilize the nanoemulsions. Surface active properties of the surfactants were determined by measuring their interfacial tension and subsequently by measuring the critical micelle concentration of the surfactants. Triton X-100 was found to be the most efficient surfactant for the current water-in-diesel nanoemulsion as it stabilized the suspensions for more than 8 h. Particle size analysis proved emulsion size to be in the order of nanometer, and zeta potential values were found to have neutral behavior at water-diesel interface. Experimental studies confirmed that that blends W/D [1 % (vol.) water] and W/DA [1 % (vol.) water, 0.1 % (wt.) nano-Al] were thermodynamically stable.

  18. Involvement of the inhibition of intestinal glucuronidation in enhancing the oral bioavailability of resveratrol by labrasol containing nanoemulsions.

    PubMed

    Zhou, Jing; Zhou, Man; Yang, Fei-Fei; Liu, Chun-Yu; Pan, Rui-Le; Chang, Qi; Liu, Xin-Min; Liao, Yong-Hong

    2015-04-01

    Nanoemulsions have been developed for the oral delivery of poorly bioavailable phenolic compounds that are sensitive to intestinal glucuronidation. However, little is known about the contribution of UDP-glucuronosyltransferase (UGT) inhibitory excipients in nanoemulsions toward the inhibition of intestinal glucuronidation and the consequent enhanced bioavailability. In this study, Labrasol but not poloxamer 188 (F68) was found to inhibit the glucuronidation of resveratrol (RES), a model phenolic compound, in an inhibition assay with rat microsomes. Subsequently, two nanoemulsions, Lab-N and F68-N, were prepared with similar particle size distribution, zeta potentials, and entrapment efficiency by coemulsifying with Labrasol or F68, respectively. Although Lab-N exhibited inferior or comparable profiles of in vitro release, cellular uptake in Caco-2 cells, and lymphatic transport in rats to F68-N, the in vitro absorption study with everted sacs suggested that Labrasol containing formulations significantly and dose-dependently increased the transport of RES relative to free RES or F68-N by decreasing the amount of permeated metabolite, RES-3-glucuronide (RES-G). The in vivo pharmacokinetic experiments indicated that Lab-N exhibited increments in the maximum plasma concentration and the bioavailability of RES by 1098% and 560%, respectively, and significant decreases in those of RES-G, compared to F68-N. The overall results demonstrated that the improved oral bioavailability of RES by Lab-N was mainly attributable to the inhibition of intestinal glucuronidation by the presence of UGT inhibitory excipient. PMID:25723098

  19. Lipid Storage Diseases

    MedlinePlus

    ... Awards Enhancing Diversity Find People About NINDS NINDS Lipid Storage Diseases Information Page Condensed from Lipid Storage ... en Español Additional resources from MedlinePlus What are Lipid Storage Diseases? Lipid storage diseases are a group ...

  20. Phase Transitions of Isotropic to Anisotropic Biocompatible Lipid-Based Drug Delivery Systems Overcoming Insoluble Benznidazole Loading.

    PubMed

    Streck, Letícia; Sarmento, Víctor H V; Machado, Paula R L; Farias, Kleber J S; Fernandes-Pedrosa, Matheus F; da Silva-Júnior, Arnóbio Antônio

    2016-01-01

    Previous studies reported low benznidazole (BNZ) loading in conventional emulsions due to the weak interaction of the drug with the most common oils used to produce foods or pharmaceuticals. In this study, we focused on how the type of surfactant, surfactant-to-oil ratio w/w (SOR) and oil-to-water ratio w/w (OWR) change the phase behavior of different lipid-based drug delivery systems (LBDDS) produced by emulsion phase inversion. The surfactant mixture composed of soy phosphatidylcholine and sodium oleate (1:7, w/w, hydrophilic lipophilic balance = 16) stabilized medium chain triglyceride in water. Ten formulations with the clear aspect or less turbid dispersions (five with the SOR ranging from 0.5 to 2.5 and five with the OWR from 0.06 to 0.4) were selected from the phase behavior diagram to assess structural features and drug-loading capacity. The rise in the SOR induced the formation of distinct lipid-based drug delivery systems (nanoemulsions and liquid crystal lamellar type) that were identified using rheological measurements and cross-polarized light microscopy images. Clear dispersions of small and narrow droplet-sized liquid-like nanoemulsions, Newtonian flow-type, were produced at SOR from 0.5 to 1.5 and OWR from 0.12 to 0.4, while clear liquid or gel-like liquid crystals were produced at SOR from 1.5 to 2.5. The BNZ loading was improved according to the composition and type of LBDDS produced, suggesting possible drug location among surfactant layers. The cell viability assays proved the biocompatibility for all of the prepared nanoemulsions at SOR less than 1.5 and liquid crystals at SOR less than 2.5, demonstrating their promising features for the oral or parenteral colloidal delivery systems containing benznidazole for Chagas disease treatment. PMID:27376278

  1. Phase Transitions of Isotropic to Anisotropic Biocompatible Lipid-Based Drug Delivery Systems Overcoming Insoluble Benznidazole Loading

    PubMed Central

    Streck, Letícia; Sarmento, Víctor H. V.; Machado, Paula R. L.; Farias, Kleber J. S.; Fernandes-Pedrosa, Matheus F.; da Silva-Júnior, Arnóbio Antônio

    2016-01-01

    Previous studies reported low benznidazole (BNZ) loading in conventional emulsions due to the weak interaction of the drug with the most common oils used to produce foods or pharmaceuticals. In this study, we focused on how the type of surfactant, surfactant-to-oil ratio w/w (SOR) and oil-to-water ratio w/w (OWR) change the phase behavior of different lipid-based drug delivery systems (LBDDS) produced by emulsion phase inversion. The surfactant mixture composed of soy phosphatidylcholine and sodium oleate (1:7, w/w, hydrophilic lipophilic balance = 16) stabilized medium chain triglyceride in water. Ten formulations with the clear aspect or less turbid dispersions (five with the SOR ranging from 0.5 to 2.5 and five with the OWR from 0.06 to 0.4) were selected from the phase behavior diagram to assess structural features and drug-loading capacity. The rise in the SOR induced the formation of distinct lipid-based drug delivery systems (nanoemulsions and liquid crystal lamellar type) that were identified using rheological measurements and cross-polarized light microscopy images. Clear dispersions of small and narrow droplet-sized liquid-like nanoemulsions, Newtonian flow-type, were produced at SOR from 0.5 to 1.5 and OWR from 0.12 to 0.4, while clear liquid or gel-like liquid crystals were produced at SOR from 1.5 to 2.5. The BNZ loading was improved according to the composition and type of LBDDS produced, suggesting possible drug location among surfactant layers. The cell viability assays proved the biocompatibility for all of the prepared nanoemulsions at SOR less than 1.5 and liquid crystals at SOR less than 2.5, demonstrating their promising features for the oral or parenteral colloidal delivery systems containing benznidazole for Chagas disease treatment. PMID:27376278

  2. Phase Transitions of Isotropic to Anisotropic Biocompatible Lipid-Based Drug Delivery Systems Overcoming Insoluble Benznidazole Loading.

    PubMed

    Streck, Letícia; Sarmento, Víctor H V; Machado, Paula R L; Farias, Kleber J S; Fernandes-Pedrosa, Matheus F; da Silva-Júnior, Arnóbio Antônio

    2016-01-01

    Previous studies reported low benznidazole (BNZ) loading in conventional emulsions due to the weak interaction of the drug with the most common oils used to produce foods or pharmaceuticals. In this study, we focused on how the type of surfactant, surfactant-to-oil ratio w/w (SOR) and oil-to-water ratio w/w (OWR) change the phase behavior of different lipid-based drug delivery systems (LBDDS) produced by emulsion phase inversion. The surfactant mixture composed of soy phosphatidylcholine and sodium oleate (1:7, w/w, hydrophilic lipophilic balance = 16) stabilized medium chain triglyceride in water. Ten formulations with the clear aspect or less turbid dispersions (five with the SOR ranging from 0.5 to 2.5 and five with the OWR from 0.06 to 0.4) were selected from the phase behavior diagram to assess structural features and drug-loading capacity. The rise in the SOR induced the formation of distinct lipid-based drug delivery systems (nanoemulsions and liquid crystal lamellar type) that were identified using rheological measurements and cross-polarized light microscopy images. Clear dispersions of small and narrow droplet-sized liquid-like nanoemulsions, Newtonian flow-type, were produced at SOR from 0.5 to 1.5 and OWR from 0.12 to 0.4, while clear liquid or gel-like liquid crystals were produced at SOR from 1.5 to 2.5. The BNZ loading was improved according to the composition and type of LBDDS produced, suggesting possible drug location among surfactant layers. The cell viability assays proved the biocompatibility for all of the prepared nanoemulsions at SOR less than 1.5 and liquid crystals at SOR less than 2.5, demonstrating their promising features for the oral or parenteral colloidal delivery systems containing benznidazole for Chagas disease treatment.

  3. p-Tertbutylcalix[4]arene nanoemulsion: preparation, characterization and comparative evaluation of its decontamination efficacy against Technetium-99m, Iodine-131 and Thallium-201.

    PubMed

    Rana, Sudha; Sharma, Navneet; Ojha, Himanshu; Shivkumar, Hosakote Gurumalappa; Sultana, Sarwat; Sharma, Rakesh Kumar

    2014-05-01

    This study aimed to develop p-tertbutylcalix[4]arene o/w nanoemulsion for decontamination of radioisotopes from skin. Formulation was characterized using dynamic light scattering (DLS), transmission electron microscopy (TEM), multi-photon confocal microscopy techniques and in vitro dissolution studies. In vivo evaluation of nano-emulsion was done using nuclear medicine technique. Stability studies and dermal toxicity studies were also carried out. Comparative decontamination efficacy (DE) studies were performed on synthetic human tissue equivalent material and Sprague Dawley rat against three commonly used medical radioisotopes, i.e., Technetium-99m ((99m)Tc), Iodine-131 ((131)I) and Thallium-201 ((201)Tl). Decontamination was performed using cotton swabs soaked in nanoemulsion at different time intervals of contaminants exposure. Whole body imaging and static counts were recorded using gamma camera before and after each decontamination attempt data was analyzed using one way analysis of variance (ANOVA) and found to be statistically significant (p<0.05). DE of the nanoemulsion loaded with p-tertbutylcalix[4]arene was observed to be 88±5%, 90±3% and 89±3% for (99m)Tc, (131)I and (201)Tl respectively. Dermal toxicity studies revealed no significant differences between treated and control animals. Skin histopathology slides with and without API (Active pharmaceutical ingredients) also found to be comparable. p-Tertbutylcalix[4]arene loaded nanoemulsion shows great promise for skin decontamination against broad ranges of radiological contaminants besides being stable and safe.

  4. Highly enhanced optical properties of indocyanine green/perfluorocarbon nanoemulsions for efficient lymph node mapping using near-infrared and magnetic resonance imaging

    NASA Astrophysics Data System (ADS)

    Bae, Pan Kee; Jung, Juyeon; Chung, Bong Hyun

    2014-03-01

    The near-infrared (NIR) fluorescence probe has better tissue penetration and lower autofluorescence. Indocyanine green (ICG) is an NIR organic dye for extensive biological application, and it has been clinically approved for human medical imaging and diagnosis. However, application of this dye is limited by its numerous disadvantageous properties in aqueous solution, including its concentration-dependent aggregation, poor aqueous stability in vitro, and low quantum yield. Its use in molecular imaging probes is limited because it loses fluorescence after binding to nonspecific plasma proteins, leading to rapid elimination from the body with a half-life of 2 - 4 min. In this study, the multifunctional perfluorocarbon (PFC)/ICG nanoemulsions were investigated with the aim of overcoming these limitations. The PFC/ICG nanoemulsions as a new type of delivery vehicle for contrast agents have both NIR optical imaging and 19 F-MR imaging moieties. These nanoemulsions exhibited less aggregation, increased fluorescence intensity, long-term stability, and physicochemical stability against external light and temperature compared to free aqueous ICG. Also, the PFC/ICG bimodal nanoemulsions allow excellent detection of lymph nodes in vivo through NIR optical imaging and 19 F-MR imaging. This result showed the suitability of the proposed nanoemulsions for non-invasive lymph node mapping as they enable long-time detection of lymph nodes.

  5. Optimization of ultrasound induced emulsification on the formulation of palm-olein based nanoemulsions for the incorporation of antioxidant β-D-glucan polysaccharides.

    PubMed

    Alzorqi, Ibrahim; Ketabchi, Mohammad Reza; Sudheer, Surya; Manickam, Sivakumar

    2016-07-01

    Polysaccharides of β-D-glucan configuration have well-known antioxidant activity against reactive free radicals generated from the oxidation of metabolic processes. In this study, β-D-glucan-polysaccharides extracted from Ganoderma lucidum were incorporated in palm olein based nanoemulsions which act as carrier systems to enhance the delivery and bioactivity of these polysaccharides and could be potentially useful for skin care applications. Initially response surface statistical design (Central Composite Design--CCD) was subjected to optimize the formulation variables of oil-in-water (O/W) nanoemulsions induced by ultrasound. The optimal formulation variables as predicted by CCD resulted in considerably improving the physical characteristics of ultrasonically formulated nanoemulsions by minimizing their droplet size, polydispersity index and viscosity. Moreover, the β-D-glucan-loaded nanoemulsions exhibited good stability over 90 days under different storage conditions (4 °C and 25 °C). The studies using palm olein based β-D-glucan-loaded nanoemulsion generated using ultrasound confirm higher antioxidant activity as compared to free β-D-glucan. PMID:26964925

  6. The Male Advantage in Child Facial Resemblance Detection: Behavioral and ERP evidence

    PubMed Central

    Wu, Haiyan; Yang, Suyong; Sun, Shiyue; Liu, Chao; Luo, Yue-jia

    2013-01-01

    Males have been suggested to have advantages over females in reactions to child facial resemblance, which reflects the evolutionary pressure on males to solve the adaptive paternal uncertainty problem and to identify biological offspring. However, previous studies showed inconsistent results and the male advantage in child facial resemblance perception, as a kin detection mechanism, is still unclear. Here we investigated the behavioral and brain mechanisms underlying the self-resembling faces processing and how it interacts with sex and age using ERP technique. The results showed a stable male advantage in self-resembling child faces processing, such that males have higher detectability to self-resembling child faces than females. For ERP results, males showed smaller N2 and larger LPC amplitudes for self-resembling child faces, which may reflect face-matching and self-referential processing in kin detection, respectively. Further source analysis showed that the N2 and LPC components were originated from the anterior cingulate cortex and medial frontal gyrus, respectively. Our results support the male advantage in self-resembling child detection and further indicate that such distinctions can be found in both early and late processing stages in the brain at different regions. PMID:24053135

  7. The Texas Adoption Project: adopted children and their intellectual resemblance to biological and adoptive parents.

    PubMed

    Horn, J M

    1983-04-01

    Intelligence test scores were obtained from parents and children in 300 adoptive families and compared with similar measures available for the biological mothers of the same adopted children. Results supported the hypothesis that genetic variability is an important influence in the development of individual differences for intelligence. The most salient finding was that adopted children resemble their biological mothers more than they resemble the adoptive parents who reared them from birth. A small subset of the oldest adopted children did not resemble their biological mothers. The suggestion that the influence of genes declines with age is treated with caution since other adoption studies report a trend in the opposite direction.

  8. An additional case of breast tumor resembling the tall cell variant of papillary thyroid carcinoma.

    PubMed

    Colella, Renato; Guerriero, Angela; Giansanti, Michele; Sidoni, Angelo; Bellezza, Guido

    2015-05-01

    A type of breast tumor histopathologically similar to the papillary thyroid carcinoma has been described and named "Breast tumor resembling the tall cell variant of papillary thyroid carcinoma." Because breast is not an uncommon site for metastasis and about 5% of all such cases are of the thyroid origin, it is important to be aware of the existence of mammary tumors that can closely mimic a thyroid tumor representing a dangerous diagnostic pitfall that can also lead to unnecessary clinical investigations. Here, we describe a singular case of "Breast tumor resembling the tall cell variant of papillary thyroid carcinoma" showing an amazing macroscopic and microscopic resemblance with thyroid tissue harboring a papillary carcinoma.

  9. Lutein and zeaxanthin: Role as macular pigment and factors that control bioavailability from egg yolks and nanoemulsions

    NASA Astrophysics Data System (ADS)

    Vishwanathan, Rohini

    ) raising serum HDL-C without an adverse affect on serum LDL-C and TC:HDL-C ratio. Increased cholesterol, lutein and zeaxanthin intake from the 2 and 4 egg yolk interventions did not decrease the absorption of other carotenoids, such as alpha-cryptoxanthin, beta-cryptoxanthin, lycopene, alpha-carotene and beta-carotene, tocopherols and retinol from the diet. An unexpected increase was observed in serum alpha-cryptoxanthin and gamma-tocopherol concentrations during the 4 egg yolk phase, these carotenoids are normally present in low concentrations in serum. Lipoprotein distribution of carotenoids and tocopherols was also not affected by the increased egg consumption. In the pursuit of designing a highly bioavailable matrix for lutein/zeaxanthin, similar to the egg yolk micellar matrix, nanoemulsion formulations of lutein were developed using the MicrofluidizerRTM Processor technology. Lutein nanoemulsions are O/W emulsions of lutein which have particle sizes in the nanometer range (≤ 200 nm). Lutein consumed orally as a nanoemulsion was shown to have significantly greater bioavailability than lutein supplement-pills in pilot-scale clinical studies described here. However, lutein nanoemulsions did not raise plasma lutein concentrations to the same extent as egg yolks in a study performed on BALB/c mice. Formation of mixed micelles in the intestinal lumen during digestion and uptake of these micelles by enterocytes are crucial steps that dictate bioavailability i.e. the proportion of ingested lutein/carotenoid that enters the blood circulation and accumulates in the peripheral tissues such as the macula. In-vitro stomach and intestinal digestion experiments showed lutein nanoemulsions have significantly greater micellarization efficiency compared to egg yolks. Nanoemulsions with a phospholipid (PL) emulsifier containing 80% phosphatidyl choline (PC) or Polysorbate 80 as the emulsifier had better ability to form micelles during the intestinal digestion phase compared to a PL

  10. Proteolytic transformation of SC5b-9 into an amphiphilic macromolecule resembling the C5b-9 membrane attack complex of complement.

