• Title/Summary/Keyword: 피부투과

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Preparation and Skin Permeation of Poloxamer 407 Hydrogel with Extract of Centella $asiatica-{\beta}-Cyclodextrin$ Solid Dispersion System (병풀(Centella asiatica) 엑스-베타시클로덱스트린 고체 분산체를 함유한 폴록사머 407 히드로겔 제조 및 피부투과)

  • Kim, Kyoung-Kook;Kwak, Eun-Sun;Lee, Gye-Won;Park, Jin-Kyu;Park, Mork-Soon;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.28 no.1
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    • pp.15-23
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    • 1998
  • Extract of Centella asiatica(ECA), which is poorly water-soluble extract from the Centella asiatica is known to express excellent wound healing properties. $ECA-{\beta}-cyclodextrin$ $(asiaticoside-{\beta}-cyclodextrin\;and\;genin-{\beta}-cyc1odextrin)$ solid dispersion system, which was prepared by freezedrying method, was formulated as gels containing poloxamer 407 and propylene glycol, and evaluated with respect to their viscosity, stability, skin permeation and drug amount in the skin of hairless mouse. The average molar ratio $asiaticoside-{\beta}-CD$ and $genin-{\beta}-CD$ was 1:1.7 and 1:22, respectively. When the molar ratio of genin and ${\beta}-CD$ was 1:5, madecassic acid made 100% solid dispersion system and asiatic acid about 65%. In dissolution study, >99% of asiaticoside from $asiaticoside-{\beta}-CD$ was dissolved in 5 minutes, and >99% madecassic acid and >64% asiatic acid from $genin-{\beta}-CD$. The apparent viscosity of poloxamer 407 gels with $ECA-{\beta}-CD$ solid dispersion system increased in proportion to poloxamer 407 and propylene glycol concentration. In the accelerated stability test, all $ECA-{\beta}-CD$ poloxamer 407 gels showed that asiaticoside was most stable and madecassic acid stable and asiatic acid similar to stability of gel with free ECA. The permeation amount of asiaticoside in poloxamer gels through hairless mouse skin decreased as the concentration of poloxamer 407 increased. When propylene glycol was added at the level of 10%, the permeation amount of asiaticoside at poloxamer gels through hairless mouse skin increased but from 15% it decreased. The permeation of asiaticoside into the skin of hairless mouse was estimated to be about $0.10\;{\mu}g/cm^2$.

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The Effect of Hydroalcoholic Gel System on Skin Permeation of Piroxicam and its Anti-inflammatory Activity (피록시캄의 피부투과 및 소염효력에 대한 알코올성 하이드로겔 시스템의 영향)

  • Ki, Min-Hyo;Shin, Hee-Jong;Lee, Kang-Woo;Kim, Jae-Wook;Kim, Jung-Woo;Hong, Chung-Il
    • Journal of Pharmaceutical Investigation
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    • v.29 no.3
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    • pp.217-225
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    • 1999
  • These studies were designed to determine the effect of hydroalcoholic gel system (lower alkanol concentration: 40-60%) compared to general hydrogel system (lower alkanol concentration: 10-35%) on transdermal delivery of piroxicam and its anti-inflammatory activity. Piroxicam was incorporated into a hydroalcoholic gel and a hydrogel containing polymers, solvents, and cosolvents. The pH of gel was about 6.3-7.3 and the solvent mixtures were composed of water and various concentrations of ethanol (35, 40, 50, and 60%). For the in vitro study, the skin permeation of piroxicam from the gel formulations was investigated using Franz modified diffusion cells fitted with hairless mouse skin. For the in vivo study, the anti-inflammatory activity of hydroalcoholic gel was compared to other commercial products (piroxicam hydrogel and ketoprofen hydrogel) in rat and human. The anti-inflammatory activity was determined using carrageenan induced foot edema model in rat. For the clinical study, it was evaluated from determining efficacy and acceptability with 98 patients suffering from musculoskeletal pain. A novel piroxicam hydroalcoholic gel was successfully formulated in the range of 40-50% of ethanol as solvent, more than 10% of propylene glycol, 5% of $Transcutol^{\circledR}$ and 1 % of benzyl alcohol. The skin permeation of piroxicam using hydroalcoholic gel system was greater than that of general hydrogel system $(flux\;:\;139.1-148.2\;{\mu}g/cm^2/hr\;vs.43.0-84.5 {\mu}g/cm^2/hr)$ in vitro. In carrageenan-induced edema model, the anti-inflammatory activity of hydroalcoholic gel was better than that of piroxicam hydrogel for edema inhibition (75.1 % vs. 62.9%, p

