星点设计-效应面法优化穿心莲内酯固体脂质纳米粒处方

以高压均质法制备穿心莲内酯固体脂质纳米粒。采用星点设计考察药物与脂质材料(即单硬脂酸甘油酯与山嵛酸甘油酯的1∶1混合物)比例、卵磷脂与脂质材料比值及表面活性剂(吐温-80)浓度对包封率和载药量的影响,并对结果进行多元线性和二项式方程拟合,用效应面法预测最佳处方。结果表明,载药量的多元线性回归拟合方程具有良好的相关性,而包封率的二项式拟合方程优于多元线性回归拟合方程。优化处方为药脂比9%、卵磷脂与脂质材料比值为1.6、吐温-80浓度为3%。优化后固体脂质纳米粒的包封率和载药量分别为(91.0±0.9)%和(3.49±0.03)%,粒径为(286.3±8.0)nm,电位为(-20.6±0.2)mV。

Optimization of Andrographolide Solid Lipid Nanoparticles by Central Composite Design and Response Surface Methodology

Andrographolide solid lipid nanoparticles were prepared by high pressure homogenization.The influence of the ratio of drug to lipid materials(the mixture of glycerin monostearate and Compritol ATO 888 with the ratio of 1∶1),ratio of lecithin to lipid materials and the concentration of surfactant(Tween-80) on entrapment efficiency and drug loading were investigated by central composite design.The results fit with multiple linear and binomial equation and the optimal formulation was predicted by response surface methodology.The results showed that there was a well correlation for drug loading by multiple linear regression while for entrapment efficiency the binomial equation was superior to the multiple linear regression.The optimal formulation was as follows: the ratio of drug to lipid materials was 9%,the ratio of lecithin to lipid materials was 1.6,and the concentration of Tween-80 was 3%.The entrapment efficiency,drug loading,mean diameter and ζ potential of the product were(91.0±0.9)%,(3.49±0.03)%,(286.3±8.0)nm and(-20.6±0.2)mV,respectively.