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生物可降解的两性超分支聚合物-药物合物用于细胞内药物输送

Sukanya Bera¹, Raju Bej¹, Pintu Kanjilal¹

¹School of Applied and Interdisciplinary Sciences, Indian Association for the Cultivation of Science, Kolkata 700032, India.

Bioconjugate chemistry

|March 21, 2024

概括

这项研究合成了一种新的可生物降解的高分支聚合物,用于药物输送. 该聚合物形成纳米颗粒,有效地将抗癌药物坎普托素 (CPT) 输送到癌细胞中,从而导致高效的细胞杀死.

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
药物运输药物运输药物运输

背景情况:

开发先进的药物输送系统对于提高治疗疗效和减少强效药物的副作用至关重要,如坎普托塞辛 (CPT).
超分支聚合物在药物输送中提供了独特的优势,因为它们的球状结构,高溶解度和众多功能化位点.
生物可降解聚合物对于针对细胞内刺激的药物释放是可取的,例如癌细胞中高谷氨 (GSH) 水平.

研究的目的:

通过简单的A2+B3方法合成一种新的生物可降解高分支 (HB) 聚合物.
将HB聚合物与坎普托素 (CPT) 功能化,以创建用于向癌症治疗的两性合物.
研究开发的CPT装载纳米粒子的自我组装,药物释放动力学,细胞吸收和抗癌疗效.

主要方法:

合成HB聚合物通过dithiothreitol (DTT) 和三功能的pyridyl-disulfide单体之间的醇激活二硫化物交换反应.
聚合后修改以结合CPT并引入氧乙烯-醇以获得两性.
聚合物特性 (分子量,分散性),纳米粒子形成,药物加载,体外药物释放 (GSH触发),细胞吸收 (聚焦显微镜) 和细胞毒性 (MTT检测) 的表征.

主要成果:

通过CPT成功合成和功能化了具有高药载荷 (∼40%) 的明确的HB多硫化物.
结合物在水中自组装成纳米粒子 (∼135 nm),通过级联降解机制通过高效的GSH触发的活性CPT释放.
HB-CPT纳米颗粒在HeLa细胞中表现出优异的细胞吸收,主要是通过内细胞分裂,导致高强度和高效的癌细胞杀死 (IC50 ~ 0.6μg/mL),表现优于线性结合体.

结论:

开发的生物可降解的高分支聚合物作为一个有效的平台,用于配制具有增强抗癌活性的CPT载荷纳米颗粒.
由GSH触发的级联降解机制促进了高效的细胞内药物释放,与线性聚合物结合物相比,有助于获得更好的治疗结果.
这种基于HB聚合物的药物输送系统对先进的癌症治疗具有重大前景.

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