    PubMed Central

    Bhakdi, S; Bhakdi-Lehnen, B; Tranum-Jensen, J

    1979-01-01

    Proteolysis of fluid-phase SC5b-9 left a major part of the macromolecule intact and caused transition of the molecule from a hydrophilic to an amphiphilic state. The transformed complex exhibited neoantigens characteristic of the C5b-9 membrane attack complex of the complement. It yielded an SDS gel electrophoresis pattern that was similar, but not identical to that of the proteolysed, membrane attack complex. The proteolytically altered SC5b-9 complex bound lipid and incorporated into artificial lipid vesicles to yield a membrane-bound structure resembling the C5b-9 complement lesion. Images Figure 7 Figure 1 Figure 2 Figure 3 Figure 4 Figure 5 Figure 6 PMID:115783

  11. Lipid-Based Nanoparticles as Pharmaceutical Drug Carriers: From Concepts to Clinic

    PubMed Central

    Puri, Anu; Loomis, Kristin; Smith, Brandon; Lee, Jae-Ho; Yavlovich, Amichai; Heldman, Eli; Blumenthal, Robert

    2010-01-01

    In recent years, various nanotechnology platforms in the area of medical biology, including both diagnostics and therapy, have gained remarkable attention. Moreover, research and development of engineered multifunctional nanoparticles as pharmaceutical drug carriers have spurred exponential growth in applications to medicine in the last decade. Design principles of these nanoparticles, including nano-emulsions, dendrimers, nano-gold, liposomes, drug-carrier conjugates, antibody-drug complexes, and magnetic nanoparticles, are primarily based on unique assemblies of synthetic, natural, or biological components, including but not limited to synthetic polymers, metal ions, oils, and lipids as their building blocks. However, the potential success of these particles in the clinic relies on consideration of important parameters such as nanoparticle fabrication strategies, their physical properties, drug loading efficiencies, drug release potential, and, most importantly, minimum toxicity of the carrier itself. Among these, lipid-based nanoparticles bear the advantage of being the least toxic for in vivo applications, and significant progress has been made in the area of DNA/RNA and drug delivery using lipid-based nanoassemblies. In this review, we will primarily focus on the recent advances and updates on lipid-based nanoparticles for their projected applications in drug delivery. We begin with a review of current activities in the field of liposomes (the so-called honorary nanoparticles), and challenging issues of targeting and triggering will be discussed in detail. We will further describe nanoparticles derived from a novel class of amphipathic lipids called bolaamphiphiles with unique lipid assembly features that have been recently examined as drug/DNA delivery vehicles. Finally, an overview of an emerging novel class of particles (based on lipid components other than phospholipids), solid lipid nanoparticles and nanostructured lipid carriers will be presented. We

  12. Lipid-based nanoparticles as pharmaceutical drug carriers: from concepts to clinic.

    PubMed

    Puri, Anu; Loomis, Kristin; Smith, Brandon; Lee, Jae-Ho; Yavlovich, Amichai; Heldman, Eliahu; Blumenthal, Robert

    2009-01-01

    In recent years, various nanotechnology platforms in the area of medical biology, including both diagnostics and therapy, have gained remarkable attention. Moreover, research and development of engineered multifunctional nanoparticles as pharmaceutical drug carriers have spurred exponential growth in applications to medicine in the last decade. Design principles of these nanoparticles, including nanoemulsions, dendrimers, nano-gold, liposomes, drug-carrier conjugates, antibody-drug complexes, and magnetic nanoparticles, are primarily based on unique assemblies of synthetic, natural, or biological components, including but not limited to synthetic polymers, metal ions, oils, and lipids as their building blocks. However, the potential success of these particles in the clinic relies on consideration of important parameters such as nanoparticle fabrication strategies, their physical properties, drug loading efficiencies, drug release potential, and, most importantly, minimum toxicity of the carrier itself. Among these, lipid-based nanoparticles bear the advantage of being the least toxic for in vivo applications, and significant progress has been made in the area of DNA/RNA and drug delivery using lipid-based nanoassemblies. In this review, we will primarily focus on the recent advances and updates on lipid-based nanoparticles for their projected applications in drug delivery. We begin with a review of current activities in the field of liposomes (the so-called honorary nanoparticles), and challenging issues of targeting and triggering will be discussed in detail. We will further describe nanoparticles derived from a novel class of amphipathic lipids called bolaamphiphiles with unique lipid assembly features that have been recently examined as drug/DNA delivery vehicles. Finally, an overview of an emerging novel class of particles (based on lipid components other than phospholipids), solid lipid nanoparticles and nanostructured lipid carriers will be presented. We

  13. Effects of parenting quality on adolescents' personality resemblance to their parents. The TRAILS study.

    PubMed

    Langenhof, M Rohaa; Komdeur, Jan; Oldehinkel, Albertine J

    2016-08-01

    This study considers the development of resemblance between 741 adolescents and their biological parents, across six NEO-PI-R personality traits known to be important in psychological problems: anger-hostility, impulsiveness, vulnerability, assertiveness, excitement-seeking, and self-discipline. We modelled the association between perceived parental warmth and rejection at age eleven and personality resemblance to parents at about age sixteen. Parenting experienced during early adolescence was related to the degree and direction in which adolescents resembled their parents five years later in life. Rejection, especially from fathers, significantly predicted a smaller resemblance to both the parents. Girls were more strongly affected by parental quality than boys, and there was some indication that adolescents responded in opposite ways to parenting from mothers and fathers. This study is a first step in uncovering the complex interplay between parenting, gender, and the current generation's ability to develop personality traits independent from the previous generation.

  14. Effects of parenting quality on adolescents' personality resemblance to their parents. The TRAILS study.

    PubMed

    Langenhof, M Rohaa; Komdeur, Jan; Oldehinkel, Albertine J

    2016-08-01

    This study considers the development of resemblance between 741 adolescents and their biological parents, across six NEO-PI-R personality traits known to be important in psychological problems: anger-hostility, impulsiveness, vulnerability, assertiveness, excitement-seeking, and self-discipline. We modelled the association between perceived parental warmth and rejection at age eleven and personality resemblance to parents at about age sixteen. Parenting experienced during early adolescence was related to the degree and direction in which adolescents resembled their parents five years later in life. Rejection, especially from fathers, significantly predicted a smaller resemblance to both the parents. Girls were more strongly affected by parental quality than boys, and there was some indication that adolescents responded in opposite ways to parenting from mothers and fathers. This study is a first step in uncovering the complex interplay between parenting, gender, and the current generation's ability to develop personality traits independent from the previous generation. PMID:27400032

  15. Enhancement of photoprotection potential of catechin loaded nanoemulsion gel against UVA induced oxidative stress.

    PubMed

    Harwansh, Ranjit K; Mukherjee, Pulok K; Kar, Amit; Bahadur, Shiv; Al-Dhabi, Naif Abdullah; Duraipandiyan, V

    2016-07-01

    The present study was aimed to develop a catechin (CA) loaded nanoemulsion based nano-gel for the protection of skin against ultraviolet radiation (UV) induced photo-damage and to ensure its enhanced skin permeability as well as bioavailability through transdermal route. The optimized nanoemulsion (CA-NE4) was prepared by spontaneous nano-emulsification method. It was composed of oil (ethyl oleate), Smix [surfactant (span 80) and co-surfactant (transcutol CG)] and aqueous system in an appropriate ratio of 15:62:23% w/w respectively. The CA-NE4 was characterized through assessment of droplet size, zeta potential, refractive index, transmission electron microscopy (TEM), UV, high performance thin layer chromatography (HPTLC) and Fourier transform infrared spectroscopy (FTIR) analysis. The average droplet size and zeta potential of CA-NE4 were found to be 98.6±1.01nm and -27.3±0.20mV respectively. The enhanced skin permeability was better with CA-NE4 based nano-gel (CA-NG4) [96.62%] compared to conventional gel (CA-CG) [53.01%] for a period of 24h. The enhanced % relative bioavailability (F) of CA (894.73), Cmax (93.79±6.19ngmL(-1)), AUC0-t∞ (2653.99±515.02nghmL(-1)) and Tmax (12.05±0.02h) was significantly obtained with CA-NG4 as compared to oral suspension for extended periods (72h). CA-NG4 could improve the level of cutaneous antioxidant enzymes like superoxide dismutase (SOD), glutathione peroxidase (GPX) and catalase (CAT) and reduce the level of thiobarbituric acid reactive substances (TBRAS) against oxidative stress induced by UVA. Nano-gel formulation of CA showed sustained release profile and enhanced photoprotection potential due to its improved permeability as well as bioavailability (P<0.05) compared to the conventional gel. Therefore, transdermal administration of nano-gel (CA-NG4) of CA offers a better way to develop the endogenous cutaneous protection system and thus could be an effective strategy for decreasing UV-induced oxidative damage in the

  16. Lipid Clustering Correlates with Membrane Curvature as Revealed by Molecular Simulations of Complex Lipid Bilayers

    PubMed Central

    Koldsø, Heidi; Shorthouse, David; Hélie, Jean; Sansom, Mark S. P.

    2014-01-01

    Cell membranes are complex multicomponent systems, which are highly heterogeneous in the lipid distribution and composition. To date, most molecular simulations have focussed on relatively simple lipid compositions, helping to inform our understanding of in vitro experimental studies. Here we describe on simulations of complex asymmetric plasma membrane model, which contains seven different lipids species including the glycolipid GM3 in the outer leaflet and the anionic lipid, phosphatidylinositol 4,5-bisphophate (PIP2), in the inner leaflet. Plasma membrane models consisting of 1500 lipids and resembling the in vivo composition were constructed and simulations were run for 5 µs. In these simulations the most striking feature was the formation of nano-clusters of GM3 within the outer leaflet. In simulations of protein interactions within a plasma membrane model, GM3, PIP2, and cholesterol all formed favorable interactions with the model α-helical protein. A larger scale simulation of a model plasma membrane containing 6000 lipid molecules revealed correlations between curvature of the bilayer surface and clustering of lipid molecules. In particular, the concave (when viewed from the extracellular side) regions of the bilayer surface were locally enriched in GM3. In summary, these simulations explore the nanoscale dynamics of model bilayers which mimic the in vivo lipid composition of mammalian plasma membranes, revealing emergent nanoscale membrane organization which may be coupled both to fluctuations in local membrane geometry and to interactions with proteins. PMID:25340788

  17. Lipid14: The Amber Lipid Force Field.

    PubMed

    Dickson, Callum J; Madej, Benjamin D; Skjevik, Age A; Betz, Robin M; Teigen, Knut; Gould, Ian R; Walker, Ross C

    2014-02-11

    The AMBER lipid force field has been updated to create Lipid14, allowing tensionless simulation of a number of lipid types with the AMBER MD package. The modular nature of this force field allows numerous combinations of head and tail groups to create different lipid types, enabling the easy insertion of new lipid species. The Lennard-Jones and torsion parameters of both the head and tail groups have been revised and updated partial charges calculated. The force field has been validated by simulating bilayers of six different lipid types for a total of 0.5 μs each without applying a surface tension; with favorable comparison to experiment for properties such as area per lipid, volume per lipid, bilayer thickness, NMR order parameters, scattering data, and lipid lateral diffusion. As the derivation of this force field is consistent with the AMBER development philosophy, Lipid14 is compatible with the AMBER protein, nucleic acid, carbohydrate, and small molecule force fields.

  18. Who resembles whom? Mimetic and coincidental look-alikes among tropical reef fishes.

    PubMed

    Robertson, D Ross

    2013-01-01

    Studies of mimicry among tropical reef-fishes usually give little or no consideration to alternative explanations for behavioral associations between unrelated, look-alike species that benefit the supposed mimic. I propose and assess such an alternative explanation. With mimicry the mimic resembles its model, evolved to do so in response to selection by the mimicry target, and gains evolved benefits from that resemblance. In the alternative, the social-trap hypothesis, a coincidental resemblance of the model to the "mimic" inadvertently attracts the latter to it, and reinforcement of this social trapping by learned benefits leads to the "mimic" regularly associating with the model. I examine three well known cases of supposed aggressive mimicry among reef-fishes in relation to nine predictions from these hypotheses, and assess which hypothesis offers a better explanation for each. One case, involving precise and complex morphological and behavioral resemblance, is strongly consistent with mimicry, one is inconclusive, and one is more consistent with a social-trap based on coincidental, imprecise resemblance. Few cases of supposed interspecific mimicry among tropical reef fishes have been examined in depth, and many such associations may involve social traps arising from generalized, coincidental resemblance. Mimicry may be much less common among these fishes than is generally thought.

  19. Who Resembles Whom? Mimetic and Coincidental Look-Alikes among Tropical Reef Fishes

    PubMed Central

    Robertson, D. Ross

    2013-01-01

    Studies of mimicry among tropical reef-fishes usually give little or no consideration to alternative explanations for behavioral associations between unrelated, look-alike species that benefit the supposed mimic. I propose and assess such an alternative explanation. With mimicry the mimic resembles its model, evolved to do so in response to selection by the mimicry target, and gains evolved benefits from that resemblance. In the alternative, the social-trap hypothesis, a coincidental resemblance of the model to the “mimic” inadvertently attracts the latter to it, and reinforcement of this social trapping by learned benefits leads to the “mimic” regularly associating with the model. I examine three well known cases of supposed aggressive mimicry among reef-fishes in relation to nine predictions from these hypotheses, and assess which hypothesis offers a better explanation for each. One case, involving precise and complex morphological and behavioral resemblance, is strongly consistent with mimicry, one is inconclusive, and one is more consistent with a social-trap based on coincidental, imprecise resemblance. Few cases of supposed interspecific mimicry among tropical reef fishes have been examined in depth, and many such associations may involve social traps arising from generalized, coincidental resemblance. Mimicry may be much less common among these fishes than is generally thought. PMID:23372795

  20. Design Expert® supported optimization and predictive analysis of selegiline nanoemulsion via the olfactory region with enhanced behavioural performance in Parkinson’s disease

    NASA Astrophysics Data System (ADS)

    Kumar, Shobhit; Ali, Javed; Baboota, Sanjula

    2016-10-01

    Selegiline is a monoamine oxidase B (MAO-B) inhibitor and is used in the treatment of Parkinson’s disease. The main problem associated with its oral administration is its low oral bioavailability (10%) due to its poor aqueous solubility and extensive first pass metabolism. The aim of the present research work was to develop a nanoemulsion loaded with selegiline for direct nose-to-brain delivery for the better management of Parkinson’s disease. A quality by design (QbD) approach was used in a statistical multivariate method for the preparation and optimization of nanoemulsion. In this study, four independent variables were chosen, in which two were compositions and two were process variables, while droplet size, transmittance, zeta potential and drug release were selected as response variables. The optimized formulation was assessed for efficacy in Parkinson’s disease using behavioural studies, namely forced swimming, locomotor, catalepsy, muscle coordination, akinesia and bradykinesia or pole test in Wistar rats. The observed droplet size, polydispersity index (PDI), refractive index, transmittance, zeta potential and viscosity of selegiline nanoemulsion were found to be 61.43 ± 4.10 nm, 0.203 ± 0.005, 1.30 ± 0.01, 99.80 ± 0.04%, -34 mV and 31.85 ± 0.24 mPas respectively. Surface characterization studies demonstrated a spherical shape of nanoemulsion which showed 3.7 times enhancement in drug permeation as compared to drug suspension. The results of behaviour studies showed that treatment of haloperidol induced Parkinson’s disease in rats with selegiline nanoemulsion (administered intranasally) showed significant improvement in behavioural activities in comparison to orally administered drug. These findings demonstrate that nanoemulsion could be a promising new drug delivery carrier for intranasal delivery of selegiline in the treatment of Parkinson’s disease.

  1. Design Expert(®) supported optimization and predictive analysis of selegiline nanoemulsion via the olfactory region with enhanced behavioural performance in Parkinson's disease.

    PubMed

    Kumar, Shobhit; Ali, Javed; Baboota, Sanjula

    2016-10-28

    Selegiline is a monoamine oxidase B (MAO-B) inhibitor and is used in the treatment of Parkinson's disease. The main problem associated with its oral administration is its low oral bioavailability (10%) due to its poor aqueous solubility and extensive first pass metabolism. The aim of the present research work was to develop a nanoemulsion loaded with selegiline for direct nose-to-brain delivery for the better management of Parkinson's disease. A quality by design (QbD) approach was used in a statistical multivariate method for the preparation and optimization of nanoemulsion. In this study, four independent variables were chosen, in which two were compositions and two were process variables, while droplet size, transmittance, zeta potential and drug release were selected as response variables. The optimized formulation was assessed for efficacy in Parkinson's disease using behavioural studies, namely forced swimming, locomotor, catalepsy, muscle coordination, akinesia and bradykinesia or pole test in Wistar rats. The observed droplet size, polydispersity index (PDI), refractive index, transmittance, zeta potential and viscosity of selegiline nanoemulsion were found to be 61.43 ± 4.10 nm, 0.203 ± 0.005, 1.30 ± 0.01, 99.80 ± 0.04%, -34 mV and 31.85 ± 0.24 mPas respectively. Surface characterization studies demonstrated a spherical shape of nanoemulsion which showed 3.7 times enhancement in drug permeation as compared to drug suspension. The results of behaviour studies showed that treatment of haloperidol induced Parkinson's disease in rats with selegiline nanoemulsion (administered intranasally) showed significant improvement in behavioural activities in comparison to orally administered drug. These findings demonstrate that nanoemulsion could be a promising new drug delivery carrier for intranasal delivery of selegiline in the treatment of Parkinson's disease.

  2. Design Expert(®) supported optimization and predictive analysis of selegiline nanoemulsion via the olfactory region with enhanced behavioural performance in Parkinson's disease.

    PubMed

    Kumar, Shobhit; Ali, Javed; Baboota, Sanjula

    2016-10-28

    Selegiline is a monoamine oxidase B (MAO-B) inhibitor and is used in the treatment of Parkinson's disease. The main problem associated with its oral administration is its low oral bioavailability (10%) due to its poor aqueous solubility and extensive first pass metabolism. The aim of the present research work was to develop a nanoemulsion loaded with selegiline for direct nose-to-brain delivery for the better management of Parkinson's disease. A quality by design (QbD) approach was used in a statistical multivariate method for the preparation and optimization of nanoemulsion. In this study, four independent variables were chosen, in which two were compositions and two were process variables, while droplet size, transmittance, zeta potential and drug release were selected as response variables. The optimized formulation was assessed for efficacy in Parkinson's disease using behavioural studies, namely forced swimming, locomotor, catalepsy, muscle coordination, akinesia and bradykinesia or pole test in Wistar rats. The observed droplet size, polydispersity index (PDI), refractive index, transmittance, zeta potential and viscosity of selegiline nanoemulsion were found to be 61.43 ± 4.10 nm, 0.203 ± 0.005, 1.30 ± 0.01, 99.80 ± 0.04%, -34 mV and 31.85 ± 0.24 mPas respectively. Surface characterization studies demonstrated a spherical shape of nanoemulsion which showed 3.7 times enhancement in drug permeation as compared to drug suspension. The results of behaviour studies showed that treatment of haloperidol induced Parkinson's disease in rats with selegiline nanoemulsion (administered intranasally) showed significant improvement in behavioural activities in comparison to orally administered drug. These findings demonstrate that nanoemulsion could be a promising new drug delivery carrier for intranasal delivery of selegiline in the treatment of Parkinson's disease. PMID:27655136

  3. Effectiveness of a novel spontaneous carvacrol nanoemulsion against Salmonella enterica Enteritidis and Escherichia coli O157:H7 on contaminated mung bean and alfalfa seeds.

    PubMed

    Landry, Kyle S; Chang, Yuhua; McClements, David Julian; McLandsborough, Lynne

    2014-09-18

    Outbreaks of foodborne illness from consumption of sprouts have been linked to contaminated seeds prior to germination. Due to the long sprouting period at ambient temperatures and high humidity, germinating seeds contaminated with low pathogen levels (0.1logCFU/g) can result in sprouts with high numbers (≥10(8)CFU/g) of pathogens. Currently, the recommended treatment method involves soaking seeds in 20,000ppm (2%) calcium hypochlorite prior to germination. In this study, an alternative treatment involving soaking seeds in a carvacrol nanoemulsion was tested for its efficacy against Salmonella enterica subspecies enterica serovar Enteritidis (ATCC BAA-1045) or EGFP expressing E. coli O157:H7 (ATCC 42895) contaminated mung bean and alfalfa seeds. The antimicrobial treatment was performed by soaking inoculated seed batches in the spontaneous nanoemulsion (4000 or 8000ppm) for 30 or 60min. The spontaneous nanoemulsion was formed by titrating the oil phase (carvacrol and medium chain triglycerides) and water-soluble surfactant (Tween 80®) into sodium citrate buffer. Following treatment, the numbers of surviving cells were determined by suspending the seeds in TSB and performing plate counts and/or Most Probable Number (MPN) enumeration. Treated seeds were sprouted and tested for the presence of the appropriate pathogen. This treatment successfully inactivated low levels (2 and 3logCFU/g) of S. Enteritidis and E. coli on either seed types when soaked for either 30 or 60min at nanoemulsion concentrations corresponding to 4000 (0.4%) or 8000 (0.8%) ppm carvacrol. Inoculated alfalfa seeds treated with 4000ppm nanoemulsion, required a 60min treatment time to show a similar 2-3 log reduction. Complete inactivation was confirmed by germinating treated seeds and performing microbiological testing. Total sprout yield was not compromised by any of the tested treatments. These results show that carvacrol nanoemulsions may be an alternative antimicrobial treatment method for

  4. Surface-active solid lipid nanoparticles as Pickering stabilizers for oil-in-water emulsions.

    PubMed

    Gupta, Renuka; Rousseau, Dérick

    2012-03-01

    Oil-in-water (O/W) emulsions solely stabilized by surface-active solid lipid nanoparticles (SLNs) were developed. The SLNs were generated by quench-cooling hot O/W nanoemulsions consisting of 7.5% glyceryl stearyl citrate (GSC) dispersed in water. Their initial volume-weighted mean particle diameter (∼152 nm) and zeta potential (ca.-49 mV) remained unchanged for 24 weeks. O/W emulsions (oil phase volume fraction: 0.2) containing 7.5% (w/w) GSC SLNs in the aqueous phase were kinetically-stable for 12 weeks and did not visually phase-separate over 24 weeks. The O/W emulsions generated with solid-state GSC SLNs had a volume-weighted mean oil droplet diameter of ∼459 nm and a zeta potential of ca.-43 mV. Emulsion microstructure evaluated with TEM revealed dispersed oil droplets sparsely covered with adsorbed Pickering-type SLNs as well aggregated SLNs present in the continuous phase. Gradual emulsion destabilization resulted from GSC SLN dissolution during the experimental timeframe. Overall, surface-active SLNs developed via nanoemulsions effectively kinetically stabilized O/W emulsions.

