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Itraconazole-loaded micelles based on linear-dendritic poly (ethylene glycol)-b-poly (ε-caprolactone)

Journal 2018 · IF 1.911 · 发表于 2018 年 12 月 12 日
作者: Shida Li,Wenxiu Wei,Weiping Jia,Lechen Zhao,Hongmei Xu,Feilong Zhou,Li Zhu,Zhimei Song,Sijia Feng,Runliang Feng
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摘要

A copolymeric micelle formulation of itraconazole (ITR-M) was prepared using linear-dendritic monoallyloxy poly (ethylene glycol)-b-poly (ε-caprolactone) (APEG-PCL) as drug carrier materials. DL and EE values of ITR-M were 5.70 ± 0.12% and 91.30 ± 1.90%, respectively. The micelle formulation enhanced the ITR solubility up to 30.42 μg/mL. In vitro release of ITR from the ITR-M was mainly drug diffusion process followed by the copolymer’s degradation. ITR-M showed similar anti-Candida albicans activity to that of crude ITR although its release of ITR was slow and continuous. The in vivo pharmacokinetic study demonstrated that the ITR-M could improve tissue distribution of ITR. In conclusion, APEG-PCL could be a potential carrier in the development of antifungal drug delivery system.

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