• Title/Summary/Keyword: rat skin

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Effect of Vehicles and Enhancers on the in vitro Skin Penetration of Aspalatone and Its Enzymatic Degradation Across Rat Skins

  • Gwak, Hye-Sun;Chun, In-Koo
    • Archives of Pharmacal Research
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    • v.24 no.6
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    • pp.572-577
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    • 2001
  • The feasibility of skin penetration was studied for aspalatone (AM, acetylsalicylic acid maltol ester), a novel antithrombotic agent. In this studys hairless mouse dorsal skins were used as a model to select composition of vehicle and AM. Based on measurements of solubility and partition coefficient, the concentration of PC that showed the highest flux for AM across the hairless mouse skin was found to be 40%. The cumulative amount permeated at 48 h, however, appear inadequate, even when the PC concentration was employed. To identify a suitable absorption enhancer and its optimal concentration for AM, a number of absorption enhancers and a variety of concentration were screened for the increase in transdermal flux of AM. Amongst these, linoleic acid (LOA) at the concentration of 5% was found to have the largest enhancement factor (i.e., 132). However, a further increase in AM flux was not found in the fatty acid concentration greater than 5%, indicating the enhancement effect is in a bell-shaped currie. In a study of the effect of AM concentration on the permeation, there was no difference in the permeation rate between 0.5 and 1% for AM, below its saturated concentration. At the donor concentration of 2%, over the saturated condition, the flux of AM was markedly increased. A considerable degradation of AM was found during permeation studies, and the extent was correlated with protein concentrations in the epidermal and serosal extracts, and skin homogenates. In rat dorsal skins, the protein concentration decreased in the rank order of skin homogenate > serosal extract > epidermal extract. Estimated first order degradation rate constants were $6.15{\pm}0.14,{\;}0.57{\pm}0.02{\;}and{\;}0.011{\pm}{\;}0.004{\;}h^{-1}$ for skin homogenate, serosal extract and epidermal extract, respectively. Therefore, it appeared that AM was hydrolyzed to some extent into salicylmaltol by esterases in the dermal and subcutaneous tissues of skin. taken together, our data indicated that transdermal delivery of AM is feasible when the combination of PC and LOA is used as a vehicle. However, since AM is not metabolically stable, acceptable degradation inhibitors may be nervessary to fully realize the transdermal delivery of the drug.

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Effects of Skin Permeation for Rat of Thioglycolic Acid (티오글리콜산의 랫드 피부에 대한 투과 영향)

  • 정덕채;오세영;황성규
    • Journal of Environmental Health Sciences
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    • v.30 no.2
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    • pp.65-70
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    • 2004
  • Hair is based upon the skin which enroll the body of high living animals and have multiple membrane structure. This study were used rats and carried out to find out the effects of commercial permanent wave products to skin which are composed of thioglycolic acid and bases. Results were as follows. Permanent wave penetrated to 3 hours later with steady state in skins and was not significant changeable after 20hr later. In case of neutralizer with thioglycolic acid lag time and permeability coefficient in healthy skin were 3.38hr and 0.96$\mu\textrm{g}$/$\textrm{cm}^2$/hr, in old skin were 3.14hr and 0.l28$\mu\textrm{g}$/$\textrm{cm}^2$/hr, and in wounded skin were 3.08hr and 0.157$\mu\textrm{g}$/$\textrm{cm}^2$/hr. In conclusion, lag time and permeability coefficient in old skin and wounded skin were faster than healthy skin. In vivo which was studied by general time and method of permanent wave. We found out that fine rinkle and rash of skin were changeable in the case of treating with permanent wave drugs than normal skin. Also, permanent wave drugs could induced rash and eruption at the skin by the naked eye.

