固体脂质纳米颗粒的配方设计,优化和评估,载有抗病毒药物诺福维尔,使用盒式设计来提高口服生物可用性
1Department of Pharmaceutics, SRM College of Pharmacy, SRMIST, Kattankulathur, Chennai, Tamil Nadu, India.
Advances in pharmacological and pharmaceutical sciences
|January 9, 2025
概括
这项研究开发了固体脂质纳米颗粒 (SLN),以提高艾滋病毒药物诺福维尔 (TNF) 的口服生物可用性. 优化的SLN显著改善了药物输送,为生物可用性挑战提供了一个有希望的解决方案.
科学领域:
- 制药纳米技术 制药纳米技术
- 药物输送系统 药物输送系统
- 抗病毒疗法 抗病毒疗法
背景情况:
- 诺福维尔 (TNF) 是艾滋病毒治疗中必不可少的抗逆转录病毒药物,其口服生物可用性较差.
- 限制包括低透性,易受肠道新陈代谢的影响,以及P-glycoprotein (P-gp) 流量输送.
- 固体脂质纳米颗粒 (SLN) 是一种新兴的基于脂质的配方策略,有可能克服这些障碍.
研究的目的:
- 为增强口服生物可用性而配制和优化载有特诺福维尔 (TNF) 的固体脂质纳米粒子 (SLN).
- 调查影响SLN特征和药物释放的关键质量属性.
- 评估优化TNF-SLN配方的体外,体外和体内性能.
主要方法:
- 通过使用微乳液方法与康普瑞托 888 ATO 制备SLN.
- 一个Box-Behnken设计优化了脂质/表面活性剂含量和均质化时间,评估了颗粒大小 (PS) 和捕获效率.
- 描述包括PS,泽塔潜力 (ZP),多分散性指数,体外释放,体外透,固态分析 (DSC,PXRD),SEM,以及在老鼠体内药理学研究.
主要成果:
- 优化的配方 (F10) 呈现出小颗粒大小 (449.90 nm),狭窄分布 (0.304),高捕获效率 (83.13%) 和负ZP (-18.10 mV).
- 在体外释放之后出现了第一阶级动力学,在24小时内释放了99%的药物.
- 在老鼠体内研究表明,与纯药物溶液相比,诺福维尔的生物可用性增加了12.4倍.
结论:
- 固体脂质纳米颗粒 (SLNs) 有效地提高了口服诺福维尔 (TNF) 的生物可用性.
- 在克服常见的药物输送挑战方面,SLN具有显著的潜力,例如透性差和流量运输.
- 这种配方策略提供了一种有前途的方法来提高tenofovir和类似药物的治疗疗效.
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