通过β-拉帕醌的二酯衍生物实现可冻干、高载药量胶束制剂的前药策略。
Prodrug strategy to achieve lyophilizable, high drug loading micelle formulations through diester derivatives of β-Lapachone.
作者信息
Ma Xinpeng, Huang Xiumei, Huang Gang, Li Longshan, Wang Yiguang, Luo Xiuquan, Boothman David A, Gao Jinming
机构信息
Departments of Pharmacology, Simmons Comprehensive Cancer Center, University of Texas Southwestern Medical Center, 6001 Forest Park Road, Dallas, TX, 75390-8807, USA.
出版信息
Adv Healthc Mater. 2014 Aug;3(8):1210-6. doi: 10.1002/adhm.201300590. Epub 2014 Feb 14.
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.
摘要
β-拉帕替尼前药胶束策略改善了β-拉帕替尼治疗药物的制剂性质。所得胶束具有明显的高β-拉帕替尼溶解度（>7毫克/毫升）、物理稳定性以及冻干后复溶的能力。在酯酶存在的情况下，β-拉帕替尼前药可有效转化为母体药物（即β-拉帕替尼），从而导致非小细胞肺癌细胞发生NQO1依赖性致死。
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