Microwave Hyperthermic Lipolysis Using External RF Antenna

  • Hwang, Joo-Sung;Woo, Tae-Hee;Park, Sang-Bok;Cheon, Chang-Yul
    • Journal of Electrical Engineering and Technology
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    • v.7 no.5
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    • pp.759-764
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    • 2012
  • In this paper, we propose a microwave hyperthermic lipolysis method to reduce subcutaneous fat without skin burn using external RF antenna. Since skin is closer to the antenna and has higher conductivity compared to the fat beneath, the temperature of the skin rises higher than that of the fat when the external antenna illuminates EM energy into a body, which may cause skin burn. In order to avoid the damages on skin, a skin cooling system is employed to the external antenna. The operating frequency is set at 5.8 GHz which is one of the ISM bands, to concentrate EM power efficiently on fat and not to heat up the muscle behind the fat. The operation time and RF power level has been determined based on experimental results with pork. The feasibility of the proposed method was shown by applying the method to the rat.

The Effects of Jowoongo on the artificial Wound on Rat skin (紫雲膏가 흰 쥐의 創傷에 미치는 效果)

  • Eo, Kyeong-Jeong;Ko, Woo-Shin;Kim, Young-Kyun
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.11 no.1
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    • pp.54-68
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    • 1998
  • The effects of Jawoongo on the Leukocyte Counts, Cortisol Level. CRP Level in the skin wounded rats. The results obtained as follows 1. On the Leukocyte counts in the skin wounded, sample Ⅰ, Ⅱ group were showed more significant effect than cotrol group. 2. On the Cortisol Level in the skin wounded, only sample Ⅲ group was showed continuous significant effect than control group. 3. On the CRP level in the skin wounded, sample Ⅰ, Ⅱ group were showed continuous significant effect but sample Ⅲ group was showed significant effect later on experiment. 4. On the Tissue staining in the skin wounded, was showed significant effect at all sample groups, especially sample Ⅱ,Ⅲ group of epidermis form were showed more significant effect after experimental eight days than control group. According to the above result, it is expected that Jawoongo can be applicable to the treatment of wound.

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Preclinical Study of DA-5018, a Non-narcotic Analgesic Agent

  • Kim, Soon-Hoe
    • Proceedings of the PSK Conference
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    • 2000.04a
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    • pp.70-81
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    • 2000
  • DA-5018 is a synthetic capsaicin derivative under development as a non-narcotic a analgesic ag$\varepsilon$nt. DA-50 18 showed a potent analgesic activity against acute and chronic pain m model(Tablel, 2.), but it had a narrow margin of safety. DA-5018 did not bind to opioid(${\kappa}, {\delta}, {\mu}$), NKl, CGRP receptors in vitro and its analgesic effect was not antagonized by naloxone, a and it did not develop analgesic tolerance. In addition DA-5018 had no inhibitory effects against c cyclooxygenase and 5-lipooxygenase activities. DA-5018 significantly increased the relcase of substance P from the slices of the rat spinal cord. These results suggest that DA-50 18 is not a narcotic nor aspirin-like analgesic and the release of substance P is one of analgesic mechanism of action of DA-5018. We found that DA-5018 was almost ten times more potent and was at l least IOO-times less irritable compared to capsaicin. Accordingly development of topical formula was adopted. Topical formula was desiged and screened by flux test of DA-5018 using hairless mouse skin and several formulas were selected. With these topical formulas we a assessed the analgesic efficacy and carried out the toxicity, skin irritation and pharmacokinetic studies. In streptozotocin-induced hyperalgesic rat and 50 % galactose-fed hyperalgesic rat as diabetic pain models, DA-5018 cream increased the pain thresh이ds up to 77.0% and 24.4% respectively, while Zostrix-HP(capsaicin cream) incr$\varepsilon$as cd by 65.9% and 21.0%. DA-5018 c cream showed a good analgesic effect as welI in FCA-induced arthritic rat. DA-5018 cream did not show any toxicological signs in acute and chronic toxicity test and had little skin irritation in car swclIing and scratching t$\varepsilon$st. Pharmacokinetics of DA-50 18 were studied after topical application of ${14}^C$-Iabelled or unlabelIed DA-5018 cream. Plasma and skin concentrations c except applied skin wcre below the dctection limit and after 7-day cummulative application, plasma concentrations were also below detection limit DA-50 18 may have an advantag$\varepsilon$ ov$\varepsilon$r c capsaicin and is now being developed as a topical agent for the treatment of pains. DA-50 18 cream was approved for Korean IND and is now under a Phase II clinical study for arthritic pain a after finising Phase I study. DA-50 18 was also liscensed out to Stiefel Company in America in

