• Journal of Pharmaceutical Investigation
• /
• v.29 no.4
• /
• pp.329-335
• /
• 1999

Clenbuterol, a selective ${\beta}_2-adrenergic$ receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic bronchitis and pulmonary emphysema. For the purpose of developing a transdermal preparation for clenbuterol, we attempted to select an optimal solvent system and permeation enhancer among fatty acids and fatty alcohols which are known to accelerate the penetration of various drugs in permeation experiments using hairless mouse skin and Franz diffusion cell. Apparent partition coefficient of clenbuterol was increased as pH of buffer solution was increased and solubility of clenbuterol was increased as the percent of propylene glycol(PG) in buffer solution(pH 10) was increased. Permeability of clenbuterol from different buffer(pH 10)/PG solvent mixtures was decreased as the percent of PG in pH 10 buffer solution was increased and among the various enhancers studied, lauryl alcohol was found to be the most effective enhancer, increasing the permeability of clenbuterol approximately 76-fold compared with control. Lauryl alcohol$(0{\sim}2%)$ enhanced the permeability of clenbuterol concentration-dependently. In this study, the optimal solvent system for the penetration of clenbuterol was found to be 50/50 buffer(pH 10)/PG solvent mixture containing 2% lauryl alcohol.

• Journal of Pharmaceutical Investigation
• /
• v.38 no.6
• /
• pp.357-363
• /
• 2008

Penetration rate of large molecule through skin is very low due to the barrier effect of stratum corneum. Novel microneedle treatment device with roll was designed for transdermal delivery of large molecular drugs such as vaccine and protein drugs. The permeation rates of FITC labelled bovine serum albumin (FITC-BSA) as a model protein were determined using modified Franz diffusion cell and hairless mouse skin which were treated by hydrogel or solution containing FITC-BSA. Fluorescent spectrophotometer was used to analyze the concentration of FITC-BSA. Microscope using fluorescent filter was used to capture the image and location of FITC-BSA in the skin. We confirmed that permeation rate of BSA was increased with the treatment by microneedle and was increased by the increasing frequency of treatment. Furthermore, the permeation rate observed from hydrogel treated skin was significantly higher than that from solution treated skin.

• Proceedings of the SCSK Conference
• /
• 2003.09b
• /
• pp.87-107
• /
• 2003

It was demonstrated that Transactivating transcriptional activator(TAT) protein from HIV-1 shown to enter cells when added to the surrounding media. TAT peptide chemically attached to various proteins was able to deliver these proteins to various cell and even in tissues in mice with high levels in heart and spleen. In this study, the tripeptide GKH(Glycine-Lysine-Histidine) derived from Parathyroid hormone (PTH), which was known as lipolytic peptide, is attached to 9-poly Lysine(TAT) to be used as a cosmetic ingredient for slimming products. When Glycerol release, expressed as extracellular glycerol concentration, is lipolysis index, TAT-GKH at $10^{-5}$mo1/L induces approximately 41.5% maximal lipolytic effects in epididymal adipocytes isolated from rats, compared with basal lipolysis. Epididymal adipose tissues of male rats is assessed ex vivo by microdialysis. Probes are perfused with Ringer solution in which increasing concentrations of TAT-GKH. The perfusion of TAT-GKH induces lipolytic effect. Penetration study showed that TAT-GKH efficiently elevates 36 times higher penetration into the excised hairless mice skin than GKH. in vivo study showed that TAT-GKH had a better effect upon the relative volume of eye bag after 28 days of application on twenty(+2) healthy female volunteers. It was identified that TAT-GKH increases penetration enhancement and lipolytic effects in both in vitro, ex vivo and in vivo.

• Journal of Pharmaceutical Investigation
• /
• v.34 no.2
• /
• pp.115-123
• /
• 2004

