• Polymer(Korea)
• /
• v.37 no.3
• /
• pp.347-355
• /
• 2013

In this study, the porous cellulose hydrogel as a carrier to enhance the skin delivery of quercetin and its glycoside, rutin known as flavonoid antioxidants was prepared and its properties were investigated. The optimum cellulose hydrogel for quercetin and rutin was made by the reaction of 2 wt% cellulose with 12% ECH. In the release test of the hydrogel containing the flavonoids, the release of quercetin was diffusion-controlled at $10{\sim}500{\mu}M$, but rutin was released by the erosion of hydrogel system at $10{\sim}50{\mu}M$. Both the encapsulation efficiency and release amount of rutin in hydrogel were higher than quercetin. However, in skin permeation experiment using Franz diffusion cell, quercetin showed higher skin permeation capacity than rutin. The hydrogel containing flavonoids showed remarkable transdermal permeation than the control group. These results suggest that porous cellulose hydrogel is potential drug delivery system to enhance transdermal permeation of water-insoluble flavonoid antioxidants.

• Microbiology and Biotechnology Letters
• /
• v.41 no.3
• /
• pp.320-326
• /
• 2013

In a previous study, we investigated the antioxidative and cellular protective effects of Parthenocissus tricuspidata stem extracts. In this study, we prepared nano-emulsion containing P. tricuspidata stem extract to improve skin permeation. The particle size of the nano-emulsion using the microfluidizer was 302 nm. Its loading efficiency was over 86%. The size distribution of the nano-emulsion took a monodispersed form and the nano-emulsion was more stable than typical emulsion without using microfluidizer during a 2 week period. In vitro skin permeation study of nano-emulsion containing P. tricuspidata stem extracts was carried out using Franz diffusion cell. The 1,3-butylene glycol used as a control group had 32.59% skin permeation efficiency. The skin permeation efficiency of the nano-emulsion was 42.47%. Also, we observed the antibacterial activity of the ethyl acetate fraction on skin flora for prospective applications as a natural antimicrobial. The ethyl acetate fraction had antibacterial activities higher than methyl paraben on Staphylococcus aureus, and Bacillus subtilis. These results indicate that nano-emulsion containing P. tricuspidata stem extracts could possess valued applications in cosmetic formulations for improving skin permeation. Also, based on the antibacterial activities on skin flora, antioxidative and cellular protective effects shown in our previous study, we suggest that P. tricuspidata stem extracts could be used as functional cosmetic materials.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.46 no.2
• /
• pp.133-145
• /
• 2020

This study utilized nano-liposomes for the purpose of stabilizing and increasing the solubility of biotin, a water-soluble active material with low solubility. The particle size, zeta potential, and polydispersity index were confirmed with a nano zetasizer. It was possible to manufacture nano liposomes at 100 to 250 nm of particle size and -80 to -30 mV of zeta potential. Dialysis membrane method (DMM) was used to measure the capsulation efficiency of biotin in biotin nano-liposomes, and results showed that pH increased biotin nano-liposomes had higher capsulation efficiency than normal biotin nano-liposome. Through this experiment, it was confirmed that the pH has a great influence on the stability of biotin nano-liposomes. In vitro franz diffusion cell method was used to measure in vitro skin absorption rate of biotin nano-liposomes. The shape of the formulation and biotin solubility in nano-liposome was observed by cryogenic transmission electron microscopy (cryo-TEM). Through this study, we confirmed that biotin, which is introduced as closely related to hair health, can be incorporated into a nano-liposome drug delivery system, to make biotin nano-liposome with improved solubility and precipitation problems.

