A mixed polymeric micellar formulation of itraconazole: Characteristics, toxicity and pharmacokinetics

Yilwoong Yi, Hye Jeong Yoon, Bong Oh Kim, Myungseob Shim, Sun Ok Kim, Sung Joo Hwang, Min Hyo Seo

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A mixed polymeric micelle formulation of itraconazole (ITZ-PM) was prepared using monomethoxy poly(ethylene glycol)-b-poly(lactic acid) and poly(lactic acid) as drug carrier materials. The ITZ-PM formulation remarkably increased the itraconazole solubility up to 15 mg/mL in aqueous media and provided stable solutions at a wide range of concentrations and pH's. In toxicity studies of single and 28-day repeated administrations to rats and dogs, ITZ-PM was well tolerated at dose levels corresponding to clinical doses. The pharmacokinetic profiles of ITZ-PM for itraconazole and its major metabolite, hydroxy-itraconazole, were comparable to those of the cyclodextrin formulations (Sporanox® Injection and Oral Solution) in rats and dogs. These results suggest that ITZ-PM can be an advantageous formulation for both intravenous and oral routes.

Original languageEnglish
Pages (from-to)59-67
Number of pages9
JournalJournal of Controlled Release
Issue number1
Publication statusPublished - 2007 Jan 22


All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

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