Geniposide and its related iridoid compounds have been used in traditional herbal medicine for thε treatment of Jaundice hepatic diseases and various inflammatorys. For the purpose to increase trandsdermal absorption, the hydrolyzed products of Gardeniae Furctus were identified and assayed of active ingredients and investigated trandsdermal absorption and anti-inflammatory effects. Geniposide was hydrolyzed to genipin by ${\beta}-glucosidase$ and it was suggested that genipin was more suitable form than geniposide for transdermal absorption by its lipophilic property. Using Franz type diffusion cell and the skin of hairless mouse, the permeation rate of hydrolyzed products and their emulsion preparation were determined. Genipin have more increased absorption ratio through the skin of hairless mouse than geniposide. Also, the emulsion of hydrolyzed products of extracts showed higher permeability than that of nonhydrolyzed preparations. After 9 hours $280.85\;{\mu}g/cm^2$ of genipin was absorbed and $193.52\;{\mu}g/cm^2$ in case of geniposide. The Js of geniposide and genipin were $26.27{\pm}4.11\;{\mu}g/cm^2/hr$ and $40.35{\pm}5.04\;{\mu}g/cm^2/hr$ respectively. After carrageenan injection, the swelling was increased repidly to 24 hr and maintained as plateau. but emulsion group weer reached about 2.5 mL and the swelling decreased successively form 24 hr to 72 hr. The anti-inflammation effects of extracts and hydrolyzed products emulsion were increased with significant difference with control group after 24 hr, 48 hr and 72 hr. In carrageenan induced edema, inhibition of swelling was increased in case of hydrolyzed product emulsion compare with nonhydrolyzed group at 24 hr, 48 hr and 72 hr after swelling. In histological study, the anti-inflammatory effects of hydrolyzed products were remarkable at 48 hr and 72 hr compare with nonhydrolyzed. Hydrolyzed products of Gardeniae Fructus extracts containing genipin would be a suitable preparation to increase the transdermal absorption and anti-inflammatory effects.

• Journal of the Korean Applied Science and Technology
• /
• v.30 no.1
• /
• pp.116-126
• /
• 2013

Glycol ethers are a group of solvents based on alkyl ethers of ethylene glycol commonly used in paints. These solvents typically have a higher boiling point, together with the favorable solvent properties of lower-molecular weight ethers and alcohols. The word "Glycol ethers" was registered as a United States trademark by Union Carbide Corp. Typically, glycol ethers are found in pharmaceuticals, sunscreens, cosmetics, inks, dyes and water based paints. On the other hand, glycol ethers are used in degreasers, cleaners, aerosol paints and adhesives. Most glycol ethers are relatively water soluble, biodegradable and only a few are considered toxic. Therefore, they are unlikely to pose an adverse risk to the environment. Recent study suggests that occupational exposure to glycol ethers is related to low motile sperm count in men, but the finding has been disputed by others. In this study, skin permeation of 3 types glycol ethers were studied in vitro using matrix such as solvent and detergent. The absorption of glycol ethers[methyl glycol ethers(MC), ethyl glycol ethers(EC) and butyl glycol ethers(BC)] has been measured in vitro through rat skin. Epidermal membranes were set up in Franz diffusion cells and their permeability to PBS measured to establish the integrity of the skin before the glycol ethers were applied to the epidermal surface. Absorption rates for each glycol ethers were determined and permeability assessment made to quantify any irreversible alterations in barrier function due to contact with the esters. Types of glycol ethers in vitro experimental results on MC> EC> BC quickly appeared in the following order: skin permeation was beneficial to the skin permeation small molecular weight, the difference in chemical structure, such as hydrophilic, because with the partition coefficient and solubility mechanisms and passive diffusion to increase the speed at which transmission is considered.

• Journal of the Korean Applied Science and Technology
• /
• v.41 no.1
• /
• pp.9-18
• /
• 2024

Smilax china is known for its excellent antimicrobial, antioxidant, and anti-inflammatory properties. As a foundational study for applying the functionality of Smilax china extracts to cosmetics, it is necessory to investigate the concentration-dependent skin permation characteristics of the flavonoids in the extract, namely quercetin, catechin, and naringenin. Therefore, it serves as a crucial method for conducting this basic research on the functional aspects fo Smilax china extracts for cosmetic applications. This investigation focused on examining the percutaneous permeability characteristics of flavonoids originating from Smilax china. Applying Marzulli's definition, the Kp value of quercetin was categorized as "fast" at 0.1 mg/mL and "moderate" at 0.2 and 0.4 mg/mL. Notably, the permeation rate exhibited a decline with increasing concentration. For naringenin, Flux values were 0.69, 1.07, and 1.42 ㎍/hr/cm² at concentrations of 0.1, 0.2, and 0.4 mg/mL, respectively, with corresponding Kp values of 6.95, 5.34, and 3.56. Naringenin's Kp value fell into the "moderate" category across all concentrations, and as observed with quercetin, the permeation rate decreased with higher concentrations. Likewise, for catechin, Flux values were 0.75, 1.09, and 1.66 ㎍/hr/cm², and corresponding Kp values were 7.55, 5.46, and 4.16. Catechin's Kp value was consistently classified as "moderate" across all concentrations. The efficacy of quercetin, catechin, and naringenin, active ingredients in high-performance and anti-inflammatory Smilax china extracts, was found to exhibit skin penetration properties above the average. This confirms their suitability as excellent natural materials for use in functional cosmetics, given their outstanding capabilities in preventing acne and reducing inflammation.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.49 no.2
• /
• pp.147-157
• /
• 2023

