• Journal of Pharmaceutical Investigation
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• 제25권2호
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• pp.125-128
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• 1995

To increase the skin permeation rate of flurbiprofen, fatty alcohols were added in propylene glycol vehicle containing 1% flurbiprofen. Their enhancing effect on the skin permeation of flurbiprofen was evaluated using Keshary-Chien diffusion cells fitted with excised rat skins. Lauryl alcohol and oleyl alcohol increased the skin permeation rate of flurbiprofen 11.3 and 8.5 fold, respectively, compared to the control vehicle.

• Biomolecules & Therapeutics
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• 제25권4호
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• pp.434-440
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• 2017

S-methyl-$\small{L}$-methionine (SMM), also known as vitamin U, is commercially available as skin care cosmetic products for its wound healing and photoprotective effects. However, the low skin permeation expected of SMM due to its hydrophilic nature with a log P value of -3.3, has not been thoroughly addressed. The purpose of this study thus was to evaluate the effect of skin permeation enhancers on the skin permeation/deposition of SMM. Among the enhancers tested for the in vitro skin permeation and deposition of SMM, oleic acid showed the most significant enhancing effect. Moreover, the combination of oleic acid and ethanol further enhanced in vitro permeation and deposition of SMM through hairless mouse skin. Furthermore, the combination of oleic acid and ethanol significantly increased the in vivo deposition of SMM in the epidermis/dermis for 12 hr, which was high enough to exert a therapeutic effect. Therefore, based on the in vitro and in vivo studies, the combination of oleic acid and ethanol was shown to be effective in improving the topical skin delivery of SMM, which may be applied in the cosmetic production process for SMM.

• Journal of Pharmaceutical Investigation
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• 제25권1호
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• pp.47-54
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• 1995

Transdermal patch formulations of estradiol to treat post-menopausal symptoms and prevent osteoporosis in women were developed and evaluated for the permeation characteristics through the excised hairless mouse abdorminal skin and the uterotropic effect on the ovariectomized rabbits. The design of patch formulations was optimized by varying several formulation parameters, such as type of enhancers, amount of enhancers, amount of drug loading and coating thickness. Compared to a commercially available transdermal product, several patch formulations showed the similar skin permeation profiles (following zero-order kinetics), but their skin permeation rates were lasted for the longer period (a week). In one-week uterotropic efficacy test in the ovariectimized rabbits, the selected patch formulations showed the positive effect in atrophy of the urogenital epithelium. The mean values of uterus weight in rabbits after application of patches containing estradiol were much higher than those in control group (containing no drug).

• 공업화학
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• 제7권6호
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• pp.1087-1095
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• 1996

Poly(dimethyl siloxane)막을 이용하여 $45^{\circ}C$에서 에탄올/이소프로판올/물의 삼성분 혼합물에 대한 투과증발실험을 행하고, 에탄올과 이소프로판올의 존재가 상호의 투과특성에 미치는 영향을 연구하였다. 에탄올과 이소프로판올은 각각 상호의 투과속도를 감소시키는 경향을 나타내었으며, 이소프로판올이 에탄올의 투과에 미치는 영향보다는 에탄올이 이소프로판올의 투과에 미치는 영향이 더 현저하였다. 투과속도의 감소는 고분자막에 대한 에탄올이나 이소프로판올의 가소화 영향보다는 투과성분 사이의 상호작용에 의한 영향이 더 크기 때문으로 생각되었다. 삼성분 혼합물에서 투과성분 사이의 강한 상호작용은 에탄올과 이소프로판올의 투과에 대한 추진력을 감소시키는 결과를 나타내었다.

• 멤브레인
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• 제6권1호
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• pp.22-31
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• 1996

35$^{\circ}$C에서 polydimethytsiloxane(PDMS)막에 의한 이소프로판올수용액의 투과증발실험을 행하여 이소프로판올의 부피분율이 0.5~0.7범위에서 이상적인 투과속도로부터 가장 크게 벗어났다. 이소프로판올의 가소화 영향은 물의 투과를 증가시키는 데 비하여 물의 존재는 이소프로판올의 투과를 감소시키는 경향을 나타내었다. 혼합물에서 농도에 의존하는 확산계수를 Vignes식으로 나타내고, Flory-Huggins열역학과 Maxwell-Stefan식을 이용하여 투과속도와 선택도를 예측하였다. 이소프로판올과 물 사이의 Flory-Huggins상호작용계수는 과잉Gibbs에너지를 이용하여 계산하였으며 각 액체 성분과 고분자 사이의 상호작용계수는 평행팽윤 실험에 의하여 결정하였다. 이론적으로 예측한 투과속도는 35%이내의 오차범위에서 실험값과 일치하였으며, 투과선택도는 전 농도 범위에서 실험값과 이론값이 잘 일치하였다.

