Trackable Water-Soluble Prodrug Micelles Capable of Rapid Mitochondrial-Targeting and Alkaline pH-Responsive Drug Release for Highly Improved Anticancer Efficacy
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Updated: Sep 21, 2025

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
Bei-Yu Liu1, Xian-Ling Yang1, Xiu Xing1
1Key Laboratory of Green Chemistry and Technology, Ministry of Education, College of Chemistry Sichuan University, 29, Wangjiang Road, Chengdu, Sichuan Province, P. R. China.
Abstract:
A trackable water-soluble prodrug conjugate possessing high contents of chlorambucil (Cb) and triphenylphosphonium cation (TPP) was designed and developed after TPP modification on the "branch" of amphipathic prodrugs based on convenient synthesis of heterobifunctional clickable poly(ethylene glycol) (PEG). The aqueous self-assembly of fluorescent polymeric micelles along precise composition can be easily prepared after directly dissolved (DD) in aqueous solution, and exhibit superior cytotoxicity to cancer cells along with highly improved selectivity and sensitivity because of their rapid mitochondrial-targeting and alkaline pH-responsive drug release capabilities. Notably, efficient codelivery of doxorubicin (DOX) for synergistic targeted drug delivery and cancer therapy was achieved.
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