Prodrug strategy to achieve lyophilizable, high drug loading micelle formulations through diester derivatives of β-Lapachone.

Ma, Xinpeng; Huang, Xiumei; Huang, Gang; Li, Longshan; Wang, Yiguang; Luo, Xiuquan; Boothman, David A; Gao, Jinming · Adv Healthc Mater · 2014

basic_science · Level V

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Abstract

β-Lap prodrug micelle strategy improves the formulation properties of β-lap therapeutics. The resulting micelles yield apparent high β-lap solubility (>7 mg mL(-1) ), physical stability, and ability to reconstitute after lyophilization. In the presence of esterase, β-lap prodrugs are efficiently converted into parent drug (i.e., β-lap), resulting in NQO1-dependent lethality of NSCLC cells.

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