基于环德的超分子储存器作为rivastigmine到大脑的鼻腔输送载体
Manli Wang1, Yuting Lv2, Huipeng Xu3
1Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Chinese Medicine, Nanchang 330004, China; Jiangsu Yungou Pharmaceutical Technology Co. Ltd., Nantong 226133, China.
Carbohydrate polymers
|November 20, 2024
概括
这项研究开发了一种新型的波醇修饰交联环素框架 (BO-CDF),用于鼻内输送里瓦斯蒂格明 (RIV). 这个系统显著增强了RIV.
科学领域:
- 超分子化学 超分子化学
- 纳米技术 纳米技术
- 神经科学是一个神经科学.
背景情况:
- 里瓦斯蒂格 (RIV) 对于治疗阿尔茨海默病至关重要.
- 目前的RIV输送方法在针对大脑和有效性方面面临挑战.
- 超分子储备提供了改善药物输送的潜力.
研究的目的:
- 通过使用循环德克斯特林金属有机框架 (CD-MOF) 和交联循环德克斯特林框架 (CDF) 合成一个超分子储.
- 为了使CDF与醇 (BO) 功能化,以创建BO-修改的CDF (BO-CDF).
- 开发一种鼻腔里瓦斯蒂格明 (RIV) 输送系统 (RIV@BO-CDF) 以加强对大脑的向.
主要方法:
- 合成CD-MOF和随后的交叉链接形成CDF.
- 将CDF与醇功能化,以获得BO-CDF.
- 将RIV封装到BO-CDF中,以创建RIV@BO-CDF纳米粒子 (约. 在250 nm) 的距离.
主要成果:
- RIV@BO-CDF的药物负载能力为15 ± 2%.
- BO-CDF 增强了 RIV 粘膜粘合和透性.
- 与口服RIV相比,内RIV@BO-CDF显著增加了大鼠血 (1.7倍AUC) 和大脑 (2.3倍AUC) 的RIV度.
- 大脑RIV度的峰值是口服的8倍.
- 证明了高药物向效率 (139.4%) 和直接鼻到脑传输 (28.3%).
结论:
- 基于超分子环极素的储显示出增强RIV大脑向和有效性的前景.
- 鼻内注射RIV@BO-CDF提供了一个可行的策略,用于直接鼻到脑药物输送.
- 这种方法可以改善需要RIV治疗的神经疾病的治疗结果.
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