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Prodrug Strategy to Achieve Lyophilizable, High Drug Loading Micelle Formulations Through Diester Derivatives of β‐Lapachone
Author(s) -
Ma Xinpeng,
Huang Xiumei,
Huang Gang,
Li Longshan,
Wang Yiguang,
Luo Xiuquan,
Boothman David A.,
Gao Jinming
Publication year - 2014
Publication title -
advanced healthcare materials
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.288
H-Index - 90
eISSN - 2192-2659
pISSN - 2192-2640
DOI - 10.1002/adhm.201300590
Subject(s) - information center , cancer , medicine , library science , gerontology , psychology , computer science , educational research , mathematics education
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.