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)nm，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。

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.

国家科技支撑计划资助课题（2006BAI09B00）；国家科技部科技型中小企业技术创新基金资助项目（07C26223201333）；江苏省“六大人才高峰”资助项目；江苏省卫生厅招标项目（H200630）