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Updated: May 9, 2026

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
Polypeptide/doxorubicin hydrochloride polymersomes prepared through organic solvent-free technique as a smart drug
Mingqiang Li1, Shixian Lv, Zhaohui Tang
1Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, 130022, P. R. China; University of Chinese Academy of Sciences, Beijing, 100039, P. R. China.
Abstract:
Rapid and efficient side-chain functionalization of polypeptide with neighboring carboxylgroups is achieved via the combination of ring-opening polymerization and subsequent thiol-yne click chemistry. The spontaneous formation of polymersomes with uniform size is found to occur in aqueous medium via electrostatic interaction between the anionic polypeptide and cationic doxorubicin hydrochloride (DOX·HCl). The polymersomes are taken up by A549 cells via endocytosis, with a slightly lower cytotoxicity compared with free DOX ·HCl. Moreover, the drug-loaded polymersomes exhibit the enhanced therapeutic efficacy, increase apoptosis in tumor tissues, and reduce systemic toxicity in nude mice bearing A549 lung cancer xenograft, in comparison with free DOX ·HCl.
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