  5. Preparation and Characterization of a Lecithin Nanoemulsion as a Topical Delivery System

    NASA Astrophysics Data System (ADS)

    Zhou, Huafeng; Yue, Yang; Liu, Guanlan; Li, Yan; Zhang, Jing; Gong, Qiu; Yan, Zemin; Duan, Mingxing

    2010-01-01

    Purpose of this study was to establish a lecithin nanoemulsion (LNE) without any synthetic surfactant as a topical delivery vehicle and to evaluate its topical delivery potential by the following factors: particle size, morphology, viscosity, stability, skin hydration and skin penetration. Experimental results demonstrated that an increasing concentration of soybean lecithin and glycerol resulted in a smaller size LNE droplet and increasing viscosity, respectively. The droplet size of optimized LNE, with the glycerol concentration above 75% (w/w), changed from 92 (F10) to 58 nm (F14). Additionally, LNE, incorporated into o/w cream, improved the skin hydration capacity of the cream significantly with about 2.5-fold increase when the concentration of LNE reached 10%. LNE was also demonstrated to improve the penetrability of Nile red (NR) dye into the dermis layer, when an o/w cream, incorporated with NR-loaded LNE, applied on the abdominal skin of rat in vivo. Specifically, the arbitrary unit (ABU) of fluorescence in the dermis layer that had received the cream with a NR-loaded LNE was about 9.9-fold higher than the cream with a NR-loaded general emulsion (GE). These observations suggest that LNE could be used as a promising topical delivery vehicle for lipophilic compounds.

  6. Antibacterial activity of neem nanoemulsion and its toxicity assessment on human lymphocytes in vitro.

    PubMed

    Jerobin, Jayakumar; Makwana, Pooja; Suresh Kumar, R S; Sundaramoorthy, Rajiv; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2015-01-01

    Neem (Azadirachta indica) is recognized as a medicinal plant well known for its antibacterial, antimalarial, antiviral, and antifungal properties. Neem nanoemulsion (NE) (O/W) is formulated using neem oil, Tween 20, and water by high-energy ultrasonication. The formulated neem NE showed antibacterial activity against the bacterial pathogen Vibrio vulnificus by disrupting the integrity of the bacterial cell membrane. Despite the use of neem NE in various biomedical applications, the toxicity studies on human cells are still lacking. The neem NE showed a decrease in cellular viability in human lymphocytes after 24 hours of exposure. The neem NE at lower concentration (0.7-1 mg/mL) is found to be nontoxic while it is toxic at higher concentrations (1.2-2 mg/mL). The oxidative stress induced by the neem NE is evidenced by the depletion of catalase, SOD, and GSH levels in human lymphocytes. Neem NE showed a significant increase in DNA damage when compared to control in human lymphocytes (P<0.05). The NE is an effective antibacterial agent against the bacterial pathogen V. vulnificus, and it was found to be nontoxic at lower concentrations to human lymphocytes.

  7. Antibacterial activity of neem nanoemulsion and its toxicity assessment on human lymphocytes in vitro

    PubMed Central

    Jerobin, Jayakumar; Makwana, Pooja; Suresh Kumar, RS; Sundaramoorthy, Rajiv; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2015-01-01

    Neem (Azadirachta indica) is recognized as a medicinal plant well known for its antibacterial, antimalarial, antiviral, and antifungal properties. Neem nanoemulsion (NE) (O/W) is formulated using neem oil, Tween 20, and water by high-energy ultrasonication. The formulated neem NE showed antibacterial activity against the bacterial pathogen Vibrio vulnificus by disrupting the integrity of the bacterial cell membrane. Despite the use of neem NE in various biomedical applications, the toxicity studies on human cells are still lacking. The neem NE showed a decrease in cellular viability in human lymphocytes after 24 hours of exposure. The neem NE at lower concentration (0.7–1 mg/mL) is found to be nontoxic while it is toxic at higher concentrations (1.2–2 mg/mL). The oxidative stress induced by the neem NE is evidenced by the depletion of catalase, SOD, and GSH levels in human lymphocytes. Neem NE showed a significant increase in DNA damage when compared to control in human lymphocytes (P<0.05). The NE is an effective antibacterial agent against the bacterial pathogen V. vulnificus, and it was found to be nontoxic at lower concentrations to human lymphocytes. PMID:26491309

  8. Antibacterial activity of neem nanoemulsion and its toxicity assessment on human lymphocytes in vitro.

    PubMed

    Jerobin, Jayakumar; Makwana, Pooja; Suresh Kumar, R S; Sundaramoorthy, Rajiv; Mukherjee, Amitava; Chandrasekaran, Natarajan

    2015-01-01

    Neem (Azadirachta indica) is recognized as a medicinal plant well known for its antibacterial, antimalarial, antiviral, and antifungal properties. Neem nanoemulsion (NE) (O/W) is formulated using neem oil, Tween 20, and water by high-energy ultrasonication. The formulated neem NE showed antibacterial activity against the bacterial pathogen Vibrio vulnificus by disrupting the integrity of the bacterial cell membrane. Despite the use of neem NE in various biomedical applications, the toxicity studies on human cells are still lacking. The neem NE showed a decrease in cellular viability in human lymphocytes after 24 hours of exposure. The neem NE at lower concentration (0.7-1 mg/mL) is found to be nontoxic while it is toxic at higher concentrations (1.2-2 mg/mL). The oxidative stress induced by the neem NE is evidenced by the depletion of catalase, SOD, and GSH levels in human lymphocytes. Neem NE showed a significant increase in DNA damage when compared to control in human lymphocytes (P<0.05). The NE is an effective antibacterial agent against the bacterial pathogen V. vulnificus, and it was found to be nontoxic at lower concentrations to human lymphocytes. PMID:26491309

  9. Tea tree oil nanoemulsions for inhalation therapies of bacterial and fungal pneumonia.

    PubMed

    Li, Miao; Zhu, Lifei; Liu, Boming; Du, Lina; Jia, Xiaodong; Han, Li; Jin, Yiguang

    2016-05-01

    Tea tree oil (TTO) is a natural essential oil with strong antimicrobial efficacy and little drug resistance. However, the biomedical applications of TTO are limited due to its hydrophobicity and formulation problems. Here, we prepared an inhalable TTO nanoemulsion (nanoTTO) for local therapies of bacterial and fungal pneumonia. The optimal formulation of nanoTTOs consisted of TTO/Cremophor EL/water with a mean size of 12.5nm. The nanoTTOs showed strong in vitro antimicrobial activities on Escherichia coli, Acinetobacter baumannii, Klebsiella pneumoniae, Staphylococcus aureus and Candida albicans. After inhalation to the lung, the nanoTTOs had higher anti-fungal effect than fluconazole on the fungal pneumonia rat models with reduced lung injury, highly microbial clearance, blocking of leukocyte recruitment, and decrease of pro-inflammatory mediators. In the case of rat bacterial pneumonia, the nanoTTOs showed slightly lower therapeutic efficacy than penicillin though at a much lower dose. Taken together, our results show that the inhalable nanoTTOs are promising nanomedicines for local therapies of fungal and bacterial pneumonia with no obvious adverse events. PMID:26895502

  10. Physical and antimicrobial properties of anise oil loaded nanoemulsions on the survival of foodborne pathogens.

    PubMed

    Topuz, Osman Kadir; Özvural, Emin Burçin; Zhao, Qin; Huang, Qingrong; Chikindas, Michael; Gölükçü, Muharrem

    2016-07-15

    The purpose of this research was to investigate antimicrobial effects of nano emulsions of anise oil (AO) on the survival of common food borne pathogens, Listeria monocytogenes and Escherichia coli O157:H7. Series of emulsions containing different level of anise oil as potential antimicrobial delivery systems were prepared. Antimicrobial activities of bulk anise oil and its emulsions (coarse and nano) was tested by the minimum inhibitory concentration and time kill assay. Our results showed that bulk anise oil reduced the population of E. coli O157:H7 and L. monocytogenes by 1.48 and 0.47 log cfu/ml respectively after 6 h of contact time. However, under the same condition anise oil nanoemulsion (AO75) reduced E. coli O157:H7 and L. monocytogenes count by 2.51 and 1.64 log cfu/ml, respectively. Physicochemical and microbial analyses indicated that both nano and coarse emulsions of anise oil showed better and long-term physicochemical stability and antimicrobial activity compared to bulk anise oil. PMID:26948596

  11. Conventional versus stealth lipid nanoparticles: formulation and in vivo fate prediction through FRET monitoring.

    PubMed

    Lainé, A-L; Gravier, J; Henry, M; Sancey, L; Béjaud, J; Pancani, E; Wiber, M; Texier, I; Coll, J-L; Benoit, J-P; Passirani, C

    2014-08-28

    The determination of the nanocarrier fate in preclinical models is required before any translation from laboratory to clinical trials. Modern fluorescent imaging techniques have gained considerable advances becoming a powerful technology for non-invasive visualization in living subjects. Among them, Forster (fluorescence) resonance energy transfer (FRET) is a particular fluorescence imaging which involves energy transfer between 2 fluorophores in a distance-dependent manner. Considering this feature, the encapsulation of an acceptor/donor pair in lipid nanoparticles (LNEs: lipid nanoemulsions, LNCs: lipid nanocapsules) allowed the carrier integrity to be tracked. Accordingly, we used this FRET technique to evaluate the behavior of LNEs, conventional LNCs and newly designed stealth LNCs. After the development through a one-step (OS) PEGylation process of these stealth LNCs (OS LNCs), in vitro guest exchange dynamics and release kinetics were evaluated for both LNC formulations. We thereafter assessed in vivo biodistribution of all types of lipid nanoparticles. Results showed enhanced stability of encapsulation in OS LNCs in comparison to conventional LNCs. Additionally, the presence of the long PEG chains on the lipid nanoparticle surface altered the biodistribution pattern. Despite different release kinetic profiles, OS LNCs and LNEs showed extended blood circulation time associated with a good structure stability over several hours after intravenous injection.

  12. Conventional versus stealth lipid nanoparticles: formulation and in vivo fate prediction through FRET monitoring.

    PubMed

    Lainé, A-L; Gravier, J; Henry, M; Sancey, L; Béjaud, J; Pancani, E; Wiber, M; Texier, I; Coll, J-L; Benoit, J-P; Passirani, C

    2014-08-28

    The determination of the nanocarrier fate in preclinical models is required before any translation from laboratory to clinical trials. Modern fluorescent imaging techniques have gained considerable advances becoming a powerful technology for non-invasive visualization in living subjects. Among them, Forster (fluorescence) resonance energy transfer (FRET) is a particular fluorescence imaging which involves energy transfer between 2 fluorophores in a distance-dependent manner. Considering this feature, the encapsulation of an acceptor/donor pair in lipid nanoparticles (LNEs: lipid nanoemulsions, LNCs: lipid nanocapsules) allowed the carrier integrity to be tracked. Accordingly, we used this FRET technique to evaluate the behavior of LNEs, conventional LNCs and newly designed stealth LNCs. After the development through a one-step (OS) PEGylation process of these stealth LNCs (OS LNCs), in vitro guest exchange dynamics and release kinetics were evaluated for both LNC formulations. We thereafter assessed in vivo biodistribution of all types of lipid nanoparticles. Results showed enhanced stability of encapsulation in OS LNCs in comparison to conventional LNCs. Additionally, the presence of the long PEG chains on the lipid nanoparticle surface altered the biodistribution pattern. Despite different release kinetic profiles, OS LNCs and LNEs showed extended blood circulation time associated with a good structure stability over several hours after intravenous injection. PMID:24878182

  13. Nanostructured lipid carriers system: recent advances in drug delivery.

    PubMed

    Iqbal, Md Asif; Md, Shadab; Sahni, Jasjeet Kaur; Baboota, Sanjula; Dang, Shweta; Ali, Javed

    2012-12-01

    Nanostructured lipid carrier (NLC) is second generation smarter drug carrier system having solid matrix at room temperature. This carrier system is made up of physiological, biodegradable and biocompatible lipid materials and surfactants and is accepted by regulatory authorities for application in different drug delivery systems. The availability of many products in the market in short span of time reveals the success story of this delivery system. Since the introduction of the first product, around 30 NLC preparations are commercially available. NLC exhibit superior advantages over other colloidal carriers viz., nanoemulsions, polymeric nanoparticles, liposomes, SLN etc. and thus, have been explored to more extent in pharmaceutical technology. The whole set of unique advantages such as enhanced drug loading capacity, prevention of drug expulsion, leads to more flexibility for modulation of drug release and makes NLC versatile delivery system for various routes of administration. The present review gives insights on the definitions and characterization of NLC as colloidal carriers including the production techniques and suitable formulations. This review paper also highlights the importance of NLC in pharmaceutical applications for the various routes of drug delivery viz., topical, oral, pulmonary, ocular and parenteral administration and its future perspective as a pharmaceutical carrier. PMID:22931500

  14. Enhancement of the antimicrobial properties of bacteriophage-K via stabilization using oil-in-water nano-emulsions.

    PubMed

    Esteban, Patricia Perez; Alves, Diana R; Enright, Mark C; Bean, Jessica E; Gaudion, Alison; Jenkins, A T A; Young, Amber E R; Arnot, Tom C

    2014-01-01

    Bacteriophage therapy is a promising new treatment that may help overcome the threat posed by antibiotic-resistant pathogenic bacteria, which are increasingly identified in hospitalized patients. The development of biocompatible and sustainable vehicles for incorporation of viable bacterial viruses into a wound dressing is a promising alternative. This article evaluates the antimicrobial efficacy of Bacteriophage K against Staphylococcus aureus over time, when stabilized and delivered via an oil-in-water nano-emulsion. Nano-emulsions were formulated via thermal phase inversion emulsification, and then bacterial growth was challenged with either native emulsion, or emulsion combined with Bacteriophage K. Bacteriophage infectivity, and the influence of storage time of the preparation, were assessed by turbidity measurements of bacterial samples. Newly prepared Bacteriophage K/nano-emulsion formulations have greater antimicrobial activity than freely suspended bacteriophage. The phage-loaded emulsions caused rapid and complete bacterial death of three different strains of S. aureus. The same effect was observed for preparations that were either stored at room temperature (18-20°C), or chilled at 4°C, for up to 10 days of storage. A response surface design of experiments was used to gain insight on the relative effects of the emulsion formulation on bacterial growth and phage lytic activity. More diluted emulsions had a less significant effect on bacterial growth, and diluted bacteriophage-emulsion preparations yielded greater antibacterial activity. The enhancement of bacteriophage activity when delivered via nano-emulsions is yet to be reported. This prompts further investigation into the use of these formulations for the development of novel anti-microbial wound management strategies.

  15. Stable poly(St-co-BA) nanoemulsion polymerization for high performance antibacterial coatings in the presence of dioctyldimethylammonium chloride.

    PubMed

    Chen, Zhao; Sun, Xiaowen; Shen, Yan; Ni, Hong; Chai, Shigan; Zou, Qichao; Zhang, Xiuhua; Zhang, Jinzhi

    2015-04-01

    In this study, a stable antibacterial poly(styrene-co-butyl acrylate) (poly(St-co-BA)) nano-latex was prepared in the presence of a dioctyldimethylammonium chloride (D821)-CTAB mixed surfactant and a novel bis-unsaturated Gemini comonomer (i.e., α,ω-hexanediyl bis(dimethyl methacrylamidopropyl ammonium bromide) (GMAP-6-MAP)) using a feasible and mild semicontinuous technology. The effects of the emulsifiers and GMAP-6-MAP on the properties and antibacterial activities of poly(St-co-BA) coatings were systematically investigated. The results indicate that an optimal monodispersed stable nanoemulsion was obtained with Dw=58.24nm and PDI=0.026, the emulsifier amount was 3.75% (D821/CTAB=4:1), and the GMAP-6-MAP amount was 1.5%. CTAB improved the stabilities and antibacterial activities of the poly(St-co-BA) nanoemulsions. The incorporation of GMAP-6-MAP into poly(St-co-BA) can enhance the antibacterial activity, improve the thermal stability of latex films, as well as the consistency among the chain segments, and decrease the roughness of latex films. This nanoemulsion exhibits effective antibacterial activity with MBCs of 2μg·mL(-1) against Staphylococcus aureus and 16μg·mL(-1) against Escherichia coli. The sterilization rates of the optimized latex film reached 100% against S. aureus and 98.74% against E. coli, which indicated that this latex film could be utilized as an outstanding antibacterial coating. PMID:25686944

  16. Development and evaluation of tocopherol-rich argan oil-based nanoemulsions as vehicles possessing anticancer activity.

    PubMed

    Jordan, Melanie; Nayel, Amy; Brownlow, Bill; Elbayoumi, Tamer

    2012-12-01

    In recent years, diverse nanoemulsion vehicles (NEs) have been developed with vast potential for improving therapeutic index of clinically approved and experimental drugs. Using oils rich in omega-3 and omega-6 polyunsaturated fatty acids (PUFA), several promising nanoemulsion formulations have been developed recently for oral and systemic administration. The aim of our present work is to successfully develop and characterize optimized nanoemulsion platform, using the PUFA-rich argan oil that contain several important anti-inflammatory and antimitotic natural components. Using various emulsifying mixtures of polyethoxylated solutol HS-15 and polyethyleneglucol Vitamin E succinyl ester (TPGS), to form different NEs showing extended shelf-life stability. The physicochemical properties of prototype argan NEs were analyzed and utilizing a 32 full factorial design, followed by biocompatibility screen, using normal vascular myocytes and areolar fibroblasts. While 90-180 day stability of NEs correlated with TPGS:solutol surfactant blend ratios, adverse effects on integrity of test cultures were only noted at high TPGS content in the emulsifier system, exceeding 80%. Finally, the anti-proliferative efficacy of selected stable and acceptably biocompatible nanoscale TPGS-emulsified argan oil formulations was investigated using murine breast and colon carcinoma cells. The IC50 values of the combination of argan oil and TPGS (40-80% wt of emulsifiers) were 5-9 folds lower compared to TPGS-free and argan-oil free control NEs. Argan oil NE, stabilized with Vitamin E TPGS and solutol HS mixtures, demonstrated significant pro-apoptotic effect on both test cancer cell lines, indicating built-in anticancer properties for such NE platform, potentially enhancing overall antineoplastic effects of incorporated candidate chemotherapeutic agents.

  17. Development and characterization of a novel nanoemulsion drug-delivery system for potential application in oral delivery of protein drugs

    PubMed Central

    Sun, Hongwu; Liu, Kaiyun; Liu, Wei; Wang, Wenxiu; Guo, Chunliang; Tang, Bin; Gu, Jiang; Zhang, Jinyong; Li, Haibo; Mao, Xuhu; Zou, Quanming; Zeng, Hao

    2012-01-01

    Background: The stability of protein drugs remains one of the key hurdles to their success in the market. The aim of the present study was to design a novel nanoemulsion drug-delivery system (NEDDS) that would encapsulate a standard-model protein drug – bovine serum albumin (BSA) – to improve drug stability. Methods: The BSA NEDDS was prepared using a phase-inversion method and pseudoternary phase diagrams. The following characteristics were studied: morphology, size, zeta potential, drug loading, and encapsulation efficiency. We also investigated the stability of the BSA NEDDS, bioactivity of BSA encapsulated within the NEDDS, the integrity of the primary, secondary, and tertiary structures, and specificity. Results: The BSA NEDDS consisted of Cremophor EL-35, propylene glycol, isopropyl myristate, and normal saline. The average particle diameter of the BSA NEDDS was about 21.8 nm, and the system showed a high encapsulation efficiency (>90%) and an adequate drug-loading capacity (45 mg/mL). The thermodynamic stability of the system was investigated at different temperatures and pH levels and in room-temperature conditions for 180 days. BSA NEDDS showed good structural integrity and specificity for the primary, secondary, and tertiary structures, and good bioactivity of the loaded BSA. Conclusions: BSA NEDDS showed the properties of a good nanoemulsion-delivery system. NEDDS can greatly enhance the stability of the protein drug BSA while maintaining high levels of drug bioactivity, good specificity, and integrity of the primary, secondary, and tertiary protein structures. These findings indicate that the nanoemulsion is a potential formulation for oral administration of protein drugs. PMID:23118537

  18. Effect of Partnership Status on Preferences for Facial Self-Resemblance

    PubMed Central

    Lindová, Jitka; Little, Anthony C.; Havlíček, Jan; Roberts, S. Craig; Rubešová, Anna; Flegr, Jaroslav

    2016-01-01

    Self-resemblance has been found to have a context-dependent effect when expressing preferences for faces. Whereas dissimilarity preference during mate choice in animals is often explained as an evolutionary adaptation to increase heterozygosity of offspring, self-resemblance can be also favored in humans, reflecting, e.g., preference for kinship cues. We performed two studies, using transformations of facial photographs to manipulate levels of resemblance with the rater, to examine the influence of self-resemblance in single vs. coupled individuals. Raters assessed facial attractiveness of other-sex and same-sex photographs according to both short-term and long-term relationship contexts. We found a preference for dissimilarity of other-sex and same-sex faces in single individuals, but no effect of self-resemblance in coupled raters. No effect of sex of participant or short-term vs. long-term attractiveness rating was observed. The results support the evolutionary interpretation that dissimilarity of other-sex faces is preferred by uncoupled individuals as an adaptive mechanism to avoid inbreeding. In contrast, lower dissimilarity preference of other-sex faces in coupled individuals may reflect suppressed attention to attractiveness cues in potential alternative partners as a relationship maintenance mechanism, and its substitution by attention to cues of kinship and psychological similarity connected with greater likelihood of prosocial behavior acquisition from such persons. PMID:27378970

  19. Older Adults' Trait Impressions of Faces Are Sensitive to Subtle Resemblance to Emotions

    PubMed Central

    Zebrowitz, Leslie A.

