姜黄素胆盐/磷脂混合胶束的制备及理化性质

Preparation of curcumin-loaded bile salt/phospholipid mixed micelles and its physicochemical properties

目的制备姜黄素胆盐/磷脂混合胶束,以提高姜黄素在水中的溶解度,改善其生物利用度。方法采用薄膜分散法制备混合胶束,以载药量(DL)和包封率(EE)为指标,在单因素考察的基础上,采用星点设计-效应面法进行处方优化,测定微观形态、粒径和zeta电位等理化性质,采用动态膜透析法观察体外释放。结果姜黄素胆盐/磷脂混合胶束粒子呈圆球形,分布均匀,平均粒径为(66.5±1.5)nm,zeta电位为(-26.96±0.95)mV,DL和EE分别为(13.48±0.21)%和(87.13±0.98)%,姜黄素溶解度为3.14 mg/mL,体外释放呈现良好的缓释特性。结论所制备的姜黄素胆盐/磷脂混合胶束可显著改善姜黄素水中溶解度。

Objective To improve the solubility of curcumin in water and its bioavailability by preparing curcuminloaded bile salt/phospholipid mixed micelles. Methods Curcumin-loaded bile salt/phospholipid mixed micelles were prepared by the film dispersion method. Based on the single factor exploration,the central composite design-response surface methodology was employed to optimize the preparation technology with drug loading and entrapment efficiency as indicators. The physicochemical properties such as micromorphology,particle size and zeta potential were evaluated. The dialysis method was used to investigate the in vitro release process of curcumin from micelles. Results The particles of curcumin-loaded bile salt/phospholipid mixed micelles were spherical and well dispersed with the average size of（66. 5 ±1. 5） nm and the zeta potential of（-26. 96 ±0. 95） mV. Curcumin was encapsulated in bile salt/phospholipid mixed micelles with loading capacity of（13. 48 ± 0. 21） % and entrapment efficiency of（87. 13 ± 0. 98） %. The solubility of curcumin in water was 3. 14 mg/mL,and the results of the in vitro release showed that the mixed micelles presented the obvious sustained-release behavior. Conclusion The curcumin-loaded bile salt/phospholipid mixed micelles system might serve as a promising nanocarrier to improve the solubility of curcumin.