欧德拉吉特S100涂层脂质体:一个响应pH的策略,以克服达比加乙酸盐的口服生物利用性挑战
Maged K Elsayad1, Abdulsalam M Kassem1,2, Elsaied H Barakat1
1Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Al-Azhar University, Nasr City 11751, Cairo, Egypt.
The Journal of pharmacy and pharmacology
|October 26, 2025
概括
欧德拉吉特S100涂层脂质体显著增强大比加乙酸口服生物利用性,通过保护它在胃中并释放它在肠道中. 这种新的纳米载体系统可以改善药物吸收和治疗潜力.
科学领域:
- 制药科学 制药科学
- 纳米技术 纳米技术
- 药物输送系统 药物输送系统
背景情况:
- 达比加特兰乙酸盐 (DAB) 由于其依赖pH的溶解度,口服生物利用性较差 (6%-7%).
- 这种局限性阻碍了其作为直接血栓激素抑制剂的治疗疗效.
研究的目的:
- 设计Eudragit S100 (EU) 涂层脂质体,以提高DAB的口服输送.
- 通过保护它在胃中并使目标肠道释放成为可能,提高DAB的生物可用性.
主要方法:
- 用薄膜水化制备了封装DAB的脂质体囊泡.
- 配方经过了全面的物理化学表征 (FTIR,DSC,泽塔潜力,粒子大小,PDI,EE%,TEM).
- 在小鼠身上进行了体外药物释放和体内药理动力学研究.
主要成果:
- 优化的配方,EU@DAB-Lip4,显示了小颗粒大小 (136.9纳米),高捕获效率 (92.67%) 和良好的体稳定性.
- 在体外释放研究证实了pH响应性行为,胃释放最小,肠释放增强.
- 药理动力学研究显示,与DAB悬浮剂相比,生物可用性增加了5.6倍,Cmax和AUC0-∞显著增加.
结论:
- 欧德拉吉特S100涂层脂质体代表了改善达比加乙酸盐生物可用性的有希望的平台.
- 这种纳米载体方法增强了药物吸收,并有可能改善治疗结果.
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