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目的 以聚乙二醇单甲醚-聚乳酸(mPEG-PLA)嵌段共聚物为载体材料制备塞来昔布载药胶束,并考察其在大鼠体内药动学情况.方法 采用薄膜分散法制备塞来昔布载药胶束,评价载药胶束的微观形态、粒径分布、Zeta电位等理化性质;采用动态膜透析法考察塞来昔布乙醇溶液和载药胶束的体外释药情况;考察塞来昔布乙醇溶液和塞来昔布载药胶束经尾静脉注射后在大鼠体内药动学情况.结果 透射电镜显示塞来昔布载药胶束粒径均一,成球状或类球状分布,平均粒径为(35.6±15.1) nm,PdI为0.152±0.05,Zeta电位为(-24.6±2.9)mV;塞来昔布载药胶束在0.5％ SDS磷酸盐缓冲液中24 h累积释放81.5％;塞来昔布乙醇溶液和塞来昔布载药胶束在大鼠体内的t1/2分别为(4.41±0.41)h和(6.38±0.81)h,AUC分别为(86.17±4.08)和(142.21±7.82) mg·(L·h)-1.结论 塞来昔布载药胶束与塞来昔布乙醇溶液相比,延长了药物在大鼠体内的滞留时间,有望提高药物治疗效果.“,”Objective To prepare celecoxib-loaded micelles with polyethylene glycol monomethyl etherpolylactic acid (mPEG-PLA) block copolymer as the carrier material and to study the pharmacokinetics of celecoxib-loaded micelles in rats.Methods Celecoxib-loaded micelles were prepared using film dispersion method.The physical and chemical properties of celecoxib-loaded micelles,such as microscopic morphology,particle size distribution and zeta potential,were evaluated.The in vitro drug release of the celecoxibethanol solution and celecoxib-loaded micelles was investigated via dynamic membrane dialysis.The pharmacokinetics of celecoxib-ethanol solution and celecoxib-loaded micelles were observed in rats after tailvein injection.Results The particle size distribution,PdI and Zeta potential of celecoxib-loaded micelles were (35.6±15.1) nm,0.152±0.05 and (-24.6±2.9) mV,respectively.In 0.5％ SDS phosphate buffered saline,the in vitro cumulative release of celecoxib-loaded micelles reached up to 81.5％ within 24 h.Half lives (t1/2) of celecoxib-ethanol solution and celecoxib-loaded micelles were (4.41±0.41) and (6.38±0.81) h respectively,and AUC(0-t) was estimated to be (86.17±4.08) and (142.21±7.82) mg·(L ·h)-1respectively.Conclusion Celecoxib-loaded micelles can prolong the residence time in rats compared with celecoxib ethanol solution,which are expected to improve the therapeutic effect of celecoxib.