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

• Korean Journal of Pharmacognosy
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• v.49 no.3
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• pp.246-254
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• 2018

Pectin lyase-modified red ginseng extract (GS-E3D) is a newly developed ginsenoside Rd-enriched ginseng extract. This study was designed to investigate the skin safety of GS-E3D. Single oral toxicity, single dermal toxicity, bovine corneal opacity and permeability (BCOP) assay, skin irritation test with $SkinEthic^{TM}$ human epidermis model, skin sensitization local lymph node assay, and human patch test, were examined. The oral and dermal $LD_{50}$ value of GS-E3D was over 2,000 mg/kg in rats. GS-E3D was identified as a non-irritant to skin in BCOP assay, human epidermis models, and patch test from the 32 human subjects. The skin sensitization potential of GS-E3D was less than 25% in local lymph node assay. These results indicate that GS-E3D can be used as a safe ingredient without adverse effects in various skin care products.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.234.1-234.1
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• 2003

The effects of vehicles and penetration enhancers on the in vitro permeation of ketorolac tromethamine (KT) across excised hairless mouse skins were investigated. Among pure vehicles examined, propylene glycol monolaurate (PGML) showed the highest permeation flux, which was 94.3${\pm}$17.3 mg/cm$^2$/hr. Even though propylene glycol monocaprylate (PGMC) alone did not show high permeation rate, the skin permeability of DT was markedly increased by the addition of diethylene glycol monoethyl ether (DGME); the enhancement factors were 19.0 and 17.1 at 20 and 40% of DGME, respectively. (omitted)

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

• Journal of Magnetics
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• v.6 no.1
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• pp.9-12
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• 2001

The dependence of the magnetoimpedance effect (MI) on magnetic properties has been investigated in mumetal thin films prepared by rf magnetron sputtering. Coercivity of thin films prepared at 400 W was about 0.4 Oe, and the magnetic anisotropy field of films deposited under a uniaxial magnetic field decreased with increasing film thickness. The saturation magnetization of mumetal films increased with rising input power and thickness and was smaller than that of permalloy films. Transverse incremental Permeability (TPR) of films of 1$\mu m$ thick increased with increasing effective permeability. The magneto impedance ratio (MIR) was proportional to TPR in films 1$\mu m$ thick but in spite of lower effective permeability at higher thicknesses, MIR increased due to skin effect. The height of the double peaks in the MIR curves decreased with decreasing anisotropy and thickness. The maximum MIR value for a 4$\mu m$ thick 75% at 36.5 MHz.

• YAKHAK HOEJI
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• v.47 no.3
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• pp.154-158
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• 2003

Lincomycin, a selective tyrosinase blocker, has been thought to be effective in the treatment of melanogenesis, ephelis, post inflammatory pigmentation, and facial discoloration. In an attempt to develop a transdermal perparation for lincomycin, this study was designed to examine the appropriate contents of various surfactants and ethanol in the cream preparation. Frans type diffusion cell was used to investigate permeation efficiency of the preparation, and lincomycin in the receptor phase was measured by HPLC. After having a 1.5 hrs of leg time, the permeability of lincomycin was rapidly increased by adding surfactants, and varied with different types of surfactants after 10 hrs, the permeability of Brij 56$^{(R)}$ preparation (501.4$\pm$45 $\mu\textrm{g}$/mι) was greater than that either of Labrasol$^{(R)}$ (263.9$\pm$33.7 $\mu\textrm{g}$/mι) or Tween$^{(R)}$20(386.2$\pm$26.7 $\mu\textrm{g}$/mι). Ethanol also increased the permeability of lincomycin.mycin.

• Archives of Pharmacal Research
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• v.28 no.1
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• pp.111-114
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• 2005

The antihistamine effects of the triprolidine were studied in rats to determine the feasibility of their enhanced transdermal delivery from the poly (4-methyl-1-pentene) (TPX) matrix system containing penetration enhancer and plasticizer. The antihistamine effects were determined by the Evans blue dye procedure by comparing the changes in vascular permeability increase following the transdermal administration. The vascular permeability increase was significantly reduced by transdermal administration of the triprolidine-TPX system containing triethyl citrate (TEC) and polyoxyethylene-2-oleyl ether (POE). Both the plasticizer and penetration enhancer played an important role in the skin permeation of triprolidine and increased the antihistamine effects. These results showed that the triprolidine-TPX matrix system containing plasticizer and penetration enhancer could be a transdermal delivery system providing the increased antihistamine effects.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.29 no.2 s.43
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• pp.205-232
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• 2003

