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

被引：45

作者：

Han, Haijie ^{[1
,2
]}

Li, Su ^{[1
,2
]}

Zhong, Yueyang ^{[1
,2
]}

Huang, Yue ^{[3
]}

Wang, Kai ^{[1
,2
]}

Jin, Qiao ^{[3
]}

Ji, Jian ^{[3
]}

Yao, Ke ^{[1
,2
]}

机构：

[1] Zhejiang Univ, Sch Med, Affiliated Hosp 2, Ctr Eye, Hangzhou 310009, Peoples R China

[2] Zhejiang Univ, Sch Med, Affiliated Hosp 2, Zhejiang Prov Key Lab Ophthalmol, Hangzhou 310009, Peoples R China

[3] Zhejiang Univ, Dept Polymer Sci & Engn, Minist Educ, MOE Key Lab Macromol Synth & Functionalizat, Hangzhou 310027, Peoples R China

来源：

ASIAN JOURNAL OF PHARMACEUTICAL SCIENCES | 2022年 / 17卷 / 01期

基金：

国家重点研发计划;

关键词：

Gemcitabine; Pro-drug; Nano-drug; Cancer therapy; POLYMER-COATED NANODIAMONDS; HUMAN PANCREATIC-CANCER; HUMAN PHASE I/II; SILICA NANOPARTICLES; CONTROLLED-RELEASE; IN-VITRO; PHARMACOKINETIC FEATURES; ANTITUMOR-ACTIVITY; TRIGGERED RELEASE; DELIVERY-SYSTEMS;

D O I：

10.1016/j.ajps.2021.06.001

中图分类号：

R9 [药学];

学科分类号：

1007 ;

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. (C) 2021 Shenyang Pharmaceutical University. Published by Elsevier B.V.

引用

页码：35 / 52

页数：18

共 132 条

[1] A PHASE-I CLINICAL, PLASMA, AND CELLULAR PHARMACOLOGY STUDY OF GEMCITABINE [J].