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Effect of Mixture of p-Phenylenediamine with Hydrogen Peroxide to Rat Skin (p-Phenylenediamine과 과산화수소 혼합액 도포가 흰쥐 피부조직에 미치는 영향)

  • Lee, Sang-Hee;Lee, Sang-Il
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.35 no.8
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    • pp.1010-1015
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    • 2006
  • p-Pheylenediamimine (PPD) is one of hair dye's ingredients, and the mixture of PPD with hydrogen peroxide is generally used to dye hair at beauty shop. This study is conducted to investigate the effect of oxidized PPD on rat skin. 6% hydrogen peroxide, PPD (5% PPD in 2% $NH_4OH$) or the mixture (isovolumed mixture of 5% PPD and 6% hydrogen peroxide in 2% $NH_4OH$) was applied to rat skin ($25\;mg/16.5\;cm^2$) five times every other day. The activity of acid phosphatase (ACP) was more increased in the mixture of PPD with hydrogen peroxide applied group than PPD applied group. Furthermore, the activity of glucose 6-phosphatase (G6Pase) in the mixture of PPD with hydrogen peroxide applied group showed higher decreasing rate than that of PPD applied group. In histopathological findings, the mixed PPD with hydrogen peroxide applied group showed more thickening of epithelium, increased numbers of dermal fibroblasts, and the dilatation of dermal capillaries than PPD applied group. The significant increasing of xanthine oxidase (XO) activity was determined in mixture of PPD with hydrogen peroxide applied group compared with PPD applied group. However, reactive oxygen species (ROS) scavenging system, the activities of superoxide dismutase (SOD) and glutathione S-transferase (GST) were more significantly decreased in mixed PPD with hydrogen peroxide applied groups than in PPD applied group. In conclusion, topical application with the mixture of PPD with hydrogen peroxide compared with PPD application resulted in imbalance with ROS generating and scavenging which probably led to severe skin injury.

Effect of fractional ablative carbon dioxide laser with lidocaine spray on skin flap survival in rats

  • Choi, Manki;Park, Youngsoo;Kim, Yong-Ha;Chung, Kyu Jin
    • Archives of Craniofacial Surgery
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    • v.20 no.4
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    • pp.239-245
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    • 2019
  • Background: Lidocaine spray is a local anesthetic that improves random-pattern skin flap survival. The fractional ablative carbon dioxide laser (FxCL) produces vertical microchannels that delivers topically applied drugs to the skin. In this study, we hypothesized that FxCL therapy would enhance the lidocaine effect to improve random-pattern skin flap survival in rats. Methods: McFarlane random-pattern skin flaps were elevated in 48 rats, which were divided into four groups according to treatment: FxCL+lidocaine, FxCL, lidocaine, and nontreatment (control). On postoperative day 7, necrotic flap areas, the number of capillary vessels, and neutrophil count were evaluated. Anti-rat vascular endothelial growth factor (VEGF) and CD31 antibody activity were also evaluated by immunohistochemical staining. Results: Flap survival rate was $53.41%{\pm}5.43%$, $58.16%{\pm}4.80%$, $57.08%{\pm}5.91%$, and $69.08%{\pm}3.20%$ in the control, lidocaine, FxCL, and FxCL+lidocaine groups, respectively. Mean neutrophil count in the intermediate zone excluding the necrotic tissue was $41.70{\pm}8.40$, $35.43{\pm}6.41$, $37.23{\pm}7.15$, and $27.20{\pm}4.24cells/field$ in the control, lidocaine, FxCL, and FxCL+lidocaine groups, respectively. Anti-rat VEGF and CD31 antibody activity were the highest in the FxCL+lidocaine group. Conclusion: FxCL with lidocaine had a positive effect on random-pattern skin flap survival in rats. Thus, FxCL with lidocaine spray should be considered as a new treatment option to improve flap viability.

