基于水溶性支柱[6]的pH敏感的超分子囊泡,用于药物输送的烯和铁衍生物
1Key Laboratory of Mesoscopic Chemistry of MOE, Center for Multimolecular Chemistry, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing 210093, China.
Journal of the American Chemical Society
|June 26, 2013
概括
从宿主-客人综合体中自组装的新型超分子囊泡使得pH响应药物递送. 这些囊泡在癌细胞中有效地加载和释放线粒 (MTZ),降低毒性,同时保持抗癌功效.
科学领域:
- 超分子化学 超分子化学
- 材料科学是一种材料科学.
- 纳米技术 纳米技术
背景情况:
- 开发先进的药物输送系统对于提高治疗疗效和减少副作用至关重要.
- 超分子自我组装为创建功能纳米结构提供了一个多功能平台.
- 对于在特定的生理环境中有针对性的药物释放而言,需要适应pH值的材料.
研究的目的:
- 开发一种新的超分子药物递送系统,使用宿主-客人包容复合体.
- 调查自组装囊泡的pH响应行为和药物释放特征.
- 评估药物载荷囊泡的细胞吸收,毒性和抗癌疗效.
主要方法:
- 从水溶性支柱[6]arene (WP6) 和ferrocene衍生物宿主-客人复合体中,超分子囊泡的自我组装.
- 使用NMR,UV-vis和光光谱学进行复杂化的表征.
- 通过DLS,TEM和光探针技术研究囊泡特性和pH响应.
- 在体外药物加载和释放研究中使用米托克桑 (MTZ).
- 使用活细胞成像和标准细胞毒性测试进行细胞吸收和细胞毒性测试.
主要成果:
- 形成了一个稳定的宿主-客人纳入复合体,具有高结合亲和力 (1.27 × 10^5 M^-1) 和 1:1 固体几何学.
- 纳入复合物自组装成在水溶液中响应pH的超分子囊泡.
- 囊泡有效地封装了米托克桑 (MTZ),在酸性条件下显示出快速释放.
- 装有MTZ的囊泡显示出癌细胞显著的细胞吸收,对正常细胞的毒性降低.
- 装有MTZ的囊泡在体外表现出与自由MTZ相比的抗癌活性.
结论:
- 基于WP6-铁宿主-客体综合体,成功开发了一种新型的pH响应的超分子囊泡系统.
- 该系统展示了有效的药物加载,可控释放和降低系统毒性.
- 这些超分子囊泡具有作为癌症治疗的有效和更安全的药物输送平台的巨大潜力.
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