• Korean Chemical Engineering Research
• /
• v.58 no.1
• /
• pp.21-28
• /
• 2020

The stem extract from Pyrus serotina var has natural antioxidant ability, but the extraction method does not result in a soluble compound in cosmetic formulations. This study investigated the cosmetic efficacy of the Pyrus serotina var stem extract and its epidermis permeation ability when combined with polymer micelles and a cell penetrating peptide. The total concentration of polyphenol compounds was determined to be 103.1644 ± 1.38 mg/g in the ethanol extract and 78.97 ± 1.45 mg/g in the hydrothermal extract. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging effects were 55.94 ± 0.22% in the ethanol extract at 1,000 mg/L. Superoxide dismutase (SOD) activity rates were 104.05 ± 3.28% in the ethanol extract at 62.5 mg/L. The elastase inhibition rate was 67.21 ± 2.72% in the ethanol extract at 1,000 mg/L. An antimicrobial effect was observed in the Propionibacterium acnes strain. In the epidermal permeability experiment, it was confirmed that formulation of the polymer micelle containing the Pyrus serotina var stem extract and cell penetrating peptide (R6, hexa-D-arginine) showed small particle size and much better skin permeability. The cumulative amount of total Pyrus serotina var stem extract that penetrated to the skin over time increased over 24 hours in three formulations. The three formulations showed 51.61 ㎍/㎠ (Formulation 0), 75.97 ㎍/㎠ (Formulation 1) and 95.23 ㎍/㎠ (Formulation 2) skin penetration, respectively. Therefore, it was confirmed that the ethanol extracts of Pyrus serotina var stem showed good cosmetic efficacy and excellent epidermis permeation ability when combined with a polymer micelle and cell penetrating peptide. Thus, this extract has the potential to be used as a safe and natural cosmetic material in the future.

• 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 Pharmaceutical Investigation
• /
• v.39 no.6
• /
• pp.437-443
• /
• 2009

To develop a topical bioadhesive formulation of clotrimazole for enhanced transdermal delivery, hydroxypropyl methylcellulose gel containing permeation enhancer was formulated and permeation studies were carried out. The release characteristics of the drug from the gel formulation were examined according to the receptor medium, drug concentration, and temperature. The rate of drug release from the gel increased with increasing drug concentration and temperature. The activation energy (Ea) of drug permeation, which was calculated from the slope of log P versus 1/T plots, was 14.41kcal/mol for a 1%(w/w) loading dose. The enhancer, such as saturated, unsaturated fatty acids, pyrrolidones, propylene glycol derivatives, glycerides, and non-ionic surfactants, were incorporated onto the gels to increase the amount of drug permeation into the skin. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the highest level of enhancement. These results show that clotrimazole gels containing polyoxyethylene 2-oleyl ether could be used for the enhanced transdermal delivery of clotrimazole.

• Journal of Pharmaceutical Investigation
• /
• v.33 no.3
• /
• pp.163-169
• /
• 2003

In order to develop a film-forming transdermal drug delivery system, polyurethane (PU) based on poly(ethylene glycol) and poly(tetramethylene oxide) was synthesized and characterized. The synthesized PU was blended with Gantrez ES 225 (GT) to improve the adhesion property of film-forming agent to the skin. When film-forming gel formulation containing 3% ketoprofen (KP) was applied, transparent thin film was obtained within 5 minutes and adhered to the skin for 8 hours. In vitro percutaneous absortion studies were performed to determine the rate of ketoprofen absorption through guinea pig skin. A prominent effect of limonene on the skin permeability of ketoprofen was observed among the various skin permeation enhancers investigated. Considering mechanica properties of film and skin permeability of ketoprofen, 2% of limonene was optimal content in the film forming transdermal formulation.

