基于的链接器用于从聚合物纳米颗粒中调节的酸敏感药物释放
Matt Timmers1,2, Marco Kong2, Peter Schuckman3
1Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, Utrecht, 3584 CG, The Netherlands.
Chemistry (Weinheim an der Bergstrasse, Germany)
|December 11, 2024
概括
研究人员开发了可调节的基于silyl的链接器,用于核心交叉链接的聚合物微粒 (CCPM). 这些链接器控制活性药物成分 (API) 的释放率,如凝胺,为向药物输送提供了潜在的潜力.
科学领域:
- 聚合物化学 聚合物化学
- 药物输送系统是药物输送系统.
- 纳米技术纳米技术
背景情况:
- 活性药物成分 (API) 通常需要载体来增强药理动力学和药理动力学特性.
- 核心交联聚合物微粒 (CCPM) 是疏水小分子API的有效载体.
- API通常通过链接器对CCPM核心进行共连接,允许控制释放调制.
研究的目的:
- 合成和研究基于西的链接剂,用于从CCPM中控制的API释放.
- 通过修改链接替代剂来探索药物释放率的可调性.
- 评估酸触发释放的潜力,以实现向药物输送.
主要方法:
- 用不同的替代剂合成基于西的链接剂.
- 链接剂通过Si乙烯键对gemcitabine进行共价附着.
- 在不同的pH值 (5.0和7.4) 和温度 (37°C) 下评估凝胺释放动力学.
主要成果:
- 在原子上的不同替代剂显著改变了gemcitabine释放半衰期 (t1/2),在pH值5.0的情况下从<1到>96小时.
- 在pH7.4下释放半衰期从24小时到240小时不等.
- 较大的替代剂增加了固体阻碍,与在酸性pH下药物释放速度较慢相关.
结论:
- 基于Silyl的链接器可以对CCPM的API释放动力学进行调节控制.
- 绝缘阻碍是调节释放速度的关键因素,特别是在酸性环境中.
- 这种方法可以适应各种API和载体系统,增强向药物输送的可能性.
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