库尔库明无形固体分散受益于基基甲基纤维素E50,以增强抗炎作用
Jiayi Zhang1, Xianbao Shi2, Wei Tao3
1Department of Ultrasonography, The First Affiliated Hospital of Jinzhou Medical University, Jinzhou, Liaoning, China.
International journal of biological macromolecules
|August 26, 2023
概括
基甲基纤维素 (HPMC) 通过减少颗粒大小和防止结晶,增强黄素 (Cur) 无形固体分散 (ASDs). 这种配方改善了黄素的功效.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 黄素 (Cur) 具有较差的溶解性和透性,限制了其治疗应用.
- 无形固体分散 (ASDs) 是一个有前途的策略,以提高药物输送.
- 欧德拉吉特EPO (EuD) 和基甲基纤维素E50 (HPMC) 是针对ASD配方进行研究的聚合物.
研究的目的:
- 调查HPMC在提高黄素无形固体分散 (ASD) 的可溶性和透性的作用.
- 阐明HPMC影响黄素结晶和跨膜传输的机制.
- 评估含有HPMC的ASD对口服生物可用性和抗炎作用的影响.
主要方法:
- 使用Eudragit EPO (EuD) 和不同比例的HPMC,制备黄素ASD.
- 动态光散射 (DLS) 用于确定颗粒大小和评估结晶抑制.
- 分子动态 (MD) 建模用于研究分子相互作用和聚合行为.
- 使用脂双层模型评估跨膜透性.
- 在体内对口服相对生物利用率和抗炎疗效的评估.
主要成果:
- 添加HPMC可以将ASD中的黄素颗粒大小从300nm降低到200nm,从而抑制结晶.
- MD模拟显示,HPMC在EuD介质中阻止了黄素的聚合.
- HPMC作为表面活性剂,破坏了脂二层,并增强了黄素的跨膜运输.
- 在Cur-EuD/HPMC 3:1的ASD中,显著改善了透性,口服生物可用性和抗炎活性.
结论:
- HPMC是开发有效的黄素ASDs的关键辅助剂.
- 通过减少颗粒大小,抑制结晶和改善跨膜传输,HPMC提高了黄素的可溶性和透性.
- 用最佳数量的HPMC配制的黄素ASD代表了医疗应用的可行的治疗策略.
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