Novel poly(ethylene glycol) and poly(N-(2-hydroxypropyl) methacrylamide) block copolymer (PEG-b-PHPMA) with well-defined composition was synthesized by RAFT polymerization. Folate and doxorubicin (DOX) were quantitatively introduced into the copolymer. The influences of folate content and pH value on folate receptor (FR) mediated cell endocytosis and pH-responsive DOX release were studied. It has been demonstrated that minimum folate content is needed for the enrichment of hydrophobic folate on the hydrophilic part of polymer conjugates. The cytotoxicity of targetable polymer drug conjugates was much higher than that of non-targetable ones and free DOX. It could be concluded that the folate plays a significant role in targeting and internalization of the conjugates against bladder cancer cells.
基金:
National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [51025314, 51390481, 81472412]; 973 project from the Ministry of Science and Technology of ChinaNational Basic Research Program of China [2011CB707703]
第一作者单位:[1]Beijing Univ Chem Technol, Coll Life Sci & Technol, Beijing Lab Biomed Mat, State Key Lab Organ Inorgan Composites, Beijing 100029, Peoples R China
通讯作者:
推荐引用方式(GB/T 7714):
Yu Qingsong,Zhang Jiajing,Zhang Guan,et al.Synthesis and Functions of Well-defined Polymer-drug Conjugates as Efficient Nanocarriers for Intravesical Chemotherapy of Bladder Cancer(a)[J].MACROMOLECULAR BIOSCIENCE.2015,15(4):509-520.doi:10.1002/mabi.201400416.
APA:
Yu, Qingsong,Zhang, Jiajing,Zhang, Guan&Gan, Zhihua.(2015).Synthesis and Functions of Well-defined Polymer-drug Conjugates as Efficient Nanocarriers for Intravesical Chemotherapy of Bladder Cancer(a).MACROMOLECULAR BIOSCIENCE,15,(4)
MLA:
Yu, Qingsong,et al."Synthesis and Functions of Well-defined Polymer-drug Conjugates as Efficient Nanocarriers for Intravesical Chemotherapy of Bladder Cancer(a)".MACROMOLECULAR BIOSCIENCE 15..4(2015):509-520