摘要
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 develop and optimize the formulation of vinpocetine solid lipid nanoparticles. METHODS The vinpocetine solid lipid nanoparticles were prepared by melt-emulsion ultrasonication and low temperature-solidification methods. The formulation variables were optimized by ＇Box-Behnken design （BBD）＇ with response surface methodology （RSM） of glyceryl behenate, fluronic F-68 and the ratio of drug to lipid as independent variables, and encapsulation efficiency and particle size as dependent variables. The optimized solid lipid nanoparticles was characterized for encapsulation efficiency, particle size, zeta potential, morphology, and in vitro drug release behavior of solid lipid nanoparticles was also studied. RESULTS For encap- sulation efficiency, particle size, zeta potential of solid lipid nanoparticles were found to be （84. 7 ± 2, 7） %, （196. 6 ± 23. 4）nm and （ - 34. 3 ± 2. 4）mV, respectively. The solid lipid nanoparticles were found to be small and spherical with smooth surface as seen in transmission electron microscopy. The in vitro release data proved that the drug release was steady during 24 h. CON- CLUSlON The Box-Behnken experimental design facilitates the process of vinpocetine solid lipid nanoparticles.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2014年第13期1083-1088,共6页
Chinese Journal of Hospital Pharmacy
