TY - JOUR
T1 - A mixed polymeric micellar formulation of itraconazole
T2 - Characteristics, toxicity and pharmacokinetics
AU - Yi, Yilwoong
AU - Yoon, Hye Jeong
AU - Kim, Bong Oh
AU - Shim, Myungseob
AU - Kim, Sun Ok
AU - Hwang, Sung Joo
AU - Seo, Min Hyo
PY - 2007/1/22
Y1 - 2007/1/22
N2 - 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.
AB - 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.
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U2 - 10.1016/j.jconrel.2006.10.001
DO - 10.1016/j.jconrel.2006.10.001
M3 - Article
C2 - 17097755
AN - SCOPUS:33846498531
SN - 0168-3659
VL - 117
SP - 59
EP - 67
JO - Journal of Controlled Release
JF - Journal of Controlled Release
IS - 1
ER -