杨梅素混合胶束的研制及其体外表征研究

Preparation of Myricetin-loaded Mixed Micelles Composed of Methoxy Polyethylene Glycol-Polylactic Acid/Pluronic F68 and Study on Its Characteristics and In Vitro Release Profile

目的研制载有杨梅素(myricetin,Myr)的聚乙二醇-聚乳酸(polyethylene glycol-polylactic acid,mPEG-PLA)/Pluronic F68混合胶束(mixed micelles,MMs),并对Myr-MMs进行表征及体外释放研究。方法通过丙酮溶剂挥发法研制Myr-MMs,以单因素及L9(34)正交实验优化处方及其工艺;并对制得的载药MMs的粒径、Zeta电位、外观形态、包封率、载药量和体外释放进行研究。结果最优处方制得的MyrMMs的包封率为(84.65±0.98)%、载药量为(2.73±0.03)%;透射电镜下观察Myr-MMs呈球形或类球形、表面光滑、无粘连;粒径为(41.74±0.27)nm,多分散系数为0.115±0.004;Zeta电位为(-25.47±1.22)mV;体外释放研究发现,MMs体外释药过程近似符合Weibull释药模型:ln(ln(1/(1-Q/100)))=0.927 1lnt-2.057 6(r=0.953 8)。结论利用丙酮溶剂挥发法成功研制了Myr-MMs,其成型好、粒径小、分布均匀,包封率和载药量均较高;且Myr经mPEG-PLA/Pluronic F68包裹后其体外释放显示出一定的缓释效果。

Objective To prepare myricetin-loaded mixed micelles composed of methoxy polyethylene glycol-polylactic acid/Pluronic F68 （Myr-MMs） and to study the characteristics and in vitro release profile of Myr-MMs.Methods The Myr-MMs were prepared by acetone solvent evaporation,and the formula and process were optimized by single-factor test and L9 （34） orthogonal experiment.The particle sizes,Zeta potential,appearance,encapsulation efficacy,drug loading,and in vitro release of Myr-MMs were studied.Results The encapsulation efficiency and drug loading of Myr-MMs based on the optimized formula were （84.65 ± 0.98）％ and （2.73± 0.03）％,respectively.The Myr-MMs were spherical or near-spherical,showed smooth surfaces,and had no adhesion,according to transmission electron microscopy.The mean particle size,polydispersity index,and Zeta potential were （41.74±0.27） nm,（0.115±0.004）,and （-25.47±1.22） mV,respectively.The in vitro release profile of Myr-MMs followed the Weibull equation：In（In（1/（1-Q/100））） =0.927 1Int-2.057 6 （r=0.953 8）.Conclusion Myr-MMs can be successfully prepared by acetone solvent evaporation,have good appearance,small and uniform particle sizes,and high encapsulation efficiency and drug loading,and show sustained in vitro release.