• Food Engineering Progress
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• v.21 no.3
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• pp.215-224
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• 2017

Resveratrol was incorporated into various combinations of single- and double-layer nanoemulsions, prepared by self-assembly emulsification and complex coacervation with chitosan, alginate, and ${\beta}$-cyclodextrin, respectively. Resveratrol nanoemulsions were composed of medium-chain trigacylglycerols (MCTs), $Tween^{(R)}$ 80, water, chitosan, alginate, and ${\beta}$-cyclodextrin. The corresponding mixtures were formulated for the purpose of being used as a nutraceutical delivery system. Resveratrol nanoemulsions were obtained with particle sizes of 10-800 nm, with the size variation dependent on the emulsification parameters including the ratio of aqueous phase and surfactant ratio. Resveratrol nanoemulsions were characterized by evaluating particle size, zeta-potential value, stability, and release rate. There were no significant changes in particle size and zeta-potential value of resveratrol nanoemulsions during storage for 28 days at $25^{\circ}C$. The stability of resveratrol in the double-layer nanoemulsions complexed with chitosan or ${\beta}$-cyclodextrin was higher, compared with the single-layer nanoemulsions.

• Biomolecules & Therapeutics
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• v.21 no.2
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• pp.173-179
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• 2013

Objective of present study was to prepare and characterize self-nanoemulsifying drug delivery system (SNEDDS) of lutein and to evaluate its effect on bioavailability of warfarin. The SNEDDS was prepared using an oil, a surfactant, and co-surfactants with optimal composition based on pseudo-ternary phase diagram. Effect of the SNEDDS on the bioavailability of warfarin was performed using Sprague Dawley rats. Lutein was successfully formulated as SNEDDS for immediate self-emulsification and dissolution by using combination of Peceol as oil, Labrasol as surfactant, and Transcutol-HP or Lutrol-E400 as co-surfactant. Almost complete dissolution was achieved after 15 min while lutein was not detectable from the lutein powder or intra-capsule content of a commercial formulation. SNEDDS formulation of lutein affected bioavailability of warfarin, showing about 10% increase in $C_{max}$ and AUC of the drug in rats while lutein as non-SNEDDS did not alter these parameters. Although exact mechanism is not yet elucidated, it appears that surfactant and co-surfactant used for SNEDDS formulation caused disturbance in the anatomy of small intestinal microvilli, leading to permeability change of the mucosal membrane. Based on this finding, it is suggested that drugs with narrow therapeutic range such as warfarin be administered with caution to avoid undesirable drug interaction due to large amount of surfactants contained in SNEDDS.

• Food Science and Biotechnology
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• v.18 no.5
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• pp.1161-1172
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• 2009

Food nanoemulsion systems consisting of water and oleoresin capsicum (OC), polyoxythylene sorbitan esters (Tween 20, 40, 60, and 80), propylene glycol (PG), sucrose monostearate (SM), and their corresponding mixtures were formulated to use as food vehicles. Tween 80 produced OC nanoemulsions with stable dispersions as one-phase systems, and the dertermined emulsification efficiencies clearly distinguished the ability of the various surfactants to emulsify OC. The nanoemulsions were prepared by both ultrasonication and self-assembly, and the nanoemulsion areas were determined using phase diagrams by measuring the sizes of the emulsions. One-phase nanoemulsions were presented, with a multiple cloudy region and phase separation that were dependent on the particle size of the emulsion. The OC nanoemulsions prepared by ultrasonication using systems of OC/Tween 80/water, OC/Tween 80/water+PG, and OC/Tween 80/water+SM, resulted in particle sizes ranging from 15 to 100 nm. Finally, the nanoemulsions maintained their initial sizes during storage, ranging from 65 to 92 nm.

