半乳糖修饰的海藻酸纳米载体构建及其抗肿瘤功效
Fabrication of Galactosylated Alginate Nanoparticles as Drug Delivery System for Hepatocellular Carcinoma

作者: 李政雄 , 吴晓盈 :复旦大学生命科学学院,遗传国家重点实验室,上海;

关键词: 肝癌海藻酸纳米粒半乳糖药物递送DOXHepatocellular Carcinoma Alginate Nanoparticle Galactose Drug Delivery DOX

摘要:
本文设计制备肝靶向聚合物纳米粒–半乳糖(Gal)修饰海藻酸酯(HA-Gal)纳米粒,以阿霉素(DOX)为抗肿瘤模型药物制备载药纳米粒(DOX/HA-Gal),研究DOX/HA-Gal的理化性质、载药与释药、体外细胞增殖抑制,考察不同Gal接枝比对体外抗肿瘤功效的影响。结果表明DOX/HA-Gal为大小均一的球形粒子,水合动力学粒径为180-250nm,荷负电(<−30 mV);随Gal接枝比的增大,DOX/HA-Gal的粒径增大,Zeta电势升高,包封率增加,肿瘤细胞杀伤率提高。

Abstract: The alginate derivative naonoparticles modified by galactose (HA-Gal) with various galactose (Gal) substitution degrees were synthesized to evaluate their potential for hepatocellular carcinoma (HCC) targeting. Their physicochemical characteristics were investigated. Doxorubicin hydrochloride (DOX) as a model antitumor drug was incorporated into the HA-Gal. The in vitro drug release and antitumor capability of DOX loaded HA-Gal (DOX/HA-Gal) with different Gal substitution degrees were evaluated. Negatively charged DOX/HA-Gal appeared monodisperse and spherical in shape with a size range of 180 - 250 nm, and their Zeta potentials were above 30 mV (absolute value). The size, Zeta potentials, encapsulation efficiency and in vitro cytotoxicity of HA-Gal were increased with the increment in Gal substitution degree.

文章引用: 李政雄 , 吴晓盈 (2016) 半乳糖修饰的海藻酸纳米载体构建及其抗肿瘤功效。 纳米技术, 6, 23-32. doi: 10.12677/NAT.2016.62004

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