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Polypeptide/ D oxorubicin Hydrochloride Polymersomes Prepared Through Organic Solvent‐free Technique as a Smart Drug Delivery Platform
Author(s) -
Li Mingqiang,
Lv Shixian,
Tang Zhaohui,
Song Wantong,
Yu Haiyang,
Sun Hai,
Liu Huaiyu,
Chen Xuesi
Publication year - 2013
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201300222
Subject(s) - polymersome , chemistry , doxorubicin hydrochloride , doxorubicin , drug delivery , cytotoxicity , endocytosis , hydrochloride , biophysics , surface modification , combinatorial chemistry , polymer chemistry , biochemistry , organic chemistry , polymer , in vitro , chemotherapy , amphiphile , copolymer , cell , medicine , surgery , biology
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.