Centella asiatica extract is widely used as a raw material for cosmetics due to its various effects, but it is difficult to expect penetration into the skin due to its high molecular weight and low solubility. In order to solve these problems, lipid-based liposomes of various types were developed to increase skin absorption. Therefore, in this study, we tried to increase the skin absorption rate by preparing transfersomes using surfactants as edge activators in existing liposomes. Liposome and transfersomes containing Span 80 and Tween 20, 60, 80, and 85, respectively, were prepared using a high-pressure homogenizer, and we evaluated the particle size, polydispersity index, zeta potential, and skin absorption rate. As a result, there was almost no change in the physical properties of particle size, polydispersity index and zeta potential from 25 ℃ to 60 d, and the particle size of transfersomes containing Tween 20, 60, and 80 increased after 60 d at 45 ℃. Madecassoside, main substances of the Centella asiatica extract was used as an standard and madecassoside was measured and calculated when measuring the skin absorption rate using Franz diffusion cells. As a result, formulations containing Tween 20 were the most, whereas formulations containing Span 80 were the least. According to the skin absorption coefficient (Kp) value, all formulations showed 'very fast', and the absorption rate was similar or greater than that of liposomes, except for formulations containing Span 80. Through this, it was confirmed that the larger the HLB value of the nonionic surfactant, the smaller the particle size of the transfersome, and the increased skin absorption rate due to the increased flexibility of the vesicle membrane. Through this study, transfersome using surfactant as an edge activator can be expected to solve local skin problems not only as a cosmetic raw material or product, but also by increasing skin absorption.

• Applied Chemistry for Engineering
• /
• v.26 no.2
• /
• pp.165-172
• /
• 2015

Quercetin and its glycoside, rutin, are flavonoids, which are well known as natural antioxidants. In this study, cationic liposomes loaded with flavonoids (quercetin or rutin) were investigated for their effects on cell and skin permeability, and protective effects against UVA. The particle size of the empty cationic liposomes was in the range of 100~130 nm, and the zeta potential was + 33.05 mV. The entrapment efficiency of 0.5R/CL was higher than that of 0.5 Q/CL. The cellular uptake of the cationic liposomes was five-fold higher than that of liposomes. The skin permeability of quercetin and rutin was investigated using Franz diffusion cells. Compared to the initial loading dose, the amount of quercetin or rutin delivered to the skin by cationic liposomes was higher than that delivered by conventional liposomes or phosphate-buffered saline. From the protective effect of cationic liposomes against UVA ($25J/cm^2$), we found that the cell viability in cationic liposomes containing flavonoids was higher than that of using UVA irradiation only. These results indicate that cationic liposomes provide enhanced delivery of flavonoids (quercetin and rutin) into the skin and may be used for antiaging and antioxidant cosmetics.

• Journal of the Korean Applied Science and Technology
• /
• v.36 no.3
• /
• pp.766-778
• /
• 2019

In this study, Poria cocos bark were extracted by supercritical process, and anti-inflammatory, whitening, and antioxidant effects were measured in comparison with ethanol extract. Also, An effective percutaneous permeation method using a selected formulation of the extract and a drug delivery peptide was proposed. Pachymic acid, known as the anti-cancer and anti-inflammatory compound of the ventricle, is an indicator component and the HPLC analysis shows that the supercritical extract of the pericardium is more than twice that of the Poria cocos bark extract. In order to confirm antioxidative effect of Bombyx mori, DPPH scavenging ability and ABTS scavenging ability test showed that the ethanol extract of Poria cocos Back had lower concentration than the supercritical extract of Poria cocos back. However, RAW 264.7 Measurements of Nitric oxide (NO) production in cells showed lower NO production at the same concentration than the Poria cocos back ethanol extract. In addition, after 72 hours of processing of $20{\mu}g/mL$ of the Poria cocos back extract in B16 melanoma cells, both the intracellular and extracellular melanin extract were effective and the supercritical extract was lower melanin content. No toxicity was observed at the concentration of $800{\mu}g/mL$ in RAW 264.7 cells used in NO production experiments. However, in B16 melanoma cells, even at $50{\mu}g/mL$, both Poria cocos back ethanol extract and supercritical extract showed a survival rate of less than 60%. The liposome formulation and drug delivery peptides were shown to be useful for percutaneous permeation of Supercritical Extract of Poria cocos back using a liposome formulation and a drug delivery peptide. it is expected that there will be great potential for development as a variety of cosmetic materials for Poria cocos back.