Self-immolative camptothecin polymeric prodrugs for controlled drug release

被引:0
|
作者
Bai H.-Y. [1 ]
Zhou Z.-X. [1 ]
Shen Y.-Q. [1 ]
机构
[1] Zhejiang Key Laboratory of Smart Biomaterials, College of Chemical and Biological Engineering, Zhejiang University, Hangzhou
关键词
camptothecin; controlled drug release; polymeric prodrug; self-immolation;
D O I
10.3969/j.issn.1003-9015.2022.04.013
中图分类号
学科分类号
摘要
Precise controlling of drug release profiles is essential for enhancing drug efficiency and reducing side effects. Self-immolative systems have been developed as promising platforms for programmable and on-demand drug release. A self-immolative camptothecin (CPT)-based polymeric prodrugs for controlled drug release was constructed. The polymeric CPT prodrugs were prepared by Grubbs 3 catalyzed (3rd generation) ring-opening metathesis polymerization (ROMP). The results show that neighboring amine groups in the polymeric prodrugs can catalyze the hydrolysis of CPT ester and promote CPT release. The drug release profile of CPT was tunable by pH, amine chain length and amine numbers. The drug release of PEGn-Em-CPT2 and PEGn-Dm-CPT2 can be tuned from 10% to 89% and 62% within 180 hours, respectively. By amidization of amine groups with acid-responsive β-carboxylic amides, polymeric CPT prodrugs with acid-responsive drug release was obtained. This work demonstrates the neighboring amine catalyzed hydrolysis can be used for self-immolative drug release. © 2022 Zhejiang University. All rights reserved.
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页码:570 / 578
页数:8
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