• Polymer(Korea)
• /
• v.38 no.5
• /
• pp.676-681
• /
• 2014

Licorice, widely used as a herbal medicine, has flavonoids such as liquiritin and its aglycone, liquiritigenin that show anti-oxidant and anti-inflammatory properties. Licorice flavonoid-loaded cellulose hydrogels were prepared as carriers for skin drug delivery, and their properties were investigated. The porous cellulose hydrogel was made by reacting cellulose with epichlorohydrin as a cross-linking agent in NaOH/urea(1~10%) solutions. Through studies on the rheological properties and water uptake of the hydrogel, a NaOH/urea(6%) solution was established as being optimum for the synthesis of the cellulose hydrogel containing liquiritin and liquiritigenin. Scanning electron microscopy (SEM) observations of a cross-section of the prepared hydrogel indicated its porosity. In particular, in skin permeation experiments using a Franz diffusion cell, hydrogel containing the licorice flavonoids showed remarkable transdermal permeation compared to the control group. These results indicate that porous cellulose hydrogel is a potential drug delivery system to enhance the skin permeation of licorice flavonoids.

• Polymer(Korea)
• /
• v.36 no.4
• /
• pp.420-426
• /
• 2012

In this study, we prepared polymer micelles containing quercetin and rutin, known as antioxidants, using poly(${\varepsilon}$-caprolactone)-b-poly(ethylene glycol), and evaluated in vitro skin permeation of the active materials. Quercetin and rutin loaded micelles were characterized by DSC (differential scanning calorimetry), HPLC (high performance liquid chromatography) and DLS (dynamic light scattering) measurements. The particle size of the polymer micelles increased in a concentration dependent manner (0.5~2.0% PCL-b-PEG). The Zeta potential of quercetin and rutin loaded micelles remained constant. To evaluate the skin penetration of PCL-b-PEG micelles, Franz diffusion cell experiment was performed. The aqueous solutions of quercetin and rutin were used as the control groups. Quercetin and rutin loaded PCL-b-PEG micelles showed more efficient skin permeation than the control groups. Safety assessment (patch test) of quercetin and rutin loaded PCL-b-PEG micelles on skin was performed to test application possibility of the polymer micelles to cosmetics. Any adverse symptoms were not observed.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.36 no.2
• /
• pp.115-120
• /
• 2010

The formidable barrier property of the stratum cornemum and the high hydrophilicity of active ingredient make it difficult to permeate through the skin and reach to its site of action. The aim of this study was to investigate the effect of chemical penetration enhancers on the skin permeation of a hydrophilic cosmetic active ingredient, such as arbutin. The enhancing effects of N-methyl-2-pyrrolidone (NMP) on the permeation of a hydrophilic cosmetic active ingredient were evaluated by using Franz diffusion cell. The study indicated that NMP has considerable influence on the skin permeability. NMP was not only the most effective enhancer but also increased the skin permeability of arbutin approximately 1.3~1.5 fold compared with control without penetration enhancer. The lag time did not change with NMP, which suggested no effect of NMP on skin lipid fluidity. This suggest that arbutin co-permeated with NMP. The results indicate NMP is effective enhancer of a hydrophilic cosmetic active ingredient in penetration, with potential applications for drug delivery system.

• Journal of Pharmaceutical Investigation
• /
• v.33 no.1
• /
• pp.29-36
• /
• 2003

Clenbuterol, a selective ${\beta}_2-adrenergic$ receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic obstructive bronchial disease, chronic bronchitis and pulmonary emphysema. The percutaneous permeation of clenbuterol was investigated in hairless mouse skin after application of 50/50 buffer(pH 10)/propylene glycol solvent mixture. The enhancing effects of various penetration enhancers such as terpenes, non-ionic surfactants, pyrrolidones, fatty acids and some other enhancers on the permeation of clenbuterol were evaluated using Franz diffusion cell. Among terpenes studied, 1,8-cineole was the most effective enhancer, which increased the permeability of clenbuterol approximately 39.33-fold compared with the control without penetration enhancer, followed by menthone with enhancement ratio of 23.57. Nonionic surfactants did not have significant enhancing effects. N-Lauryl-2-pyrrolidone increased the permeability of clenbuterol approximately 4.51-fold compared with the control. Lauric acid increased the permeability of clenbuterol approximately 35.57-fold with decreasing the lag time from 2.64 to 0.52 hr. Oleic acid, linoleic acid, linolenic acid and capric acid showed enhancement ratio of 22.62, 19.60, 17.45 and 16.51, respectively. $Labrafil^{\circledR}$ enhanced the permeability of clenbuterol 9.24-fold compared with that without enhancer.

