塞来昔布载药胶束的制备与表征

Preparation and Characterization of Celecoxib-loaded Micelles

目的:以聚乙二醇单甲醚-聚乳酸(m PEG-PLA)嵌段共聚物为载体材料制备塞来昔布载药胶束并评价其药剂学性质。方法:采用薄膜分散法制备塞来昔布载药胶束,采用单因素试验法初步筛选塞来昔布载药胶束的处方和制备工艺,并采用Box-Behnken效应面法进一步优化。评价了载药胶束的微观形态、粒径分布、Zeta电位等理化性质,并采用动态膜透析法考察载药胶束的体外释药情况。结果:透射电镜显示塞来昔布载药胶束粒径均一,成球状分布,平均粒径为(35.6±15.1)nm,多聚分散系数(Pd I)为(0.152±0.05),Zeta电位为(-24.6±2.9)m V;塞来昔布载药胶束在0.5%十二烷基硫酸钠(SDS)磷酸盐缓冲液(p H 6.8)中24 h累积释放81.5%。结论:采用Box-Behnken效应面法优化塞来昔布载药胶束处方与制备工艺是简单、可行的。

Objective： To prepare cetecoxib-loaded micelles with polyethylene glycol monomethyl ether-polylactic acid （mPEG- PLA） block copolymer as the carrier material and evaluate the physical and chemical properties. Methods： Celecoxib-loaded micelles were prepared by a film dispersion method. The micelle formula and preparation process were screened by single factor experiment and further optimized by Box-Behnken response surface method. The physical and chemical properties of celecoxib-loaded mieelles such as microscopic morphology, particle size distribution and zeta potential were evaluated. The in vitro drug release of celecoxib-loaded mi- celles was investigated by dynamic membrane dialysis. Results： Celecoxib-loaded micelles prepared according to the optimized formula showed the following properties： the particle size distribution was （35.6 ± 15.1 ） nm, PdI was （0. 152 ±0.05）, and the zeta potential was （ - 24.6 ± 2.9 ） inV. In 0.5% SDS phosphate buffered saline （ pH 6.8 ）, the in vitro cumulative release of celecoxib-loaded mi- celles reached up to 81.5% in 24 h. Conclusion： It is simple and feasible to prepare eeleeoxib-loaded miceUes by the thin film dis- persion method.