基托桑基热凝系统用于鼻到大脑的多内佩西尔输送:优化配方特性和鼻腔沉积概况
Mirna Perkušić1, Laura Nižić Nodilo1, Ivo Ugrina2
1Department of Pharmaceutical Technology, University of Zagreb Faculty of Pharmacy and Biochemistry, 10000 Zagreb, Croatia.
Pharmaceutics
|June 28, 2023
概括
这项研究开发了一种基于酸盐的新型热凝鼻喷雾,用于将多尼佩西尔输送到大脑,显示出高沉积率和阿尔茨海默病治疗的有希望的结果.
科学领域:
- * 制药科学 制药科学
- * 纳米技术的使用
- * 神经科学是一门神经科学.
背景情况:
- *阿尔茨海默病 (AD) 治疗需要有效的针对大脑的药物输送.
- *目前的多尼佩西尔输送方法在达到最佳治疗度时面临挑战.
- * 鼻腔输送提供了一个有希望的,非侵入性途径,用于直接鼻到脑药物运输.
研究的目的:
- * 开发和优化基于基托桑的,装有多尼的热凝配方,以改善鼻至脑的输送.
- * 在临床前模型中评估配方的物理化学性质,稳定性和性能.
- * 评估这种配方作为阿尔茨海默病治疗的有效输送系统的潜力.
主要方法:
- *使用实验的统计设计进行优化而制定公式的开发.
- *使用3D打印的鼻模特进行粘度,凝,喷能力和鼻沉积的表征.
- *在体外释放,透性研究 (Calu-3细胞),ex vivo粘膜粘附 (猪鼻膜) 和 in vivo易怒性 (子粘膜刺激测定).
主要成果:
- *优化喷雾配方,可在34°C即时凝结.
- * 达到71.8%的嗅觉沉积,显著提高了目标传递.
- * 药物释放时间延长 (t1/2~90分钟),粘粘度增加20倍,透率增加1.5倍.
- *可接受的体内易怒性概况表明可用于鼻腔的安全性.
结论:
- *开发的热凝配方是一个有希望的平台,可以有效地向大脑向donepezil.
- *这种鼻喷雾策略为阿尔茨海默病治疗提供了一个可行的替代方案.
- *需要进一步的体内研究来确认最终的可行性和治疗疗效.
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