    2013-01-01

    Younger adults (YA) attribute emotion-related traits to people whose neutral facial structure resembles an emotion (emotion overgeneralization). The fact that older adults (OA) show deficits in accurately labeling basic emotions suggests that they may be relatively insensitive to variations in the emotion resemblance of neutral expression faces that underlie emotion overgeneralization effects. On the other hand, the fact that OA, like YA, show a ‘pop-out’ effect for anger, more quickly locating an angry than a happy face in a neutral array, suggests that both age groups may be equally sensitive to emotion resemblance. We used computer modeling to assess the degree to which neutral faces objectively resembled emotions and assessed whether that resemblance predicted trait impressions. We found that both OA and YA showed anger and surprise overgeneralization in ratings of danger and naiveté, respectively, with no significant differences in the strength of the effects for the two age groups. These findings suggest that well-documented OA deficits on emotion recognition tasks may be more due to processing demands than to an insensitivity to the social affordances of emotion expressions. PMID:24058225

  20. Behavioural and neurochemical features of olfactory bulbectomized rats resembling depression with comorbid anxiety.

    PubMed

    Wang, Dayong; Noda, Yukihiro; Tsunekawa, Hiroko; Zhou, Yuan; Miyazaki, Masayuki; Senzaki, Koji; Nabeshima, Toshitaka

    2007-03-28

    In order to probe the nature and validity of olfactory bulbectomized (OB) rats as a model of depression, we reevaluated their behavioural and neurochemical deficits in relation to the symptoms and neurochemical abnormalities of depression using our protocols, which distinguish anhedonia-resembling behaviour in sexual behavioural test, the hippocampus (Hip)-dependent long-term memory and anxiety-resembling behaviour specially. Besides exploratory hyperactivity in response to a novel environmental stress resembling the psychomotor agitation, OB rats showed a decrease of libido, and a deficit of long-term explicit memory, resembling loss of interest and cognitive deficits in depressive patients, respectively. OB rats also exhibited the anxiety symptom-resembling behaviour in social interaction and plus-maze tests. In the OB rats, we found degenerated neurons in the piriform cortex, decreased protein expression of NMDA receptor subunit 1 (NR1), but not NR2A or NR2B, in the prefrontal cortex (PFC), Hip and amygdala (Amg), and decreased phosphorylation of cAMP-response element-binding protein (CREB) in the PFC and Hip, but not Amg. The behavioural and neurochemical abnormalities in OB rats, except for the performance in the plus-maze task and neuronal degeneration, were significantly attenuated by repeated treatment with desipramine (10 mg/kg), a typical antidepressant. The present study indicated that OB rats may be a model of depression with comorbid anxiety, characterized by agitation, sexual and cognitive dysfunction, neuronal degeneration, decreased protein expression of NR1, and decreased phosphorylation of CREB.

  1. Effect of Partnership Status on Preferences for Facial Self-Resemblance.

    PubMed

    Lindová, Jitka; Little, Anthony C; Havlíček, Jan; Roberts, S Craig; Rubešová, Anna; Flegr, Jaroslav

    2016-01-01

    Self-resemblance has been found to have a context-dependent effect when expressing preferences for faces. Whereas dissimilarity preference during mate choice in animals is often explained as an evolutionary adaptation to increase heterozygosity of offspring, self-resemblance can be also favored in humans, reflecting, e.g., preference for kinship cues. We performed two studies, using transformations of facial photographs to manipulate levels of resemblance with the rater, to examine the influence of self-resemblance in single vs. coupled individuals. Raters assessed facial attractiveness of other-sex and same-sex photographs according to both short-term and long-term relationship contexts. We found a preference for dissimilarity of other-sex and same-sex faces in single individuals, but no effect of self-resemblance in coupled raters. No effect of sex of participant or short-term vs. long-term attractiveness rating was observed. The results support the evolutionary interpretation that dissimilarity of other-sex faces is preferred by uncoupled individuals as an adaptive mechanism to avoid inbreeding. In contrast, lower dissimilarity preference of other-sex faces in coupled individuals may reflect suppressed attention to attractiveness cues in potential alternative partners as a relationship maintenance mechanism, and its substitution by attention to cues of kinship and psychological similarity connected with greater likelihood of prosocial behavior acquisition from such persons. PMID:27378970

  2. Galantamine-loaded PLGA nanoparticles, from nano-emulsion templating, as novel advanced drug delivery systems to treat neurodegenerative diseases

    NASA Astrophysics Data System (ADS)

    Fornaguera, C.; Feiner-Gracia, N.; Calderó, G.; García-Celma, M. J.; Solans, C.

    2015-07-01

    Polymeric nanoparticles could be promising drug delivery systems to treat neurodegenerative diseases. Among the various methods of nanoparticle preparation, nano-emulsion templating was used in the present study to prepare galantamine-loaded nano-emulsions by a low-energy emulsification method followed by solvent evaporation to obtain galantamine-loaded polymeric nanoparticles. This approach was found to be suitable because biocompatible, biodegradable and safe nanoparticles with appropriate features (hydrodynamic radii around 20 nm, negative surface charge and stability higher than 3 months) for their intravenous administration were obtained. Encapsulation efficiencies higher than 90 wt% were obtained with a sustained drug release profile as compared to that from aqueous and micellar solutions. The enzymatic activity of the drug was maintained at 80% after its encapsulation into nanoparticles that were non-cytotoxic at the required therapeutic concentration. Therefore, novel galantamine-loaded polymeric nanoparticles have been designed for the first time using the nano-emulsification approach and showed the appropriate features to become advanced drug delivery systems to treat neurodegenerative diseases.Polymeric nanoparticles could be promising drug delivery systems to treat neurodegenerative diseases. Among the various methods of nanoparticle preparation, nano-emulsion templating was used in the present study to prepare galantamine-loaded nano-emulsions by a low-energy emulsification method followed by solvent evaporation to obtain galantamine-loaded polymeric nanoparticles. This approach was found to be suitable because biocompatible, biodegradable and safe nanoparticles with appropriate features (hydrodynamic radii around 20 nm, negative surface charge and stability higher than 3 months) for their intravenous administration were obtained. Encapsulation efficiencies higher than 90 wt% were obtained with a sustained drug release profile as compared to that from

  3. Family resemblance for glucose tolerance in a Melanesian population, the Tolai.

    PubMed

    King, H; Rao, D C; Bhatia, K; Koki, G; Collins, A; Zimmet, P

    1989-01-01

    Path analysis of family resemblance for plasma glucose concentration, 2 h after an oral glucose challenge, failed to detect significant genetic heritability. There were no intergenerational differences and marital resemblance was moderate. Over one-third of sibling environmental similarity was due to non-inherited factors. Cultural inheritance was very strong, tending to mimic genetic inheritance, and cultural heritability was considerable. Measures of obesity were included in the environmental index, an estimate of familial environment, in this analysis, for comparability with previous studies. Since obesity appears, in part, to be a heritable trait, in future studies a bivariate approach to family resemblance for both glucose tolerance and obesity could yield important additional insight.

  4. From similitude to success: The effects of facial resemblance on perceptions of team effectiveness.

    PubMed

    Wang, Ze; He, Xin; Liu, Fan

    2016-03-01

    Scant empirical research has focused on how impressions of teams are formed based on members' collective appearance, even though team photos are omnipresent in visual communications and teamwork is a common theme to elicit positive responses. Across 4 studies, we show that a subtle increase in the facial resemblance among team members enhances observers' evaluations of team effectiveness. This resemblance effect is mediated by perceived cooperative intent among team players. Furthermore, we demonstrate a reversal of the resemblance effect through the moderating role of information valence and extend the finding from team perception to behavioral intention. These results hold across different manipulations, contexts, stimuli, and sample characteristics. Collectively, this research presents the first empirical evidence that inferences based on facial morphology persist well beyond evaluations of individuals to influence the way a team, as a whole, is perceived.

  5. Study of O/W micro- and nano-emulsions based on propylene glycol diester as a vehicle for geranic acid.

    PubMed

    Jaworska, Małgorzata; Sikora, Elżbieta; Ogonowski, Jan; Konieczna, Monika

    2015-01-01

    Nano- and microemulsions containing as the oil phase caprylic/capric propylene glycol diesters (Crodamol PC) were investigated as potential vehicle for controlled release of geranic acid. The influence of emulsifiers and co-surfactants on stability of the emulsions was investigated. Different kind of polysorbates (ethoxylated esters of sorbitan and fatty acids) were applied as the emulsifiers. The short-chain alcohols (ethanol, 1-propanol, 1-butanol) were used as co-surfactants. The emulsions were prepared at ambient temperature (25°C), by the phase inversion composition method (PIC). The stable O/W high dispersed emulsion systems based on Crodamol PC, of mean droplets size less than 200 nm, were prepared. Microemulsions stabilized by the mixture of Polisorbat 80 and 1-butanol were characterized by the largest degree of dispersion (137 nm) and the lowest PDI value (0.094), at surfactant/co-surfactant: oil weight ratio 90:10. The stable nano-emulsion (mean droplet size of 33 nm) was obtained for surfactant: oil (S:O) weight ratio 90:10, without co-surfactant addition. This nano-emulsion was chosen to release studies. The obtained results showed that the prepared stable nano-emulsion can be used as a carrier for controlled release of geranic acid. The active substance release from the nano-emulsion and the oil solution, after 24 hours was 22%.

  6. Nanoemulsions containing octyl methoxycinnamate and solid particles of TiO₂: preparation, characterization and in vitro evaluation of the solar protection factor.

    PubMed

    Silva, Flavia F F; Ricci-Júnior, Eduardo; Mansur, Claudia R E

    2013-09-01

    The objective of this work was to develop and evaluate the physical-chemical properties of oil-in-water nanoemulsions for application as nanocosmetics for sun protection. Oil-in-water dispersions were processed by ultrasound (US) to obtain small emulsion droplets. These emulsions were obtained in the presence of commercial nonionic surfactants based on polyoxides and avocado oil as the oil phase. The US generated small but unstable droplets. This problem was solved by using a different surfactant, with a longer ethylene oxide chain, able to promote stabilization by steric mechanisms. The light scattering technique was used to characterize the nanoemulsions by their dispersed droplets' size, size distribution and variation of distribution with time (stability). Chemical and physical sunscreens - octyl methoxycinnamate (OMC) and titanium dioxide (TiO₂), respectively - were added to the stable system. The anti-UVB activity of the nanoemulsions and their components were evaluated by the method of Mansur et al. (1986) and spectral transmittance. The solar protection factor (SPF) was proportional to the OMC and TiO₂ concentrations. The in vitro OMC release was evaluated, and the presence of TiO₂ in the nanoemulsion did not affect the release profile, which showed the diffusion-dependent kinetics of the active ingredient in the formulation.

  7. Nanoemulsions containing octyl methoxycinnamate and solid particles of TiO₂: preparation, characterization and in vitro evaluation of the solar protection factor.

    PubMed

    Silva, Flavia F F; Ricci-Júnior, Eduardo; Mansur, Claudia R E

    2013-09-01

    The objective of this work was to develop and evaluate the physical-chemical properties of oil-in-water nanoemulsions for application as nanocosmetics for sun protection. Oil-in-water dispersions were processed by ultrasound (US) to obtain small emulsion droplets. These emulsions were obtained in the presence of commercial nonionic surfactants based on polyoxides and avocado oil as the oil phase. The US generated small but unstable droplets. This problem was solved by using a different surfactant, with a longer ethylene oxide chain, able to promote stabilization by steric mechanisms. The light scattering technique was used to characterize the nanoemulsions by their dispersed droplets' size, size distribution and variation of distribution with time (stability). Chemical and physical sunscreens - octyl methoxycinnamate (OMC) and titanium dioxide (TiO₂), respectively - were added to the stable system. The anti-UVB activity of the nanoemulsions and their components were evaluated by the method of Mansur et al. (1986) and spectral transmittance. The solar protection factor (SPF) was proportional to the OMC and TiO₂ concentrations. The in vitro OMC release was evaluated, and the presence of TiO₂ in the nanoemulsion did not affect the release profile, which showed the diffusion-dependent kinetics of the active ingredient in the formulation. PMID:22998354

  8. Interactions between Phospholipids and Organic Phases: Insights into Lipoproteins and Nanoemulsions.

    PubMed

    Hildebrandt, Ellen; Dessy, Alberto; Sommerling, Jan-Hendrik; Guthausen, Gisela; Nirschl, Hermann; Leneweit, Gero

    2016-06-14

    showed that combinations of solvent or solute saturation affect the outcome for nanoemulsions forming either expanded or condensed monolayers or multilayers.

  9. Acoustic cavitation-mediated delivery of small interfering ribonucleic acids with phase-shift nanoemulsions

    PubMed Central

    Burgess, Mark T.; Porter, Tyrone M.

    2015-01-01

    Localized, targeted delivery of small interfering ribonucleic acid (siRNA) has been the foremost hurdle in the use of siRNA for the treatment of various diseases. Major advances have been achieved in the synthesis of siRNA, which has led to greater target messenger RNA (mRNA) silencing and stability in physiological conditions. Although numerous delivery strategies have shown promise, there are still limited options for targeted delivery and release of siRNA administered systemically. In this in vitro study, phase-shift nanoemulsions (PSNE) were explored as cavitation nuclei to facilitate free siRNA delivery to cancer cells via sonoporation. A cell suspension containing varying amounts of PSNE and siRNA was exposed to 5 MHz pulsed ultrasound at fixed settings (6.2 MPa peak negative pressure, 5 cycle pulses, 250 Hz pulse repetition frequency, and total exposure duration of 100 seconds). Inertial cavitation emissions were detected throughout the exposure using a passive cavitation detector. Successful siRNA delivery was achieved (i.e. > 50% cell uptake) with high viability (> 80% viability). The percentage of cells with siRNA uptake was correlated with the amount of inertial cavitation activity generated from vaporized PSNE. The siRNA remained functional after delivery, significantly reducing expression of green fluorescent protein (GFP) in a stably transfected cell line. These results show that vaporized PSNE can facilitate siRNA entry into the cytosol of a majority of sonicated cells and may provide a non-endosomal route for siRNA delivery. PMID:25979417

  10. Interactions between Phospholipids and Organic Phases: Insights into Lipoproteins and Nanoemulsions.

    PubMed

    Hildebrandt, Ellen; Dessy, Alberto; Sommerling, Jan-Hendrik; Guthausen, Gisela; Nirschl, Hermann; Leneweit, Gero

    2016-06-14

    showed that combinations of solvent or solute saturation affect the outcome for nanoemulsions forming either expanded or condensed monolayers or multilayers. PMID:27159619

  11. Nondermal irritating hyperosmotic nanoemulsions reduce treatment times in a contamination model of wound healing.

    PubMed

    Connell, Sean; Li, Jianming; Durkes, Abigail; Zaroura, Mohammed; Shi, Riyi

    2016-07-01

    Increased microbial burden within the wound often complicates wound healing and may lead to subsequent infection or delayed healing. Here, we investigate a novel topical for addressing wound contamination that utilizes hyperosmotic saccharides with a cell membrane disrupting emulsion. These hyperosmotic nanoemulsions (HNE) were administered topically in a full-thickness biopsy model of wound healing. Results show that HNE were well tolerated in noninfected animals with no indications of dermal irritation or acute toxicity. Additionally, HNE was able to reduce bacterial bioburden (Escherichia coli and Enterococcus faecalis) levels by 3 logs within 24 h when wounds were inoculated with 5 × 10(6) total CFU. These bactericidal values were similar to wounds treated with silver sulfadiazine. Wound closure showed HNE wounds closed in 7.6 ± 0.2 days while SSD and control required 10.2 ± 0.4 and 10.4 ± 0.3 days, respectively. HNE maintained a moist wound environment, were well debrided, and exhibited improved hemostatic response. Further histological examination revealed enhanced granulation tissue as compared to silver sulfadiazine and control cohorts. These results were corroborated with 3D topographical imprints of the wounds at day 14 which qualitatively showed a smoother surface. In contrast, silver sulfadiazine appeared to delay wound closure. Finally, dermal sensitization and irritation studies conducted in guinea pig and rabbits did not reveal any acute dermal side effects from HNE exposure. The cumulative data indicates nonantibiotic-based HNEs may be a promising topical treatment for the management of contaminated wounds. PMID:27090977

  12. Design of the interface of edible nanoemulsions to modulate the bioaccessibility of neuroprotective antioxidants.

    PubMed

    Plaza-Oliver, M; Baranda, J Fernández Sainz de; Rodríguez Robledo, V; Castro-Vázquez, L; Gonzalez-Fuentes, J; Marcos, P; Lozano, M V; Santander-Ortega, M J; Arroyo-Jimenez, M M

    2015-07-25

    Most frequently the use of bioactive molecules for the supplementation of food and beverages is hampered by stability limitations or inadequate intestinal absorption. This work evaluates in vitro the role that the interface of the nanoemulsion has on the physicochemical properties, the stability behavior and the enzymatic degradation after oral intake. For that purpose three soybean oil (SB) formulations were studied. These formulations were based on the emulsifier lecithin but modified with two non-ionic surfactants Pluronic(®) F68 (PF68) or Pluronic(®) F127 (PF127) yielding (i) SB-NE (only lecithin on the interface), (ii) SB-NE PF68 (lecithin plus PF68) and 9 (iii) SB-NE PF127 (lecithin plus PF127). All the formulations tested were low polydispersed and showed a size of about 200 nm and ζ-potential of -50 mV. The in vitro colloidal stability assay showed that lecithin itself was able to promote that formulations reach unaltered to the small intestine and facilitate the absorption of the antioxidant payload on a tunable fashion there (with in vitro bioaccessibility values from around 40% up to a 70%). PF68 was able to sterically stabilize the formulation against the aggregation induced by the pH and electrolytes of the simulated gastrointestinal track; however, this surfactant was easily displaced by the lipases of the simulated intestinal milieu being unable to modulate the digestion pattern of the oil droplets in the small intestine. Finally, PF127 displayed a strong steric potential that dramatically reduced the interaction of the oil droplets with lipases in vitro, which will compromise the capacity of the formulation to improve the bioaccessibility of the loaded antioxidant. PMID:25997659

  13. Distinct Pathways of Humoral and Cellular Immunity Induced with the Mucosal Administration of a Nanoemulsion Adjuvant

    PubMed Central

    Makidon, Paul E.; Janczak, Katarzyna W.; Blanco, Luz P.; Swanson, Benjamin; Smith, Douglas M.; Pham, Tiffany; Szabo, Zsuzsanna; Kukowska-Latallo, Jolanta F.; Baker, James R.

