制备和评估HPMC和pullulan-based含有cilnidipine纳米悬浮的快速溶解薄膜
Shirleen Miriam Marques1, Salwa1, Cheryl Rhea Lewis2
1Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, 576 104 Udupi, Karnataka, India.
International journal of biological macromolecules
|April 20, 2025
概括
这项研究开发了尼迪平 (CLD) 纳米悬浮的快速溶解薄膜 (RDF),以提高其生物可用性. 新的口腔输送系统增强了CLD.
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:
- 锡利尼迪平 (CLD) 是一种有效的抗高血压药物.
- 较差的水溶性和广泛的第一通代谢限制了CLD的口服生物利用性.
- 口分娩提供了一种潜在的绕过肝脏代谢的途径.
研究的目的:
- 为了制定和描述含有尼迪平 (CLD) 纳米悬浮的快速溶解薄膜 (RDF),用于口腔输送.
- 通过绕过第一通代谢来提高CLD的生物可用性.
- 为了评估开发的CLD装载RDF的抗高血压疗效.
主要方法:
- 通过使用中央复合设计 (CCD) 进行纳米沉和优化来制备纳米悬浮.
- 纳米粒子 (大小,泽塔潜力) 和薄膜特性 (拉伸强度,分解,溶解) 的表征.
- 在实验室中进行药物透研究和在实验室中对大鼠进行抗高血压疗效评估.
主要成果:
- 优化的CLD纳米悬浮显示颗粒大小为362.23nm,泽塔电位为-39.1mV.
- 装有CLD的RDF表现出快速分解 (17.21秒) 和高的体外释放率 (91.77%在60分钟内).
- 口腔CLD纳米悬浮RDF显示药物透率,AUC和Cmax显著增加,与传统膜相比,Tmax和MRT降低,并对大鼠的血压控制优越.
结论:
- 含有西尼迪平纳米悬浮的快速溶解薄膜是通过口腔输送改善药物的生物可用性的有希望的策略.
- 这种方法有效地绕过了第一通代谢,从而提高了药物动力学参数和优异的抗高血压活性.
- 开发的基于纳米悬浮的RDF为高血压管理提供了可行的替代方案.
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