• Journal of Pharmaceutical Investigation
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• 제32권2호
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• pp.87-93
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• 2002

This study is to enhance drug penetration via skin and investigate anti-inflammation effect following adoption of ultrasound. For this goal gel containing triamcinolone was prepared and the skin penetration rate and the change effects of blood plasma ingredients and serum enzyme were investigated. Using Franz type diffusion cell and the skin of hairless mouse, the permeation enhancing effect of ultrasound was tested. After the injury by direct trauma, the blood test was performed by measuring WBC, lymphocyte, and neutrophyl, and by analyzing CPK and LDH. The ultrasound transducer whose technical specification is geometric area(GA) $1.4\;cm^2$, effective radiation area(ERA) $0.8\;cm^2$, and beam non-uniformity ratio(BNR) 6.0 max was used. The influence of frequency having an effect on skin permeation rate was higher in the case of using 1MHz and continuous treatment. The temperature of receptor phase was not influenced in skin permeation by phonophoresis. Skin permeation increase attended by intensity of ultrasound, the permeation of triamcinolone was accelerated at $2.5\;w/cm^2\;than\;1.0\;w/cm^2$. Following muscle injury phonophoretic group the number of WBC, neutrophil and lympholyte were decreased significantly as compared with both control group and ultrasound group. The result of variation of serum CPK and LDH activity conformed to the phonophoretic effect as same pattern with the variation of WBC, neutrophil and lymphocyte.

• Journal of Pharmaceutical Investigation
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• 제25권3호spc1호
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• pp.53-59
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• 1995

Ethinylestradiol (EE)-containing matrix was fabricated with ethylene-vinyl acetate(EVA) copolymer to control the release of the drug, Effect of addition of PEG 400 as receptor solution, the stripping of skin and Azone pretreatment on skin on the permeation of EE through the excised mouse skin was also studied. The permeation rate of EE through the excised mouse skin was affected by the PEG 400 volume fraction. The Azone pretreatment on skin didn't affect on the steady state flux, however, the lag time was shortened. The permeation rate of EE through the stripped skin was much larger than that through the whole skin. It showed that the stratum corneum acts as a barrier of skin permeation. The fact that there is little difference in EE permeation between the intact skin and the stripped skin with EVA membrane shows the permeation of EE through the mouse skin is mainly controlled by the membrane.

• Archives of Pharmacal Research
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• 제27권11호
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• pp.1177-1182
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• 2004

The effect of poly[2-methacryloyloxyethyl phosphorylcholine] (pMPC) on the skin permeation property was investigated by performing in vitro skin permeation study of a model drug, nicotinic acid (NA). Effect of pMPC polymer in donor solution on skin permeation rates was evaluated using side-by-side diffusion cells. Also, the structural alterations in the stratum corneum (SC), inter-lamellar bilayer (ILB) and dermis layers in pMPC-treated and -untreated skin sections were investigated with transmission electron microscopy (TEM). The permeation profile of NA without pMPC in donor solution showed biphasic mode: initial $1^{st} phase and 2^{nd}$ hydration phase. The sudden, more than 10-fold increase in flux from the initial steady state (43.5 $\mu g/cm^2$/hr) to the $2^{nd}$ hydration phase (457.3 $\mu g/cm^2$/hr) suggests the disruption of skin barrier function due to extensive hydration. The permeation profile of NA with 3% pMPC in the donor solution showed monophasic pattern: the steady state flux (10.9 $\mu g/cm^2$/hr) without abrupt increase of the flux. The degree of NA permeation rate decreased in a concentration-dependent manner of pMPC. TEM of skin equilibrated with water or 2% pMPC for 12 h showed that corneocytes are still cohesive and epidermis is tightly bound to dermis in 2% pMPC-treated skin, while wider separation between corneocytes and focal dilations in inter-cellular spaces were observed in water-treated skin. This result suggests that pMPC could protect the barrier property of the stratum corneum by preventing the disruption of ILB structure caused by extensive skin hydration during skin permeation study.

• Journal of Pharmaceutical Investigation
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• 제25권2호
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• pp.129-136
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• 1995

In order to reduce the systemic side effects and the gastrointestinal irritation of indomethacin following its oral administration, the drug was formulated as a transdermal gel using poloxamer 407. In vitro diffusion cells fitted with excised rat skins were used to evaluate the effects of formulation variables on skin permeation of indomethacin from poloxamer gels. The formulation variables were the concentrations of indomethacin, poloxamer 407 and ethanol, and the gel pH. The increase of the drug amount in the gel from 0.5% to 2.0% induced a direct but nonlinear increase in the skin permeation rate of indomethacin. The increase of poloxamer concentration from 17.5% to 25% in the gel resulted in a decrease of skin permeation rate of indomethacin, which was due to a reduction in the amount of free drug molecules available for permeation through skin by entrapping more drug molecules within the micelles formed by poloxamer. The increase of ethanol concentration from 10% to 20% in the gel resulted in a linear increase of permeation rate of indomethacin through skin, possibly due to the penetration enhancing effect of ethanol. The skin permeation of indomethacin was substantially influenced by the gel pH, exhibiting a maximum at pH 4.

• Journal of Pharmaceutical Investigation
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• 제38권4호
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• pp.223-228
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• 2008

The purpose of this study was to investigate the feasibility of developing transdermal drug delivery system (TDDS) for fentanyl used for the management of chronic cancer pain. The effect of type of pressure sensitive adhesive on the permeation of fentanyl from polyisobutylene (PIB), silicone and acrylic adhesive was evaluated. Due to the good adhesive force and relatively steady flux for 3 days, both acrylic and PIB adhesives were chosen for further study. The permeation rate of fentanyl was the highest from acrylic adhesive with hydroxyl functional group. Permeation rate increased linearly as the concentration of fentanyl in acrylic adhesive was increased from 2.5% to 10%. In case of PIB adhesive, crystals of fentanyl were developed above 5% drug load. $Crovol^{(R)}$ A40, $Crovol^{(R)}$ PK40 and Plurol $oleique^{(R)}$ provided higher flux of fentanyl.