基于薄荷醇的自我微乳化药物输送系统,用于增加edoxaban的肠道吸收
Ola A Refaey1,2, Gamal M El Maghraby1, Mona F Arafa1,3
1Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta University, Al-Geish Street, Tanta 31527, Egypt.
The Journal of pharmacy and pharmacology
|September 19, 2025
概括
这项研究开发了一个微乳液系统,以改善edoxaban的可溶性和肠道透性. 该系统显著增强了药物的溶解和吸收,提高了治疗效果.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 纳米技术 纳米技术
背景情况:
- 埃多克萨班的临床疗效受到溶解性差和P-glycoprotein (P-gp) 介导的排泄物限制,减少了其口服吸收.
- 制定克服这些障碍的策略对于增强edoxaban的治疗潜力至关重要.
研究的目的:
- 使用微乳液系统增强edoxaban的溶解和肠道透性.
- 在微乳液中将薄荷醇作为油相成分和P-gp抑制剂.
主要方法:
- 在37°C时构建伪三元相位图,以确定最佳的微乳液配方.
- 选择和评估由薄荷醇,Tween 80,乙醇和水 (20:30:30:20比) 组成的微乳液.
- 微乳液性质的表征,包括滴滴大小,多分散度指数和泽塔潜力.
主要成果:
- 优化微乳液的液滴大小为163.47nm,PDI为0.28,泽塔电位为-16.43mV.
- 在溶解介质中的自我微乳化提高了edoxaban的溶解效率,达到95.39% (与未加工药物的66.64%相比).
- 实地肠道输液研究显示,十二指管的透率增加了2.96倍,阴道的透率增加了2.06倍,这归因于P-gp抑制和增强的膜流动性.
结论:
- 开发的微乳液系统有效地提高了edoxaban的可溶性和肠道透性.
- 这种方法具有显著的潜力,可以提高edoxaban的口服生物可用性和整体治疗疗效.
- 薄荷和Tween 80在抑制P-gp流量和促进药物吸收方面发挥着关键作用.
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