载绞股蓝皂苷纳米结构脂质载体的制备及体外评价

Preparation and in vitro evaluation of gypenosides-loaded nanostructured lipid carriers

目的:采用高压均质法制备载绞股蓝皂苷纳米结构脂质载体(gypenosides-loaded nanostructured lipid carriers,GPS-NLCs),考察其性质并对其进行体外评价。方法:单因素考察搅拌功率、搅拌时间、均质压力、循环次数对纳米结构脂质载体(NLCs)粒径和多分散系数(polydispersity index,PDI)的影响,并采用透射电镜对GPS-NLCs进行形态学观察,同时评价GPS-NLCs的体外溶出行为。结果:优化所得GPS-NLCs的粒径为(159.6±6.6)nm,PDI为(0.221±0.009),包封率和载药量分别达到(74.30±3.17)%和(4.91±0.39)%。与绞股蓝皂苷原料药和载绞股蓝皂苷固体脂质纳米粒比较,GPS-NLCs的体外溶出明显提高。结论:高压均质法制备的GPS-NLCs粒径分布均匀,药物包封率高,能显著提高药物的体外溶出度且具有明显的缓释效果。

Objective:To prepare gypenosides-loaded nanostructured lipid carriers(GPS-NLCs)by hot melting high-pressure homogenization method and investigate its properties and in vitro release.Methods:The effects of stirring power,stirring time,homogeneous pressure and cycle times on the particle size and polydispersity index(PDI)of GPS-NLCs were investigated by single-factor test.The morphology of GPS-NLCs was characterized by transmission electron microscopy(TEM)and dissolution behavior of GPS-NLCs was evaluated in vitro.Results:The optimized particle size of GPS-NLCs was(159.6±6.6)nm,PDI was(0.221±0.009)and entrapment efficiency(EE)and drug loading(DL)were(74.30±3.17)%and(4.91±0.39)%,respectively.As compared with GPS powder and gypenosides-loaded solid lipid nanoparticles,GPS-NLCs could improve drug dissolution significantly.Conclusion:The particle size distribution of GPS-NLCs prepared by high pressure homogenization method was uniform,the drug entrapment efficiency was high,the dissolution rate of the drug in vitro could be significantly improved with obvious sustained drug release.