title: Tumor redox heterogeneity-responsive prodrug nanocapsules for cancer chemotherapy.
abstract: A prodrug forms nanocapsules responsive to tumor GSH/ROS heterogeneity releasing the parent drug SN38 via thiolysis in the presence of GSH (glutathione) or via enhanced hydrolysis due to ROS (reactive oxygen species)-oxidation of the linker, giving rise to high in vitro cytotoxicity and in vivo anticancer therapeutic activity. The nanocapsules are a suitable size for tumor targeting by means of the EPR effect and have a fixed SN38 loading content of 35 wt%, ideal for translational nanomedicine.
authors.affiliation: Center for Bionanoengineering and State Key Laboratory of Chemical Engineering, Zhejiang University, Hangzhou 310027, P.R. China.
authors.forename: Jinqiang
authors.initials: J
authors.lastname: Wang
authors.forename: Xuanrong
authors.initials: X
authors.lastname: Sun
authors.forename: Weiwei
authors.initials: W
authors.lastname: Mao
authors.forename: Weilin
authors.initials: W
authors.lastname: Sun
authors.forename: Jianbin
authors.initials: J
authors.lastname: Tang
authors.forename: Meihua
authors.initials: M
authors.lastname: Sui
authors.forename: Youqing
authors.initials: Y
authors.lastname: Shen
authors.forename: Zhongwei
authors.initials: Z
authors.lastname: Gu
mesh_terms: D000818:Animals; D000971:Antineoplastic Combined Chemotherapy Protocols / Q000737:chemistry / Q000494:pharmacology*; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D000077146:Irinotecan; D051379:Mice; D015394:Molecular Structure; D053769:Nanocapsules / Q000737:chemistry*; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D010084:Oxidation-Reduction; D011355:Prodrugs / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D053769:Nanocapsules; D011355:Prodrugs; D000077146:Irinotecan; D002166:Camptothecin
keywords: drug delivery; nanocapsules; nanomedicine; self-assembling prodrug; triggered release