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Preparation and Characterization of Lipid Nanoparticles Containing Fat-Soluble Vitamin C Derivatives and Gallic Acid (지용성 비타민 C 유도체 및 갈릭산을 함유한 지질나노입자 제조 및 특성)

  • Ji Soo Ryu;Ja In Kim;Jae Yong Seo;Young-Ah Park;Yu-Jin Kang;Ji Soo Han;Jin Woong Kim
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.50 no.2
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    • pp.103-110
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    • 2024
  • Lipid nanoparticles (LNPs) are a stable and an effective system that protects cell-impermeable biologically active compounds such as nucleic acids, proteins, and peptides against degradation caused by subtle environmental changes. This study focuses on developing LNPs encapsulating gallic acid (GA), an antioxidant, to effectively prolong the half-life of tetrahexyldecyl ascorbate (THDC), a oil-soluble vitamin C derivative. These LNPs were synthesized in small, uniform sizes at room temperature and pressure conditions using a microfluidics chip. Compared to liposomes manufactured under high pressure and high temperature conditions through conventional microfluidizers, LNPs manufactured through microfluidics chips had excellent dispersion and temperature stability, and improved skin absorption as well as improved oxidative stability of fat-soluble vitamin C derivatives. Future studies will focus on ex vivo and in vivo evaluations to study skin improvement to further validate these results.

In vitro Rat Skin Permeation of Various NSAIDs (다양한 비스테로이드성 소염진통제의 쥐 피부 투과)

  • Kim, Min-Jung;Doh, Hea-Jeong;Cho, Won-Jea;Yong, Chul-Soon;Choi, Han-Gon;Lee, Chi-Ho;Kim, Dae-Duk
    • Journal of Pharmaceutical Investigation
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    • v.32 no.4
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    • pp.313-319
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    • 2002
  • Rat skin permeation of various nonsteroidal antiinflammatory drugs (NSAIDs) was investigated in vitro using Franz diffusion cell at $37^{\circ}C$. The effect of various skin permeation enhancers was also observed as a preliminary study of developing transdermal delivery systems of NSAIDs. Lipophilicity of NSAIDs was determined from thε partition coefficient (log P) in 1-octanol/water and 1-octanol/IPB mutual-saturated solutions. The solubility was determined in water, isotonic phosphate buffer (IPB), and propylene glycol (PG) at $37^{\circ}C$. The rat skin permeation rate of acetaminophen, piroxicam, and aceclofenac was almost negligible, although they were saturated in PG. Addition of 1 % permeation enhancer increased the permeation rate of ketoprofen, ketorolac, and diclofenac. However, the skin permeation rate of ibuprofen did not increase with the addition of various enhancers. Among the permeation enhancers testεd, oleic acid was the most effective for various NSAIDs. Based on the daily dose, lipophilicity, and the skin permeation ratε achieved in this study, ketoprofen and ketorolac seem to be the most promising drug candidates for transdermal delivery systems, especially when formulated with unsaturated fatty acids, such as oleic acid.

Development of Bioavailability Enhancement System for the Skin Permeation Promotion of Psolarea corylifolia Extract (보골지 추출물의 피부 투과 촉진 시스템 개발)

