一个新型的酸盐涂层Leciplex装有Ambrisentan作为可能的肺纳米系统:优化,特征和药理动力学评估
Hussein M Eid1, Toqa H Turkia1, Adel A Ali1
1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, 62514, Egypt.
Journal of pharmaceutical sciences
|April 6, 2024
概括
这项研究开发了AMS-CTS-LPX (ambrisentan chitosan-coated LeciPlex) 纳米粒子. 新的AMS-CTS-LPX配方显著提高了Ambrisentan的生物可用性,并显示了肺部药物输送的有希望的结果.
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:
- 肺动脉高血压 (PAH) 需要有效的药物输送系统.
- 安布里森坦 (AMS) 是PAH的关键药物,但其口服生物利用性有限.
- 新型纳米载体可以提高药物的疗效,减少副作用.
研究的目的:
- 为了制定,优化和表征Ambrisentan酸盐涂层LeciPlex (AMS-CTS-LPX) 纳米粒子.
- 为了提高阿姆布里森坦的治疗效果和生物可用性,用于肺部.
- 评估新型AMS-CTS-LPX配方的安全性和药理动力学特征.
主要方法:
- 使用中央复合设计 (CCD) 和设计专家®软件制定和优化AMS-CTS-LPX.
- 对AMS-CTS-LPX的捕获效率,粒子大小,表面电荷和药物释放动力学的表征.
- 在小鼠模型中进行的体内药理动力学研究,将AMS-CTS-LPX与口服AMS溶液进行比较.
- 在体内组织病理学研究,以评估内AMS-CTS-LPX的安全性.
主要成果:
- 优化的AMS-CTS-LPX配方实现了82.39%的捕获效率,137.53nm粒子大小和+43.65mV表面电荷.
- 在8小时内观察到90.41%的持续药物释放,表明良好的稳定性.
- 通过组织病理学分析,AMS-CTS-LPX的内注射被发现是安全的.
- 药理动力学研究表明,与口服相比,安布里森坦的生物可用性增加了5.6倍.
结论:
- 涂有素的LeciPlex纳米颗粒 (AMS-CTS-LPX) 是一个有前途的肺部药物输送系统.
- 增强的生物可用性和安全性概况表明了改善肺部疾病治疗的潜力.
- 需要进一步研究AMS-CTS-LPX作为安布里森坦的肺纳米系统.
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