title: Prodrug strategy to achieve lyophilizable, high drug loading micelle formulations through diester derivatives of β-Lapachone.
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.
authors: Departments of Pharmacology, Simmons Comprehensive Cancer Center, University of Texas Southwestern Medical Center, 6001 Forest Park Road, Dallas, TX, 75390-8807, USA.
authors: Xinpeng
authors: X
authors: Ma
authors: Xiumei
authors: X
authors: Huang
authors: Gang
authors: G
authors: Huang
authors: Longshan
authors: L
authors: Li
authors: Yiguang
authors: Y
authors: Wang
authors: Xiuquan
authors: X
authors: Luo
authors: David A
authors: DA
authors: Boothman
authors: Jinming
authors: J
authors: Gao
mesh_terms: D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D001728:Dicumarol / Q000737:chemistry / Q000633:toxicity; D004952:Esters; D005612:Freeze Drying; D006801:Humans; D008823:Micelles; D016660:NAD(P)H Dehydrogenase (Quinone) / Q000037:antagonists & inhibitors / Q000378:metabolism; D009285:Naphthoquinones / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry; D011107:Polylysine / Q000737:chemistry; D011355:Prodrugs / Q000737:chemistry* / Q000633:toxicity
chemical_list: C099578:(O-methylpoly(ethylene glycol)-O'-succinyl)-N-epsilon-poly(L-lysine); D004952:Esters; D008823:Micelles; D009285:Naphthoquinones; D011355:Prodrugs; D011107:Polylysine; D011092:Polyethylene Glycols; C014638:beta-lapachone; D001728:Dicumarol; D016660:NAD(P)H Dehydrogenase (Quinone); C447479:NQO1 protein, human
keywords: cancer nanomedicine; diester prodrug; enzyme activation; polymeric micelles; β-lapachone