作为肝脏特异性输送系统的telmisartan装载乳糖基托纳米颗粒:合成,优化和准效率
Mohamed Nasr1,2, Ahmed Y Kira3, Sameh Saber4
1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo, 11790, Egypt. m2nasr@yahoo.com.
AAPS PharmSciTech
|June 23, 2023
概括
乳糖修饰的奇托桑纳米颗粒增强了telmisartan的肝脏向性,用于肝细胞癌治疗. 这些新型纳米粒子提高了药物输送和生物可用性,为HCC提供了有前途的治疗方法.
科学领域:
- 生物材料科学 生物材料科学
- 纳米技术纳米技术
- 药物输送系统 药物输送系统
背景情况:
- 肝细胞癌 (HCC) 的死亡率和经济负担显著.
- 泰尔米沙坦 (TLM) 显示出对HCC的治疗潜力,但其生物可用性较差和分布不可预测.
- 有效的药物输送系统对于提高HCC治疗TLM疗效至关重要.
研究的目的:
- 准备和评估乳糖修饰的奇托桑纳米颗粒 (LCH NPs) 用于向肝脏输送TLM.
- 研究LCH NPs作为一种纳米载体,用于增强TLM在HCC中的治疗潜力.
主要方法:
- 乳糖修饰基托 (LCH) 是通过梅拉德反应合成的.
- 装有特尔米沙坦的LCH纳米粒子 (TLM-LCH NPs) 使用2^3全因数设计进行了准备和优化.
- 在体外和体内表征包括颗粒大小,捕获效率,药物释放研究和生物分布分析.
主要成果:
- 与原生奇多相比,LCH具有显著增强的水溶性.
- 优化的TLM-LCHNP (F1) 显示了有利的特征:粒子大小为145.46nm,捕获效率为90.21%,表面电荷为正 (+27.13mV).
- 在体外释放研究表明,Higuchi模型的一致性和在pH值5.5.时更高的释放. 在体内研究显示,与普通TLM和未经修改的TLM-NP相比,TLM-LCHNP的肝血度比显著更高.
结论:
- 基托的乳糖修饰成功地改善了其用于纳米粒子配方的特性.
- TLM-LCH NPs显示出高效的封装和特尔米沙坦向肝脏的向输送.
- 这些发现表明TLM-LCHNP是一种有希望的纳米载体,可以通过改善肝脏向来增强HCC治疗.
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