• Journal of Pharmaceutical Investigation
• /
• v.35 no.4
• /
• pp.273-278
• /
• 2005

Nicotine transdermal therapeutic systems $(TTS_S)$ have been regarded as an effective mean to aid smoking cessation. However, most of nicotine $TTS_S$ in the market have some problems such as unpleasant side effects and skin irritation due to the excess amount of the drug permeated and the properties of the additives employed. In order to solve these problems, new nicotine $TTS_S$ were formulated using biocompatible additives. The optimized formula of the drug layer consisted of nicotine, propylene glycol and poloxamer 188 at the ratio of 1.2: 17.0: 2.0. The drug layer had the sickness of $1,250\;{\mu}m$, the pH of 8.12. The skin permeation rate of nicotine from optimized nicotine patch (NP) was $21.5\;{\mu}g/cm^2/h$. Transdermal administration of nicotine patch has been carried out for the determination of pharmacokinetic parameters in rats. Steady-state plasma concentration of nicotine following transdermal application of NP (area of patch = $15\;cm^2$) on the dorsal skin of rats was 143.2 ng/ml and AUC for 24 hrs was 3,022 ng h/ml. In case of $EXODUS^{\circledR}$ and Nicotinell $TTS^{\circledR}$, the steady-state plasma concentration of nicotine and ACU for 24 hrs were 428.9 ng/ml, $9,121\;ng{\cdot}hr/ml$ and 155.3 ng/ml, $3,152\;ng{\cdot}h/ml$, respectively. NP showed the experimental plasma nicotine concentration profile was very similar to the simulated one and had an appropriate skin permeation rate and a steady-state concentration of nicotine, which can show therapeutic blood levels of the drug for 24 hrs without severe side effects.

• Journal of Pharmaceutical Investigation
• /
• v.41 no.1
• /
• pp.1-7
• /
• 2011

The effects of different formulation variables including pressure sensitive adhesive (PSA), permeation enhancer, thickness of the matrix and loading amount of drug on the transdermal absorption of galantamine were investigated across the hairless mouse skin. The permeation profile of galantamine was different depending on the types of PSA, loading amount of drug, thickness of the matrix and type of enhancer used. Highest flux of galantamine was obtained from acrylic PSA but crystals were formed in the patch within 72 h. Among the PSAs screened, crystal formation was not observed only in the patches formulated in Styrene Butadiene Styrene (SBS) matrix. Permeation rate increased linearly as the concentration of galantamine in SBS matrix increased from 2.5 to 15% w/w. Among the enhancers screened, Brij$^{(R)}$ 30 provided highest flux of galantamine. Matrix thickness of 80 ${\mu}m$ was optimum for maintaining adhesiveness as well as consistently delivering galantamine for longer period of time.

• Archives of Pharmacal Research
• /
• v.24 no.3
• /
• pp.224-228
• /
• 2001

DA-5018, a recently synthesized capsaicin analog, appears to possess potent analgesic activity when administered topically. The objective of this study is to test the feasibility of the topical administration of this compound. Specifically, our goal was to identify vehicle system that permit a reasonable transdermal permeation of the compound in mice. Among the vehicles examined, isopropyl myristate (IPM) showed the largest in vitro permeability across the intact skin (83.6 ${\pm}$ 5.42${\mu}$l/$\textrm{cm}^2$/h ). However, due to the limited solubility of DA-5018 in IPM (0.53 mg/ml), the maximal flux from the IPM medium remained at only 44.3 ${\pm}2.87{\mu}$g/$\textrm{cm}^2$/hr. In order to increase the flux, addition of better solvents for DA-5018 was attempted, under the assumption that flux is the result of both solubility and permeability. Ethoxydiglycol (EG) and oleic acid (OA) were selected as examples of food solvents. The addition of IC or OA to IPM at a 1:1 volume ratio resulted in a comparable increase in the solubility of the compound (i.e., to 61.1 and 50.2 mg/ml for EG and OA, respectively). However, the addition of EG at a 1:1 volume ratio, for example, increased the flux 6.3 fold (i.e., $279{\mu}$g/$\textrm{cm}^2$/hr), while OA, at a 1:1 volume ratio, decreased the flux 5 fold (i.e., $9.26{\mu}$g/$\textrm{cm}^2$//hr). The mechanism of this discrepancy between EG and OA was investigated by measuring the permeabilty of DA-5018 across the stratum corneum-removed skin of the mouse, under the hypothesis that the viable skin layer may serve as a barrier for the permeation of lipophilic substances such as DA 5018. The permeability of DA-5018, from the medium of EG or OA, across the viable skin differed greatly for EG ($0.41{\mu}$l/$\textrm{cm}^2$/hr) and OA ($0.086{\mu}$l/$\textrm{cm}^2$/hr), suggesting that a higher permeability across the viable skin layer is needed for the second solvents. The maximum flux across the intact skin was achieved for DA-5018 when EG was added to IPM at a 1:1 volume ratio. Thus, the use of a binary system appears to be the best approach for realizing the transdermal delivery of DA-5018 at a reasonable rate.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.30 no.4 s.48
• /
• pp.471-477
• /
• 2004

