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KMID : 0369820100400050305
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Jorunal of Korean Pharmaceutical Sciences
2010 Volume.40 No. 5 p.305 ~ p.311
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Microemulsion-based Hydrogel Formulation of Itraconazole for Topical Delivery
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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
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Abstract
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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 (~1 μg/cm2/h) with their corresponding MBHs (0.25-0.64 μg/cm2/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.
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KEYWORD
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Itraconazole, Benzyl alcohol, Microemulsion-based gel, Topical skin delivery
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