• Journal of Pharmaceutical Investigation
• /
• v.37 no.2
• /
• pp.95-99
• /
• 2007

To develop topical nitroglycerin (NTG) preparation far chronic anal fissure treatment, the release rate of NTG should be controlled carefully. For this, microemulsion was prepared from the phase diagram construction with Cremophor ELP, ethanol and Labrafil $M1944CS^{(R)}$ and the topical gel was prepared by dispersing NTG containing microemulsion into hydrophilic polymers. in viかo release characteristics were evaluated with Franz diffusion cell using cellulose membrane and compared with control hydrogels. The release rate of NTG was followed $1^{st}$ order kinetics and, when comparing the NTG release from control hydrogel with that from the microemulsion-based hydrogel, the NTG release rate was controlled by the content of polymers within continuous phase and the concentration of dispersed phase.

• Journal of Pharmaceutical Investigation
• /
• v.35 no.3
• /
• pp.207-224
• /
• 2005

The objective of this study was to explore the principles of SUPAC-SS and its regulatory application in handling postapproval changes to nonsterile semisolid dosage forms. The types of postapproval changes that SUPAC-SS described were modifications in formulation (components and composition), batch size, manufacturing equipment & process, and the site of manufacturing. SUPAC-SS defined the levels of postapproval changes and what chemistry, manufacturing, and control tests should be conducted for each change level. The guidance also specified several occasions the manufacturers should perform in vitro release test (Franz cell diffusion test) and/or in vivo bioequivalence test. Finally, SUPAC-SS classified appropriate filing forms to be used in supporting postapproval changes. It was crystal clear that SUPAC-SS helped maintain the safety and quality of approved semisolid dosage forms when they were subject to certain postapproval changes. The availability of SUPAC-SS made contributions to reducing regulatory burdens of the industry, as well as expediting the postapproval process of regulatory agencies. This study also shed light on the background of relevant pharmaceutical sciences that the SUPAC-SS guidance adopted. Finally, the KFDA and the industry were strongly urged to implant a similar guidance in handling postapproval changes to semisolid dosage forms available in the Korean marketplace.

• Journal of Pharmaceutical Investigation
• /
• v.35 no.1
• /
• pp.7-16
• /
• 2005

Gardeniae Fructus is consisted of geniposide and it's derivatives. For the purpose of treatment of skin disease, geniposide and hydrolyzed products (HP) of Gardeniae Fructus were studied on skin permeation and cross1inking with biological tissue. The hydrolyzed products (HP) and active ingredients of Gardeniae Fructus were identified and investigated about skin permeability. Genipin has provided low cytotoxic cross1inking reagents and formed stable and biocompatible crosslinked products. The permeation enhancing effects of geniposide and genipin under the hydrolyzed products of cream and hydrogel preparations were tested using Franz type diffusion cell and the skin of hairless mouse. The remaining proportions of geniposide and genipin were measured in the hydrolyzed products of cream and hydrogel preparations. The crosslinking of epidermic and endodermic tissue with genipin under the hydrolyzed prodcuts of cream and hydrogel preparation was observed using light microscopy. Increased absorption ratio of the skin of hairless mouse about genipin was higher than that of geniposide. Loads at break, tensile strengths and skin permeation rate of the hydrolyzed products (HP) of cream and hydrogel preparations were higher than the nonhydrolyzed products (NHP). The hydrolyzed products (HP) of cream and hydrogel of Gardeniae Fructus Extracts were proper preparations and crosslinking agents to increase the transdermal absorption with epidermic and endodermic tissue.