通过胺功能化聚烯酸改善药物输送:增强载荷能力和持续的药物释放
Himanshu Polara1, Tejas Shah1, Godwin Babanyinah1
1Department of Chemistry and Biochemistry, The University of Texas at Dallas, Richardson, Texas 75080, United States.
Biomacromolecules
|April 30, 2025
概括
新型异位胺功能化单体增强了聚合物菌根的稳定性和药物载荷能力,改善了药物输送. 这些先进的细胞显示pH响应释放和有效的癌细胞向.
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
- 纳米技术 纳米技术
背景情况:
- 聚合物微粒是有希望的药物输送载体.
- 挑战包括不稳定性,低药物载荷能力 (DLC) 和药物过早泄漏.
研究的目的:
- 开发具有改进性质的增强聚合物微粒.
- 为了研究异位的γ-胺功能化e-caprolactone (e-CL) 单体对菌形成.
- 评估药物加载,释放和体外疗效.
主要方法:
- 三种疏水性e-CL单体的合成,具有不同的替代剂.
- 使用聚乙烯糖醇 (PEG) 作为水友性块的环开聚合.
- 自组装成小粒和多克索鲁比 (DOX) 装载.
- 在体外药物释放研究和细胞活力测定.
主要成果:
- 失置的单体使替代物密度增加了一倍,增强了菌根的特性.
- 在PEG-b-poly ((N-propyl-N-benzyl-7-oxopane-4-carboxamide) (PEG-b-PBnPyCL) 微粒中,达到了7.33重量%的DLC.
- 在酸性条件下观察到pH响应的DOX释放.
- 载有DOX的PEG-b-PBnPyCL小粒在MDA-MB-231癌细胞中显示了~20%的活力.
结论:
- 异位胺功能化e-CL单体显著提高了聚合物微粒的性能.
- 这些增强的细胞显示出具有临床翻译可能性的先进药物输送潜力.
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