    2014-01-01

    Nasal administration of an oil-in-water nanoemulsion (NE) adjuvant W805EC produces potent systemic and mucosal, Th-1– and Th-17–balanced cellular responses. However, its molecular mechanism of action has not been fully characterized and is of particular interest because NE does not contain specific ligands for innate immune receptors. In these studies, we demonstrate that W805EC NE adjuvant activates innate immunity, induces specific gene transcription, and modulates NF-κB activity via TLR2 and TLR4 by a mechanism that appears to be distinct from typical TLR agonists. Nasal immunization with NE-based vaccine showed that the TLR2, TLR4, and MyD88 pathways and IL-12 and IL-12Rβ1 expression are not required for an Ab response, but they are essential for the induction of balanced Th-1 polarization and Th-17 cellular immunity. NE adjuvant induces MHC class II, CD80, and CD86 costimulatory molecule expression and dendritic cell maturation. Further, upon immunization with NE, adjuvant mice deficient in the CD86 receptor had normal Ab responses but significantly reduced Th-1 cellular responses, whereas animals deficient in both CD80 and CD86 or lacking CD40 failed to produce either humoral or cellular immunity. Overall, our data show that intranasal administration of Ag with NE induces TLR2 and TLR4 activation along with a MyD88-independent Ab response and a MyD88-dependent Th-1 and Th-17 cell–mediated immune response. These findings suggest that the unique properties of NE adjuvant may offer novel opportunities for understanding previously unrecognized mechanisms of immune activation important for generating effective mucosal and systemic immune responses. PMID:24532579

  14. Nondermal irritating hyperosmotic nanoemulsions reduce treatment times in a contamination model of wound healing.

    PubMed

    Connell, Sean; Li, Jianming; Durkes, Abigail; Zaroura, Mohammed; Shi, Riyi

    2016-07-01

    Increased microbial burden within the wound often complicates wound healing and may lead to subsequent infection or delayed healing. Here, we investigate a novel topical for addressing wound contamination that utilizes hyperosmotic saccharides with a cell membrane disrupting emulsion. These hyperosmotic nanoemulsions (HNE) were administered topically in a full-thickness biopsy model of wound healing. Results show that HNE were well tolerated in noninfected animals with no indications of dermal irritation or acute toxicity. Additionally, HNE was able to reduce bacterial bioburden (Escherichia coli and Enterococcus faecalis) levels by 3 logs within 24 h when wounds were inoculated with 5 × 10(6) total CFU. These bactericidal values were similar to wounds treated with silver sulfadiazine. Wound closure showed HNE wounds closed in 7.6 ± 0.2 days while SSD and control required 10.2 ± 0.4 and 10.4 ± 0.3 days, respectively. HNE maintained a moist wound environment, were well debrided, and exhibited improved hemostatic response. Further histological examination revealed enhanced granulation tissue as compared to silver sulfadiazine and control cohorts. These results were corroborated with 3D topographical imprints of the wounds at day 14 which qualitatively showed a smoother surface. In contrast, silver sulfadiazine appeared to delay wound closure. Finally, dermal sensitization and irritation studies conducted in guinea pig and rabbits did not reveal any acute dermal side effects from HNE exposure. The cumulative data indicates nonantibiotic-based HNEs may be a promising topical treatment for the management of contaminated wounds.

  15. Formulation Development and Toxicity Assessment of Triacetin Mediated Nanoemulsions as Novel Delivery Systems for Rapamycin

    PubMed Central

    Sobhani, Hamideh; Tarighi, Parastoo; Ostad, Seyed Nasser; Shafaati, Alireza; Nafissi-Varcheh, Nastaran; Aboofazeli, Reza

    2015-01-01

    The aim of this investigation was to design and develop nanoemulsions (NEs) as novel delivery systems for rapamycin. Phase behavior of quaternary systems composed of Traicetin (as oil), various surfactants and co-surfactants and water at different surfactant/co-surfactant weight ratios was investigated by the construction of phase diagrams. Formulations were taken from the o/w NE region of the phase diagrams, depending upon the extent of NE domain. The spontaneous emulsification method was used to prepare various formulations containing 1 mg/mL of the drug. The NEs were characterized and subjected to stability tests at various temperatures over 9-12 months. Cumulative drug release from the selected formulations was determined for a period of 48 h using a dialysis sac. The assay of rapamycin was carried out using an HPLC technique. The effect of NEs on the viability of SKBR-3 cells was evaluated by MTT assay. The integrity of Caco-2 cell monolayers was measured by Transepithelial Electrical Resistance (TEER) and the transport of rapamycin-loaded NEs across Caco-2 cell monolayers was then assessed. The uptake of NEs by SKBR-3 cells was also investigated using florescence microscopy. Maximum drug release was observed in case of 4 formulations prepared with Tween 80 and Tween 20. MTT test results revealed different toxicity of NEs for SKBR-3 cell line and TEER demonstrated that formulations containing Tween 20 caused a more considerable decrease in cell integrity in comparison with those prepared with Tween 80. The results obtained from cellular uptake experiments were in consistent with those obtained from TEER and cytotoxicity experiments. PMID:26185501

  16. In Vitro Activities of a Novel Nanoemulsion against Burkholderia and Other Multidrug-Resistant Cystic Fibrosis-Associated Bacterial Species▿

    PubMed Central

    LiPuma, John J.; Rathinavelu, Sivaprakash; Foster, Bridget K.; Keoleian, Jordan C.; Makidon, Paul E.; Kalikin, Linda M.; Baker, James R.

    2009-01-01

    Respiratory tract infection, most often involving opportunistic bacterial species with broad-spectrum antibiotic resistance, is the primary cause of death in persons with cystic fibrosis (CF). Species within the Burkholderia cepacia complex are especially problematic in this patient population. We investigated a novel surfactant-stabilized oil-in-water nanoemulsion (NB-401) for activity against 150 bacterial isolates recovered primarily from CF respiratory tract specimens. These specimens included 75 Burkholderia isolates and 75 isolates belonging to other CF-relevant species including Pseudomonas, Achromobacter, Pandoraea, Ralstonia, Stenotrophomonas, and Acinetobacter. Nearly one-third of the isolates were multidrug resistant, and 20 (13%) were panresistant based on standard antibiotic testing. All isolates belonging to the same species were genotyped to ensure that each isolate was a distinct strain. The MIC90 of NB-401 was 125 μg/ml. We found no decrease in activity against multidrug-resistant or panresistant strains. MBC testing showed no evidence of tolerance to NB-401. We investigated the activity of NB-401 against a subset of strains grown as a biofilm and against planktonic strains in the presence of CF sputum. Although the activity of NB-401 was decreased under both conditions, the nanoemulsion remained bactericidal for all strains tested. These results support NB-401's potential role as a novel antimicrobial agent for the treatment of infection due to CF-related opportunistic pathogens. PMID:18955531

  17. Production and characterization of cosmetic nanoemulsions containing Opuntia ficus-indica (L.) mill extract as moisturizing agent.

    PubMed

    Ribeiro, Renato Cesar de Azevedo; Barreto, Stella Maria de Andrade Gomes; Ostrosky, Elissa Aarantes; da Rocha-Filho, Pedro Alves; Veríssimo, Lourena Mafra; Ferrari, Márcio

    2015-02-02

    This study aimed to produce and characterize an oil in water (O/W) nanoemulsion containing Opuntia ficus-indica (L.) Mill hydroglycolic extract, as well as evaluate its preliminary and accelerated thermal stability and moisturizing efficacy. The formulations containing 0.5% of xanthan gum (FX) and 0.5% of xanthan gum and 1% of Opuntia ficus-indica MILL extract (FXE) were white, homogeneus and fluid in aspect. Both formulations were stable during preliminary and accelerated stability tests. FX and FXE presented a pH compatible to skin pH (4.5-6.0); droplet size varying from 92.2 to 233.6 nm; a polydispersion index (PDI) around 0.200 and a zeta potential from -26.71 to -47.01 mV. FXE was able to increase the water content of the stratum corneum for 5 h after application on the forearm. The O/W nanoemulsions containing 1% of Opuntia ficus-indica (L.) Mill extract presented suitable stability for at least for 60 days. Besides, this formulation was able to increase the water content of stratum corneum, showing its moisturizing efficacy.

  18. Sensing of biologically important cations such as Na(+), K(+), Ca(2+), Cu(2+), and Fe(3+) using magnetic nanoemulsions.

    PubMed

    Mahendran, V; Philip, John

    2013-04-01

    We report a simple approach to the ultrasensitive detection of biologically important metal ions using a magnetic nanoemulsion. The nanoemulsion used in our study was an oil-in-water emulsion droplet of average size ∼190 nm containing ferrimagnetic iron oxide nanoparticles of average size ∼10 nm. In a static magnetic field, the emulsion droplets self-assemble into a nanoarray with distinct interdroplet spacing. In the presence of cations in the solution, the nanofluid array shows a large blue shift in the diffracted Bragg peak and a visually perceivable color change due to changes in the electrical double layer upon the diffusion of cations. The colloidal force-distance measurements in the presence of cations show large variations at the onset of repulsion in the presence of cations. The sensor shows good selectivity to Na(+), K(+), Ca(2+), Cu(2+), and Fe(3+) ions and offers a rapid response compared to conventional techniques. This approach can be useful for the recognition of biologically important cations. PMID:23477486

  19. Galantamine-loaded PLGA nanoparticles, from nano-emulsion templating, as novel advanced drug delivery systems to treat neurodegenerative diseases.

    PubMed

    Fornaguera, C; Feiner-Gracia, N; Calderó, G; García-Celma, M J; Solans, C

    2015-07-28

    Polymeric nanoparticles could be promising drug delivery systems to treat neurodegenerative diseases. Among the various methods of nanoparticle preparation, nano-emulsion templating was used in the present study to prepare galantamine-loaded nano-emulsions by a low-energy emulsification method followed by solvent evaporation to obtain galantamine-loaded polymeric nanoparticles. This approach was found to be suitable because biocompatible, biodegradable and safe nanoparticles with appropriate features (hydrodynamic radii around 20 nm, negative surface charge and stability higher than 3 months) for their intravenous administration were obtained. Encapsulation efficiencies higher than 90 wt% were obtained with a sustained drug release profile as compared to that from aqueous and micellar solutions. The enzymatic activity of the drug was maintained at 80% after its encapsulation into nanoparticles that were non-cytotoxic at the required therapeutic concentration. Therefore, novel galantamine-loaded polymeric nanoparticles have been designed for the first time using the nano-emulsification approach and showed the appropriate features to become advanced drug delivery systems to treat neurodegenerative diseases. PMID:26118655

  20. O/W nano-emulsion formation using an isothermal low-energy emulsification method in a mixture of polyglycerol polyricinoleate and hexaglycerol monolaurate with glycerol system.

    PubMed

    Wakisaka, Satoshi; Nishimura, Takahisa; Gohtani, Shoichi

    2015-01-01

    We investigated how phase behavior changes by replacing water with glycerol in water/mixture of polyglycerol polyricinoleate (PGPR) and hexaglycerol monolaurate (HGML) /vegetable oil system, and studied the effect of glycerol on o/w nano-emulsion formation using an isothermal low-energy method. In the phase behavior study, the liquid crystalline phase (Lc) + the sponge phase (L3) expanded toward lower surfactant concentration when water was replaced with glycerol in a system containing surfactant HLP (a mixture of PGPR and HGML). O/W nano-emulsions were formed by emulsification of samples in a region of Lc + L3. In the glycerol/surfactant HLP/vegetable oil system, replacing water with glycerol was responsible for the expansion of a region containing Lc + L3 toward lower surfactant concentration, and as a result, in the glycerol/surfactant HLP/vegetable oil system, the region where o/w nano-emulsions or o/w emulsions could be prepared using an isothermal low-energy emulsification method was wide, and the droplet diameter of the prepared o/w emulsions was also smaller than that in the water/surfactant HLP/vegetable oil system. Therefore, glycerol was confirmed to facilitate the preparation of nano-emulsions from a system of surfactant HLP. Moreover, in this study, we could prepare o/w nano-emulsions with a simple one-step addition of water at room temperature without using a stirrer. Thus, the present technique is highly valuable for applications in several industries.

  1. Depigmenting action of a nanoemulsion containing heartwood extract of Artocarpus incisus on UVB-induced hyperpigmentation in C57BL/6 mice.

    PubMed

    Buranajaree, Supasiri; Donsing, Piyaporn; Jeenapongsa, Rattima; Viyoch, Jarupa

    2011-01-01

    Melasma hyperpigmentation is an acquired disorder predominantly affecting the female population. The present study was conducted to determine the potential of a botanical extract to reduce observable hyperpigmentation. The extract from heartwood of Artocarpus incisus was formulated into nanoemulsions, and the depigmenting efficacy of the formulated nanoemulsion was determined in vivo. HPLC analysis showed that the extract contained artocarpin in an amount of 44.5 ± 0.1% w/w. The extract exhibited melanogenesis inhibition with an IC(50) value of 30.2 ± 2.4 mg/ml, while kojic acid, a well known lightening agent, exhibited an IC(50) of 51.4 ± 5.1 mg/ml. The nanoemulsion containing the extract was then formulated and prepared by the phase inversion technique. The concentration of the extract used was about six times its IC(50). The optimal formula containing 0.02% w/w extract, 41.6% w/w isopropyl myristate, 0.03% w/w α-tocopherol, 5% w/wglyc-eryl monostearate (co-emulsifier), 8% w/w ceteareth-10 (emulsifier), 0.05% triethanolamine, 0.03% w/w carbopol 940, and water adjusted to 100% w/w provided a homogeneous o/w emulsion with a droplet size of 325 ± 15 nm and a polydispersity of 0.31 ± 0.02. The depigmenting efficacy was then observed following topical application of the formulated nanoemulsion to UVB-stimulated hyperpigmented dorsal skin of C57BL/6 mice. A strongly visible decrease in hyperpigmentation was observed after six weeks of treatment with the formulated nanoemulsion. The degree of pigmentation decreased after the application was 84 ± 4 units, while that after the application of the extracted prepared into solution was 51 ± 3 units. The applied areas would return to their original color after treatment was stopped for four weeks.

  2. Immunohistochemical localization in rabbit brain of a peptide resembling the COOH-terminal octapeptide of cholecystokinin.

    PubMed Central

    Straus, E; Muller, J E; Choi, H S; Paronetto, F; Yalow, R S

    1977-01-01

    Immunohistochemical techniques were used to demonstrate the presence of a material resembling the COOH-terminal octapeptide of cholecystokinin in rabbit cerebral cortical neurons. Deep staining was seen in cell bodies throughout the cortical grey matter and diffusely in the subcortical white matter. Images PMID:331325

  3. Palmar fascial thickening and contractures of fingers resembling arthritis--a paraneoplastic symptom?

    PubMed

    Strobel, E S; Lacour, M; Peter, H H

    1992-01-01

    A 59-year-old women presented with contractures of the fingers of both hands 11 months before a diagnosis of an ovarian carcinoma with paraaortic lymph node metastases was made. We suggest that the contractures, which were associated with palmar fascial thickening and which clinically resembled arthritis, might have been a paraneoplastic sign.

  4. A highly crystalline microporous hybrid organic-inorganic aluminosilicate resembling the AFI-type zeolite.

    PubMed

    Bellussi, Giuseppe; Millini, Roberto; Montanari, Erica; Carati, Angela; Rizzo, Caterina; Parker, Wallace O; Cruciani, Giuseppe; de Angelis, Alberto; Bonoldi, Lucia; Zanardi, Stefano

    2012-07-28

    ECS-14, a crystalline microporous hybrid organic-inorganic aluminosilicate, has been synthesized by using 1,4-bis-(triethoxysilyl)-benzene (BTEB) as a source of silica. Its structure contains a system of linear channels with 12-membered ring openings, running along the [001] direction, resembling the pore architecture of the AFI framework type. PMID:22717682

  5. An Analysis of the Claim that "Physical Education" Has Become a "Family Resemblance" Term.

    ERIC Educational Resources Information Center

    Zeigler, Earle F.

    In this paper, the author examines the confusion that currently exists concerning the term "physical education." In particular, he analyzes the claim that"physical education" is a "family resemblance" term--a word or phrase which may be used to denote fundamentally different concepts, but concepts in which there is some overlapping of…

  6. Children and Adolescents' Understandings of Family Resemblance: A Study of Naive Inheritance Concepts

    ERIC Educational Resources Information Center

    Williams, Joanne M.

    2012-01-01

    This paper aims to provide developmental data on two connected naive inheritance concepts and to explore the coherence of children's naive biology knowledge. Two tasks examined children and adolescents' (4, 7, 10, and 14 years) conceptions of phenotypic resemblance across kin (in physical characteristics, disabilities, and personality traits). The…

  7. LINGAM AS A SACRED OBJECT AND THE HEAD-DRESS OF SUFI RESEMBLING IT

    PubMed Central

    Mahdihassan, S.

    1990-01-01

    This study scans into past of ancient man and discusses meticulously how the reproductive organ Lingam became sacred object to Hindus and why a sufi wore a phallus shaped head-dress resembling to it. In this manner the author demystifies here the procreation, the law of nature. PMID:22557692

  8. Solid Matrix Based Lipidic Nanoparticles in Oral Cancer Chemotherapy: Applications and Pharmacokinetics.

    PubMed

    Ahmad, Javed; Amin, Saima; Rahman, Mahfoozur; Rub, Rehan Abdur; Singhal, Madhur; Ahmad, Mohammad Zaki; Rahman, Ziyaur; Addo, Richard T; Ahmad, Farhan Jalees; Mushtaq, Gohar; Kamal, Mohammad Amjad; Akhter, Sohail

    2015-01-01

    Chemotherapeutic delivery by oral route in cancer patients has the potential to create "hospitalization free chemotherapy" which is a vision of oncologists, formulation scientists and patients. Such a therapeutic approach will improve patients' compliance, ease the burden of the patients' caregivers and significantly reduce the cost of treatment. In current clinical practice, chemotherapy carried out by intravenous injection or infusion leads to undesired side-effects such as plasma concentrations crossing the maximum safe concentration, rapid body clearance and lower bioavailability. Despite the presence of challenges such as poor aqueous solubility and stability of drugs and the presence of biological barriers like multidrug efflux transporter in the GI tract, oral cancer chemotherapy has the potential to surmount those obstacles. Lipid nanoparticles (LNPs) such as solid lipid nanoparticle, nanostructured lipid carriers, nano lipid-drug conjugates, mixed micelles, liposomes and nanoemulsions have shown some promising results for use in oral anticancer drug delivery through nanotechnological approach. LNPs demonstrate enhanced oral bioavailability owing to their ability to inhibit first pass metabolism via lymphatic absorption by chylomicron-linked and/or M-cell uptake. LNPs reduce the inter- and intrasubject pharmacokinetics variability of administrated drugs. Moreover, certain classes of phospholipids and surfactants used in the formulations of LNPs can suppress the P-glycoprotein efflux system. Here, we shall be discussing the biopharmaceutical challenges in oral cancer chemotherapy and how the LNPs may provide solutions to such challenges. The effect of GI tract environment on LNPs and pharmacokinetics shall also be discussed. PMID:26264206

  9. Role of lymphatics in removal of sheep lung surfactant lipid.

    PubMed

    Tarpey, M M; O'Brodovich, H M; Young, S L

    1983-04-01

    To study the role of lung lymphatics in the removal of surfactant lipid from the sheep lung, we injected [1-14C]palmitate intravenously into six animals previously fitted with a cannula draining the caudal mediastinal lymph node. Lung lymph was collected for 100 h after injection of radiolabel. We obtained alveolar lavage material through a tracheostomy in four other animals after intravenous injection of [9,10-3H]palmitate. We measured radioactivity at several time points in lipid extracts from lymph, lavage fluid, and lung tissue. Alveolar lavage disaturated phosphatidylcholine (DSPC) specific activity peaked at about 40 h and was reduced to 30% of this value by 82 h. About 2% of the injected radiolabel was incorporated into lung tissue lipids. Only 4% of the level of labeling achieved in lung tissue lipids was found in lung lymph lipid during 100 h of lymph collection. Sixty-three percent of radiolabel in lymph lipid was recovered in phospholipids, and 29% of phospholipid radiolabel was found in DSPC. The distribution of phosphorus and palmitate radiolabel in lung lymph phospholipid did not closely resemble that of surfactant lipid. No rise in lung lymph DSPC specific activity was observed following the peak in lavage specific activity. If surfactant lipid is removed from the alveolar compartment without extensive recycling, then we conclude that the lung lymphatics do not play a major role in the clearance of surfactant lipid from the alveolar surface. PMID:6687883

  10. Development and Evaluation of Lipid Nanoparticles for Drug Delivery: Study of Toxicity In, Vitro and In Vivo.

    PubMed

    Winter, Evelyn; Dal Pizzol, Carine; Locatelli, Claudriana; Crezkynski-Pasa, Tânia Beatriz

    2016-02-01

    Lipid nanoparticles have received considerable attention in the field of drug delivery, due their ability to incorporate lipophilic drugs and to allow controlled drug release. Solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), and nanoemulsion (NE) are three different lipid nanostructured systems presenting intrinsically physical properties, which have been widely studied in recent years. Despite the extensive applicability of lipid nanoparticles, the toxicity of these systems has not been sufficiently investigated thus far. It is generally believed that lipids are biocompatible. However, it is known that materials structured in nanoscale might have their intrinsic physicochemical properties modified. Thus, the aim of this study was to evaluate the cytotoxicity of these three nanoparticle systems. To this end, in vitro and in vivo toxicity studies were carried out. Our results indicate that nanoparticles containing the solid lipid GMS (SLN and NLC) induced an important cytotoxicity in vitro, but showed minimal toxicity in vivo--evidenced by the body weight analysis. The NE did not induce in vitro toxicity and did not induce body weight alteration. On the contrary, the SLN and NLC possibly induce an inflammatory process in vivo. All nanoparticle systems induced lipid peroxidation in the animals' livers, but only SLN and NLC induced a decrease of antioxidant defences indicating that the main mechanism of toxicity is the induction of oxidative stress in liver. The higher toxicity induced by SLN and NLC indicates that the solid lipid GMS could be the responsible for this effect. Nevertheless, this study provides important insights for toxicological studies of different lipid nanoparticles systems. PMID:27433582

  11. Development and Evaluation of Lipid Nanoparticles for Drug Delivery: Study of Toxicity In, Vitro and In Vivo.

    PubMed

    Winter, Evelyn; Dal Pizzol, Carine; Locatelli, Claudriana; Crezkynski-Pasa, Tânia Beatriz

    2016-02-01

    Lipid nanoparticles have received considerable attention in the field of drug delivery, due their ability to incorporate lipophilic drugs and to allow controlled drug release. Solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), and nanoemulsion (NE) are three different lipid nanostructured systems presenting intrinsically physical properties, which have been widely studied in recent years. Despite the extensive applicability of lipid nanoparticles, the toxicity of these systems has not been sufficiently investigated thus far. It is generally believed that lipids are biocompatible. However, it is known that materials structured in nanoscale might have their intrinsic physicochemical properties modified. Thus, the aim of this study was to evaluate the cytotoxicity of these three nanoparticle systems. To this end, in vitro and in vivo toxicity studies were carried out. Our results indicate that nanoparticles containing the solid lipid GMS (SLN and NLC) induced an important cytotoxicity in vitro, but showed minimal toxicity in vivo--evidenced by the body weight analysis. The NE did not induce in vitro toxicity and did not induce body weight alteration. On the contrary, the SLN and NLC possibly induce an inflammatory process in vivo. All nanoparticle systems induced lipid peroxidation in the animals' livers, but only SLN and NLC induced a decrease of antioxidant defences indicating that the main mechanism of toxicity is the induction of oxidative stress in liver. The higher toxicity induced by SLN and NLC indicates that the solid lipid GMS could be the responsible for this effect. Nevertheless, this study provides important insights for toxicological studies of different lipid nanoparticles systems.

