Tumor Redox Heterogeneity-Responsive Prodrug Nanocapsules for Cancer Chemotherapy

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 anti...

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Bibliographic Details
Published in:Advanced materials (Weinheim) 2013-07, Vol.25 (27), p.3670-3676
Main Authors: Wang, Jinqiang, Sun, Xuanrong, Mao, Weiwei, Sun, Weilin, Tang, Jianbin, Sui, Meihua, Shen, Youqing, Gu, Zhongwei
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Combined Chemotherapy Protocols - chemistry
Antineoplastic Combined Chemotherapy Protocols - pharmacology
Camptothecin - analogs & derivatives
Camptothecin - chemistry
Camptothecin - pharmacology
Cell Line, Tumor
Cell Proliferation - drug effects
Chemical compounds
Chemotherapy
Dose-Response Relationship, Drug
drug delivery
Drug Screening Assays, Antitumor
Drugs
Heterogeneity
Humans
Mice
Molecular Structure
nanocapsules
Nanocapsules - chemistry
Nanocomposites
Nanomaterials
nanomedicine
Nanostructure
Neoplasms - drug therapy
Neoplasms - metabolism
Neoplasms - pathology
Oxidation-Reduction
Prodrugs - chemistry
Prodrugs - pharmacology
self-assembling prodrug
Structure-Activity Relationship
triggered release
Tumors
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Summary: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.
ISSN:0935-9648
1521-4095
DOI:10.1002/adma.201300929