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目的合成乳糖化-去甲斑蝥素作为主动肝靶向性修饰物,并将其制成纳米粒。方法利用乙二胺为连接臂合成乳糖化-去甲斑蝥素修饰物,并考察其相关理化性质;采用离子诱导法制备乳糖化-去甲斑蝥素壳聚糖纳米粒,以粒径分布、包封率、载药量为综合指标,正交设计优化载药纳米粒的制备工艺,并考察其体外释放特性。结果乳糖化-去甲斑蝥素是一种具有良好水溶性的多羟基化合物,其合成产率为68.35%;经优化工艺制备的乳糖化-去甲斑蝥素的纳米粒的平均粒径(149.46±1.79)nm,包封率(80.29±0.56)%,载药量(9.58±0.09)%,其体外释药遵循Higuchi方程。结论乳糖化-去甲斑蝥素合成简单,产率高,其纳米粒体外释放具有良好的缓释特性。
OBJECTIVE: To synthesize lactose-norcantharidin as an active liver-targeted modification and make it into nanoparticles. Methods Ethylene diamine was used as the linker to synthesize lactose-norcantharidin modified and its physical and chemical properties were investigated. The lactose-norcantharidin chitosan nanoparticles were prepared by ion-induced method. The particle size distribution, The encapsulation efficiency and drug loading were comprehensive indexes, and the orthogonal design was used to optimize the preparation process of drug-loaded nanoparticles. The release characteristics were also investigated. Results The lactylated-norcantharidin was a kind of polyhydroxy compound with good water-solubility, and its synthetic yield was 68.35%. The average particle size of the lactose-norcantharidin nanoparticles prepared by the optimization process was 149.46 ± 1.79) nm, encapsulation efficiency (80.29 ± 0.56)% and drug loading (9.58 ± 0.09)%. The in vitro drug release followed the Higuchi equation. Conclusion The lactacycline-norcantharidin synthesis is simple and the yield is high. The in vitro release of nanoparticles has good sustained-release properties.