正交设计优化尼美舒利NLC处方组成与制备工艺

运用高压均质法制备了加载尼美舒利的纳米结构脂质载体（Nanostructured Lipid Nanoparticles, NLC），采用单因素设计考察了固液态油脂比、脂质用量、乳化剂用量、药脂比、均质压力和均质次数对纳米粒质量的影响。采用正交设计优化了制备条件。确定的最适宜制备方案为油酸与单硬脂酸甘油酯（glycerin monostearate，GMS）投料比为3:10，药脂比为1:40， TPGS用量为1.4 g，均质压力为90 MPa。依据最适宜处方制备的纳米粒粒径为132.6± 1.4 nm，包封率为82.35±1.23%。扫描电镜显示所制备纳米粒呈类球形，体外释放实验表明其释放行为符合Higuchi模型。

Optimization of Formulation and Preparation Parameters for Nimesulide Loaded NLC by Orthogonal Design

High pressure homogenization method was used to prepare Nimesulide loaded nanostructured lipid nanoparticles（NLC）.Single factor design was chosen to study the influence of solid-liquid lipid ratio,amount of lipid,amount of emulsifier,drug-lipid ratio,homogenization pressure and homogenization cycles on quality of the prepared nanoparticles.Orthogonal design was used to optimize the preparation parameters.The optimal preparation method was 3∶ 10 of oleic acid-glycerin monostearate（GMS） ratio,1∶ 40 of drug-lipid ratio,1.4 g of TPGS,90 MPa of homogenization pressure.Particle size and entrapment efficiency of NLC prepared by optimal conditions were 132.6 ± 1.4 nm and 82.35 ± 1.23%,respectively.The scanning electron microscope showed that the nanoparticles were of spherical shape.The in vitro release study showed that release behavior accorded with Higuchi model.