• Journal of Pharmaceutical Investigation
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• v.37 no.6
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• pp.339-347
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• 2007

SMEDDS is mixture of oils, surfactants, and cosurfactants, which are emulsified in aqueous media under conditions of gentle agitation and digestive motility that would be encountered in the gastro-intestinal(GI) tract. The main purpose of this work is to prepare self-microemulsifying drug delivery system(SMEDDS) for oral bioavailability enhancement of a poorly water soluble drug, atorvastatin calcium. Solubility of atorvastatin calcium was determined in various vehicles. Pseudo-ternary phase diagrams were constructed to identity the efficient self-emulsification region and particle size distributions of the resultant micro emulsions were determined using a laser diffraction sizer. Optimized formulations for in vitro dissolution and bioavailability assessment were $Capryol^{(R)}$ 90(50%), Tetraglycol(16%), and $Cremophor^{(R)}$ EL(32%). The release rate of atorvastatin from SMEDDS was significantly higher than the conventional tablet ($Lipitor^{(R)}$), 2-fold. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin calcium by the oral route.

• Journal of Pharmaceutical Investigation
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• v.32 no.4
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• pp.267-275
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• 2002

A self-microemulsifying drug delivery system (SMEDDS) was developed to increase the dissolution rate, solubility, and ultimately bioavailability of a poorly water soluble drug, lovastatin. SMEDDS was thε mixtures of oils, surfactants, and cosurfactants, which emulsify under conditions of gentle agitation, similar to those which would be encountered in the gastro-intestinal (GI) tract. Various types of self-emulsifying formulations were prepared using four types of oil (Capryol 90, Lauroglycol 90, Labrafil M 1944 CS and Labrafil M 2125), two surfactants (Cremophor EL and Tween 80), and three cosurfactants (Carbitol, PEG 400 and propylene glycol). Thε efficiency of emulsification was studied using a laser diffraction size analyzer to determine particle size distributions of the resultant emulsions. Optimized formulations selected for bioavailability assessment were Carpryol 90 (40%), Cremophor EL (30%) and Carbitol (30%). SMEDDS containing lovastatin (20 mg and 5 mg) were compared to a conventional lovastatin tablet $(Mevacor^{\circledR},\;20\;mg/tab)$ by the oral administration as prefilled hard gelatin capsules to fasted beagle dogs for in vivo study. The arεa under the serum concentration-time curve from time zero to the last measured time in serum, $AUC_{0{\rightarrow}24h}$, was significantly greater in SMEDDS, suggesting that bioavailability increase 130% and 192% by the SMEDDS, respectively. The self-emulsifying formulations of lovastatin afforded the improvement in absolute oral bioavailability relative to previous data of lovastatin tablet formulation. These data indicate the utility of dispersed self-emulsifying formulations for the oral delivery of lovastatin and potentially other poorly absorbed drugs.

• Journal of the Korean Chemical Society
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• v.50 no.6
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• pp.464-470
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• 2006

the coricosteroid drug dexamethasone is an efficacious antiinflammatory drug, it is difficult to formulate in an injectable formulation due to its poor aqueous solubility. A lipid-based nanosphere formulation containing dexamethasone was designed for solubilization of the drug in aqueous solution and sustained release of the drug from the nanosphere. The lipid nanospheres, composed of phospholipid, cholesterol and cationic lipid, were prepared by self emulsification-solvent diffusion method followed by diafiltration. Physicochemical characteristics such as mean particle diameter, zeta potential and drug loading efficiency of the lipid nanospheres were investigated according to the variation of either the kind of lipid or the lipid composition. The lipid nanospheres had a mean diameter 80-120 nm and dexamethasone loading efficiency of greater than 80%. The drug loading efficiency increased with the increase of the length of aliphatic chain attached to the phospholipid. However, the drug loading efficiency was inversely proportional to the increase of cholesterol content in the lipid composition. The lipid nanosphere could not be prepared without the use of cationic lipid and the drug loading efficiency was proportional to the increase of cationic lipid content. The lipid nanospheres containing dexamethasone are a promising novel drug carrier for an injectable formulation of the poorly water-soluble drugs.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.32 no.3 s.58
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• pp.149-152
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• 2006