  12. Proteome Analysis of Cytoplasmatic and Plastidic β-Carotene Lipid Droplets in Dunaliella bardawil1[OPEN

    PubMed Central

    Davidi, Lital; Levin, Yishai; Ben-Dor, Shifra; Pick, Uri

    2015-01-01

    The halotolerant green alga Dunaliella bardawil is unique in that it accumulates under stress two types of lipid droplets: cytoplasmatic lipid droplets (CLD) and β-carotene-rich (βC) plastoglobuli. Recently, we isolated and analyzed the lipid and pigment compositions of these lipid droplets. Here, we describe their proteome analysis. A contamination filter and an enrichment filter were utilized to define core proteins. A proteome database of Dunaliella salina/D. bardawil was constructed to aid the identification of lipid droplet proteins. A total of 124 and 42 core proteins were identified in βC-plastoglobuli and CLD, respectively, with only eight common proteins. Dunaliella spp. CLD resemble cytoplasmic droplets from Chlamydomonas reinhardtii and contain major lipid droplet-associated protein and enzymes involved in lipid and sterol metabolism. The βC-plastoglobuli proteome resembles the C. reinhardtii eyespot and Arabidopsis (Arabidopsis thaliana) plastoglobule proteomes and contains carotene-globule-associated protein, plastid-lipid-associated protein-fibrillins, SOUL heme-binding proteins, phytyl ester synthases, β-carotene biosynthesis enzymes, and proteins involved in membrane remodeling/lipid droplet biogenesis: VESICLE-INDUCING PLASTID PROTEIN1, synaptotagmin, and the eyespot assembly proteins EYE3 and SOUL3. Based on these and previous results, we propose models for the biogenesis of βC-plastoglobuli and the biosynthesis of β-carotene within βC-plastoglobuli and hypothesize that βC-plastoglobuli evolved from eyespot lipid droplets. PMID:25404729

  13. Proteome analysis of cytoplasmatic and plastidic β-carotene lipid droplets in Dunaliella bardawil.

    PubMed

    Davidi, Lital; Levin, Yishai; Ben-Dor, Shifra; Pick, Uri

    2015-01-01

    The halotolerant green alga Dunaliella bardawil is unique in that it accumulates under stress two types of lipid droplets: cytoplasmatic lipid droplets (CLD) and β-carotene-rich (βC) plastoglobuli. Recently, we isolated and analyzed the lipid and pigment compositions of these lipid droplets. Here, we describe their proteome analysis. A contamination filter and an enrichment filter were utilized to define core proteins. A proteome database of Dunaliella salina/D. bardawil was constructed to aid the identification of lipid droplet proteins. A total of 124 and 42 core proteins were identified in βC-plastoglobuli and CLD, respectively, with only eight common proteins. Dunaliella spp. CLD resemble cytoplasmic droplets from Chlamydomonas reinhardtii and contain major lipid droplet-associated protein and enzymes involved in lipid and sterol metabolism. The βC-plastoglobuli proteome resembles the C. reinhardtii eyespot and Arabidopsis (Arabidopsis thaliana) plastoglobule proteomes and contains carotene-globule-associated protein, plastid-lipid-associated protein-fibrillins, SOUL heme-binding proteins, phytyl ester synthases, β-carotene biosynthesis enzymes, and proteins involved in membrane remodeling/lipid droplet biogenesis: VESICLE-INDUCING PLASTID PROTEIN1, synaptotagmin, and the eyespot assembly proteins EYE3 and SOUL3. Based on these and previous results, we propose models for the biogenesis of βC-plastoglobuli and the biosynthesis of β-carotene within βC-plastoglobuli and hypothesize that βC-plastoglobuli evolved from eyespot lipid droplets.

  14. Plasma lipids, lipoprotein metabolism and HDL lipid transfers are equally altered in metabolic syndrome and in type 2 diabetes.

    PubMed

    Silva, Vanessa M; Vinagre, Carmen G C; Dallan, Luis A O; Chacra, Ana P M; Maranhão, Raul C

    2014-07-01

    Metabolic syndrome (MetS) refers to states of insulin resistance that predispose to development of cardiovascular disease and type 2 diabetes (T2DM). The aim was to investigate whether plasma lipids and lipid metabolism differ in MetS patients compared to those with T2DM with poor glycemic control (glycated hemoglobin > 7.0). Eighteen patients with T2DM, 18 with MetS and 14 controls, paired for age (40-70 years) and body mass index (BMI), were studied. Plasma lipids and the kinetics of a triacylglycerol-rich emulsion labeled with [(3)H]-triolein ([(3)H]-TAG) and [(14)C]-cholesteryl esters ([(14)C]-CE) injected intravenously followed by one-hour blood sampling were determined. Lipid transfers from an artificial nanoemulsion donor to high-density lipoprotien (HDL) were assayed in vitro. Low-density lipoprotein (LDL) and HDL cholesterol (mg/dl) were not different in T2DM (128 ± 7; 42 ± 7) and MetS (142 ± 6; 39 ± 3), but triacylglycerols were even higher in MetS (215 ± 13) than in T2DM (161 ±11, p < 0.05). Fractional clearance rate (FCR, in min(1)) of [(3)H]-TAG and [(14)C]-CE were equal in T2DM (0.008 ± 0.018; 0.005 ± 0.024) and MetS (0.010 ± 0.016; 0.006 ± 0.013), and both were reduced compared to controls. The transfer of non-esterified cholesterol, phospholipids and triacylglycerols to HDL was higher in MetS and T2DM than in controls (p < 0.01). Cholesteryl ester transfer and HDL size were equal in all groups. Results imply that MetS is equal to poorly controlled T2DM concerning the disturbances of plasma lipid metabolism examined here, and suggest that there are different thresholds for the insulin action on glucose and lipids. These findings highlight the magnitude of the lipid disturbances in MetS, and may have implications in the prevention of cardiovascular diseases. PMID:24719245

  15. Plasma lipids, lipoprotein metabolism and HDL lipid transfers are equally altered in metabolic syndrome and in type 2 diabetes.

    PubMed

    Silva, Vanessa M; Vinagre, Carmen G C; Dallan, Luis A O; Chacra, Ana P M; Maranhão, Raul C

    2014-07-01

    Metabolic syndrome (MetS) refers to states of insulin resistance that predispose to development of cardiovascular disease and type 2 diabetes (T2DM). The aim was to investigate whether plasma lipids and lipid metabolism differ in MetS patients compared to those with T2DM with poor glycemic control (glycated hemoglobin > 7.0). Eighteen patients with T2DM, 18 with MetS and 14 controls, paired for age (40-70 years) and body mass index (BMI), were studied. Plasma lipids and the kinetics of a triacylglycerol-rich emulsion labeled with [(3)H]-triolein ([(3)H]-TAG) and [(14)C]-cholesteryl esters ([(14)C]-CE) injected intravenously followed by one-hour blood sampling were determined. Lipid transfers from an artificial nanoemulsion donor to high-density lipoprotien (HDL) were assayed in vitro. Low-density lipoprotein (LDL) and HDL cholesterol (mg/dl) were not different in T2DM (128 ± 7; 42 ± 7) and MetS (142 ± 6; 39 ± 3), but triacylglycerols were even higher in MetS (215 ± 13) than in T2DM (161 ±11, p < 0.05). Fractional clearance rate (FCR, in min(1)) of [(3)H]-TAG and [(14)C]-CE were equal in T2DM (0.008 ± 0.018; 0.005 ± 0.024) and MetS (0.010 ± 0.016; 0.006 ± 0.013), and both were reduced compared to controls. The transfer of non-esterified cholesterol, phospholipids and triacylglycerols to HDL was higher in MetS and T2DM than in controls (p < 0.01). Cholesteryl ester transfer and HDL size were equal in all groups. Results imply that MetS is equal to poorly controlled T2DM concerning the disturbances of plasma lipid metabolism examined here, and suggest that there are different thresholds for the insulin action on glucose and lipids. These findings highlight the magnitude of the lipid disturbances in MetS, and may have implications in the prevention of cardiovascular diseases.

  16. Lipid14: The Amber Lipid Force Field.

    PubMed

    Dickson, Callum J; Madej, Benjamin D; Skjevik, Age A; Betz, Robin M; Teigen, Knut; Gould, Ian R; Walker, Ross C

    2014-02-11

    The AMBER lipid force field has been updated to create Lipid14, allowing tensionless simulation of a number of lipid types with the AMBER MD package. The modular nature of this force field allows numerous combinations of head and tail groups to create different lipid types, enabling the easy insertion of new lipid species. The Lennard-Jones and torsion parameters of both the head and tail groups have been revised and updated partial charges calculated. The force field has been validated by simulating bilayers of six different lipid types for a total of 0.5 μs each without applying a surface tension; with favorable comparison to experiment for properties such as area per lipid, volume per lipid, bilayer thickness, NMR order parameters, scattering data, and lipid lateral diffusion. As the derivation of this force field is consistent with the AMBER development philosophy, Lipid14 is compatible with the AMBER protein, nucleic acid, carbohydrate, and small molecule force fields. PMID:24803855

  17. Content of lipids in blood and tissues of animals during hypodynamia

    NASA Technical Reports Server (NTRS)

    Federov, I. V.; Rylnikov, Y. P.; Lobova, T. M.

    1980-01-01

    Experiments on 97 rats and 50 rabbits were undertaken to study the influence of hypodynamia on the lipid content in the blood, liver, heart, and in the aorta. Reduction of muscular activity contributed to the increase of cholesterol and beta lipoprotein levels in the blood and to accumulation of cholesterol in the liver and the heart. The total lipid content in these tissues decreased. In the aorta the total lipid content increased, while lecithin and cephalin figures went down. The character of biochemical changes in hypodynamia resembles in many ways the lipid metabolism changes in atherosclerosis.

  18. A Family Resemblance Approach to the Nature of Science for Science Education

    NASA Astrophysics Data System (ADS)

    Irzik, Gürol; Nola, Robert

    2011-07-01

    Although there is universal consensus both in the science education literature and in the science standards documents to the effect that students should learn not only the content of science but also its nature, there is little agreement about what that nature is. This led many science educators to adopt what is sometimes called "the consensus view" about the nature of science (NOS), whose goal is to teach students only those characteristics of science on which there is wide consensus. This is an attractive view, but it has some shortcomings and weaknesses. In this article we present and defend an alternative approach based on the notion of family resemblance. We argue that the family resemblance approach is superior to the consensus view in several ways, which we discuss in some detail.

  19. Formulation and Characterization of Nanoemulsion Intranasal Adjuvants: Effects of Surfactant Composition on Mucoadhesion and Immunogenicity

    PubMed Central

    Wong, Pamela T.; Wang, Su He; Ciotti, Susan; Makidon, Paul E.; Smith, Douglas M.; Fan, Yongyi; Schuler, Charles F.; Baker, James R.

    2014-01-01

    Development of effective intranasal vaccines is of great interest due to their potential to induce both mucosal and systemic immunity. Here we produced oil-in-water nanoemulsion (NE) formulations containing various cationic and nonionic surfactants for use as adjuvants for the intranasal delivery of vaccine antigens. NE induced immunogenicity and antigen delivery are believed to be facilitated through initial contact interactions between the NE droplet and mucosal surfaces which promote prolonged residence of the vaccine at the site of application, and thus cellular uptake. However, the details of this mechanism have yet to be fully characterized experimentally. We have studied the physicochemical properties of the NE droplet surfactant components and demonstrate that properties such as charge and polar head group geometry influence the association of the adjuvant with the mucus protein, mucin. Association of NE droplets with mucin in vitro was characterized by various biophysical and imaging methods including dynamic light scattering (DLS), zeta potential (ZP), and surface plasmon resonance (SPR) measurements as well as transmission electron microscopy (TEM). Emulsion surfactant compositions were varied in a systematic manner to evaluate the effects of hydrophobicity and polar group charge/size on the NE-mucin interaction. Several cationic NE formulations were found to facilitate cellular uptake of the model antigen, ovalbumin (OVA), in a nasal epithelial cell line. Furthermore, fluorescent images of tissue sections from mice intranasally immunized with the same NEs containing green fluorescent protein (GFP) antigen demonstrated that these NEs also enhanced mucosal layer penetration and cellular uptake of antigen in vivo. NE-mucin interactions observed through biophysical measurements corresponded with the ability of the NE to enhance cellular uptake. Formulations that enhanced antigen uptake in vitro and in vivo also led to the induction of a more consistent

  20. Product development studies on surface-adsorbed nanoemulsion of olmesartan medoxomil as a capsular dosage form.

    PubMed

    Singh, Sumita; Pathak, Kamla; Bali, Vikas

    2012-12-01

    The present study aimed at development of capsular dosage form of surface-adsorbed nanoemulsion (NE) of olmesartan medoxomil (OLM) so as to overcome the limitations associated with handling of liquid NEs without affecting their pharmaceutical efficacy. Selection of oil, surfactant, and cosurfactant for construction of pseudoternary phase diagrams was made on the basis of solubility of drug in these excipients. Rationally selected NE formulations were evaluated for percentage transmittance, viscosity, refractive index, globule size, zeta potential, and polydispersity index (PDI). Formulation (F3) comprising of Capmul MCM® (10% v/v), Tween 80® (11.25% v/v), polyethylene glycol 400 (3.75% v/v), and double-distilled water (75% v/v) displayed highest percentage cumulative drug release (%CDR; 96.69 ± 1.841), least globule size (17.51 ± 5.87 nm), low PDI (0.203 ± 0.032), high zeta potential (-58.93 ± 0.98 mV), and hence was selected as the optimized formulation. F3 was adsorbed over colloidal silicon dioxide (2 ml/400 mg) to produce free-flowing solid surface-adsorbed NE that presented a ready-to-fill capsule composition. Conversion of NE to surface-adsorbed NE and its reconstitution to NE did not affect the in vitro release profile of OLM as the similarity factor with respect to NE was found to be 66% and 73% respectively. The %CDR after 12 h for optimized NE, surface-adsorbed NE, and reconstituted NE was found to be 96.69 ± 0.54, 96.07 ± 1.76, and 94.78 ± 1.57, respectively (p > 0.05). The present study established capsulated surface-adsorbed NE as a viable delivery system with the potential to overcome the handling limitations of NE.

  1. Inhibited biofilm formation and improved antibacterial activity of a novel nanoemulsion against cariogenic Streptococcus mutans in vitro and in vivo

    PubMed Central

    Li, Yun Fei; Sun, Hong Wu; Gao, Rong; Liu, Kai Yun; Zhang, Hua Qi; Fu, Qi Huan; Qing, Sheng Li; Guo, Gang; Zou, Quan Ming

    2015-01-01

    The aim of this study was to prepare a novel nanoemulsion loaded with poorly water-soluble chlorhexidine acetate (CNE) to improve its solubility, and specifically enhance the antimicrobial activity against Streptococcus mutans in vitro and in vivo. In this study, a novel CNE nanoemulsion with an average size of 63.13 nm and zeta potential of −67.13 mV comprising 0.5% CNE, 19.2% Tween 80, 4.8% propylene glycol, and 6% isopropyl myristate was prepared by the phase inversion method. Important characteristics such as the content, size, zeta potential, and pH value of CNE did not change markedly, stored at room temperature for 1 year. Also, compared with chlorhexidine acetate water solution (CHX), the release profile results show that the CNE has visibly delayed releasing effect in both phosphate-buffered saline and artificial saliva solutions (P<0.005). The minimum inhibitory concentration and minimum bactericidal concentration of CHX for S. mutans (both 0.8 μg/mL) are both two times those of CNE (0.4 μg/mL). Besides, CNE of 0.8 μg/mL exhibited fast-acting bactericidal efficacy against S. mutans, causing 95.07% death within 5 minutes, compared to CHX (73.33%) (P<0.01). We observed that 5 mg/mL and 2 mg/mL CNE were both superior to CHX, significantly reducing oral S. mutans numbers and reducing the severity of carious lesions in Sprague Dawley rats (P<0.05), in an in vivo test. CNE treatment at a concentration of 0.2 μg/mL inhibited biofilm formation more effectively than CHX, as indicated by the crystal violet staining method, scanning electron microscopy, and atomic force microscopy. The cell membrane of S. mutans was also severely disrupted by 0.2 μg/mL CNE, as indicated by transmission electron microscopy. These results demonstrated that CNE greatly improved the solubility and antimicrobial activity of this agent against S. mutans both in vitro and in vivo. This novel nanoemulsion is a promising medicine for preventing and curing dental caries. PMID:25624759

  2. Uterine tumors resembling ovarian sex cord tumors are polyphenotypic neoplasms with true sex cord differentiation.

    PubMed

    Irving, Julie A; Carinelli, Silvestro; Prat, Jaime

    2006-01-01

    In this study, we present the clinicopathologic features and immunophenotypic characteristics of five cases of uterine tumors resembling ovarian sex cord tumors and three cases of endometrial stromal tumors with sex cord-like elements, with emphasis on immunohistochemical markers of sex cord differentiation. The mean patient age was 42 years (range 19-69 years), and vaginal bleeding was the most common clinical presentation. The tumors were usually polypoid masses arising in the uterine fundus, with a mean tumor size of 6.7 cm. Sex cord patterns in uterine tumors resembling ovarian sex cord tumors, including anastomosing cords, trabeculae, small nests, tubules, and in one case, a striking retiform architecture with Leydig-like cells, comprised from 70 to 100% of the tumor volume. All uterine tumors resembling ovarian sex cord tumors were positive for two or more markers of sex cord differentiation; all five cases showed strong immunoreactivity for calretinin, with coexpression of CD99 (four cases), Melan-A (two cases), and inhibin (two cases). Endometrial stromal tumors with sex cord-like elements were less frequently positive for markers of sex cord differentiation, with each case positive for one marker (calretinin, two cases; CD99, one case). In addition, all eight cases were frequently positive for cytokeratin, CD10, vimentin, estrogen receptor, and progesterone receptor; desmin immunoreactivity, when present, was limited to minor foci of smooth muscle. Overall, the morphologic and immunohistochemical findings in uterine tumors resembling ovarian sex cord tumors strongly support that these unusual uterine tumors are polyphenotypic neoplasms with true sex cord differentiation.

