Polypeptide/Doxorubicin Hydrochloride Polymersomes Prepared Through Organic Solvent‐free Technique as a Smart Drug Delivery Platform |
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| Authors: | Mingqiang Li Shixian Lv Zhaohui Tang Wantong Song Haiyang Yu Hai Sun Huaiyu Liu Xuesi Chen |
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| Institution: | 1. Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, , Changchun, 130022 P. R. China;2. University of Chinese Academy of Sciences, , Beijing, 100039 P. R. China;3. Laboratory Animal Center, Jilin University, , Changchun, 130012 P. R. China |
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| 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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| Keywords: | drug delivery system pH‐responsive polypeptide self‐assembly thiol‐yne photochemistry |
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