  • Cho, Young-Ho;Ahn, Ghe-Whan;Yang, Seung-Won;Cho, Kwan-Hyun;Kim, Sang-Won;Baek, Ki-Myoung;Lee, Gye-Won
    • KSBB Journal
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    • v.26 no.6
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    • pp.505-512
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    • 2011
  • Psolarea corylifolia extract that contains bakuchiol is known to have anti-microbial, anti-inflammatory and anti-scarring effects. In this study, a vesicles such as liposome, niosome, and transfersome were produced to encapsulate P. corylifolia extract and measured their stability and physiochemical property. The skin permeation and partitioning of P. corylifolia extract in the vesicles were elucidated in nude mouse skin by using Franz diffusion cells after topical application for 24 h. After storage at 25, 40, $70^{\circ}C$, and light, the stability of bakuchiol incorporated into the vesicles was maintained for 30 days. The optimal concentration of P. corylifolia extract entrapped into the vesicles was found to be 5~10%. From the physicochemical studies, after storage at 4, 25, and $40^{\circ}C$, the viscosity and particle size of the vesicles remained in 30~80 cP and the nanosize range for 6 months, respectively. From the permeation experiments, niosome showed a higher amount of bakuchiol permeated through the mouse skin compared to liposome and transfersome after 24 h. From these results, niosome and transfersome could be a good bioavailability enhancement system (BAES) for P. corylifolia extract to improve the skin permeation and stability.

Study of Microwave Propagation Characteristics of Matching Liquids for the Microwave Cancer Detection System (유방암 진단 시스템을 위한 정합 액체의 전파 특성에 관한 연구)

  • Kim, Jang-Yeol;Minz, Laxmikant;Lee, Kwang-Jae;Son, Seong-Ho;Jeon, Soon-Ik
    • The Journal of Korean Institute of Electromagnetic Engineering and Science
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    • v.25 no.4
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    • pp.442-450
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    • 2014
  • This paper is a study of the propagation characteristic of matching liquids in the skin-covered breast model. In order to evaluate the matching liquids, we investigated six kinds of matching liquids applied to proposed 1-D breast model from frequency range of 3~6 GHz. A uniform plane wave is projected / transmitted inside the multi-layered breast model. Then the propagation characteristics inside the model and the transmission loss of each matching liquids were analyzed. The studying method presented in the paper can be used in the breast cancer detection system, the field of cancer detection using human tissue and the field of other medical devices. This paper was applied to the breast cancer detection system. Consequently, these studies could be used to determine the suitable type of matching liquids for breast cancer detection system and to apply useful for performance analysis.

Permeation Characteristics of Hazardous Substances in Tattoo Dye using Franz Diffusion Cells (Franz Diffusion Cell을 이용한 문신용 염료 내 유해물질의 피부 투과특성 연구)

  • Park, Kyo-Hyun;Jung, Se-Hoon;Shin, Ho-Sang;Kim, Bae-Hwan
    • Journal of Environmental Health Sciences
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    • v.42 no.1
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    • pp.61-70
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    • 2016
  • Objectives: The purpose of this study is to determine the exposure risk to tattoo components by analyzing skin absorption using the in vitro method. Tattoos are commonly used for cosmetic purposes, and the skin of not only the operator but of the people who are undergoing the cosmetic procedure is continuously exposed to hazardous chemicals. Methods: Skin permeation risk determination was conducted by the in vitro Franz diffusion cell method according to the ingredient types of tattoo dyes, such as volatile organic compounds (VOCs), non-volatile organic compounds and heavy metals, using hairless mouse full skin and human cadaver epidermis. Results: The major components with good skin penetration for each type of tattoo dye ingredient were clarified. Among the tatto dye ingredients, 1,2-Dichlorobenzene, Zn, Al, Pb and Ti showed good skin penetration. Most of the skin transmission rates were higher in hairless mouse full skin than in human cadaver epidermis. Conclusion: A possible exposure risk to hazardous substances in tattoo dyes was confirmed from this study. These results are expected to provide a positive contribution to the establishment of management regulations for tattoo dyes.

Enhanced Penetration of Loxoprofen across Excised Guinea Pig Skin from Solution Formulations (용액 처방으로부터 록소프로펜의 기니아픽 피부 투과 증진)

