摘要
目的:以聚乙二醇单甲醚-聚乳酸(PEDLA)制备冬凌草甲素(ORI)嵌段共聚物胶束,并对其进行体外释放研究。方法:采用熔融开环聚合法合成了PEDLA嵌段共聚物,采用溶剂扩散法制备ORI胶束,并对制得的ORI胶束的粒径、Zeta电位、载药量、包封率和体外释放进行了研究。结果:制得的ORI胶束的平均粒径为(136.7±1.54)nm,Zeta电位为(-18.9±0.79)mv,载药量为(5.19±0.06)%,包封率为(73.9±0.6)%。体外释放研究发现,ORI胶束体外释药过程近似符合Higuchi释药模型:Q=8.2197t1/2+12.439(r=0.9911)。结论:采用溶剂扩散法制备ORI胶束方法简单,重现性好,其体外释放显示出一定的缓释效果。
Objectives ： To prepare oridonin-loaded methoxy poly （ ethylene glycol ） -poly （ D, L-laetide ） （PEDLA） block copolymer mieelles, and to study the characteristics and in vitro release behaviors of the micelles. Methods：The PEDLA were prepared by melting polymerization. The oridonin-loaded block copolymer micelles were made by the solvent exchange method with PEDLA as carrier materials. The mean size and Zeta potential of mieelles were determined by dynamic light scattering. The drug loading and encapsulation efficiency of micells were examined by ultraviolet spectrophotometry. The in vitro release of oridonin-loaded block copolymer mieelles was evaluated using a dialysis method. Results：The mean size of oridonin-loaded block eopolymer micelles was （136.7 ± 1.54） nm, and Zeta potential, drug loading and encapsulation efficiency were estimated to be （ - 18.9 ± 0.79 ） mv, （ 5.19 ± 0.06） % and （73.9 ±0.6） % , respectively. In vitro release behavior was described by Higuehi equation ： Q=8.2197t1/2＋12.439（r=0.9911） . Conclusion： Oridonin can be encapsulated in PEDLA by solvent exchange method. The method is simple and reproducible. The in vitro release study showed significant sustained release of oridonin-loaded block copolymer micelles.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2009年第16期1560-1565,共6页
Chinese Journal of New Drugs
