Intracellular Delivery of Mitomycin C with Targeted Polysaccharide Conjugates Against Multidrug Resistance

被引：13

作者：

Cao, Yu ^{[1
,2
]}

Chen, Didi ^{[1
]}

Zhao, Peiguang ^{[1
]}

Liu, Lina ^{[1
]}

Huang, Xueying ^{[1
]}

Qi, Chao ^{[2
]}

Liu, Yanli ^{[2
]}

He, Hongxuan ^{[3
]}

Wang, Qian ^{[1
]}

Liu, Yang ^{[1
]}

Chen, Sha ^{[1
]}

机构：

[1] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China

[2] Cent China Normal Univ, Coll Life Sci, Hubei Key Lab Genet Regulat & Integrat Biol, Wuhan 430079, Peoples R China

[3] Chinese Acad Sci, Inst Zool, Key Lab Anim Ecol & Conservat Biol, Natl Res Ctr Wildlife Born Dis, Beijing 100101, Peoples R China

来源：

ANNALS OF BIOMEDICAL ENGINEERING | 2011年 / 39卷 / 09期

关键词：

Intracellular drug delivery; Polymeric conjugates; Hepatoma-targeting; Drug resistance; HEPATOCYTES IN-VIVO; MACROMOLECULAR PRODRUGS; DRUG-RESISTANCE; NANOPARTICLES; EFFICIENCY; COMPLEXES; POLYMERS; CHITOSAN; THERAPY; SYSTEMS;

D O I：

10.1007/s10439-011-0333-2

中图分类号：

R318 [生物医学工程];

学科分类号：

0831 ;

摘要：

Intracellular targeted conjugates of xyloglucan and mitomycin C (MMC) were synthesized with a lysosomally degradable peptide spacer and galactosamine, a terminal moiety that can be used to target polymeric conjugates to hepatoma. The content of the MMC was about 3.5% (mol) in this conjugate. In an in vitro cytotoxicity experiment, the targeted prodrugs have higher cytotoxicity than free MMC against the drug resistant HepG2 cells. In a human tumor xenograft nude mouse model, the targeted prodrugs generated higher therapeutic effect than non-targeted prodrugs or free MMC. Together, these results suggest that targeted prodrugs, which have improved transfer efficiency and hepatocyte specificity, may be useful for the reversion of drug resistant HepG2 cells.

引用

页码：2456 / 2465

页数：10

共 22 条

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