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阿皮克萨班的质量设计驱动的纳米结构脂质支架:优化,表征和药物动力学评估

Kiran Patil¹, Nayan Gujarathi¹, Charu Sharma²

¹Shri Vile Parle Kelavani Mandal's Institute of Pharmacy, Dhule 424001, Maharashtra, India.

|July 27, 2024

概括

这项研究开发了纳米结构脂质载体 (NLCs),以提高Apixaban的生物可用性. 优化的NLCs显示药物释放的增强和药物动力学参数的显著增加,这表明这种抗凝剂的治疗结果更好.

科学领域:

制药科学制药科学
纳米技术纳米技术
药物运输药物运输药物运输

背景情况:

抗凝剂阿皮克萨班 (Apixaban) 面临生物可用性挑战,原因是溶解性差和广泛的代谢.
提高阿皮克萨班的口服吸收对于改善其治疗疗效和患者结果至关重要.

研究的目的:

开发和表征纳米结构脂质载体 (NLCs) 以改善Apixaban的口服输送.
评估Apixaban载荷的NLCs的药理动力学和体外释放特征.

主要方法:

通过高压均质化准备NLC,并通过2^3因数设计进行优化.
分析了粒子大小,PDI,泽塔潜力,捕获效率和药物辅助剂兼容性.
进行了体外药物释放和体外药理动力学研究,将NLC与自由阿皮克萨班进行比较.

主要成果:

经过优化后的NLC的粒子大小为232nm,PDI为0.514,泽塔电位为-21.9mV,捕获效率很高.
NLC 维持了阿皮克萨班的功效,并显示持续释放长达 48 小时.
在体内实验中,与自由Apixaban相比,Apixaban-NLCs的Cmax,AUC0-∞和t1/2显著更高,这表明其生物可用性有所提高.

结论:

纳米结构脂质载体有效地增强了Apixaban的口服生物可用性,并延长了它的治疗效果.
这种配方策略具有降低剂量频率和改善患者遵守的潜力.
NLCs代表了一种有希望的方法来克服像阿皮克萨班这样的溶解不良药物的局限性.

关键词:

23个完全的因数设计.阿皮克萨班 (Apixaban) 是一种药物.抗凝固剂是一种抗凝固剂.高压均化高压均化纳米结构的脂质载体 (NLCs)

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