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目的:通过优化固体脂质纳米粒处方,制备长春西汀固体脂质纳米粒。方法:采用热熔乳化超声-低温固化法制备固体脂质纳米粒,通过对处方优化:山嵛酸甘油酯质量分数(X1)、泊洛沙姆188质量分数(X2)、药脂比(X3)为考察对象,以包封率(Y1,EE%)、粒径(Y2,nm)为评价指标,利用Box-Behnken效应面法优化长春西汀固体脂质纳米粒处方;采用Malvern粒度仪测定纳米粒的粒径分布和Zeta电位,透射电镜考察其形态;并考察纳米粒的体外释药行为。结果:长春西汀固体脂质纳米粒的包封率为(84.7±2.7)%,粒径为(196.6±23.4)nm,Zeta电位为(-34.3±2.4)mV,透射电镜显示微乳粒径均一,成球状分布,纳米粒在24 h内平稳缓慢释药。结论:长春西汀固体脂质纳米粒处方采用Box-Behnken实验设计法优化是简单、可行的。
OBJECTIVE: To prepare vinpocetine solid lipid nanoparticles by optimizing the formulation of solid lipid nanoparticles. Methods: The solid lipid nanoparticles were prepared by hot-melt emulsification ultrasound and low temperature solidification. The optimal formulation was optimized by the following formula: the mass fraction of behenic acid ester (X1), the mass fraction of poloxamer 188 (X2) ), And the encapsulation efficiency (Y1, EE%) and particle size (Y2, nm) were used as evaluation indexes to optimize the formulation of vinpocetine solid lipid nanoparticles by the Box-Behnken effect surface method. The particle size distribution and Zeta potential of the nanoparticles were investigated by transmission electron microscopy. The in vitro drug release behavior of the nanoparticles was also investigated. Results: The encapsulation efficiency of vinpocetine solid lipid nanoparticles was (84.7 ± 2.7)%, the diameter was (196.6 ± 23.4) nm and the zeta potential was (-34.3 ± 2.4) mV. Uniform, into a spherical distribution, smooth and slow release of nanoparticles within 24 h. Conclusion: The prescription of vinpocetine solid lipid nanoparticles by Box-Behnken experimental design method is simple and feasible.