使用未涂层和聚合物涂层固体脂质纳米粒子提高simvastatin的口服生物可用性
Amira E Abd-Elghany1, Omar El-Garhy1, Adel Al Fatease2
1Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia 61519, Egypt.
Pharmaceutics
|June 27, 2024
概括
这项研究开发了固体脂质纳米颗粒 (SLN) 来改善simvastatin (SVA) 的生物可用性. 与传统悬浮相比,涂层SLN显著提高了SVA交付.
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:
- 西姆瓦斯塔丁 (SVA) 的口服生物可用性很差 (5%),这是由于肝脏的广泛第一通代谢和低溶解度.
- 这限制了它在治疗心血管疾病和高胆固醇血症方面的有效性.
- 需要新的药物输送系统来增强SVA的治疗潜力.
研究的目的:
- 开发和描述固体脂质纳米颗粒 (SLN) 和水凝涂层SLN,以改善simvastatin (SVA) 口服生物可用性.
- 评估脂质组成和涂层材料 (酸盐和酸盐) 对SLN特性和药物释放的影响.
- 评估开发的SLN配方的体内药理学性能和生物可用性.
主要方法:
- 使用各种脂质和稳定剂制成13种不同的SLN.
- 用两种度的酸盐 (CS) 和酸盐 (AL) 涂层选定的SLN.
- 用颗粒大小,泽塔潜力,风学,体外药物释放和体内生物可用性研究来表征SLN.
主要成果:
- 裸体和涂层SLN都表现出剪切稀释的质行为.
- 与涂层的F11-CS 1%SLN (524.3 ± 80.31 nm) 相比,F11 SLN (260.1 ± 3.72 nm) 的药物释放率更高.
- 在体内研究表明,F11 SLNs达到最高的血度,与SVA悬浮剂 (272 ng·h/mL) 和F11-CS 1% SLNs (3562.18 ng·h/mL) 相比,AUC0→24 (1880.4 ng·h/mL) 显著更高.
结论:
- 固体脂质纳米粒子 (SLN) 和它们的凝涂层对应物有效地提高了simvastatin (SVA) 口服生物可用性.
- 与未涂层SLN和SVA悬浮剂相比,F11-CS 1%的配方显示出优异的生物利用性增强.
- 这些发现表明,SLN是一种有前途的纳米载体系统,可以提高像simvastatin这样生物可用性较差的药物的治疗疗效.
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