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.
出处
《中草药》
CAS
CSCD
北大核心
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)
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
tripterygium glycosides
chitosan-modified
nanoparticles
orthogonal design
in vitro release
self-emulsifying solvent diffusion method
