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塞拉斯特衍生物/DOX联合组装纳米药物用于增强抗瘤治疗

Jiangtao Su^1,2,3, Xue Chen¹, Fan Ye¹

¹School of Biological Engineering and Food Science, Hubei University of Technology, Wuhan,430068, China.

Current drug delivery

|August 28, 2024

概括

这项研究开发了新型纳米颗粒,封装了多克索鲁比辛 (DOX) 和醇模拟物 (CEN),以对抗多药物耐药性. 这些双药纳米颗粒有效地增强了对抗性细胞的抗癌疗效.

科学领域:

生物医学工程生物医学工程
纳米技术纳米技术
癌症治疗癌症治疗

背景情况:

多种药物耐药性 (MDR) 显著挑战临床化疗的疗效.
组合疗法提供了一个有希望的策略来克服MDR.
开发有效的药物输送系统对于组合疗法至关重要.

研究的目的:

开发新型纳米颗粒封装多克索鲁比 (DOX) 和一个 celastrol 模拟物 (CEN) 来克服MDR.
研究这些双药纳米颗粒的药物释放特征和抗癌疗效.
评估这些纳米载体作为化学敏感剂的潜力.

主要方法:

合成的PEG 合成的聚 (α-利波酸) -甲胺胺类同类的切拉斯特 (mPEG-PαLA-CEN) 前药聚合物.
通过静电相互作用将封装的DOX转化为mPEG-PαLA-CEN纳米粒子.
使用光谱和显微镜 (1H NMR,FT-IR,UV-Vis,DLS,TEM) 进行了纳米粒子结构和尺寸的特征.
评估药物负载,释放动力学和体外细胞毒性 (MTT测定).

主要成果:

球形纳米粒子 (大约. 229.7 nm) 已成功制备,具有很高的生物相容性.
纳米粒子在瘤微环境 (低pH,高GSH) 中显示了92%的DOX和71.8%的CEN的刺激反应释放.
与无DOX的细胞相比,mPEG-PαLA-CEN-DOX纳米颗粒显著提高了对敏感 (MCF-7) 和抗性 (MCF-7/ADR) 细胞系的抗癌疗效.
通过纳米颗粒配方,MCF-7/ADR细胞的IC50从46.10μM减少到8.36μM.

结论:

PEGylated poly (α-lipoic acid) -CEN共聚物作为有效的,生物相容的和对刺激有反应的纳米载体,用于双重药物输送.
这些纳米载体通过作为化学敏感剂来克服多种药物耐药性的巨大潜力.
这些发现为CEN/DOX纳米药物在癌症治疗中的临床应用提供了坚实的理论基础.

关键词:

在GSH的响应式响应.多种药物耐药性多种药物耐药性化学敏感剂化学敏感剂化学疗法化疗化疗纳米颗粒.纳米颗粒.它们的pH值为pH.聚 (α-利波酸) 聚 (α-利波酸) 是一种

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