• KSBB Journal
• /
• v.25 no.4
• /
• pp.379-386
• /
• 2010

In the present study, biocompatible poly (ethylene glycol) (PEG) microparticles containing coriander essential oil were prepared using a supercritical particles from gas saturated solution (PGSS) process to improve the stability of the coriander oil. The effects of various process parameters such as temperature, pressure, and nozzle diameter on the morphology and entrapment efficiency of coriander oil loaded PEG microparticles were then investigated. A positive influence on the formation of spherical microparticles was observed with increasing temperature and decreasing pressure. Furthermore, somewhat more porous microparticles were produced with an increase in pressure. At a given temperature, the highest entrapment efficiency of coriander essential oil in PEG microparticles was observed under the lowest experimental pressure condition.

• Polymer(Korea)
• /
• v.34 no.6
• /
• pp.527-533
• /
• 2010

The pioglitazone loaded poly(lactide-co-glycolide)(PLGA) nanospheres were prepared by emulsion-evaporation method and optimized for particle size and entrapment efficiency. The optimized particles were 125~170 nm in size with narrow size distribution and showed above 85% entrapment efficiency at 30% of pioglitazone loading when prepared with 3% w/v of poly(vinyl alcohol) (PVA) as a surfactant. These particulate carriers exhibited a controlled in vitro release of pioglitazone for 40 days at a nearly constant rate. The pioglitazone loaded PLGA nanospheres were not only effective to reduce the blood sugar level of diabetic rats but also non-toxic for the animal body, in particular for sensitive organs like kidney, liver, heart, lung and spleen. These results indicate that PLGA nanospheres have a great potential for oral delivery of pioglitazone.

• Asian Pacific Journal of Cancer Prevention
• /
• v.17 no.4
• /
• pp.2277-2284
• /
• 2016

Ribosome-inactivating protein (RIP) from Mirabilis jalapa L. leaves has cytotoxic effects on breast cancer cell lines but is less toxic towards normal cells. However, it can easily be degraded after administration so it needs to be formulated into nanoparticles to increase its resistance to enzymatic degradation. The objectives of this study were to develop a protein extract of M. jalapa L. leaves (RIP-MJ) incorporated into nanoparticles conjugated with Anti-EpCAM antibodies, and to determine its cytotoxicity and selectivity in the T47D breast cancer cell line. RIP-MJ was extracted from red-flowered M. jalapa L. leaves. Nanoparticles were formulated based on polyelectrolyte complexation using low viscosity chitosan and alginate, then chemically conjugated with anti-EpCAM antibody using EDAC based on carbodiimide reaction. RIP-MJ nanoparticles were characterised for the particle size, polydispersity index, zeta potential, particle morphology, and entrapment efficiency. The cytotoxicity of RIP-MJ nanoparticles against T47D and Vero cells was then determined with MTT assay. The optimal formula of RIP-MJ nanoparticles was obtained at the concentration of RIP-MJ, low viscosity chitosan and alginate respectively 0.05%, 1%, and 0.4% (m/v). RIP-MJ nanoparticles are hexagonal with high entrapment efficiency of 98.6%, average size of 130.7 nm, polydispersity index of 0.380 and zeta potential +26.33 mV. The $IC_{50}$ values of both anti-EpCAM-conjugated and non-conjugated RIP-MJ nanoparticles for T47D cells (13.3 and $14.9{\mu}g/mL$) were lower than for Vero cells (27.8 and $33.6{\mu}g/mL$). The $IC_{50}$ values of conjugated and non-conjugated RIP-MJ for both cells were much lower than $IC_{50}$ values of non-formulated RIP-MJ (>$500{\mu}g/mL$).

• Journal of Pharmaceutical Investigation
• /
• v.36 no.5
• /
• pp.299-304
• /
• 2006

The aim of this study was to investigate the effect of deformable liposomes with sodium cholate on the skin permeation and skin deposition of arbutin, a hydrophilic skin-whitening agent. Various compositions of liposomes were prepared by the extrusion method. Particle size distribution and entrapment efficiency were determined by the laser light scattering and the gel permeation chromatography, respectively. The in vitro rat skin permeation and deposition of arbutin in various skin layers were investigated using the Keshary-Chien diffusion cells at $37^{\circ}C$. The average particle size of the deformable liposomes ranged from 217.4 to 117.4 nm, depending on the composition. The entrapment efficiency was dependent on surfactant concentration and loading dose of arbutin. The permeation rate of 5% arbutin in deformable liposomes was $8.91({\pm}1.33){\mu}g/cm^2/h$, and was not significantly different from 5% arbutin aqueous solution $[9.82({\m}0.86){\mu}g/cm^2/h]$. The deposition of arbutin was $43.34({\pm}12.13)$ and $16.99({\pm}7.83){\mu}g/cm^2$ in stratum corneum layer and epidermis/dermis layer, respectively, after 12 h of permeation study. These results are consistent with several earlier studies for the localization effect of liposomal formulations in stratum corneum, and demonstrated the feasibility of the deformable liposomes as a promising carrier for the skin deposition of hydrophilic skin-whitening compounds.

