基于环德克斯的奎尔丁粉末,用于潜在的鼻至大脑输送:配方和体外评估
Elmina-Marina Saitani1, Paraskevi Papakyriakopoulou1, Theodora Bogri1
1Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimiopolis Zografou, 15771 Athens, Greece.
Molecules (Basel, Switzerland)
|July 12, 2025
概括
使用基-β-环氧 (HPβCD) 的喷雾干燥奎尔 (Que) 鼻粉显示出增强的输送. 使用HPMC和MLMP等辅助剂的配方优化可以定制物理化学性质,以改善鼻至大脑药物输送.
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:
- 奎尔 (Que) 具有抗氧化和神经保护作用,但具有较差的溶解性和生物利用性.
- 鼻腔药物输送提供了直接的,非侵入性途径进入大脑,绕过第一通代谢.
- xypropyl-β-cyclodextrin (HPβCD) 可以提高难以溶解药物的溶解性和输送.
研究的目的:
- 研究制备方法 (喷雾干燥与冷化) 和辅料 (HPMC,MLMPs) 对基于HPβCD的鼻Que粉制剂的影响.
- 评估这些鼻粉的物理化学性质,结构特征和体外扩散.
- 为了优化 Que 鼻腔传递,以提高大脑准.
主要方法:
- 使用喷雾干燥和冷化制备Que/HPβCD鼻粉.
- 加入基甲基纤维素 (HPMC) 和曼尼托尔/莱西丁微粒 (MLMP).
- 使用TGA,SEM和使用弗朗茨细胞的体外扩散研究进行表征.
主要成果:
- 喷雾干燥的HPβCD/Que粉末 (F4) 显示了最高的透率 (0.11 ± 0.01 mg/cm2) 在120分钟).
- 由于粘度增加,HPMC增强了热稳定性,但降低了Que扩散.
- MLMPs改善了粉末流量和剂量放置,但稍微降低了扩散效率.
结论:
- 喷雾干燥的基于HPβCD的粉末是用于鼻腔氏素输送的有希望的平台.
- HPMC和MLMP可以在战略上用于调节粉末特性和传递性能.
- 这项研究提供了对优化鼻腔配方的见解,以改善鼻至脑药物输送.
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