净阳离子多{β-氨基}:合成,pH依赖性行为,并与阴离子载荷复合
Mara K Kuenen1, Alexa M Cuomo1, Vincent P Gray1
1Department of Chemical Engineering, University of Virginia, Charlottesville, VA, 22903, USA.
概括
研究人员通过逆转电荷,为药物输送创造了阳离子聚β氨基 (PBAE). 这些新的阳离子PBAE提供可调节的降解和复杂化,使离子疗法的控制释放成为可能.
科学领域:
- 聚合物化学 聚合物化学
- 材料科学 材料科学 材料科学
- 生物医学工程 生物医学工程
背景情况:
- 聚β-氨基 (PBAE) 通常是阴离子和水溶性不稳定,可用于复合离子化合物,如核酸.
- 由于它们固有的正电荷,现有的PBAE在输送阴离子疗法方面存在局限性.
研究的目的:
- 通过逆转PBAE的净电荷来设计完全可降解的多电解质复合物和离子疗法的输送车辆.
- 使用基功能化单体和含有离子二醇的分子合成净离子PBAE.
主要方法:
- 合成了基因功能化的PBAE,并通过激素基因反应安装了阳离子硫醇.
- 开发了用于净化的制剂尺寸排除色谱,避免了聚合物水解.
- 使用1H NMR光谱学特征净-阳离子PBAE,并评估它们的复杂化与一个阴离子.
主要成果:
- 成功合成了具有取决于pH值的可调节溶液行为的净离子PBAE.
- 在水性环境中经过水含量依赖的水解和降解.
- 展示了与阴离子 (GR) 10的复合,与与聚合物水解相关的时间依赖的分解.
结论:
- 建立了一个新的合成和净化路径,用于以前无法获取的净阳离子PBAE.
- 阳离子PBAE提供可调节的溶液和降解特性,可控制复合和释放.
- 这些阳离子PBAE为可降解的多电解质复合物和阴离子治疗输送系统提供了新的机会.
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