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

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

SUBMITTER: Ma X

PROVIDER: S-EPMC4133338 | biostudies-literature | 2014 Aug

REPOSITORIES: biostudies-literature

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

Ma Xinpeng X Huang Xiumei X Huang Gang G Li Longshan L Wang Yiguang Y Luo Xiuquan X Boothman David A DA Gao Jinming J

Advanced healthcare materials 20140214 8

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. ...[more]

PMID: 24532286

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