Emerging pro-drug and nano-drug strategies for gemcitabine-based cancer therapy  

作　　者：Haijie Han Su Li Yueyang Zhong Yue Huang Kai Wang Qiao Jin Jian Ji Ke Yao 

机构地区：[1]Eye Center,the Second Affiliated Hospital,School of Medicine,Zhejiang University,Hangzhou 310009,China [2]Zhejiang Provincial Key Lab of Ophthalmology,the Second Affiliated Hospital,School of Medicine,Zhejiang University,Hangzhou 310009,China [3]MOE Key Laboratory of Macromolecule Synthesis and Functionalization of Ministry of Education,Department of Polymer Science and Engineering,Zhejiang University,Hangzhou 310027,China

出　　处：《Asian Journal of Pharmaceutical Sciences》2022年第1期35-52,共18页亚洲药物制剂科学（英文）

基　　金：supported by the Natural Science Foundation of China (Grant Nos. 52022090, 22005265, 82070739, 81870641);National Key R&D Program of China (Grant No. 2018YFC1106104);Key Research and Development Program of Zhejiang Province (Grant No. 2020C03035);Zhejiang Provincial Natural Science Foundation of China (Grant No. LQ20E030011);Zhejiang Medical Health Science and Technology Program (Grant No. 2021RC061);Zhejiang Provincial Ten Thousand Talents Program (2018R52001)。

摘　　要：Gemcitabine has been extensively applied in treating various solid tumors. Nonetheless,the clinical performance of gemcitabine is severely restricted by its unsatisfactory pharmacokinetic parameters and easy deactivation mainly because of its rapid deamination, deficiencies in deoxycytidine kinase (DCK), and alterations in nucleoside transporter. On this account, repeated injections with a high concentration of gemcitabine are adopted, leading to severe systemic toxicity to healthy cells. Accordingly, it is highly crucial to fabricate efficient gemcitabine delivery systems to obtain improved therapeutic efficacy of gemcitabine. A large number of gemcitabine pro-drugs were synthesized by chemical modification of gemcitabine to improve its biostability and bioavailability. Besides,gemcitabine-loaded nano-drugs were prepared to improve the delivery efficiency. In this review article, we introduced different strategies for improving the therapeutic performance of gemcitabine by the fabrication of pro-drugs and nano-drugs. We hope this review will provide new insight into the rational design of gemcitabine-based delivery strategies for enhanced cancer therapy.

关 键 词：GEMCITABINE PRO-DRUG Nano-drug Cancer therapy 

分 类 号：R730.5[医药卫生—肿瘤]