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KMID : 0369820070370030167
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Jorunal of Korean Pharmaceutical Sciences
2007 Volume.37 No. 3 p.167 ~ p.171
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Formulations of Itraconazole for Topical Skin Delivery
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Lee Eun-A
Heo Sung-Koun
Choi Myeong-Jun
Chung Suk-Jae
Shim Chang-Koo
Kim Dae-Duk
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Abstract
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Itraconazole is one of the most potent antifungal agents available in the market today. However, the low bioavailability due to its poor-water solubility calls for an alternative formulation to the current oral type. A topical itra-conazole-containing formulation may be of use for several reasons including the opportunity to reduce adverse events and generate high local tissue levels, more rapid drug delivery, and lower systemic exposure. The purpose of the present study was to investigate the vehicles for topical skin delivery of itraconazole. The effect of formulations on the hairless mouse skin permeation and deposition of itraconazole was determined using Franz diffusion cells at $37^{\circ}C$. Benzyl alcohol in micro-emulsion significantly increased the solubility of itraconazole, thereby increasing the skin permeation rate. However, lipo-some formulation showed the lowest solubility and permeation rate of itraconazole. Although the solubility of itraconazole in hydrogel formulation was lower than that in microemulsion, skin permeation rate was significantly higher probably due to its adhesive property. Therefore, microemulsion-based hydrogel formulation is expected to synergistically increase the skin permeation rate and skin deposition of itraconazole.
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KEYWORD
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Benzyl alcohol, Itraconazole, Topical skin delivery
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