瓦尔萨坦装载固体自纳米乳化输送系统,以增强口服吸收和生物可用性
Lusi Chen1, Xin Zhang2, Jiayu Xie1
1College of Pharmacy, Jiangxi University of Chinese Medicine, Nanchang, 330004, China.
AAPS PharmSciTech
|January 23, 2025
概括
这项研究开发了一种固体自纳米乳化药物输送系统 (S-SNEDDS),以改善沙坦 (VST) 的口服吸收. 新的S-SNEDDS显著提高了VST的生物可用性,为高血压提供了有前途的治疗方法.
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:
- 瓦尔萨坦 (VST) 是用于高血压管理的必不可少的血管激素II受体对抗剂.
- 口服VST的低生物可用性限制了其治疗功效.
- 需要新的药物输送系统来增强VST口服吸收.
研究的目的:
- 开发和描述瓦尔沙坦 (VST) 的固体自纳米乳化药物输送系统 (S-SNEDDS).
- 使用S-SNEDDS配方增强VST的口服吸收和生物可用性.
- 评估开发的VST装载S-SNEDDS的体外和体内性能.
主要方法:
- 通过可溶性研究和伪三次相图,制备VST加载液体SNEDDS (VST@L-SNEDDS).
- 在固体载体 (Neusilin® UFL2) 上吸附VST@L-SNEDDS,形成VST@S-SNEDDS.
- 在体外评估包括溶解,稳定性,细胞毒性和Caco-2细胞吸收.
- 在体内药理动力学研究以确定口服生物可用性增强.
主要成果:
- VST@L-SNEDDS表现出最佳特征 (19.90纳米大小,-20.57毫伏泽塔电位),并成功地被纳西林® UFL2.2吸收.
- 与VST@S-SNEDDS相比,VST@S-SNEDDS显示药物释放快 (>90%在60分钟内) 独立于pH值,并改善了长期稳定性.
- 这两种配方都显著增加了Caco-2细胞的吸收.
- 在体内研究显示,与原始VST相比,VST@S-SNEDDS的AUC0-24h增加了2.28倍,Cmax增加了4.86倍.
结论:
- 开发的VST@S-SNEDDS是一种有效的系统,可以提高瓦尔萨坦的口服吸收和生物可用性.
- 这种新的S-SNEDDS配方在改善高血压治疗方面具有重大前景.
- 固体自纳米乳化药物输送系统是改善沙坦等生物可用性较差药物的口服输送的可行策略.
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