优化ibrutinib的生物可用性:构建和评估基于基基基-β-环素的纳米海绵输送系统
Sunitha Sampathi1, Nitiraj Kulkarni1,2, D V R N Bhikshapathi3
1School of Pharmacy, Vishwakarma University, 411048, Pune, Maharashtra, India.
Current research in pharmacology and drug discovery
|June 30, 2025
概括
将易布鲁替尼 (IBR) 制成基甲基β-环极氨酸纳米海绵 (HPβCD-NSPs) 显著提高了口服生物可用性. 这种新的药物输送系统显示了改善黑色素瘤治疗的前景.
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:
- 易布鲁替尼 (IBR) 是一种II类药物,溶解性差,限制了其口服生物利用性.
- 纳米海绵 (NSP) 提供了一种潜在的解决方案,可以增强难溶性药物的输送.
- 在NSP配方中使用了 propyl β-cyclodextrin (HPβCD) 和 1,1'-carbonyldiimidazole (CDI).
研究的目的:
- 为了制定和优化ibrutinib载荷的HPβCD-NSPs以改善口服生物利用性.
- 描述开发的纳米海绵的物理化学特性和药物捕获效率.
- 评估IBR载荷的HPβCD-NSPs的体外和体内性能.
主要方法:
- 使用基于设计的方法制定IBR载荷的HPβCD-NSP.
- 优化HPβCD与CDI的摩尔比率,速率和持续时间.
- 使用粒子大小分析,泽塔潜力,捕获效率,X射线衍射,FT-IR和DSC进行表征.
- 在体外释放药物,透性研究和体内药物动力学评估.
主要成果:
- 优化IBR载荷的HPβCD NSPs的粒子大小为145.6 ± 6.8 nm,PDI为0.170 ± 0.036,捕获效率为71.04 ± 2.40%.
- 药理动力学研究显示,与自由IBR相比,AUC0-t增加了14.96倍,Cmax增加了6.45倍.
- 这些结果表明,口服ibrutinib的生物可用性得到了显著改善.
结论:
- 装有IBR的HPβCD NSPs代表了增强药物释放和口服生物可用性的有希望的纳米载体系统.
- 这种配方策略具有显著的潜力,可以提高ibrutinib的治疗疗效,特别是在黑色素瘤治疗中.
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