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.