马钱子总碱脂质液晶纳米粒的制备及工艺优化

Preparation and Process Optimization of Total Alkali Lipid Liquid Crystal Nanoparticles from Strychnine Seed

乙醇注入结合硫酸铵主动载药技术制备马钱子总碱脂质液晶纳米粒(LLCN)。在筛选并确定脂质体制备方法的基础上,选择磷脂-胆固醇比、脂-药比、硫酸铵浓度、乙醇的体积为影响因素,以LLCN包封率为考察指标,单因素分析确定响应值,正交设计L_(9)(3^(4))优化处方参数,电镜检测LLCD的粒径、表面电荷,分析其稳定性。实验得出的最佳工艺参数为:磷脂-胆固醇比6:1、脂-药比为10:1、硫酸铵浓度0.2 moL/L、乙醇的体积12 mL/100 g, LLCN的表证和稳定性均符合制剂标准。

Brucine total alkaloids of strychnos nux~vomica Linn Lipid liquid crystal nanoparticles(LLCN) by ethanol injection combined with active drug loading of ammonium sulfate was prepared. On the basis of screening and determining the preparation method of liposomes, selecting lecithin cholesterol ratio, fat-drug ratio, concentration of ammonium sulfate, the volume of ethanol for the influence factors of LLCN coating rate as index, the single factor analysis was used to determine the response value, orthogonal design L_(9)(3^(4)) was used to optimize the prescription parameter, electron microscopy was used to detect particle size and surface charge of LLCD, its stability was analyzed. The optimal process parameters were obtained as follows: phospholipid-cholesterol ratio was 6:1, lipo-drug ratio was 10:1, ammonium sulfate concentration was 0.2 mol/L, volume of ethanol was 12 mL/100 g. The surface and stability of LLCN were in line with the preparation standard.