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

Research output: Contribution to journalArticle

59 Citations (Scopus)

Abstract

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
Volume117
Issue number1
DOIs
Publication statusPublished - 2007 Jan 22

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Itraconazole
Pharmacokinetics
Dogs
Drug Carriers
Cyclodextrins
Micelles
Solubility
Injections

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

Yi, Yilwoong ; Yoon, Hye Jeong ; Kim, Bong Oh ; Shim, Myungseob ; Kim, Sun Ok ; Hwang, Sung Joo ; Seo, Min Hyo. / A mixed polymeric micellar formulation of itraconazole : Characteristics, toxicity and pharmacokinetics. In: Journal of Controlled Release. 2007 ; Vol. 117, No. 1. pp. 59-67.
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abstract = "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{\circledR} 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.",
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A mixed polymeric micellar formulation of itraconazole : Characteristics, toxicity and pharmacokinetics. / Yi, Yilwoong; Yoon, Hye Jeong; Kim, Bong Oh; Shim, Myungseob; Kim, Sun Ok; Hwang, Sung Joo; Seo, Min Hyo.

In: Journal of Controlled Release, Vol. 117, No. 1, 22.01.2007, p. 59-67.

Research output: Contribution to journalArticle

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