Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Formulations of Itraconazole for Topical Skin Delivery

국소 피부 투여를 위한 이트라코나졸 제제의 조성

  • Lee, Eun-A (College of Pharmacy, Seoul National University) ;
  • Heo, Sung-Koun (College of Pharmacy, Pusan National University) ;
  • Choi, Myeong-Jun (Charmzone Research & Development Center, Biomaterials Research Institute) ;
  • Chung, Suk-Jae (College of Pharmacy, Seoul National University) ;
  • Shim, Chang-Koo (College of Pharmacy, Seoul National University) ;
  • Kim, Dae-Duk (College of Pharmacy, Seoul National University)
  • Published : 2007.06.21
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Abstract

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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