• Journal of Pharmaceutical Investigation
• /
• v.26 no.4
• /
• pp.245-256
• /
• 1996

Solid lipid nanoparticles (SLN) have been developed as a new drug delivery system. Although many particulate drug carriers, such as microsphere, liposome, niosome, emulsion, etc. have been introduced, they have some disadvantage; low efficiency of incorporation and stability, lack of reproducibility, and so on. Meanwhile, SLN as a new drug delivery system is known to entrap rugs with a high efficiency and a good reproducibility. Moreover, small size SLN can circulate in blood for a prolonged time. Although many preparation methods were introduced, microfluidization method is recommended to be the most useful. This study was attempted to prepare and evaluate ketoprofen-incorporated SLNs (keto-SLN), which were prepared by two methods, ultrasonication and microfluidization. Keto-SLN was evaluated by measurement of particle size and zeta potential, efficacy of entrapment, sedimentation volume, in virto release pattern. The mean particle size was about $0.1\;{\mu}m$, and the size was dependent on the type and the amount of emulsifier. Zeta potential was negative, $-9{\sim}-13mV$ and entrapment efficacy was very high and stability was good for at least 60 days in the respect of particle size and sedimentation volume ratio. Analgesic effect was also determined as well as pharmacokinetic parameters. The former was comparable to that of that of ketoprofen loaded suspension (keto-sus) and the latter revealed that consistent with the delayed release of keto-SLN. $T_{max}$ was longer than keto-sus. Therefore, keto-SLN was favourable dosage forms in the field of drug delivery system such as anti-cancer, analgesics and anti-inflammatory agents.

• Food Science of Animal Resources
• /
• v.39 no.5
• /
• pp.831-843
• /
• 2019

The purposes of this research were to form chitosan oligosaccharide (CSO)/A2 ${\beta}$-casein nano-delivery systems (NDSs) and to investigate the effects of production variables, such as CSO concentration levels (0.1%, 0.2%, and 0.3%, w/v) and manufacturing temperature ($5^{\circ}C$, $20^{\circ}C$, and $35^{\circ}C$), on the production and physicochemical characteristics of CSO/A2 ${\beta}$-casein NDSs to carry resveratrol. The morphological characteristics of CSO/A2 ${\beta}$-casein NDSs were assessed by the use of transmission electron microscopy (TEM) and particle size analyzer. High-performance liquid chromatography (HPLC) was applied to determine the entrapment efficiency (EE) of resveratrol. In the TEM images, globular-shaped particles with a diameter from 126 to 266 nm were examined implying that NDSs was successfully formed. As CSO concentration level was increased, the size and zeta-potential values of NDSs were significantly (p<0.05) increased. An increase in manufacturing temperature from $5^{\circ}C$ to $35^{\circ}C$ resulted in a significant (p<0.05) increase in the size and polydispersity index of NDSs. Over 85% of resveratrol was favorably entrapped in CSO/A2 ${\beta}$-casein NDSs. The entrapment efficiency (EE) of resveratrol was significantly (p<0.05) enhanced with an increase in manufacturing temperature while CSO concentration level did not significantly affect EE of resveratrol. There were no significant (p<0.05) changes observed in the size and polydispersity index of NDSs during heat treatments and storage in model milk and yogurt indicating that CSO/A2 ${\beta}$-casein NDSs exhibited excellent physical stability. In conclusion, the CSO concentration level and manufacturing temperature were the crucial determinants affecting the physicochemical characteristics of CSO/A2 ${\beta}$-casein NDSs containing resveratrol.

