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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。
OBJECTIVE: To prepare ORI block copolymer micelles by polyethylene glycol monomethyl ether-polylactic acid (PEDLA) and to study its in vitro release. Methods: The PEDLA block copolymer was synthesized by melt ring-opening polymerization. The ORI micelles were prepared by solvent diffusion method. The particle size, Zeta potential, drug loading, encapsulation efficiency and in vitro release of ORI micelles Were studied. Results: The average diameter of ORI micelles was (136.7 ± 1.54) nm, the Zeta potential was (-18.9 ± 0.79) mv, the drug loading was (5.19 ± 0.06)% and the entrapment efficiency was (73.9 ± 0.6) )%. In vitro release studies showed that ORI micelles in vitro release process in line with Higuchi release model: Q = 8.2197t1 / 2 +12.439 (r = 0.9911). CONCLUSION: The method of solvent diffusion to prepare ORI micelles is simple and reproducible, and its in vitro release shows some sustained release effect.