姜黄素维生素E聚乙二醇琥珀酸酯-聚乙二醇硬脂酸酯15胶束对姜黄素溶解度和口服生物利用度的影响

发布时间：2018-08-30 10:34

【摘要】：目的以维生素E聚乙二醇琥珀酸酯(VE-TPGS)和聚乙二醇硬脂酸酯15(Solutol HS 15,SHS15)为载体制备姜黄素胶束,并研究该胶束对姜黄素溶解度和口服生物利用度的影响。方法采用薄膜分散法制备姜黄素胶束;通过胶束平均粒径、载药量、包封率等指标表征该胶束,同时测定姜黄素的溶解度;通过体外释放考察该胶束的释放特性;进一步通过大鼠实验评估胶束对姜黄素口服生物利用度的影响。结果当VE-TPGS与SHS15加入质量比为3∶7时,胶束粒径为(35.79±1.23)nm,多分散性指数(PDI)为0.12±0.03;在该条件下,胶束的载药量和包封率分别为9.34%和90.03%,姜黄素的溶解度达到2.03 mg/m L;体外释放实验中,胶束组较姜黄素组有缓慢释放特性;大鼠口服生物利用度实验中,胶束组较姜黄素组的相对生物利用度提高到303.5%(P0.01)。结论本实验制备的胶束不仅有较好的缓释特性,还提高了姜黄素的溶解度和口服生物利用度。利用药物-胶束体系来改善难溶性药物的溶解度,具有较高的临床应用潜力。
[Abstract]:Objective to prepare curcumin micelles with vitamin E polyethylene glycol succinate (VE-TPGS) and polyethylene glycol stearate (15 (Solutol HS 15 SHS15) as carriers, and to study the effects of the micelles on the solubility and oral bioavailability of curcumin. Methods the curcumin micelles were prepared by thin-film dispersion method. The micelles were characterized by the mean particle size, drug loading and encapsulation efficiency, and the solubility of curcumin was also determined, and the release characteristics of curcumin micelles were investigated by in vitro release. The effects of micelles on oral bioavailability of curcumin were further evaluated in rats. Results when the mass ratio of VE-TPGS to SHS15 was 3:7, the particle size of micelle was (35.79 卤1.23) nm, polydispersity index (PDI) was 0.12 卤0.03.The drug loading and entrapment efficiency of micelle were 9.34% and 90.03%, respectively, and the solubility of curcumin was 2.03 mg/m L in vitro release experiment. The relative bioavailability of micelle group was increased to 303.5% compared with curcumin group (P0.01). Conclusion the micelles prepared in this study not only have good sustained-release properties, but also improve the solubility and oral bioavailability of curcumin. It has high clinical application potential to improve the solubility of insoluble drugs by using drug-micelle system.
【作者单位】：南通市中医院;江苏省中医药研究院;
【分类号】：R943

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