  3. Gastrointestinal symptoms resembling ulcerative proctitis caused by larvae of the drone fly Eristalis tenax.

    PubMed

    Desoubeaux, Guillaume; Gaillard, Julien; Borée-Moreau, Diane; Bailly, Éric; Andres, Christian R; Chandenier, Jacques

    2014-04-01

    We report a case of facultative intestinal myiasis due to larvae of the drone fly Eristalis tenax, also named the rat-tailed maggots. The development of larvae in the lower bowel was responsible for non-specific gastrointestinal symptoms that resembled ulcerative proctitis. The diagnosis was established upon the observation of four spontaneously excreted mobile larvae. The definite identification of the E. tenax species was made possible by scanning electron microscopy. The clinical outcome was satisfactory.

  4. Gastrointestinal symptoms resembling ulcerative proctitis caused by larvae of the drone fly Eristalis tenax.

    PubMed

    Desoubeaux, Guillaume; Gaillard, Julien; Borée-Moreau, Diane; Bailly, Éric; Andres, Christian R; Chandenier, Jacques

    2014-04-01

    We report a case of facultative intestinal myiasis due to larvae of the drone fly Eristalis tenax, also named the rat-tailed maggots. The development of larvae in the lower bowel was responsible for non-specific gastrointestinal symptoms that resembled ulcerative proctitis. The diagnosis was established upon the observation of four spontaneously excreted mobile larvae. The definite identification of the E. tenax species was made possible by scanning electron microscopy. The clinical outcome was satisfactory. PMID:24766340

  5. “Groundsubstance” Resembling Amyloid Extracted from the Cervical Portion of Human Cervix Uteri

    PubMed Central

    Gröschel-Stewart, U.; Hermann, U.; Schwalm, H.

    1973-01-01

    A groundsubstance glycoprotein has been isolated from normal human cervix uteri that has a remarkable resemblance in its primary structure to a protein found in amyloid disease and to other acidic fibrous proteins found in mammalian tissue. Cervical groundsubstance, acidic fibrous protein from human uterus and the cardiac groundsubstance, which is significantly increased in amyloid disease, are immunologically identical or closely related. ImagesFigs. 1-4 PMID:4633712

  6. Gastrointestinal symptoms resembling ulcerative proctitis caused by larvae of the drone fly Eristalis tenax

    PubMed Central

    Desoubeaux, Guillaume; Gaillard, Julien; Borée-Moreau, Diane; Bailly, Éric; Andres, Christian R; Chandenier, Jacques

    2014-01-01

    We report a case of facultative intestinal myiasis due to larvae of the drone fly Eristalis tenax, also named the rat-tailed maggots. The development of larvae in the lower bowel was responsible for non-specific gastrointestinal symptoms that resembled ulcerative proctitis. The diagnosis was established upon the observation of four spontaneously excreted mobile larvae. The definite identification of the E. tenax species was made possible by scanning electron microscopy. The clinical outcome was satisfactory. PMID:24766340

  7. Enhanced efficacy and anti-biofilm activity of novel nanoemulsions against skin burn wound multi-drug resistant MRSA infections.

    PubMed

    Song, Zhen; Sun, Hongwu; Yang, Yun; Jing, Haiming; Yang, Liuyang; Tong, Yanan; Wei, Chao; Wang, Zelin; Zou, Quanming; Zeng, Hao

    2016-08-01

    Multi-drug resistant MRSA (methicillin-resistant Staphylococcus aureus) is a global problem for human health, especially skin burn wound patients. Therefore, we estimated the antibacterial and anti-biofilm activity of a chlorhexidine acetate nanoemulsion (CNE) by previously ourselves designed against skin burn wound MRSA infections. Compared with its water solution (CHX), CNE showed a better and faster action against MRSA both in vitro and in vivo. Importantly, CNE was more effective at inhibiting biofilm formation and clearing the biofilm. We also found that the cell walls and membranes of MRSA were severely disrupted after treatment with CNE. Moreover, the relative electrical conductivity and the leakage of alkaline phosphates, K(+), Mg(2+), DNA and protein obviously increased because the cell wall and membrane were damaged. These data show that novel CNE is a promising potential antimicrobial candidate, especially for skin burn wound MRSA infections.

  8. Nanomedicine-nanoemulsion formulation improves safety and efficacy of the anti-cancer drug paclitaxel according to preclinical assessment.

    PubMed

    Lee, King C; Maturo, Claudia; Rodriguez, Robert; Nguyen, Hoang-Lan; Shorr, Robert

    2011-08-01

    Paclitaxel is an important anticancer drug and is currently used to treat a variety of cancers, including ovarian carcinomas, breast cancer, non-small cell lung cancer, and AIDS-related Kaposi's sarcoma. The objectives of the studies were to assess and compare the safety and efficacy of EmPAC (a newly developed nanoemulsion formulation of paclitaxel) versus Taxol (the injectable formulation of paclitaxel involving the use of polyethylated or polyoxyl castor oil currently used in the clinic). The objectives were also to investigate the mechanism for the improved safety and efficacy of EmPAC over Taxol. These results showed that EmPAC had better anti-tumor efficacy than Taxol, according to in vitro cell culture studies and studies in animal tumor models. EmPAC had improved anti-tumor efficacy even in tumor cell lines that are known to be multi-drug resistant. Part of the mechanism of action for the improved efficacy may be related to EmPAC inducing greater cellular uptake of paclitaxel into tumor cells than Taxol did, according to the in vitro cell culture radioactive-labeled studies and in vitro cell culture antibody studies. It may also partly be because EmPAC delivered more paclitaxel to the tumor mass than Taxol, while the delivery of paclitaxel to other tissues (e.g., blood, muscle, liver, spleen, kidney and lung) were similar between the two formulations of paclitaxel, according to studies in animals with tumor xenograft. EmPAC also had better safety than Taxol according to toxicology studies in rabbits. This may be because EmPAC does not contain the toxic ingredients used in formulating Taxol (such as polyethylated or polyoxyl castor oil). These results support the clinical development of the nanoemulsion formulation of paclitaxel.

  9. Anticancer activity of an ultrasonic nanoemulsion formulation of Nigella sativa L. essential oil on human breast cancer cells.

    PubMed

    Periasamy, Vaiyapuri Subbarayan; Athinarayanan, Jegan; Alshatwi, Ali A

    2016-07-01

    Nigella sativa L. (NS) is a plant renowned in traditional holistic medicine systems for almost 1400 years because of its remarkable antioxidant, antimicrobial, anti-inflammatory and anti-cancer properties. The essential oil of N. sativa, in particular, possesses these significant biological properties. However, N. sativa essential oil has many insoluble constituents with properties that have not been fully explored. Nanoemulsion-based insoluble formulations are a widely used carrier system for lipophilic materials. In the present study, we used ultrasonic emulsification, polysorbate 80 and water to formulate a highly stable N. sativa essential oil nanoemulsion (NSEO-NE). To optimize the NSEO-NE preparation, we changed the surfactant concentration, the oil-surfactant mixing ratio and the emulsification time. The droplet size distribution and morphology of the prepared NE was analyzed using dynamic light scattering and scanning electron microscopy, respectively. The droplet size of the NSEO-NE was approximately 20-50 nm in diameter. The anticancer properties of the NE preparation were studied using a modified methyl-thiazolyl-diphenyl tetrazolium bromide (MTT) assay as well as cellular uptake and nuclear morphological analyses. The NSEO-NE significantly reduced the viability of Michigan Cancer Foundation-7 (MCF-7) breast cancer cells. The nucleo-cytoplasmic morphological features of NSEO-NE-treated cells included cell membrane blebbing, cytoplasmic vacuolation, marginalization of chromatin, and fragmentation of the nucleus. The results clearly indicate that NSEO-NE induced apoptosis in MCF-7 cells. These findings support the potential application of NSEO-NE in breast cancer therapy, and also merit future translational research. PMID:26964971

  10. Protective effect of a hydrogel containing Achyrocline satureioides extract-loaded nanoemulsion against UV-induced skin damage.

    PubMed

    Balestrin, L A; Bidone, J; Bortolin, R C; Moresco, K; Moreira, J C; Teixeira, H F

    2016-10-01

    Achyrocline satureioides is a medicinal plant widely used in South America that exhibits a well-documented antioxidant activity. Such activity has been related to their main aglycone flavonoids quercetin, luteolin, and 3-O-methylquercetin (3MQ). This study addresses the development of antioxidant hydrogels containing an A. satureioides extract-loaded nanoemulsions aimed at topical application. The systems investigated were A. satureioides extract-loaded nanoemulsions (ASNE) obtained by spontaneous emulsification procedure formulated in semisolid hydrogels composed of Carbopol® Ultrez 20 (HASNE). Hydrogels exhibit a non-Newtonian pseudoplastic behavior. A higher release of 3MQ from ASNE (3.61μg/cm(2)/h) was observed when compared with HASNE (2.83μg/cm(2)/h). Different parameters that may have an influence on the retention of flavonoids into the skin were investigated by using a Franz-type diffusion cells. Indeed, the amount of formulation applied on donor compartment was found to play a crucial role. At the optimized conditions, retention of approximately 2μg/cm(2) of flavonoids was detected into the skin. A higher retention of 3MQ was detected (approximately 1.0μg/cm(2)) in comparison with the other flavonoids. Finally, a protection the porcine ear skin by formulations, against oxidative stress generated by UVA/UVB light was demonstrated by means of TBARS, protein carbonylation, and protein thiol content assays. The overall results showed the potential of the formulations developed in this study for the prevention of oxidative stress on the skin. PMID:27599114

  11. Protective effect of a hydrogel containing Achyrocline satureioides extract-loaded nanoemulsion against UV-induced skin damage.

    PubMed

    Balestrin, L A; Bidone, J; Bortolin, R C; Moresco, K; Moreira, J C; Teixeira, H F

    2016-10-01

    Achyrocline satureioides is a medicinal plant widely used in South America that exhibits a well-documented antioxidant activity. Such activity has been related to their main aglycone flavonoids quercetin, luteolin, and 3-O-methylquercetin (3MQ). This study addresses the development of antioxidant hydrogels containing an A. satureioides extract-loaded nanoemulsions aimed at topical application. The systems investigated were A. satureioides extract-loaded nanoemulsions (ASNE) obtained by spontaneous emulsification procedure formulated in semisolid hydrogels composed of Carbopol® Ultrez 20 (HASNE). Hydrogels exhibit a non-Newtonian pseudoplastic behavior. A higher release of 3MQ from ASNE (3.61μg/cm(2)/h) was observed when compared with HASNE (2.83μg/cm(2)/h). Different parameters that may have an influence on the retention of flavonoids into the skin were investigated by using a Franz-type diffusion cells. Indeed, the amount of formulation applied on donor compartment was found to play a crucial role. At the optimized conditions, retention of approximately 2μg/cm(2) of flavonoids was detected into the skin. A higher retention of 3MQ was detected (approximately 1.0μg/cm(2)) in comparison with the other flavonoids. Finally, a protection the porcine ear skin by formulations, against oxidative stress generated by UVA/UVB light was demonstrated by means of TBARS, protein carbonylation, and protein thiol content assays. The overall results showed the potential of the formulations developed in this study for the prevention of oxidative stress on the skin.

  12. Disorders of Lipid Metabolism

    MedlinePlus

    ... Metabolic Disorders Disorders of Carbohydrate Metabolism Disorders of Amino Acid Metabolism Disorders of Lipid Metabolism Fats (lipids) are ... carbohydrates and low in fats. Supplements of the amino acid carnitine may be helpful. The long-term outcome ...

  13. Irinotecan Lipid Complex Injection

    MedlinePlus

    Irinotecan lipid complex is used in combination with other medications to treat pancreatic cancer that has spread to other parts of ... after treatment with other chemotherapy medications. Irinotecan lipid complex is in a class of antineoplastic medications called ...

  14. Vincristine Lipid Complex Injection

    MedlinePlus

    Vincristine lipid complex is used to treat a certain type of acute lymphoblastic leukemia (ALL; a type of cancer of the ... two different treatments with other medications. Vincristine lipid complex is in a class of medications called vinca ...

  15. Daunorubicin Lipid Complex Injection

    MedlinePlus

    Daunorubicin lipid complex is used to treat advanced Kaposi's sarcoma (a type of cancer that causes abnormal tissue to grow on ... related to acquired immunodeficiency syndrome (AIDS). Daunorubicin lipid complex is in a class of medications called anthracyclines. ...

  16. Cytarabine Lipid Complex Injection

    MedlinePlus

    Cytarabine lipid complex is used to treat lymphomatous meningitis (a type of cancer in the covering of the spinal cord and brain). Cytarabine lipid complex is in a class of medications called antimetabolites. ...

  17. Doxorubicin Lipid Complex Injection

    MedlinePlus

    Doxorubicin lipid complex is used to treat ovarian cancer that has not improved or that has worsened after treatment with other medications. Doxorubicin lipid complex is also used to treat Kaposi's sarcoma (a ...

  18. Lutein and zeaxanthin: Role as macular pigment and factors that control bioavailability from egg yolks and nanoemulsions

    NASA Astrophysics Data System (ADS)

    Vishwanathan, Rohini

    ) raising serum HDL-C without an adverse affect on serum LDL-C and TC:HDL-C ratio. Increased cholesterol, lutein and zeaxanthin intake from the 2 and 4 egg yolk interventions did not decrease the absorption of other carotenoids, such as alpha-cryptoxanthin, beta-cryptoxanthin, lycopene, alpha-carotene and beta-carotene, tocopherols and retinol from the diet. An unexpected increase was observed in serum alpha-cryptoxanthin and gamma-tocopherol concentrations during the 4 egg yolk phase, these carotenoids are normally present in low concentrations in serum. Lipoprotein distribution of carotenoids and tocopherols was also not affected by the increased egg consumption. In the pursuit of designing a highly bioavailable matrix for lutein/zeaxanthin, similar to the egg yolk micellar matrix, nanoemulsion formulations of lutein were developed using the MicrofluidizerRTM Processor technology. Lutein nanoemulsions are O/W emulsions of lutein which have particle sizes in the nanometer range (≤ 200 nm). Lutein consumed orally as a nanoemulsion was shown to have significantly greater bioavailability than lutein supplement-pills in pilot-scale clinical studies described here. However, lutein nanoemulsions did not raise plasma lutein concentrations to the same extent as egg yolks in a study performed on BALB/c mice. Formation of mixed micelles in the intestinal lumen during digestion and uptake of these micelles by enterocytes are crucial steps that dictate bioavailability i.e. the proportion of ingested lutein/carotenoid that enters the blood circulation and accumulates in the peripheral tissues such as the macula. In-vitro stomach and intestinal digestion experiments showed lutein nanoemulsions have significantly greater micellarization efficiency compared to egg yolks. Nanoemulsions with a phospholipid (PL) emulsifier containing 80% phosphatidyl choline (PC) or Polysorbate 80 as the emulsifier had better ability to form micelles during the intestinal digestion phase compared to a PL

  19. Feasibility of lipid nanoparticles for ocular delivery of anti-inflammatory drugs.

    PubMed

    Souto, Eliana B; Doktorovova, Slavomira; Gonzalez-Mira, Elisabet; Egea, Maria Antonia; Garcia, Maria Luisa

    2010-07-01

    Due to the multiple barriers imposed by the eye against the penetration of drugs, the ocular delivery and targeting are considered difficult to achieve. A major challenge in ocular drug therapy is to improve the poor bioavailability of topically applied ophthalmic drugs by overcoming the severe constraints imposed by the eye on drug absorption. One of the promising strategies nowadays is the use of colloidal carrier systems characterized by a submicron-meter size. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) represent promising alternatives to conventional and very popular ocular carrier systems, such as the nanoemulsions, liposomes, and polymeric nanoparticles. Nevertheless, taking into account the characteristics of the eye, morphometrical properties of the colloidal systems (e.g., average particle size and polydispersion) may represent a limiting factor for topical application without induced corneal irritation, being responsible for the selected system. This review article focuses on the application of lipid nanoparticles (SLN, NLC) as carriers for both non-steroidal and steroidal anti-inflammatory drugs for the treatment of ocular inflammatory disorders. Major benefits, as well as shortcomings, of ocular inflammation conditions are described, in particular upon management of inflammation induced by ocular surgery (e.g., cataracts, refractive surgery). Particular emphasis is given to the clinical choices currently available, while examining the most recent drugs that have been approved. PMID:20597640

  20. Studies on the formation of polymeric nano-emulsions obtained via low-energy emulsification and their use as templates for drug delivery nanoparticle dispersions.

    PubMed

    Calderó, G; Montes, R; Llinàs, M; García-Celma, M J; Porras, M; Solans, C

    2016-09-01

    Ethylcellulose nanoparticles have been obtained from O/W nano-emulsions of the water/polyoxyethylene 10 oleyl ether/[ethyl acetate+4wt% ethylcellulose] system by low energy-energy emulsification at 25°C. Nano-emulsions with droplet sizes below 200nm and high kinetic stability were chosen for solubilising dexamethasone (DXM). Phase behaviour, conductivity and optical analysis studies of the system have evidenced for the first time that both, the polymer and the drug play a role on the structure of the aggregates formed along the emulsification path. Nano-emulsion formation may take place by both, phase inversion and self-emulsification. Spherical polymeric nanoparticles containing surfactant, showing sizes below 160nm have been obtained from the nano-emulsions by organic solvent evaporation. DXM loading in the nanoparticles was high (>90%). The release kinetics of nanoparticle dispersions with similar particle size and encapsulated DXM but different polymer to surfactant ratio were studied and compared to an aqueous DXM solution. Drug release from the nanoparticle dispersions was slower than from the aqueous solution. While the DXM solution showed a Fickian release pattern, the release behaviour from the nanoparticle dispersions was faster than that expected from a pure Fickian release. A coupled diffusion/relaxation model fitted the results very well, suggesting that polymer chains undergo conformational changes enhancing drug release. The contribution of diffusion and relaxation to drug transport in the nanoparticle dispersions depended on their composition and release time. Surfactant micelles present in the nanoparticle dispersion may exert a mild reservoir effect. The small particle size and the prolonged DXM release provided by the ethylcellulose nanoparticle dispersions make them suitable vehicles for controlled drug delivery applications.

  1. Studies on the formation of polymeric nano-emulsions obtained via low-energy emulsification and their use as templates for drug delivery nanoparticle dispersions.

    PubMed

    Calderó, G; Montes, R; Llinàs, M; García-Celma, M J; Porras, M; Solans, C

    2016-09-01

    Ethylcellulose nanoparticles have been obtained from O/W nano-emulsions of the water/polyoxyethylene 10 oleyl ether/[ethyl acetate+4wt% ethylcellulose] system by low energy-energy emulsification at 25°C. Nano-emulsions with droplet sizes below 200nm and high kinetic stability were chosen for solubilising dexamethasone (DXM). Phase behaviour, conductivity and optical analysis studies of the system have evidenced for the first time that both, the polymer and the drug play a role on the structure of the aggregates formed along the emulsification path. Nano-emulsion formation may take place by both, phase inversion and self-emulsification. Spherical polymeric nanoparticles containing surfactant, showing sizes below 160nm have been obtained from the nano-emulsions by organic solvent evaporation. DXM loading in the nanoparticles was high (>90%). The release kinetics of nanoparticle dispersions with similar particle size and encapsulated DXM but different polymer to surfactant ratio were studied and compared to an aqueous DXM solution. Drug release from the nanoparticle dispersions was slower than from the aqueous solution. While the DXM solution showed a Fickian release pattern, the release behaviour from the nanoparticle dispersions was faster than that expected from a pure Fickian release. A coupled diffusion/relaxation model fitted the results very well, suggesting that polymer chains undergo conformational changes enhancing drug release. The contribution of diffusion and relaxation to drug transport in the nanoparticle dispersions depended on their composition and release time. Surfactant micelles present in the nanoparticle dispersion may exert a mild reservoir effect. The small particle size and the prolonged DXM release provided by the ethylcellulose nanoparticle dispersions make them suitable vehicles for controlled drug delivery applications. PMID:27341306

  2. Resembling a viper: implications of mimicry for conservation of the endangered smooth snake.

    PubMed

    Valkonen, Janne K; Mappes, Johanna

    2014-12-01

    The phenomenon of Batesian mimicry, where a palatable animal gains protection against predation by resembling an unpalatable model, has been a core interest of evolutionary biologists for 150 years. An extensive range of studies has focused on revealing mechanistic aspects of mimicry (shared education and generalization of predators) and the evolutionary dynamics of mimicry systems (co-operation vs. conflict) and revealed that protective mimicry is widespread and is important for individual fitness. However, according to our knowledge, there are no case studies where mimicry theories have been applied to conservation of mimetic species. Theoretically, mimicry affects, for example, frequency dependency of predator avoidance learning and human induced mortality. We examined the case of the protected, endangered, nonvenomous smooth snake (Coronella austriaca) that mimics the nonprotected venomous adder (Vipera berus), both of which occur in the Åland archipelago, Finland. To quantify the added predation risk on smooth snakes caused by the rarity of vipers, we calculated risk estimates from experimental data. Resemblance of vipers enhances survival of smooth snakes against bird predation because many predators avoid touching venomous vipers. Mimetic resemblance is however disadvantageous against human predators, who kill venomous vipers and accidentally kill endangered, protected smooth snakes. We found that the effective population size of the adders in Åland is very low relative to its smooth snake mimic (28.93 and 41.35, respectively).Because Batesian mimicry is advantageous for the mimic only if model species exist in sufficiently high numbers, it is likely that the conservation program for smooth snakes will fail if adders continue to be destroyed. Understanding the population consequences of mimetic species may be crucial to the success of endangered species conservation. We suggest that when a Batesian mimic requires protection, conservation planners should

  3. Spectral transformation of the unusual variable star MWC560 to resemble a nova

    NASA Technical Reports Server (NTRS)

    Maran, Stephen P.; Michalitsianos, Andrew G.; Oliversen, Ronald J.; Sonneborn, George

    1991-01-01

    A dramatic change has occurred in the ultraviolet spectrum of the emission-line star MWC560, so that it now closely resembles the spectrum of a nova shortly after outburst. This event may signal a major mass-ejection episode such as presumably occurred in past centuries in the symbiotic star R Aquarii to produce the well-known bipolar nebula, and it may herald the emergence of a standard symbiotic-star emission-line spectrum in MWC560, corresponding to a change in evolutionary state.