Ursolic acid (UA) and Oleanolic acid (ONA), known as urson, micromerol and malol, are pentacyclic triterpenoid compounds which naturally occur in a large number of vegetarian foods, medicinal herbs, and plants. They may occur in their free acid form or as aglycones for triterpenoid saponins, which are comprised of a triterpenoid aglycone, linked to one or more sugar moieties. Therefore UA and ONA are similar in pharmacological activity. Lately scientific research, which led to the identification of UA and ONA, revealed that several pharmacological effects, such as antitumor, hepato-protective, anti-inflammatory, anticarcinogenic, antimicrobial, and anti-hyperlipidemic could be attributed to UA and ONA. Here, we introduced the effect of UA and ONA on acutely barrier disrupted and normal hairless mouse skin. To evaluate the effects of UA and ONA on epidermal permeability barrier recovery, both flanks of 8-12 week-old hairless mice were topically treated with either 0.01-0.1 mg/ml UA or 0.1-1 mg/ml ONA after tape stripping, and TEWL (Transepidermal water loss) was measured . The recovery rate increased in those UA or ONA treated groups (0.1 mg/ml UA and 0.5 mg/ml ONA) at 6 h more than $20\%$ compared to vehicle treated group (p<0.05). Here, we introduced the effects of UA and ONA on acute barrier disruption and normal epidermal permeability barrier function. For verifying the effects of UA and ONA on normal epidermal barrier, hydration and TEWL were measured for 1 and 3 weeks after UA and ONA applications (2mg/ml per day). We also investigated the features of epidermis and dermis using electron microscopy (EM) and light microscopy (LM). Both samples increased hydration compared to vehicle group from f week without TEWL alteration (p<0.005). EM examination using RuO4 and OsO4 fixation revealed that secretion and numbers of lamellar bodies and complete formation of lipid bilayers were most prominent $(ONA{\geq}UA>Vehicle)$. LM finding showed that thickness of stratum corneum (SC) was slightly increased and especially epidermal thickening and flattening was observed (UA>ONA>Veh). We also observed that UA and ONA stimulate epidermal keratinocyte differentiation via $PPAR\;\alpha$. Protein expression of involucrin, loricrin, and filaggrin increased at least 2 and 3 fold in HaCaT cells treated with either $ONA\;(10{\mu}M)$ or UA $(10{\mu}M)$ for 24h respectively. This result suggested that the UA and ONA can improve epidermal permeability barrier function and induce the epidermal keratinocyte differentiation via $PPAR\;{\alpha}$. Using Masson-trichrome and elastic fiber staining, we observed collagen thickening and elastic fiber elongation by UA and ONA treatments. In vitro results of collagen and elastin synthesis and elastase inhibitory activity measurements were also confirmed in vivo findings. These data suggested that the effects of UA and ONA related to not only epidermal permeability barrier functions but also dermal collagen and elastic fiber synthesis. Taken together, UA and ONA can be relevant candidates to improve epidermal and dermal functions and pertinent agents for cosmeseutical applications.

• Korean Chemical Engineering Research
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• v.58 no.1
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• pp.29-35
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• 2020

In this study, the skin permeability was measured by adding cell penetrating peptides, arginine oligomers; (tetra-D-arginine (R4) and hexa-D-arginine (R6)) to little skin-permeable anti-wrinkle peptides (GHK, GHK-Cu, and Pal-GHK), and the results were analyzed by the following six cases. First, in cases where only anti-wrinkle peptides were contained, copper ions (Cu₂⁺) and palmitic acid enhanced the transdermal permeability. Second, when arginine oligomers (R4, R6) were added to GHK, arginine oligomers (R4, R6) increased percutaneous permeability, and R4 showed better percutaneous permeability. Third, the addition of R4 and R6 to GHK-Cu resulted in increased percutaneous transmittance, followed by R6 < R4 percutaneous transmittance. Fourth, when R4 and R6 were added to Pal-GHK, the percutaneous permeability increased with results in R6 < R4 order. Fifth, when R4 was added to GHK, GHK-Cu, and Pal-GHK, the transdermal permeability increased in the order of GHK+R4 < GHK-Cu+R4 < Pal-GHK+R4. Finally, the addition of R6 to GHK, GHK-Cu and Pal-GHK also resulted in increased percutaneous transmittance in the order of GHK+R4 < GHK-Cu+R4 < Pal-GHK+R4. This study provides optimal conditions for enhancing skin absorption of anti-wrinkle peptides GHK, GHK-Cu, and Pal-GHK, and propose a wide range of applications in anti-wrinkle functional cosmetics by suggesting ways to maximize their efficacy.

• Journal of Physiology & Pathology in Korean Medicine
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• v.32 no.6
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• pp.384-395
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• 2018

The aim of this study was to investigate whether a novel formulation of an herbal extracts has an inhibitory effect on obesity. To determine its anti-obesity effects, we performed anti-obesity-related experiments in vitro and in vivo. Thus, our present study was carried out to evaluate the anti-obesity effect of herbal extracts using a high fat diet (HFD)-induced obese mouse model and 3T3-L1 adipose cells. The effects of each herbal extracts on lipid accumulation in 3T3-L1 cells were examined using Oil Red O staining. Results showed that treatment with each herbal extracts at $10{\sim}100{\mu}g/ml$ had no effect on cell morphology and viability. Without evidence of toxicity, herbal extracts treatment decreased lipid accumulation compared with the untreated adipocytes controls as shown by the lower absorbance of Oil Red O stain. Futhermore, compared with control-differentiated mature adipocytes, each herbal extracts significantly inhibited lipid accumulation in mature 3T3-L1 adipocytes. In the HFD-fed obese mice, body weight, liver weight and white adipose tissue weights were significantly reduced by mixture of herbal extracts administration in mouse skin. Futhermore, we found that mixture of herbal extracts administration suppressed serum triglyceride (TG), and total cholesterol (TCHO) in HFD-induced obese mouse model. The mixture of herbal extracts of permeability was estimated by measuring the transepithelial electrical resistance (TEER) value in pig skin. The optimized formulations of herbal extracts (Test 3 formulation) showed skin permeation. However, test 1 formulation containing essential oil as enhancer showed maximum skin permeation. After confirming the enhanced skin permeability, in vivo studies were performed to assess whether skin irritation potential on the basis of a primary irritation index (PII) in rabbit skin. Reactions were scored for erythema/edema reactions at 24 h, 48 h and 72 h post-application. It was concluded that the test 1 formulation was not irritation (PII = 0). The present study suggests that the test 1 formulation might be of therapeutic interest with respect to the treatment of obesity.