雷公藤甲素壳聚糖纳米粒的制备与初步评价

Preparation and Evaluation of Triptolide-Loaded Chitosan Nanoparticles

目的:制备包载雷公藤甲素的壳聚糖纳米粒系统(triptolide-chitosan nanoparticles,TP-CS NPs),并考察其理化性质及体外释药性能。方法:采用非溶剂辅助络合-化学交联法制备壳聚糖纳米粒。利用透射电镜、粒度仪、HPLC法等对制备的纳米粒性质进行表征。结果:制得的纳米粒呈球形,平均粒径为(151.2±5.4)nm,Zeta电位(20.1±1.2)m V,纳米粒收率(78.0±3.3)%,包封率(77.0±1.2)%,载药量(2.0±0.4)%,体外模拟释药结果表明载药纳米粒药物释放速率在24 h内持续稳定。结论:非溶剂辅助络合-化学交联法制备的雷公藤甲素壳聚糖纳米粒简便可靠,体外释药具有明显的缓释作用。

Objective： To prepare the triptolide-loaded chitosan nanoparticles（ TP-CS NPs） and to investigate their physicochemical properties and in vitro release characteristics. Methods： TP-CS NPs were prepared by non-solvent-aided complexation-chemical cross-linking method. Their properties were determined by transmission electron microscopy,particle size analyzer,HPLC and so on. Results： The prepared nanoparticles were spherical with an average size at（ 151. 2 ± 5. 4） nm,a Zeta potential at（ 20. 1 ± 1. 2） m V,a yield of（ 78. 0 ± 3. 3） %,encapsulation efficiency of（ 77. 0 ± 1. 2） % and drug loading content of（ 2. 0 ± 0. 4） %. In vitro,the drug release rate was continuously stable in 24 h. Conclusion： TP-CS NPs prepared by non solvent assisted complexation-chemical crosslinking method is convient and reliable,showing a sustained release behavior in vitro.