壳聚糖修饰雷公藤多苷纳米粒的制备及其体外释药研究  

Preparation and in vitro release of tripterygium glycosides-loaded nanoparticles modified by chitosan

作　　者：魏颖慧[1] 赵燕敏[1] 李静[1,2] 徐小玉[1] 郭曼曼[1] 李范珠[1] 

机构地区：[1]浙江中医药大学,浙江杭州310053 [2]贵州大学,贵州贵阳550025

出　　处：《中草药》2013年第5期541-546,共6页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(30902007);浙江省重点科技创新团队资助项目(2012R10044-05)

摘　　要：目的制备壳聚糖修饰雷公藤多苷纳米粒(LMWC-TG-NPs),并研究其体外释药行为。方法采用改良的自乳化溶剂扩散法制备LMWC-TG-NPs;正交试验设计优化雷公藤多苷纳米粒(TG-NPs)处方,单因素试验考察壳聚糖(LMWC)修饰方式;以含20%乙醇的PBS(pH 7.4)为释放介质考察LMWC-TG-NPs的体外释药行为。结果优化的处方工艺:以1.0%Poloxamer 188、80 mg PLA、12 mL有机相、丙酮-乙醇(2∶3)制备TG-NPs混悬液,以与TG-NPs混悬液等体积的10%LMWC溶液修饰TG-NPs制备LMWC-TG-NPs;根据优化条件制备的LMWC-TG-NPs,外观呈圆形或类圆形,平均粒径为(207.6±3.4)nm,多分散指数(PDI)为0.078±0.009(n=3),包封率和载药量分别为(61.83±2.43)%、(10.70±0.37)%(n=3);体外释药符合Higuchi方程。结论所制备的LMWC-TG-NPs包封率较高,粒径小,体外释药具有明显的缓释特征,为后期研究其肾脏靶向和毒性奠定了基础。Objective To prepare tripterygium glycosides-loaded nanoparticles modified by 50% N-acetylated low molecular weight chitosan （LMWC-TG-NPs） and to investigate their in vitro release behavior. Methods The LMWC-TG-NPs were prepared by modified self-emulsifying solvent diffusion method; The formulation of TG-NPs was optimized by orthogonal design and the modified condition of LMWC was determined based on the single factor analysis. The in vitro drug release of LMWC-TG-NPs was characterized with PBS （pH 7.4） containing 20% ethanol. Results The optimized formulation of TG-NPs was as follows： Poloxamer 188 （1.0%）, PLA （80 rag）, organic phase （12 mL）, and acetone-ethanol （2 ： 3） were used to prepare TG-NPs suspension. The LMWC-TG-NPs were prepared by incubating TG-NPs suspension with 10% LMWC solution at the ratio of 1 ： 1. The shape of the prepared LMWC-TG-NPs was spherical. The mean particle size, polydispersity index, entrapment efficiency, and drug loading were （207.6± 3.4） nm, 0.078 ± 0.009, （61.83 ± 2.43）%, and （10.70 ± 0.37）% （n=3）, respectively. The in vitro release characteristics of LMWC-TG-NPs conform to Higuchi equation in PBS buffer composed of 20% ethanol at pH 7.4. Conclusion The prepared LMWC-TG-NPs show a sustained-release characteristics with well-distributed particle size as well as high entrapment efficiency and drug loading, which could lay the foundation for the research on kidney targeting and toxicity.

关 键 词：雷公藤多苷 壳聚糖修饰 纳米粒 正交试验设计 体外释药 自乳化溶剂扩散法 

分 类 号：R283.6[医药卫生—中药学]