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载有奥沙利铂的肝靶向胶束的制备与评价

Preparation and evaluation of liver-targeting micelles loaded with oxaliplatin.

作者信息

Yan Guowen, Chen Qian, Xu Lisa, Wei Haitian, Ma Chao, Sun Yong

机构信息

a College of Pharmacy, Qingdao University , Qingdao, Shandong , P. R. China.

出版信息

Artif Cells Nanomed Biotechnol. 2016;44(2):491-6. doi: 10.3109/21691401.2014.962747. Epub 2014 Oct 7.

DOI:10.3109/21691401.2014.962747
PMID:25287740
Abstract

We prepared liver-targeting micelles loaded with oxaliplatin (OXA), using a polymer modified by a liver-targeting ligand, namely, glycyrrhetinic acid-conjugated and stearic acid-grafted chitosan (GA-CS-SA). The particles had a uniform size, which was 138.6 ± 0.72 nm. The encapsulation efficiency was up to 71.7 ± 0.46%. The hepatic distribution of OXA in mice given OXA-GA-CS-SA was significantly superior to that in the controls (P < 0.05), which means that liver-targeted delivery of OXA was achieved. These results reveal that OXA-GA-CS-SA could be a potential and promising candidate for efficiently targeted delivery of OXA.

摘要

我们使用一种经肝脏靶向配体修饰的聚合物,即甘草次酸共轭且硬脂酸接枝的壳聚糖(GA-CS-SA),制备了负载奥沙利铂(OXA)的肝脏靶向胶束。这些颗粒尺寸均匀,为138.6 ± 0.72纳米。包封率高达71.7 ± 0.46%。给予OXA-GA-CS-SA的小鼠体内奥沙利铂的肝脏分布显著优于对照组(P < 0.05),这意味着实现了奥沙利铂的肝脏靶向递送。这些结果表明,OXA-GA-CS-SA可能是高效靶向递送奥沙利铂的一个潜在且有前景的候选物。

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