Body Distribution of $^{125}I-rhEGF$ Across Normal and Damaged Rat Skins (정상 및 손상된 흰쥐 피부에 국소 적용된 $^{125}I-rhEGF$의 체내 이행)

  • Lee, Jeong-Uk;Chung, Suk-Jae;Lee, Min-Hwa;Shim, Chang-Koo
    • YAKHAK HOEJI
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    • v.41 no.6
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    • pp.730-736
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    • 1997
  • Distribution of radioactivity in the skin tissues, subcutaneous tissues, blood and body organs was examined following topical application of $^{125}I-rhEGF$(0.4 ${\mu}Ci$), in the form of a Pluronic F-127 gel, on the normal and damaged (burned and stripped) skins of SD male rats. The radioactivity in the skin tissues and subcutaneous tissues was 3-5 times higher for the damaged skins than for the normal skin. But pretreatment of the skin with rhEGF (1${\mu}g$)) twice at 24 hr dose intervals affected the distribution of the radioactivity yielding the order of burned skin> stripped skin=normal skin. The decrease for the stripped skin by the pretreatment might be related either to the pathophysiological change of the skin or to the down regulation of the EGF receptor. Liver showed the highest radioactivity in amount following single and multiple administration of the drug to the normal and damaged skins. But,in concentration, the kidney and stomach showed higher value than the liver which is consistent with that kidney is a major eliminating organ of EGF and that EGF exerts its pharmacological effect specifically for the stomach.

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Grape skin improves antioxidant capacity in rats fed a high fat diet

  • Lee, Su-Jin;Choi, Soo-Kyong;Seo, Jung-Sook
    • Nutrition Research and Practice
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    • v.3 no.4
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    • pp.279-285
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    • 2009
  • This study was conducted to investigate the effect of dietary grape skin on lipid peroxidation and antioxidant defense system in rats fed high fat diet. The Sprague-Dawley rats were fed either control (5% fat) diet or high fat (25% fat) diet which was based on AIN-93 diet for 2 weeks, and then they were grouped as control group (C), control + 5% grape skin group (CS), high-fat group (HF), high fat + 5% grape skin group (HFS) with 10 rats each and fed corresponding diets for 4 weeks. The hepatic thiobarbituric acid reacting substances (TBARS) were increased in high fat group as compared with control group, but reduced by grape skin. The serum total antioxidant status, and activities of hepatic catalase and superoxide dismutase, xanthine oxidase and glucose-6-phosphatase were increased by supplementation of grape skin. Glutathione peroxidase activity was significantly higher in CS group than in C group. Grape skin feeding tended to increase the concentration of total glutathione, especially in control group. The ratio of reduced glutathione to oxidized glutathione was lower in high fat groups than in control groups. The ratio was increased by dietary supplementation of grape skin in control group. These results suggest that dietary supplementation of grape skin would be effective on protection of oxidative damage by lipid peroxidation through improvement of antioxidant defense system in rats fed high fat diet as well as rats with low fat diet.

Enhanced In Vitro Skin Deposition Properties of Retinyl Palmitate through Its Stabilization by Pectin

  • Suh, Dong-Churl;Kim, Yeongseok;Kim, Hyeongmin;Ro, Jieun;Cho, Seong-Wan;Yun, Gyiae;Choi, Sung-Up;Lee, Jaehwi
    • Biomolecules & Therapeutics
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    • v.22 no.1
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    • pp.73-77
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    • 2014
  • The purpose of this study was to examine the effect of stabilization of retinyl palmitate (RP) on its skin permeation and distribution profiles. Skin permeation and distribution study were performed using Franz diffusion cells along with rat dorsal skin, and the effect of drug concentration and the addition of pectin on skin deposition profiles of RP was observed. The skin distribution of RP increased in a concentration dependent manner and the formulations containing 0.5 and 1 mg of pectin demonstrated significantly increased RP distributions in the epidermis. Furthermore, it was found that skin distribution of RP could be further improved by combined use of pectin and ascorbyl palmitate (AP), due largely to their anti-oxidative effect. These results clearly demonstrate that the skin deposition properties of RP can be improved by stabilizing RP with pectin. Therefore, it is strongly suggested that pectin could be used in the pharmaceutical and cosmetic formulations as an efficient stabilizing agent and as skin penetration modulator.