通过皮肤应用的基托桑贴片中的Repaglinide-固体脂质纳米颗粒:盒式设计,表征和体内评估
Hany S M Ali1,2, Nader Namazi1, Hossein M Elbadawy3
1Department of Pharmaceutics and Pharmaceutical Industries, College of Pharmacy, Taibah University, Madinah, Al-Madinah Al-Munawwarah, Saudi Arabia.
International journal of nanomedicine
|January 15, 2024
概括
这项研究开发了一种新型的通过皮肤递送系统,使用repaglinide-固体脂质纳米颗粒 (REP-SLNs) 在基索基中. REP-SLN-TDDS增强了药物的生物可用性,并有效降低了大鼠的血糖水平.
科学领域:
- 制药科学 制药科学
- 生物材料工程 生物材料工程
- 药物输送系统 药物输送系统
背景情况:
- 雷帕格利尼德 (REP) 由于溶解度低和广泛的第一通代谢,具有较差的口服生物利用性.
- 开发替代性输送系统对于提高REP的治疗疗效至关重要.
研究的目的:
- 设计一种可生物降解的基托基础的通过皮肤递送系统 (REP-SLN-TDDS),载有repaglinide固体脂质纳米颗粒 (REP-SLN).
- 为了提高REP的生物可用性,并通过通过皮肤给药实现可控释放.
主要方法:
- 使用超声波热化乳化方法制造REP-SLN.
- 使用Box-Behnken设计优化处理变量 (脂质含量,表面活性剂度,超声波振幅).
- 用物理化学性质,药物释放动力学和ex vivo皮肤透性来表征REP-SLN-TDDS.
- 对实验大鼠的药理动力学和药理动力学概况的评估.
主要成果:
- 优化的REP-SLN实现了249±9.8nm的粒子大小和78%±2.3%的捕获效率.
- REP-SLN-TDDS显示了持续的药物释放 (在24小时后80%),并显著增强了皮肤透 (流量为2.481±0.22 μg/cm2/h).
- 透皮系统维持了较高的REP血水平,并显示出相比未经加工的REP和商用药片在老鼠中的血糖降低优异.
结论:
- 开发的REP-SLN-TDDS提供了一种有效的Repaglinide管理策略.
- 这种新的系统有望通过提高生物可用性和持续的药物输送来改善糖尿病的治疗管理.
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