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Nanocarrier Formulation of a Geldanamycin Prodrug in ABC Micelles: Pharmacokinetics and Tolerability in Rats

机译:Geldanamycin前体药物在ABC胶束中的纳米载体制剂:大鼠的药代动力学和耐受性

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摘要

A Cremophor~R-free formulation of a geldanamycin prodrug was prepared using amphiphilic block co-polymer micelles of poly(ethylene glycol)-b-poly(ε-caprolactone) (PEG-b-PCL). Rats were dosed intravenously with PEG-b-PGL micelles and DMAG as control. The area under the curve, mean residence time, and tolerability increased. Total clearance, volume of distribution, and nonspecific systemic exposure decreased.
机译:使用聚(乙二醇)-b-聚(ε-己内酯)(PEG-b-PCL)的两亲嵌段共聚物胶束,制备了不含克雷莫尔的格尔德霉素前药制剂。给大鼠静脉内注射PEG-b-PGL胶束和DMAG作为对照。曲线下的面积,平均停留时间和耐受性增加。总清除率,分布量和非特异性全身暴露均下降。

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