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自靶向多糖前药抑制原位肝癌

Self-Targeted Polysaccharide Prodrug Suppresses Orthotopic Hepatoma.

作者信息

Li Di, Xu Weiguo, Li Pengqiang, Ding Jianxun, Cheng Zhiliang, Chen Li, Yan Lesan, Chen Xuesi

机构信息

Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun 130022, P. R. China.

Department of Chemistry, Northeast Normal University , Changchun 130024, P. R. China.

出版信息

Mol Pharm. 2016 Dec 5;13(12):4231-4235. doi: 10.1021/acs.molpharmaceut.6b00747. Epub 2016 Oct 31.

DOI:10.1021/acs.molpharmaceut.6b00747
PMID:27784155
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5464407/
Abstract

Self-targetability is an emerging targeting strategy for polymer nanocarriers with facile preparation and high targeting efficiency. An acid-sensitive dextran-doxorubicin prodrug (Dex-g-DOX) has been synthesized and used as a self-targeted drug delivery system for the treatment of orthotopic hepatoma. The polysaccharide prodrug exhibits ultraselective accumulation in cancerous liver tissue, acid-sensitive DOX release within cells, and high antitumor efficacy in vitro and in vivo. Therefore, Dex-g-DOX demonstrates great potential for chemotherapy of orthotopic hepatoma.

摘要

自靶向性是一种新兴的聚合物纳米载体靶向策略,具有制备简便和靶向效率高的特点。一种酸敏性葡聚糖-阿霉素前药(Dex-g-DOX)已被合成,并用作原位肝癌治疗的自靶向给药系统。这种多糖前药在癌性肝组织中表现出超选择性积累、细胞内酸敏性阿霉素释放以及体外和体内的高抗肿瘤疗效。因此,Dex-g-DOX在原位肝癌化疗方面显示出巨大潜力。

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