通过热挤出技术制备的黄素纳米晶体的增强溶解和生物利用性
Yujie Zhao1, Xiaoyin Xu1, Anyin Dai2
1College of Pharmacy, Zhejiang University of Technology, Hangzhou, People's Republic of China.
International journal of nanomedicine
|June 19, 2024
概括
热挤出 (HME) 技术被用于制造黄素纳米晶体 (Cur-NCs),显著增强黄素.
科学领域:
- 材料科学 材料科学 材料科学
- 制药技术 制药技术 制药技术
- 纳米技术 纳米技术
背景情况:
- 黄素 (Cur) 具有较差的溶解性和生物可用性,限制了其治疗应用.
- 纳米晶体配方是一种有前途的策略,可以增强难溶药物的溶解和吸收.
- 热挤出 (HME) 为药物输送系统提供了一种连续和可扩展的制造工艺.
研究的目的:
- 使用HME技术制备素纳米晶体 (Cur-NCs).
- 提高黄素的溶解率和口服生物可用性.
- 评估HME生产不溶性药物纳米晶的可行性.
主要方法:
- 通过使用Eudragit® EPO作为载体在各种药物载体比率上,通过一阶段的HME过程制备Cur-NCs.
- 描述包括粒子大小分析 (DLS),固态分析 (SEM,DSC,XRD) 和热稳定性评估 (TGA,HPLC).
- 为了评估Cur-NCs的性能,进行了溶解概况和药理动力学研究.
主要成果:
- 成功准备的Cur-NCs颗粒大小在50-150nm之间.
- 与纯黄相比,Cur-NCs的溶解速率显著提高 (例如,在<2分钟内80%),而纯黄的溶解速率显著提高.
- 药理动力学研究显示,黄素吸收显著增加,Cmax为代谢物的1.68倍,AUC为代谢物的4.07倍.
结论:
- HME技术提供了一种高效的一步方法,用于制备黄素纳米晶体.
- 库尔-NC配方显著改善了黄素的溶解和生物可用性.
- 这种基于HME的方法显示了制造不溶性药物的纳米晶体的广泛潜力.
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