水飞蓟宾纳米粒的制备及其理化性质研究

目的 制备水飞蓟宾纳米粒并对其进行质量评价.方法 采用乳化-蒸发-固化法制备水飞蓟宾纳米粒,以包封率、多分散指数、载药量等为评价指标优化制备工艺.考察体外释药规律,考察3～5℃、15～25℃、37℃(相对湿度为75%)条件下纳米粒的稳定性.结果 以硬脂酸和表面活性剂为载体材料,优化工艺制备的水飞蓟宾纳米粒包封率为96.88%,多分散指数为0.168,载药量为7.55%.差示量热分析确证形成了纳米粒,水飞蓟宾以无定形态分散在纳米粒内.纳米粒体外释放缓慢,可用Higuchi方程拟合.纳米粒静置观察具有良好的稳定性.结论 采用乳化-蒸发-固化法可制备得到水飞蓟宾纳米粒,工艺简便,粒径和分散度小,包封率和载药量高,体外释药缓慢,稳定性好.

Preparation and physicochemical characterization of silibinin nanoparticles

Objective To prepare silibinin nanoparticles and investigate their properties.Methods Silibinin nanoparticles were prepared by the emulsion evaporation-solidification method at low temperature.The entrapment efficiency,polydispersity index,drug loading were set as evaluation indexes to optimize the preparation processing.Drug release from nanoparticles and the stability of nanoparticles were investigated at the different temperatures of 3-5℃,15-25℃,and 37℃,respectively,and with the relative humidity of 75%.Results Taking stearic acid and surfactant Brij 78 as carrier,the entrapment efficiency of silibinin nanoparticles prepared by optimized technology was up to 96.88%,the dispersion index of the smallest was 0.168,and durg loading was 7.55%.Analysis by using differential scanning calorimetry showed that silibinin was dispersed in the nanoparticles at an amorphous state.The in vitro silibinin released slowly from nanoparticles and the release profile fitted well into Higuchi equation.Nanoaparticles were stable under storage conditions.Conclusion Silibinin nanoparticles could be prepared by the emulsion evaporationsolidification method,with the advantages of techniques simple,diameter and dispersion small,entrapment efficiency and drug loading high,in vitro release slow,and stability good.