设计,合成和响应酸性拆卸标有甲乙烯接口标记的可置区块共聚物
Brandon Andrade-Gagnon1, Sofia Nieves Casillas-Popova1, Arman Moini Jazani1,2
1Department of Chemistry and Biochemistry, Concordia University, Montreal, QC, H4B 1R6, Canada.
Macromolecular rapid communications
|March 18, 2024
概括
研究人员开发了智能纳米组件,这些纳米组件在响应pH值变化时会降解. 这些可酸降解的药物输送系统显示了改善瘤向和细胞吸收的前景.
科学领域:
- 材料科学 材料科学 材料科学
- 纳米技术 纳米技术
- 聚合物化学 聚合物化学
背景情况:
- 酸性链接对于智能纳米组件至关重要,特别是用于瘤组织中的药物输送.
- 了解影响pH敏感性的结构因素是有效的酸可降解,可脱的纳米组件的关键.
- 基于聚乙烯甘醇 (PEG) 的纳米组件在瘤向和内细胞分裂方面面临着挑战.
研究的目的:
- 通过使用新的酸-无效链接,合成和表征酸响应纳米组件.
- 为了评估这些纳米组件的pH依赖性降解和分解.
- 为改进瘤向药物输送系统建立设计原则.
主要方法:
- 三种乙和二醇的合成,用于酸-性链接.
- 鉴定甲乙 (BzAA) 的最佳水解概况.
- 基于聚乙烯糖醇的块共聚合物纳米组件的形成,具有BzAA链接.
- 在不同pH值 (7.4,6.5,5.0) 上对酸催化水解和分解的研究.
主要成果:
- 甲乙 (BzAA) 证明了针对目标pH值范围的最佳水解.
- 基于精确定义的聚乙烯甘醇 (PEG) 的块共聚合物纳米组件成功合成.
- 纳米组件在瘤pH (6.5) 时呈现缓慢的降解,在内/溶酶体pH (5.0) 时呈现快速的分解.
- 在生理学pH (7.4) 时保持结合体稳定.
结论:
- BzAA是一个适合的酸-无活性连接,用于创建有效的外可脱落的纳米组件.
- 开发的纳米组件符合基于pH敏感度的向药物释放标准.
- 这项研究提供了一种设计策略,以克服PEG限制并增强瘤向药物输送.
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