Natural safflower oleosomes are small ($1{\sim}3{\mu}m$) spherical shaped "reservoir", inside which the seed stores triglycerides for use as a future energy source. The surface of the oleosome is covered with a high molecular weight ($20{\sim}24$ KDa) oleosin protein which has been demonstrated to have emulsification properties. Traditionally, oleosomes from oil bearing seeds such as safflower were simply crushed to liberate the oil within. Our patented DermaSphere technology allows for the isolation of oleosomes in the intact state. Once isolated, these materials can be used in skin care formulations to deliver the emolliency, occlusivity, and anti-oxidant effects typically associated with safflower oil. However, because of the presence of the emulsifying oleosin protein covering the spherical oil body, oleosomes have self-emulsification property as well as can emulsify other oil phase in typical oil-in-water (O/W) emulsion. The oleosomes can literally serve as the entire non-active portion of the oil phase of a typical skin care product. Most importantly, natural oleosomes can be loaded with other oil-soluble active materials and can therefore be used as delivery systems for improved cosmetic efficacies. Oleosomes can be loaded with various actives, such as fragrances, vitamins, inset repellents, and UV chromophores. The loaded oleosomes can be utilized to either protect the active ingredients within the formulation itself or to allow for control release of those actives over time.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.39 no.1
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• pp.55-63
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• 2013

Applications of nano-emulsion for cosmetics as a means of promoting dermal absorption have been the subject of interest. In this study, the stability of nano-emulsions prepared by low-energy emulsification method and varying the composition of raw materials was investigated. By measuring the particle size of the nano-emulsion against time, the stability of nano-emulsions prepared by adding polyol to water phase was increased significantly compared with the nano-emulsions prepared by adding polyol to ethanol phase. The speed of adding ethanol phase to water phase did not have a significant impact on the particle size and stability. Depending on the type of oil, stability was not affected. However, there would be a correlation between the initial size of the nano-emulsion droplets and the molecular weight and polarity of the oil. Stability and the initial particle size according to the type of polyols showed a similar trend except 1,2 hexanediol. The initial droplet size was affected by the concentration of surfactant and oil. However, the initial droplet size did not change against time. Concentration of ethanol was observed to have a significant impact on the initial particle size and stability.

• Journal of Pharmaceutical Investigation
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• v.41 no.2
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• pp.103-109
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• 2011

The objective of the study was to prepare self-microeulsifying drug delivery system (SMEDDS) incorporating atorvastatin calcium and evaluate its properties and oral bioavailability. Solubility of atorvastatin in various vehicles was determined. Pseudo-ternary phase diagrams were constructed to identify the good self-emulsification region. The droplet size distributions of the resultant emulsions were determined by dynamic light scattering measurement. The mean droplet size of chosen formulation (20% ethyl oleate, 40% tween-80, 40% Carbitol$^{(R)}$) was $23.4{\pm}1.3$ nm. The SMEDDS incorporating atorvastatin calcium appeared to be associated with better performance in dissolution and pharmacokinetic studies, compared with raw atorvastatin calcium. In dissolution test, the release percentage of atorvastatin from SMEDDS mixture could rapidly reach more than 95% within 3 min. Oral $AUC_{0{\rightarrow}8hr}$ values in SD rats was $1994{\pm}335\;ng{\cdot}hr/mL$, which significantly increased (P<0.05) compared with raw atorvastatin calcium. The SMEDDS formulation was relatively stable when stored at $4^{\circ}C$ during 3 months. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin, by the oral route.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.38 no.3
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• pp.201-207
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• 2012

The influence of different dilution procedures on the properties of oil-in-water (O/W) nano-emulsions obtained by dilution of oil-in-ethanol (O/E) microemulsions with water has been studied. The system water/ethanol/nonionic surfactant/silicone oil with ethanol was chosen as model system. The dilution procedures consisted of adding water (or microemulsion) stepwise. By mixing O/E microemulsions into water, nano-emulsions with droplet diameters of 30 nm were obtained. In contrast, by mixing water into O/E microemulsion, emulsions with diameter of 400 nm were obtained The dilution methods were shown to be a key factor determining the properties of the emulsions. There were no change in diameters of nanoemulsion droplets against time, however sizes of droplets in the emulsion with larger droplets were increased with time and the mechanism of unstability was thought to be Ostwald ripening.