文献类型：期刊文献

英文题名：Convenient and Controllable Synthesis of Poly(2-oxazoline)-Conjugated Doxorubicin for Regulating Anti-Tumor Selectivity

作者：Zhou, Min[1];Cui, Ruxin[2];Luo, Zhengjie[2];Cong, Zihao[2];Shao, Ning[2];Yuan, Ling[2];Gu, Jiawei[2];He, Hongyan[2];Liu, Runhui[1,2,3]

机构：[1]East China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Sch Mat Sci & Engn, Key Lab Ultrafine Mat, Minist Educ, Shanghai 200237, Peoples R China;[3]East China Univ Sci & Technol, Shenzhen Res Inst, Shenzhen 518063, Peoples R China

年份：2023

卷号：14

期号：7

外文期刊名：JOURNAL OF FUNCTIONAL BIOMATERIALS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:001038537500001)】；

基金：This research was supported by the China National Postdoctoral Program for Innovative Talents (BX2021102), China Postdoctoral Science Foundation (2022M710050), Program of Shanghai Academic/Technology Research Leader (20XD1421400), Free exploring basic research project at the Shenzhen Research Institute of ECUST (2021Szvup042), Open Research Fund of the State Key Laboratory of Polymer Physics and Chemistry (Changchun Institute of Applied Chemistry, Chinese Academy of Sciences), Open Project of the Engineering Research Center of Dairy Quality and Safety Control Technology, Ministry of Education (R202201), and Shanghai Frontiers Science Center of Optogenetic Techniques for Cell Metabolism (Shanghai Municipal Education Commission)).

语种：英文

外文关键词：poly(2-oxazoline); poly(2-oxazoline)-doxorubicin conjugation; facile synthesis; anti-tumor selectivity

摘要：Polyethylene glycol (PEG)-doxorubicin (DOX) conjugation is an important strategy to improve toxicity and enhance clinically therapeutic efficacy. However, with the frequent use of PEG-modified drugs, the accumulation of anti-PEG antibodies has become a tough issue, which limits the application of PEG-drug conjugation. As an alternative solution, poly(2-oxazoline) (POX)-DOX conjugation has shown great potential in the anti-tumor field, but the reported conjugation process of POX with DOX has drawbacks such as complex synthetic steps and purification. Herein, we propose a convenient and controllable strategy for the synthesis of POX-DOX conjugation with different chain lengths and narrow dispersity by N-boc-2-bromoacetohydrazide-initiated 2-ethyl-oxazoline polymerization and the subsequent deprotection of the N-Boc group and direct reaction with DOX. The DOX-PEtOx conjugates were firstly purified, and the successful conjugations were confirmed through various characterization methods. The synthetic DOX-PEtOx(n) conjugates reduce the toxicity of DOX and increase the selectivity to tumor cells, reflecting the promising application of this POX-DOX conjugation strategy in drug modification and development.