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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。
Nanostructured Lipid Nanoparticles (NLC) loaded with nimesulide were prepared by high pressure homogenization. The ratio of solid to liquid lipid, lipid content, emulsifier, drug-lipid ratio, Effect of mass pressure and homogenization times on the quality of nanoparticles. Orthogonal design was used to optimize preparation conditions. The most suitable preparation method was oleic acid and glycerol monostearate (glycerol monostearate, glycerol monostearate (glycerol monostearate, GMS feed ratio of 3:10, lipid ratio of 1:40, TPGS dosage of 1.4 g, homogeneous pressure of 90 MPa. Nanoparticles prepared according to the most appropriate prescription have a diameter of 132.6 ± 1.4 nm and an encapsulation efficiency of 82.35 ± 1.23%. Scanning electron microscopy showed that the prepared nanoparticles were spherical in shape, and the in vitro release experiments showed that the release behavior of the nanoparticles was consistent with the Higuchi model.