循环德克斯特林复合作为一个有成效的策略,以提高从固体脂质纳米颗粒 nebivolol 交付的性能
P Mura1, F Maestrelli1, L M D Gonçalves2
1Department of Chemistry, School of Sciences of Human Health, University of Florence, via Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
International journal of pharmaceutics
|November 20, 2024
概括
这项研究开发了一种改进的nebivolol (NEB) 口服配方,使用基基基基 (HPβCD) 和固体脂质纳米颗粒 (SLN). 这种组合增强了NEB.
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:
- 尼比沃醇 (NEB) 是一种选择性β1-上腺素受体对抗剂,用于高血压.
- 低水溶性限制了NEB的口服生物可用性.
- 需要新的口服配方来提高NEB的疗效.
研究的目的:
- 开发一种有效的口服配方NEB.
- 通过与xypropyl-β-cyclodextrin (HPβCD) 复合并纳入固体脂质纳米颗粒 (SLN) 来增强NEB口服生物可用性.
主要方法:
- 用于选择SLN制剂的固体脂质 (Imwitor 491,988) 的溶解性研究.
- 对纳米粒子特征的脂质组成和表面活性剂的研究.
- 对NEB和NEB-HPβCD配方的药物载荷,物理化学性质,形态,捕获效率和药物释放的评估.
主要成果:
- HPβCD复合改善了SLN质量 (减小了尺寸,增强了同质性,增加了稳定性).
- HPβCD 阻止了 Zeta Potential 在药物加载时的减少,并提高了捕获效率.
- HPβCD允许药物负载增加一倍,同时保持物理化学性质和高捕获效率.
- HPβCD的结合改善了药物释放的控制.
结论:
- 在NEB口服配方中,HPβCD复合和SLN结合的联合策略是有效的.
- 这种方法显著提高了NEB的物理化学特性和口服输送潜力.
- 开发的配方为高血压治疗提供了更好的稳定性,负载能力和受控的药物释放.
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