物理化学刺激介导的沉方法,用于调节里芬素的溶解和口服生物可用性
Vineet Kumar Rai1, Deepak Pradhan1, Jitu Halder1
1Department of Pharmaceutics, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to Be University), Bhubaneswar, Odisha, 751003, India.
AAPS PharmSciTech
|August 19, 2024
概括
研究人员使用人血清白素 (HSA) 纳米颗粒增强了口服里法素 (RMP) 的生物可用性. 与自由RMP相比,甲醇沉产生了最好的结果,显著增加了药物复杂化和改善了吸收.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 生物化学 生化学
背景情况:
- 药物与蛋白质的结合影响药物相互作用和可溶性.
- 改善口服生物可用性,如利芬素 (RMP) 溶解不良的药物是一个重大挑战.
- 人类血清白蛋白 (HSA) 由于其生物相容性,是药物输送的有希望的载体.
研究的目的:
- 通过配制与人血清白蛋白纳米颗粒 (HSA NPs) 来增强里芬素 (RMP) 的溶解和口服生物利用性.
- 研究不同沉技术对HSANP的特性及其药物结合能力的影响.
- 评估RMP-HSANP复合体的体外药物释放和体内药理动力学性能.
主要方法:
- 使用甲醇沉,硫酸沉和热处理准备HSANP.
- 对HSANP的表征包括疏水性,大小,表面电荷,FTIR,TG-DSC,XRD和形态.
- 确定了药物复合效率,并在模拟的胃和肠介质中进行了体外药物释放研究.
- 药物动力学研究在体内进行,以评估生物可用性.
主要成果:
- 与原生白蛋白相比,RMP-HSA NPs-M13复合物 (甲醇沉) 显示出最高的复合效率 (增加3.5倍).
- 降水方法显著改变了HSA NP的特性,包括疏水性和尺寸.
- 在模拟的胃介质中观察到加速药物释放,与自由RMP相比,RMP-HSA NPs-M13的透和药理动力学参数 (Cmax,AUC,t1/2,MRT) 增强.
结论:
- 沉技术在设计稳定的合体HSA NP载体系统中是有效的,用于溶解不良的药物.
- 甲醇沉方法提供了一种可扩展和高效的方法来增强利芬素的口服生物可用性.
- 该战略为改善药物输送提供了传统表面活性剂或聚合物的可行替代品.
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