多西他赛Pluronic F68聚合物胶束的制备与体外评价

Docetaxel-loaded Pluronic F68 polymeric micelles: preparation and in vitro evaluation

目的制备多西他赛(DTX)的普朗尼克F68(Pluronic F68)聚合物胶束,并对其理化性质进行研究。方法采用纳米沉淀法制备DTX胶束,以L9(34)正交实验优化处方;高效液相色谱法测定药物的含量;通过透射电镜观察DTX胶束的形态,并进行粒度分布和zeta电位的测定;采用动态膜透析法考察DTX胶束的体外释药行为。结果 DTX胶束的包封率为(89.10±1.50)%,载药量为(0.060±0.003)%,外观形态呈现球形或类球形,粒径为(135.1±3.42)nm,zeta电位为(-10.56±3.52)mV。体外释放结果显示DTX胶束具有一定的缓释能力。结论利用纳米沉淀法成功制备了DTX胶束,成型好,粒径小,改善了DTX的溶解性。

Objective To prepare docetaxel（DTX）-loaded Pluronic F68 polymeric micelles（DTX-micelles） and evaluate their physicochemical characterization.Methods The DTX-micelles were prepared by nano-precipitation methods.Based on the results of single factor experiments,the DTX-micelle formulation was optimized by orthogonal design.The encapsulation efficacy（EE%） and drug loading（DL%） were determined by the RP-HPLC method.The physicochemical characteristics were evaluated,including surface morphology,particle size and size distribution as well as zeta potential.The in vitro release behaviors of DTX-micelles were carried out by the dynamic membrane dialysis technique.Results The drug-loading rate and entrapment rate were（0.060±0.003）% and（89.10±1.50）%,respectively.The DTX-micelles were spherical with a mean particle size of（135.1±3.42） nm and a zeta potential of（-10.56±3.52）mV.The release of DTX from DTX-micelles followed the Weibull equation.Conclusions DTX-micelles were successfully prepared and improved the solubility of DTX.