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目的以聚乙二醇单甲醚-聚乳酸[methoxy poly(ethylene glycol)-poly(lactide),m PEG-PLA]嵌段共聚物为载体材料,制备他克莫司载药胶束,考察其制剂学性质。方法采用薄膜分散法制备他克莫司载药胶束。超速离心法测定他克莫司载药胶束的载药量和包封率。以载药量、包封率、粒径以及粒径分布为评价指标,采用单因素试验和正交试验优化他克莫司载药胶束制备处方。应用透射电镜、粒度测定仪和zeta电位分析仪对他克莫司载药胶束的形态、粒径和电位进行表征。结果在优化条件下制备的他克莫司载药胶束载药量为7.77%,包封率为84.31%,胶束粒子外观圆整且分散良好,平均粒径为23.20 nm,PDI为0.058,zeta电位为-0.831 m V。结论单因素试验联合正交试验可有效地优化他克莫司m PEG-PLA胶束处方和制备工艺。优化条件下制备的他克莫司载药胶束具有较高的载药量和包封率,粒径较小且分布均匀,24 h内稳定性良好。
OBJECTIVE To prepare the tacrolimus drug-loaded micelles by using methoxy poly (ethylene glycol) -poly (lactide), m PEG-PLA block copolymer as carrier material, Preparation properties. Methods Tacrolimus drug-loaded micelles were prepared by membrane dispersion method. Determination of drug loading and entrapment efficiency of tacrolimus loaded micelles by ultracentrifugation. Taking drug loading, encapsulation efficiency, particle size and particle size distribution as evaluation indexes, single factor experiment and orthogonal experiment were used to optimize the formulation of the drug-loaded micelles of tacrolimus. The morphology, particle size and potential of drug-loaded micelles of tacrolimus were characterized by transmission electron microscopy, particle sizer and zeta potential analyzer. Results Under optimal conditions, the drug loading volume of tacrolimus was 7.77% and the entrapment efficiency was 84.31%. The appearance of the micelles was well rounded and well dispersed. The average particle size was 23.20 nm and the PDI was 0.058. The zeta potential is -0.831 mV. Conclusion The single factor experiment combined with orthogonal experiment can effectively optimize the formulation and preparation of tacrolimus m PEG-PLA micelles. Optimized conditions prepared tacrolimus drug-loaded micelles with higher drug loading and encapsulation efficiency, smaller particle size and uniform distribution, good stability within 24 h.