  4. Villous Tumor of the Urinary Bladder Resembling Low-grade Mucinous Neoplasm of the Appendix.

    PubMed

    Ito, Ayako; Sakura, Yuma; Sugimoto, Mikio; Kakehi, Yoshiyuki; Kuroda, Naoto

    2016-05-01

    Mucinous neoplasms of the urinary tract are very rare. We present a 63-year-old-women who had a sessile papillary villous tumor in urinary bladder. Although transurethral resection of the bladder tumor (TURBT) was performed, the villous tumor repetitively recurred and gradually spread to the entire surface of bladder lumen. Histopathologic and immunohistochemical examination showed that the lesion was very similar to low-grade mucinous neoplasm arising in appendix vermiformis. There are no reports on appendiceal metaplasia of urinary bladder mucosa. In this case, we describe this unprecedented neoplasm as "villous tumor of the urinary bladder resembling low-grade mucinous neoplasm of the appendix."

  5. Charge on luminous bodies resembling natural ball lightning produced via electrical arcs through lump silicon

    NASA Astrophysics Data System (ADS)

    Porter, Christina L.; Miley, Galen P.; Griffiths, David J.; Sánchez, Erik

    2014-12-01

    A phenomenon resembling natural ball lightning can be produced via electrical arcing through silicon. We use lump silicon instead of silicon wafers to achieve higher production rates and larger, longer-lived luminous balls than previously reported. The luminous balls consist of a silicon core surrounded by a porous network of loosely bound silicon dioxide nanoparticles. We find that the balls carry a small net charge on the order of 10-12 C and propose that the nanoparticles are electrostatically bound to the core due to this charge.

  6. Multibubble sonoluminescence spectra of water which resemble single-bubble sonoluminescence

    PubMed

    Didenko; Gordeychuk

    2000-06-12

    Multibubble sonoluminescence (MBSL) spectra of water from cavitation clouds were collected in the presence of different noble gases and at different acoustic intensities. Results show that at high acoustic intensity and with xenon as a dissolved gas the emission of the OH* radical becomes indiscernible from the continuum. These spectra resemble single-bubble sonoluminescence (SBSL) spectra. It is concluded that the source of emission in MBSL and SBSL can be the same, the difference in spectra is due to the higher temperature inside the bubble during SBSL.

  7. An unusual neurological disorder of copper metabolism clinically resembling Wilson's disease but biochemically a distinct entity.

    PubMed

    Godwin-Austen, R B; Robinson, A; Evans, K; Lascelles, P T

    1978-11-01

    A patient with progressive neurological disease resembling Wilson's disease but in whom Kayser-Fleischer rings were absent, was given 67Cu and 64Cu, orally and intravenously, to measure the rate of absorption of copper using a convolution integral. The data show an abnormal distribution of body copper resulting in low copper concentrations in plasma, urine and liver but with an accumulation in the lower bowel probably due to a defect in mucosal transport. The importance of differentiating this condition from Wilson's disease is stressed.

  8. Charge on luminous bodies resembling natural ball lightning produced via electrical arcs through lump silicon.

    PubMed

    Porter, Christina L; Miley, Galen P; Griffiths, David J; Sánchez, Erik

    2014-12-01

    A phenomenon resembling natural ball lightning can be produced via electrical arcing through silicon. We use lump silicon instead of silicon wafers to achieve higher production rates and larger, longer-lived luminous balls than previously reported. The luminous balls consist of a silicon core surrounded by a porous network of loosely bound silicon dioxide nanoparticles. We find that the balls carry a small net charge on the order of 10(-12) C and propose that the nanoparticles are electrostatically bound to the core due to this charge. PMID:25615201

  9. Early and prolonged ECG alterations resembling a myocardial injury after severe amitriptyline poisoning.

    PubMed

    Berlot, G; Vergolini, A; Calderan, C

    2010-01-01

    Evidence of cardiovascular toxicity is present in the majority of tricyclic antidepressant overdoses. We report the case of a 63-year-old woman admitted to our department with a severe amitriptyline poisoning. The ECG at admission showed a pattern mimicking an acute anteroseptal subepicardial infarction. This pattern persisted for 11 days. Myocardial enzymes and echocardiographic findings never confirmed an ischemic event. At discharge, the ECG returned normal without cardiac or neurologic sequelae. Our experience suggest that after severe tricyclic antidepressant ingestion, ECG alterations resembling myocardial injury may occur early and last for a longer period than previously reported.

  10. A case of secondary syphilis with HIV, resembling borderline lepromatous leprosy

    PubMed Central

    Mani, Mohan Zachariah; Kanish, Bimal; Kwatra, Kanwardeep; Chaudhary, Paulina R.; Bhatia, Anuradha

    2015-01-01

    We are reporting an unusual case of secondary syphilis, in a homosexual male patient, which resembled borderline lepromatous leprosy, and in whom the diagnosis was considered on clinical grounds. The patient also had concomitant HIV infection, with asymptomatic neurosyphilis. His rapid plasma reagin test was reactive in 1:128 dilution. He improved with three standard, weekly injections of benzathine penicillin, along with 2 g of intravenous ceftriaxone daily for 15 days. This case is being reported to highlight the need for a high index of suspicion in diagnosing unusual cases of secondary syphilis, especially in those with concomitant HIV infection. PMID:26692613

  11. A case of secondary syphilis with HIV, resembling borderline lepromatous leprosy.

    PubMed

    Mani, Mohan Zachariah; Kanish, Bimal; Kwatra, Kanwardeep; Chaudhary, Paulina R; Bhatia, Anuradha

    2015-01-01

    We are reporting an unusual case of secondary syphilis, in a homosexual male patient, which resembled borderline lepromatous leprosy, and in whom the diagnosis was considered on clinical grounds. The patient also had concomitant HIV infection, with asymptomatic neurosyphilis. His rapid plasma reagin test was reactive in 1:128 dilution. He improved with three standard, weekly injections of benzathine penicillin, along with 2 g of intravenous ceftriaxone daily for 15 days. This case is being reported to highlight the need for a high index of suspicion in diagnosing unusual cases of secondary syphilis, especially in those with concomitant HIV infection. PMID:26692613

  12. A Drosophila gene encoding a protein resembling the human. beta. -amyloid protein precursor

    SciTech Connect

    Rosen, D.R.; Martin-Morris, L.; Luo, L.; White, K. )

    1989-04-01

    The authors have isolated genomic and cDNA clones for a Drosophila gene resembling the human {beta}-amyloid precursor protein (APP). This gene produces a nervous system-enriched 6.5-kilobase transcript. Sequencing of cDNAs derived from the 6.5-kilobase transcript predicts an 886-amino acid polypeptide. This polypeptide contains a putative transmembrane domain and exhibits strong sequence similarity to cytoplasmic and extracellular regions of the human {beta}-amyloid precursor protein. There is a high probability that this Drosophila gene corresponds to the essential Drosophila locus vnd, a gene required for embryonic nervous system development.

  13. Vaccinia Virus N1l Protein Resembles a B Cell Lymphoma-2 (Bcl-2) Family Protein

    SciTech Connect

    Aoyagi, M.; Zhai, D.; Jin, C.; Aleshin, A.E.; Stec, B.; Reed, J.C.; Liddington, R.C.; /Burnham Inst.

    2007-07-03

    Poxviruses encode immuno-modulatory proteins capable of subverting host defenses. The poxvirus vaccinia expresses a small 14-kDa protein, N1L, that is critical for virulence. We report the crystal structure of N1L, which reveals an unexpected but striking resemblance to host apoptotic regulators of the B cell lymphoma-2 (Bcl-2) family. Although N1L lacks detectable Bcl-2 homology (BH) motifs at the sequence level, we show that N1L binds with high affinity to the BH3 peptides of pro-apoptotic Bcl-2 family proteins in vitro, consistent with a role for N1L in modulating host antiviral defenses.

  14. Charge on luminous bodies resembling natural ball lightning produced via electrical arcs through lump silicon.

    PubMed

    Porter, Christina L; Miley, Galen P; Griffiths, David J; Sánchez, Erik

    2014-12-01

    A phenomenon resembling natural ball lightning can be produced via electrical arcing through silicon. We use lump silicon instead of silicon wafers to achieve higher production rates and larger, longer-lived luminous balls than previously reported. The luminous balls consist of a silicon core surrounded by a porous network of loosely bound silicon dioxide nanoparticles. We find that the balls carry a small net charge on the order of 10(-12) C and propose that the nanoparticles are electrostatically bound to the core due to this charge.

  15. Effectiveness of a spontaneous carvacrol nanoemulsion against Salmonella enterica Enteritidis and Escherichia coli O157:H7 on contaminated broccoli and radish seeds.

    PubMed

    Landry, Kyle S; Micheli, Sean; McClements, David Julian; McLandsborough, Lynne

    2015-10-01

    The incidence of foodborne illness associated with the consumption of fresh produce has continued to increase over the past decade. Sprouts, such as mung bean, alfalfa, radish, and broccoli, are minimally processed and have been sources for foodborne illness. Currently, a 20,000 ppm calcium hypochlorite soak is recommended for the treatment of sprouting seeds. In this study, the efficacy of an antimicrobial carvacrol nanoemulsion was tested against Salmonella enterica subspecies enterica serovar Enteritidis (ATCC BAA-1045) or EGFP expressing Escherichia coli O157:H7 (ATCC 42895) contaminated sprouting seeds. Antimicrobial treatments were performed by soaking inoculated seeds in nanoemulsions (4000 or 8000 ppm) for 30 or 60 min. Following treatment, surviving cells were determined by performing plate counts and/or Most Probable Number (MPN) enumeration. Treated seeds were sprouted and tested for the presence of pathogens. Treatment successfully inactivated low levels (2 and 3 log CFU/g) of S. Enteritidis and E. coli on radish seeds when soaked for 60 min at concentrations ≥4000 (0.4%) ppm carvacrol. This treatment method was not affective on contaminated broccoli seeds. Total sprout yield was not influenced by any treatments. These results show that carvacrol nanoemulsions may be an alternative treatment method for contaminated radish seeds. PMID:26187822

  16. Herbal infusions of black seed and wheat germ oil: Their chemical profiles, in vitro bio-investigations and effective formulations as Phyto-Nanoemulsions.

    PubMed

    Gumus, Z Pinar; Guler, Emine; Demir, Bilal; Barlas, F Baris; Yavuz, Murat; Colpankan, Dilara; Senisik, A Murat; Teksoz, Serap; Unak, Perihan; Coskunol, Hakan; Timur, Suna

    2015-09-01

    The reported studies related to black seed oil (BSO) and wheat germ oil (WGO) have illustrated that they have a wide range of biological activities. Therefore, enhancing the amount of bio-active compounds that caused higher cell based anti-oxidative effect as well as cell proliferation, etc. in seed oils, infusion of crude plant material has been gained importance as a traditional technique. Herein, we accomplished the infusion of Calendula flowers that also contains many phyto-constituents into BSO and WGO. After the infusion of oils, the change of phytochemical amount was investigated and evaluated according to the oils by chromatography, radical scavenging activity. Subsequently, for investigating the biological impact upon live cells, cytotoxicity, cell-based antioxidant capacity, wound healing and radioprotective activity were tested with monkey kidney fibroblast like cells (Vero) and HaCaT keratinocytes. In vitro cell based experiments (wound healing and radioprotective activity) confirmed that Calendula infused BSO and WGO have greater bio-activity when compared to those plain forms. The herbal oils prepared with an effective extraction technique were incorporated into nanoemulsion systems which will be then called as 'Phyto-Nanoemulsion'. After herbal oil biomolecules were encapsulated into nanoemulsion based delivery systems, the designed formulations were investigated in terms of biological activities. In conclusion, these preparations could be a good candidate as a part of dermal cosmetic products or food supplements which have the therapeutic efficiency, especially after radio- or chemotherapy. PMID:26087391

  17. Effectiveness of a spontaneous carvacrol nanoemulsion against Salmonella enterica Enteritidis and Escherichia coli O157:H7 on contaminated broccoli and radish seeds.

    PubMed

    Landry, Kyle S; Micheli, Sean; McClements, David Julian; McLandsborough, Lynne

    2015-10-01

    The incidence of foodborne illness associated with the consumption of fresh produce has continued to increase over the past decade. Sprouts, such as mung bean, alfalfa, radish, and broccoli, are minimally processed and have been sources for foodborne illness. Currently, a 20,000 ppm calcium hypochlorite soak is recommended for the treatment of sprouting seeds. In this study, the efficacy of an antimicrobial carvacrol nanoemulsion was tested against Salmonella enterica subspecies enterica serovar Enteritidis (ATCC BAA-1045) or EGFP expressing Escherichia coli O157:H7 (ATCC 42895) contaminated sprouting seeds. Antimicrobial treatments were performed by soaking inoculated seeds in nanoemulsions (4000 or 8000 ppm) for 30 or 60 min. Following treatment, surviving cells were determined by performing plate counts and/or Most Probable Number (MPN) enumeration. Treated seeds were sprouted and tested for the presence of pathogens. Treatment successfully inactivated low levels (2 and 3 log CFU/g) of S. Enteritidis and E. coli on radish seeds when soaked for 60 min at concentrations ≥4000 (0.4%) ppm carvacrol. This treatment method was not affective on contaminated broccoli seeds. Total sprout yield was not influenced by any treatments. These results show that carvacrol nanoemulsions may be an alternative treatment method for contaminated radish seeds.

  18. Lipid Vesicle-mediated Affinity Chromatography using Magnetic Activated Cell Sorting (LIMACS): a Novel Method to Analyze Protein-lipid Interaction

    PubMed Central

    Bieberich, Erhard

    2011-01-01

    The analysis of lipid protein interaction is difficult because lipids are embedded in cell membranes and therefore, inaccessible to most purification procedures. As an alternative, lipids can be coated on flat surfaces as used for lipid ELISA and Plasmon resonance spectroscopy. However, surface coating lipids do not form microdomain structures, which may be important for the lipid binding properties. Further, these methods do not allow for the purification of larger amounts of proteins binding to their target lipids. To overcome these limitations of testing lipid protein interaction and to purify lipid binding proteins we developed a novel method termed lipid vesicle-mediated affinity chromatography using magnetic-activated cell sorting (LIMACS). In this method, lipid vesicles are prepared with the target lipid and phosphatidylserine as the anchor lipid for Annexin V MACS. Phosphatidylserine is a ubiquitous cell membrane phospholipid that shows high affinity to the protein Annexin V. Using magnetic beads conjugated to Annexin V the phosphatidylserine-containing lipid vesicles will bind to the magnetic beads. When the lipid vesicles are incubated with a cell lysate the protein binding to the target lipid will also be bound to the beads and can be co-purified using MACS. This method can also be used to test if recombinant proteins reconstitute a protein complex binding to the target lipid. We have used this method to show the interaction of atypical PKC (aPKC) with the sphingolipid ceramide and to co-purify prostate apoptosis response 4 (PAR-4), a protein binding to ceramide-associated aPKC. We have also used this method for the reconstitution of a ceramide-associated complex of recombinant aPKC with the cell polarity-related proteins Par6 and Cdc42. Since lipid vesicles can be prepared with a variety of sphingo- or phospholipids, LIMACS offers a versatile test for lipid-protein interaction in a lipid environment that resembles closely that of the cell membrane

  19. SMALL CYSTEINE-RICH PEPTIDES RESEMBLING ANTIMICROBIAL PEPTIDES HAVE BEEN UNDER-PREDICTED IN PLANTS

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Multicellular organisms produce small cysteine-rich anti-microbial peptides as an innate defense against pathogens. While defensins, a well-known class of such peptides, are common among eukaryotes, there are classes restricted to the plant kingdom. These include thionins, lipid transfer proteins,...

  20. Nutrients and neurodevelopment: lipids.

    PubMed

    González, Horacio F; Visentin, Silvana

    2016-10-01

    Nutrients, lipids in particular, make up the central nervous system structure and play major functional roles: they stimulate development, migration, and nerve cell differentiation. They are part of gray matter, white matter, nerve nuclei, and synaptogenesis. Breast milk contains lipids which are crucial for infant brain development. The lipid profile of breast milk was used as a guideline for the development of breast milk substitutes. However, to date, no substitute has matched it. Complementary feeding should include docosahexaenoic acid, arachidonic acid, other polyunsaturated fatty acids, saturated fatty acids, and complex lipids found in milk fat. The lipid composition of breast milk depends on maternal intake and nutritional status during pregnancy and breast-feeding. It has a great impact on development. Our goal is to review scientific literature regarding the role of lipids on infant brain development and the importance of breast milk lipid composition, maternal diet, and complementary feeding. PMID:27606648

  1. Nutrients and neurodevelopment: lipids.

    PubMed

    González, Horacio F; Visentin, Silvana

    2016-10-01

    Nutrients, lipids in particular, make up the central nervous system structure and play major functional roles: they stimulate development, migration, and nerve cell differentiation. They are part of gray matter, white matter, nerve nuclei, and synaptogenesis. Breast milk contains lipids which are crucial for infant brain development. The lipid profile of breast milk was used as a guideline for the development of breast milk substitutes. However, to date, no substitute has matched it. Complementary feeding should include docosahexaenoic acid, arachidonic acid, other polyunsaturated fatty acids, saturated fatty acids, and complex lipids found in milk fat. The lipid composition of breast milk depends on maternal intake and nutritional status during pregnancy and breast-feeding. It has a great impact on development. Our goal is to review scientific literature regarding the role of lipids on infant brain development and the importance of breast milk lipid composition, maternal diet, and complementary feeding.

  2. Like father, like son: young children's understanding of how and why offspring resemble their parents.

    PubMed

    Solomon, G E; Johnson, S C; Zaitchik, D; Carey, S

    1996-02-01

    4 studies investigated the broad claim that preschoolers understand biological inheritance. In Study 1, 4-7-year-old children were told a story in which a boy was born to one man and adopted by another. The biological father was described as having one set of features (e.g., green eyes) and the adoptive father as having another (e.g., brown eyes). Subjects were asked which man the boy would resemble when he grew up. Preschoolers showed little understanding that selective chains of processes mediate resemblance to parents. It was not until age 7 that children substantially associated the boy with his biological father on physical features and his adoptive father on beliefs. That is, it was not until age 7 that children demonstrated that they understood birth as part of a process selectively mediating the acquisition of physical traits and learning or nurturance as mediating the acquisition of beliefs. In Study 2, subjects were asked whether, as a boy grew up, various of his features could change. Children generally shared our adult intuitions, indicating that their failure in Study 1 was not due to their having a different sense of what features can change. Studies 3 and 4 replicated Study 1, with stories involving mothers instead of fathers and with lessened task demands. Taken together, the results of the 4 studies refute the claim that preschooler