去甲斑蝥素N-乳糖酰壳聚糖纳米粒的制备及其特性研究

目的 合成N-乳糖酰壳聚糖作为肝靶向载体,制备去甲斑蝥素纳米粒.方法 通过碳二亚胺缩合法制备N-乳糖酰壳聚糖,并以之为载体,采用离子诱导法制备去甲斑蝥素N-乳糖酰壳聚糖纳米粒,以粒径分布、包封率、载药量为综合指标,正交试验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 合成的N-乳糖酰壳聚糖的取代度为8.92%,优化工艺制备的N-乳糖酰壳聚糖载药纳米外观圆整,平均粒径(118.7±8.84)niB,包封率(57.92±0.40)%,载药量(10.38±0.06)%,其体外释药遵循Higuchi方程.结论 半乳糖修饰壳聚糖载药纳米粒具有良好的缓释特性.

Preparation of norcantharidin N-galactosylated chitosan nanoparticles and its characteristics

Objective To synthesize N-galactosylated chitosan as hepatocyte-targeting carrier and prepare loading norcantharidin nanoparticles.Methods N-Galactosylated chitosan was prepared by carbodiimide condensation reaction;loading norcantharidin nanoparticles were achieved by ionic cross-linkage process with N-galactosylated chitosan as carrier.Taking distribution of particle size,entrapment efficiency,and drug-loading capacity as comprehensive indexes,the orthogonal test design was used to optimize the preparation process and the in vitro release was investigated.Results Substitution degree of N-galactosylated chitosan reached to 8.92%.Novel nanoparticles were spherical,average in particle size(118.7±8.84)nm,entrament efficiency(57.92±0.40)%,drug-loading capacity(10.38±0.06)%,and the in vitro release followed Higuchi equation.Conclusion Effect of drug sustained release of galactosylated chitosan nanoparticles is significant.