具有超低毒性向治疗性输送的氨酸反应性多聚红氨酸衍生物

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A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles

Published on: December 23, 2016

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Bowen Zhao¹, Xiao Zhang¹, Daniel Bilbao^2,3

¹Department of Chemistry, University of Miami, 1301 Memorial Drive, Coral Gables, Florida 33146, United States.

Biomacromolecules

|October 20, 2025

概括

研究人员开发了一种简单的方法来制造含有二硫化物的合成聚类,用于药物和基因输送. 这些可生物降解的聚合物提供触发释放和低毒性,在癌症治疗和基因疗法方面显示出希望.

科学领域:

生物材料科学生物材料科学
聚合物化学聚合物化学
药物输送系统药物输送系统

背景情况:

含有二硫化物的合成聚类因其生物降解性,生物相容性和触发释放性而有望用于控制药物和基因传递.
将二硫化键纳入聚酸中,通过直接聚合或聚合后修饰提出了合成挑战.

研究的目的:

开发一种创新且简单的策略,将二硫化物键融入多中.
为各种生物医学应用创造多功能,GSH响应的多载体.

主要方法:

采用了含有硫醇的氨基酸homocysteine的N-carboxyanhydride的环开聚合.
控制的聚合,以实现高分子量 (高达100个重复单位) 的狭窄分散.
功能化吊侧链分为各种GSH响应部分和结合治疗剂.

主要成果:

实现了对同类氨酸N-碳素化的良好控制的聚合.
证明侧链容易转化为阳离子,中性,离子,离子和药物合物.
含有药物的合物显示触发释放和强大的抗癌活性.
阴离子衍生物有效地提供了siRNA,mRNA和CRISPR组件,具有高转染效率和低细胞毒性.

结论:

开发的方法提供了一种简单而有效的途径来合成含有二硫化物的多.
这些多作为药物输送,基因疗法和其他生物医学应用的多功能平台.
合成的聚合物表现出卓越的生物相容性,可控释放能力和治疗疗效.

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