Exposure to elevated temperatures, chemical (active oxigen), or physical stress (UV light) induces immediate physiological response, the expression of heat shock proteins in cells. Thus, cells with elevated Heat Shock Protein levels become more tolerant to stress conditions that are otherwise lethal. First, we studied on the new function of glucuronic acid (GA) as preventive material of skin aging. The application of the GA shows significant induction of Heat Shock Protein 70 kDa (HSP 70 kDa) in contrast to cells without it. GA at the concentration which can induce HSP 70 kDa, protects the cell death induced by second stress (heat shock and hydrogen peroxide) in NIH3T3 cells. Second, we studied on in vitro transdermal permeation characteristic of GA through the excised mouse skin. In this study, we compared the skin permeability of GA in water with O/W emulsion. As a result, skin permeation parameters of GA shows lag time 1.2 h, partition coefficient 0.114, permeation flult rate $0.83114 mg/cm^2/h.$ In case of lag time, O/W emulsion containing GA increase 2.48 h. Also, the total accumulation permeation content decreased in contrast to GA solution after 24 h. But it has long-term permeability of glucuronic acid. These results suggest that glucuronic acid could be a good cosmetic active ingredient.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.49 no.1
• /
• pp.17-27
• /
• 2023

A study was performed to increase skin permeation of tocopheryl acetate, an oil-soluble component among tocopheryl acetate, salicylic acid, and niacinamide, which are the active ingredients of the anti-hair loss toner. As a method of transparently solubilizing tocopheryl acetate while containing salicyl acid and niacinamide, we used a swollen micelle structure that increased the size of the micelle formed by the aggregation of surfactants. The prepared swollen micelle solution contains three kinds of active ingredients, and poloxamer 407 and octyldodeceth-16 were used as surfactants to increase transparent properties and stability. In addition, isostearic acid was used as a co-surfactant to increase the size of micelles. To evaluate the physical properties of the prepared swollen micelles, turbidity at room temperature (25 ℃) was measured. The Franz diffusion cell method was used to evaluate the skin permeation rate of tocopheryl acetate among the hair-loss prevention components contained in swollen micelles. After 24 h, tocopheryl acetate showed a 6-fold improvement in skin permeation compared to the control group. Therefore, it can be seen that the swollen micelles developed in this study can be applied to hair-loss prevention products or solubilized formulations of various functional cosmetics.

• Fire Science and Engineering
• /
• v.24 no.2
• /
• pp.21-30
• /
• 2010

We have test chemical resistance and flame retardant properties of chemical protective clothing Fabrics by the ASTM and ISO standard methods. The flame retardant test results show that polyethylene is poor in flame resistance but fluoroelastomer add to decabrom is excellent in flame resistance. Especially, nowadays heat protective clothing for firefighters, which is aluminized film layers laminated to aramid fabric, show the excellent flame resistance. However, the chemical resistance test results show that aluminium is high corrosive in 4M NaOH solution alone. The problem of corrosion can be overcome by employing multiple barrier film. Also, based on the result of flame retardant test, duel skin of polymer barrier film add to aluminum film and single skin of fluorinated rubber with flame retardant materials seems to be fit for the chemical protective clothing. Also the thermal protection and heat transfer test results show that TPP and HTI is increased assured that the continued study on fire risk assessment & chemical resistance of chemical protective clothing fabrics will contribute to the upgrade the performances of chemical protective clothing fabrics.