机械化学介导的动态胺基键结合用于使用碳点的药物输送
Gianluca Fuoco1,2, Gabrielle A Mandl1,2, Carissa De Mesa1,2
1Department of Chemistry and Biochemistry and the Centre for NanoScience Research, Concordia University, Montreal H4B 1R6, Canada. rafik.naccache@concordia.ca.
Nanoscale
|November 25, 2025
概括
这项研究介绍了一种无溶剂的方法,利用机械化学将分子附着在碳点 (CD) 上,为具有低细胞毒性的潜在药物输送应用创造稳定的 imine 键.
科学领域:
- 材料科学 材料科学 材料科学
- 纳米技术 纳米技术
- 生物结合化学 生物结合化学
背景情况:
- 有效的治疗交付受到生物流体中溶解性问题的阻碍.
- 碳点 (CD) 是有前途的药物载体,因为它们具有可分散性和可功能化的表面.
- 传统的CD结合使用难以分裂的胺键和危险的试剂.
研究的目的:
- 为碳点 (CD) 开发一种替代性的共价链接.
- 为了研究CD上的 imine 键的固态机械化学形成.
- 为了评估香结合CD的药物载荷能力和释放概况.
主要方法:
- 瓦尼林 (VAN) 与碳点 (CD) 在固态中的机械化学结合.
- 使用1H-NMR和XPS (N1s) 进行表征,以确认胺基结合的形成.
- 药物负载能力的评估和体外响应pH的药物释放动态.
- 在体外细胞毒性测定使用A549肺癌细胞.
主要成果:
- 在没有溶剂和催化剂的情况下,成功地通过imine键将VAN与CD的机械化学结合.
- 谱学证据 (1H-NMR,XPS) 证实了新的 imine 链接的形成.
- 达到5.02%的药物载荷能力 (DLC),持续释放24小时.
- CDs表现出较低的细胞毒性,在72小时后保持>90%的细胞活力.
结论:
- 固态机械化学提供了一种高效,绿色的替代方案,用于将分子与CD结合.
- 由此产生的素结合CD显示出良好的药物加载和受控释放特性.
- 机械化学修饰的CD显示出极好的生物相容性,适合生物医学应用.
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