  • Kim, Tae-Sung;Chun, In-Koo
    • Journal of Pharmaceutical Investigation
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    • v.31 no.4
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    • pp.217-224
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    • 2001
  • To develop a novel transdermal delivery system of loxoprofen (LP), a potent antiinflammatory and analgesic agent, the effects of various vehicles and penetration enhancers on the skin permeation of LP from solution formulations were investigated. The permeation rate of LP through excised guinea pig skin was measured using a side-by-side permeation system at $32^{\circ}C$. The solubilities of LP in various vehicles were determined by the equilibrium solubility method, and partition coefficients $(P_c)$ were determined. The solubility of LP increased in the rank order of water & isopropyl myristate (IPM) & glyceryl dicaprylate/dicaprate & propylene glycol dicaprylate/caprate & propylene glycol laurate (PGL) & polyethylene glycol 400 & diethylene glycol monoethyl ether (DGME) & ethanol. n-Octanol-water $P_c$ value was 15.5. Among pure vehicles tested, IPM and PGL showed highest fluxes of $89.9{\pm}5.0$ and $45.4{\pm}0.3\;{\mu}g/cm^2/hr$ from saturated solutions, respectively. However, it was not possible to demonstrate any correlation between the solubility of LP and its permeation rate, indicating the change in the barrier property of the skin and/or carrier mechanisms by vehicles tested. The addition of DGME to IPM or PGL markedly increased the solubility of LP, but the permeation rate did not decrease when the concentration of DGME in the cosolvent was increased upto 40%. The addition of linoleic acid (3%) in the cosolvent slightly increased the permeation rate, but others such as lauroyl sarcosine, fatty alcohols and fatty acids tested did not show enhancing effect. In conclusion, the DGME-IPM or DGME-PGL cosolvent system proved to be a good vehicle to enhance the skin permeation of LP.

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Skin Penetration and Localization Characteristics of Lipogel Containing Ascorbyl Palmitate (아스코르빈산 팔미테이트를 함유한 리포겔의 피부 투과 및 잔류 특성)

  • Lee, Sang-Kil;Woo, Hye-Seoung;Lee, Yeon-Ah;Kwon, Yong-Nam;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.31 no.4
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    • pp.225-232
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    • 2001
  • The present study was carried out to observe the effect of liposome dispersed gel formulation (Lipogel) on topical delivery of ascorbyl palmitate (AsP). Neutral and negatively charged MLV liposomes containing AsP were prepared with dimyristoylphosphadtidylcholine (DMPC) and dicetyl phosphate (DCP), and dispersed to poloxamer gel matrix. In the hydrolysis study in rat's skin homogenates, AsP hydrolyzed to ascorbic acid (AsA) according to the first-order kinetics with the rate constant of $2.46{\times}10^{-2}\;min^{-1}$. In the passive skin penetration study using Franz diffusion cell, lipogel systems exhibited the greater values in the flux $(J_s)$ and the amount penetrated $(Q_p)$ compared to control hydrogels containing diethyleneglycol monoethyl ether $(Transcutol^{\circledR})$ as a solubilizing agent and a penetration enhancer for AsP. The total amount penetrated $(Q_{Total})$, which is expressed as a summation of $Q_P\;and\;Q_L$, for lipogel system was about 1.4 times higher in average than that of control hydrogel. However the amount localized in the skin $(Q_L)$ was similar in both formulations. As a result, lipogel system enhanced the skin penetration of AsP, possibly due to the increase in local concentration of AsP by preferential adsorption of liposome to the skin and the enhancing effect of phospholipid in liposome composition. Moreover it was expected that the penetrated AsP would generate AsA during skin penetration by the skin esterase. In conclusion, lipogel formulation was considered as a good candidate for topical delivery of AsP.

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Percutaneous Absorption Characteristics of Antidepressant Paroxetine (항우울제인 Paroxetine의 피부 투과 특성 연구)

  • Jung, Duck-Chae;Hwang, Sung-Kwy;Oh, Se-Young
    • Journal of the Korean Applied Science and Technology
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    • v.28 no.2
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    • pp.170-177
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    • 2011
  • Transdermal drug delivery(TDS) offers many important advantages. For instance, it is easy and painless, it protects the active compound from gastric enzymes, and it avoids the hepatic first-pass effect. Also, it is simple to terminate the therapy if any adverse or undesired effect occurs. But skin is a natural barrier, and only a few drugs can penetrate the skin easily and in sufficient quantities to be effective. Therefore, in recent years, numerous studies have been conducted in the area of penetration enhancement. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other method of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stopped if the drug dosage lead to side effect. Polysaccharide, such as xanthan gum and algin were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers and drug contents. Among these polysaccharide, the permeation rate of Paroxetine such as lipophilic drug was the fastest in xanthan gum matrix in vitro. We used glycerin, PEG400 and PEG800 as enhancers. Since dermis has more water content(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when PEG400 was more effective for lipophilic drug. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate.