• Title/Summary/Keyword: Skin Permeation

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The Effect of Methylsulfonylmethane on Hair Growth Promotion of Magnesium Ascorbyl Phosphate for the Treatment of Alopecia

  • Shanmugam, Srinivasan;Baskaran, Rengarajan;Nagayya-Sriraman, Santhoshkumar;Yong, Chul-Soon;Choi, Han-Gon;Woo, Jong-Soo;Yoo, Bong-Kyu
    • Biomolecules & Therapeutics
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    • v.17 no.3
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    • pp.241-248
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    • 2009
  • The purpose of this study was to evaluate the effect of methylsulfonylmethane (MSM) on hair growth promotion of magnesium ascorbyl phosphate (MAP) for the treatment of alopecia. Aqueous solutions of MAP 7.5% with or without MSM 1%, 5% or 10% were prepared and applied onto the depilated back skin of the male mice once a day for 20 days. The degree of hair growth was evaluated by visual scoring using hair growth quantification scale (0-5, 0 being initial state and 5 being complete hair growth). In vitro transdermal penetration and intradermal retention studies of MAP were performed with Franz diffusion cell using hairless mice skin. Hair growth in the group treated with the aqueous solution containing MAP 7.5% and MSM 10% was comparable to or better than the result in the group treated with minoxidil 5% solution. Hair growth promotion of MAP was dose-dependently increased by the presence of MSM used in combination with MAP 7.5% solution. The in vitro transdermal penetration of the MAP was decreased in proportion to the concentration of MSM. However, intradermal retention of MAP was profoundly and dose-proportionally increased as a function of MSM concentration, reaching 802 ${\mu}g/cm^2$ in the presence of MSM 10% (200-fold increase). The effect of MSM on hair growth promotion of MAP was dose-proportional to the concentration of MSM due to the enhanced intradermal retention of MAP in the presence of MSM. Therefore, topical application of MAP together with MSM appears to be useful for the treatment of alopecia.

Effect of Toluene Added to Casting Solution on Characteristic of Phase Inversion Polysulfone Membrane (상전환 공정에 의한 폴리설폰막의 제조에 있어 제막용액에 첨가된 톨루엔의 영향)

  • Choi, Seung-Rag;Park, So-Jin;Seo, Bum-Kyoung;Lee, Kune Woo;Han, Myeong-Jin
    • Applied Chemistry for Engineering
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    • v.19 no.6
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    • pp.633-639
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    • 2008
  • Polysulfone membranes were prepared via the phase inversion process. Toluene was added as a nonsolvent additive in the casting solution containing a mixture of polysulfone and n-methylpyrrolidone. When prepared via the diffusion-induced process using isopropanol as a precipitation nonsolvent, the solidified membranes revealed a similar asymmetric structure irrespective of the addition of toluene, presenting both a dense skin layer and a sponge-like support layer. The added toluene played a role of enhancing liquid-liquid phase separation of the casting solution, and skin layer thickness of a prepared membrane increased with toluene content in the casting solution. On membrane performance, the solute rejection showed a uniform behavior irrespective of the addition of toluene. However, in spite of the significant increase in dense skin layer thickness, the water permeation through the membrane prepared with 60 wt% toluene revealed five times as much flux, compared with that of the membrane prepared without toluene additive.

Transdermal permeation-enhancing activity of N-adamantyl n-alkanamides for lbuprofen in the rabbit

  • Han, Suk-Kyu;Park, Yong-Hoon;Ko, Young-Ill;Kim, Young-Mi
    • Archives of Pharmacal Research
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    • v.19 no.2
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    • pp.95-99
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    • 1996
  • Four N-adamantyl n-alkanamides were prepared by amide condensation reaction between amantadine and n-alkanoic acid. Their enhancing activity on the penetration of ibuprofen through rabbit skin from petrolatum ointment was evaluated in in-vivo experiment. The experiments showed that the compounds have a strong transdermal penetration-enhancing activity, and their activities were comparable with that of Azone. The measurements of the fluorescence polarization of DP[-i-labelled DPPC liposomes showed that these compounds considerablly decreased the phase transition temperature of the liposomes. The mechanism of the transdermal penetration-enhancing activity of the compounds was ascribed to the reduction of the resistance to drug flux of the stratum corneum lipid layers due to the loose packing of the layers when the bulk head group of the enhancers inserts into the layers.

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Enhancement of Transdermal Drug Delivery Using Ultrasound (초음파를 이용한 경피약물수송의 촉진)

  • Park, Seung-Kyu;Kim, Tae-Youl
    • The Journal of Korean Physical Therapy
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    • v.13 no.3
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    • pp.719-726
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    • 2001
  • Transdermal drug delivery offers various advantages over conventional drug delivery systems, such as avoidance gastrointestinal degradation and hepatic first-pass effect. encourages patient compliance. and possible sustained release of drugs. However, transdermal transport of drugs is low permeability of the stratum corneum, the superficial layer of the skin. Many physicochemical and biological factors influencing transdermal transport is described together with the corresponding experimental and clinical results. Phonophoresis is medical treatment with drugs introduced into the skin by ultrasound energy. Enhanced drug penetration is through to result from the biophysical alterations of skin structure by ultrasound waves. The frequency used for phonophoresis is usually from 20 kHz to 15MHz. Phonophoresis can be categorized in to three ranges: low-frequency range(below 1 MHz). therapeutic frequency range(1 to 3MHz), and high-frequency range(above 3 MHz). The depth of penetration of ultrasound into skin is inversely proportional to the frequency. Cavitation may cause mechanical stress. temperature elevation, or enhanced chemical reactivity causing drug transport. One theory is that ultrasound affects the permeation of the stratum corneum lipid structure as the limiting step in permeating through the skin. The range of indications for phonophoresis is wide. Aspecific classification of the range of indications is obtained by classification of pathological conditions. The continuous research is needed for many interesting issucs of phonophoretic transdermal delivory in new future.

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XS-E is Induced Atopic Dermatitis NC/Nga Mice the Impact of Skin Conditions (XS-E가 아토피피부염이 유발된 NC/Nga Mice의 피부상태에 미치는 영향)

  • Kim, Kum-Lan
    • KSBB Journal
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    • v.29 no.4
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    • pp.263-270
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    • 2014
  • This study reports significant improvement of atopic dermatitis condition as a result of experiment using Xanthium strumarium L. extract (XS-E) at the dorsal skin of induced atopic dermatitis Nc/Nga mice. Skin clinical score has decreased ($2.75{\pm}0.85$, *p<0.05), showing visible change of skin condition. IgE (***p<0.001) and IgG1 ($2522.00{\pm}32.80$, ***p<0.001) in plasma also decreased significantly. mRNA (gene expression) level increased ($RQ=2.75{\pm}0.10$, ***p<0.001) within skin tissue of CD4+CD25+Foxp3+ Treg cell that's activated by XS-E dosage, thereby discovering that there is an effect of suppressing proliferation and viability of Th2 cell, eosinophils, mast cell and inflammatory cell. Upon examining cells permeated with H&E and toluidine blue staining technique, thickness of epidermis and mast cell's permeation decreased, and the result of examining the distribution of CCR 3+ eosinophils within ALN showed that it's level fell down to that of wild type (normal group, NC/Nga-WT). By such results, it is suggested that XS-E is highly effective on atopic dermatitis, and it is considered that continued quantitative research and case study of clinical research such as effect of cell number in individual tissues or change of total cell number are necessary.

Separation Permeation Characteristics of N2-O2 Gas in Air at Cell Membrane Model of Skin which Irradiated by High Energy Electron (고에너지 전자선을 조사한 피부의 세포막모델에서 공기 중의 O2-N2 혼합기체의 분리투과 특성)

  • Ko, In-Ho;Yeo, Jin-Dong
    • Journal of the Korean Society of Radiology
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    • v.13 no.2
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    • pp.261-270
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    • 2019
  • The separation permeation characteristics of $N_2-O_2$ gas in air at cell membrane model of skin which irradiated by high energy electron(linac 6 MeV) were investigated. The cell membrane model of skin used in this experiment was a sulfonated polydimethyl siloxane(PDMS) non-porous membrane. The pressure range of $N_2$ and $O_2$ gas were appeared from $1kg_f/cm^2$ to $6kg_f/cm^2$. In this experiment(temperature $36.5^{\circ}C$), the permeation change of $N_2$ and $O_2$ gas in non-porous membrane by non-irradiation were found to be $1.19{\times}10^{-4}-2.43{\times}10^{-4}$, $1.72{\times}10^{-4}-2.6{\times}10^{-4}cm^3(STP)/cm^2{\cdot}sec{\cdot}cmHg$, respectively. That of $N_2$ and $O_2$ gas in non-porous membrane by irradiation were found to be $0.19{\times}10^{-4}-0.56{\times}10^{-4}$, $0.41{\times}10^{-4}-0.76{\times}10^{-4}cm^3(STP)/cm^2{\cdot}sec{\cdot}cmHg$, respectively. The irradiated membrane was significantly decreased about 4-10 times than membrane which was not irradiated. And ideal separation factor of $N_2$ and $O_2$ gas by non-irradiation was found to be from 1.32 to 0.42 and that of $N_2$ and $O_2$ gas by irradiation was found to be from 0.237 to 0.125. The irradiated membrane was significantly decreased about 4-5 times than membrane which was not irradiated. When the operation change(cut) and pressure ratio(Pr) by non-irradiation were about 0, One was increased to the oxygen enrichment and the other was decreased to the oxygen enrichment. The irradiated membrane was significantly decreased about 4-19 times than membrane which was not irradiated. As the pressure of $N_2$ and $O_2$ gas was increased, the selectivity was decreased. As separation permeation characteristics of $N_2-O_2$ gas in cell membrane model of skin were abnormal, cell damages were appeared at cell.

Microemulsion-based Hydrogel Formulation of Itraconazole for Topical Delivery

  • Lee, Eun-A;Balakrishnan, Prabagar;Song, Chung-Kil;Choi, Joon-Ho;Noh, Ga-Ya;Park, Chun-Geon;Choi, Ae-Jin;Chung, Suk-Jae;Shim, Chang-Koo;Kim, Dae-Duk
    • Journal of Pharmaceutical Investigation
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    • v.40 no.5
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    • pp.305-311
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    • 2010
  • The present study was aimed at preparing microemulsion-based hydrogel (MBH) for the skin delivery of itraconazole. Microemulsion prepared with Transcutol as a surfactant, benzyl alcohol as an oil and the mixture of ethanol and phasphatidyl choline (3:2) as a cosurfactant were characterized by solubility, phase diagram, particle size. MBHs were prepared using 0.7 % of xanthan gum (F1-1) or carbopol 940 (F1-2) as gelling agents and characterized by viscosity studies. The in vitro permeation data obtained by using the Franz diffusion cells and hairless mouse skin showed that the optimized microemulsion (F1) consisting of itraconazole (1% w/w), benzyl alcohol (10% w/w), Transcutol (10% w/w) and the mixture of ethanol and phospahtidylcholine (3:2) (10% w/w) and water (49% w/w) showed significant difference in the flux (${\sim}1{\mu}g/cm^2/h$) with their corresponding MBHs (0.25-0.64 ${\mu}g/cm^2/h$). However, the in vitro skin drug content showed no significant difference between F1 and F1-1, while F1-2 showed significantly low skin drug content. The effect of the amount of drug loading (0.02, 1 and 1.5% w/w) on the optimized MBH (F1-2) showed that the permeation and skin drug content increased with higher drug loading (1.5%). The in vivo study of the optimized MBH (F1-2 with1.5% w/w drug loading) showed that this formulation could be used as a potential topical formulation for itraconazole.

Development of Porous Cellulose Hydrogel for Enhanced Transdermal Delivery of Liquiritin and Liquiritigenin as Licorice Flavonoids (감초 플라보노이드 Liquiritin 및 Liquiritigenin을 담지한 피부전달체인 셀룰로오스 다공성 하이드로젤 제형 개발)

  • Kim, Su Ji;Kwon, Soon Sik;Yu, Eun Ryeong;Park, Soo Nam
    • Polymer(Korea)
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    • v.38 no.5
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    • pp.676-681
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    • 2014
  • Licorice, widely used as a herbal medicine, has flavonoids such as liquiritin and its aglycone, liquiritigenin that show anti-oxidant and anti-inflammatory properties. Licorice flavonoid-loaded cellulose hydrogels were prepared as carriers for skin drug delivery, and their properties were investigated. The porous cellulose hydrogel was made by reacting cellulose with epichlorohydrin as a cross-linking agent in NaOH/urea(1~10%) solutions. Through studies on the rheological properties and water uptake of the hydrogel, a NaOH/urea(6%) solution was established as being optimum for the synthesis of the cellulose hydrogel containing liquiritin and liquiritigenin. Scanning electron microscopy (SEM) observations of a cross-section of the prepared hydrogel indicated its porosity. In particular, in skin permeation experiments using a Franz diffusion cell, hydrogel containing the licorice flavonoids showed remarkable transdermal permeation compared to the control group. These results indicate that porous cellulose hydrogel is a potential drug delivery system to enhance the skin permeation of licorice flavonoids.

Formulation and Skin Permeation Characteristics of Ketoprofen Patches (케토프로펜 패취제의 제제설계 및 피부 투과 특성)

  • 오흥설;이용석;김하영;이광표
    • YAKHAK HOEJI
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    • v.45 no.5
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    • pp.506-512
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    • 2001
  • Ketoprofen (KP) was formulated as a transdermal patch using the percutaneous penetration enhancers sorbitan monmmleate(SMO), polyvinylpyrrolidone(PVP). The control patch without penetration enhancers showed a KP flux of 8.9$\pm$0.75$\mu\textrm{g}$/$\textrm{cm}^2$/h The flux was increased in proportion to the concentration of SMO added. Furthermore, lag times were decreased upon addition of SMO. Conversely; the skin flux of KP was decreased in proportion to the concentration of PVP added. Pharmacokinetic parameters including $C_{max}$, $T_{max}$, and AUC were increased when SMO was added. However, $C_{mas}$ significantly decreased by the addition of PVP. $T_{max}$ was not significantly different in 2%, 4%, and 8% PVP patches. Patches containing 4% PVP showed the highest AUC value (19.158$\mu\textrm{g}$.h/ml). We found that the effectiveness of the two percutaneous penetration enhancers for topical KP patches was similar, with the addition of appropriate amounts of HPC modifying both skin flux and lag time of KP in the patches. In conclusion, it is possible to manufacture KP patches exhibiting high AUC, high skin flux, and short lag time using percutaneous penetration enhancers of SMO and PVP.

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Characteristics of Percutaneous Absorption of Glycol ethers (Glycol ethers에 대한 피부 투과 특성)

  • Lee, Han-Seob;Choi, Sung-Boo;Kim, Nac-Joo;Keun, Jang-Hyoun;Hwang, Hyun-Suk;Baek, Jung-Hun;Choi, Jin-Ho;Lee, Ho-Joon
    • Journal of the Korean Applied Science and Technology
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    • v.30 no.1
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    • pp.116-126
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    • 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.