• Korean Journal of Food Science and Technology
• /
• v.39 no.6
• /
• pp.658-662
• /
• 2007

In this study, wild sesame leaf aromas (WSLA) were extracted and the extracted aromas were entrapped in porous potato starch micelles. The entrapped aromas did not evaporate, even by heated water treatments, and remained until a physical treatment such as chewing. Thus, the entrapped WSLA starch was used to make precooked instant noodles in order to mask or/and reduce an unpleasant raw flour flavor. The efficiencies of the flavor entrapment were analyzed using gas-chromatography equipped with solid phase micro-extraction (SPME), as well as by sensory evaluation. The highest yield of the porous potato starch was shown as 82.4% at an inlet temperature (IT) of $170^{\circ}C$, an exhaust temperature (ET) of $90^{\circ}C$, and a feeding rate (FR) of 40 mL/min. In the porous starch made by IT at $200^{\circ}C$, ET at $100^{\circ}C$, and FR at 50 mL/min, the entrapment efficiency was 68% by GC analysis; this starch also had the highest WSLA and consumer acceptability, but the lowest raw flour flavor, according to the sensory evaluation results.

• Macromolecular Research
• /
• v.17 no.12
• /
• pp.969-975
• /
• 2009

This article describes the topical delivery and localization of budesonide through the hairless mouse skin. Two poly(ethylene oxide)-block-poly($\varepsilon$-caprolactone)-block-poly(ethylene oxide) (PEO-PCL-PEO) triblock copolymers (T 222 and T 252) having different CL:EO ratios were added in the preparation of budesonide particles stabilized with poly(vinyl alcohol) (PVA) and Tween 80 under ultrasonication. For comparison, a commercial PEO-PPO-PEO triblock copolymer (F68) was studied under the same condition. To demonstrate the effects of the triblock copolymer, the particle size of budesonide emulsion, entrapment efficiency, and in vitro release were measured and compared. The budesonide particles stabilized by the triblock copolymers had a diameter of ca. 350 nm with entrapment efficiencies of 66-76%. The In vitro release profiles of all samples showed an initial burst followed by sustained release. The skin penetration and permeation of budesonide were analyzed by using a Frantz diffusion cell. T 222 and T 252 exhibited higher total permeation amounts, but lower budesonide penetration amounts, than F68. The results suggest that the partitioning of budesonide in each skin layer can be adjusted in order to avoid skin thinning and negative immune response arising from the penetration of budesonide in blood vessels.

• Applied Chemistry for Engineering
• /
• v.24 no.6
• /
• pp.639-644
• /
• 2013

In this study, ethosomes loaded with Eucommia ulmoides extracts that have anti-inflammatory and anti-aging activities on the skin were prepared as cosmetic materials. The particle size, physical property, and entrapment efficiency of ethosomes to identify their stabilities during 4 weeks were measured. Ethosomes containing 0.01~0.05% E. ulmoides extracts did not show either precipitation or separation. The mean particle size of these ethosomes was 136.4 nm, and monodisperse. The particle size of ethosome containing 0.05% E. ulmoides extracts was 151.15 nm and the entrapment efficiency was 81.79%. Therefore, in vitro skin permeation experiment was performed with ethosome containing 0.05% E. ulmoides extracts that showed the high loading efficiency and stability during 4 weeks. The order of skin permeation of E. ulmoides extracts was ethosome (77.16%) > liposome (62.80%) > ethanolic solutoin (41.59%). These results suggest that ethosomes containing 0.05% E. ulmoides extracts are effective for the skin permeation and may be used as a cosmetic formulation containing plant extracts.

• KSBB Journal
• /
• v.17 no.6
• /
• pp.531-536
• /
• 2002

In this study, we attempted to increase the survivability of bifidobacteria in simulated gastric juices and bile salts after cell entrapment with alginate and various food additives, such as erythritol, isomalt, palatinose, skim milk, xanthan gum, isomalto-oligosaccharide, fructo-oligosaccharide, galacto-oligosaccharide, pectin, and mono-sodium glutamate. Additionaly, the stability of bifidobacteria during storage was investigated by measuring survival rate at different temperatures, i.e. at 4$^{\circ}C$, 25$^{\circ}C$ and -20$^{\circ}C$. Bifidobacteria were immobilized in alginate beads and the survival rate was monitored. It was found that bifidobacieria entrapped with 2.5％, alginate showed the highest survival rate at 12%. After addition of the various protective agents, erythritol(1％) showed the best protective efficiency with a survival rate of 56.0% among the additives tested when exposed to simulated gastric juices for 3 h. Immobilized cells suspended in 5% skim milk and stored at 4$^{\circ}C$ survived significantly more than cells stored at 25$^{\circ}C$ and -20$^{\circ}C$. Consequently, the study shows that the survival rate of bifidobacteria immobilized in combination with 2.5% alginate beads and 1% erythritol may be signifcantly increased in simulated gastric juices and bile salts.