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Assembly and Characterization of Polyelectrolyte Complex Micelles
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卡菲尔佐米布装载的三级多纳米颗粒通过多化复合稳定.

Preye Agbana1, Ji Eun Park1, Piotr Rychahou2

  • 1Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, USA.

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概括

稳定三元多纳米颗粒 (tPNPs) 增强了对固体癌症的卡菲尔佐米布的输送. 这些适应pH值的纳米颗粒提高了药物释放和对抗抗性癌细胞的疗效.

关键词:
药物输送是药物输送的过程.包容性复杂的包容性复杂的多离子复合体是多离子复合体.聚胺纳米颗粒的多种类型.自己组装的自组件.药物释放反应于pH的药物释放.

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科学领域:

  • 生物医学工程 生物医学工程
  • 纳米技术 纳米技术
  • 癌症治疗方法 癌症治疗方法

背景情况:

  • 卡菲尔佐米布 (CFZ) 对多发性骨髓瘤有效,但由于溶解性和稳定性差,对固体癌症有效性有限.
  • 以前的三元聚胺纳米颗粒 (tPNPs) 改善了CFZ传递,但需要增强颗粒稳定性才能持续释放.
  • 从tPNPs的初始突发释放需要在体内延长蛋白酶体抑制的改善稳定性.

研究的目的:

  • 为了稳定CFZ装载的tPNPs,使用具有不同pKa值的聚合物.
  • 为了研究稳定tPNPs的pH取决于药物释放动力学和粒子稳定性.
  • 评估稳定型tPNPs对抗CFZ抗性癌细胞的增强疗效.

主要方法:

  • 通过聚化复合稳定CFZ载荷tPNPs的形成.
  • 在冷干燥前后的颗粒大小和稳定性的表征.
  • 评估pH依赖的体外药物释放概况.
  • 在体外细胞毒性和蛋白质酶活性测定对癌细胞.

主要成果:

  • 聚化复合稳定了CFZ加载tPNPs的核心,保持了均的粒子大小.
  • CFZ/tPNPs表现出pH依赖的释放,随着酸度的增加 (pH < 6) 加快释放,同时在pH 7.4.4保持稳定.
  • 稳定的tPNPs在体外对抗CFZ抗性癌细胞的生物活性得到改善.

结论:

  • 在固体癌症中,多聚稳定的tPNPs提供了一种有希望的策略来克服CFZ的局限性.
  • 这种依赖pH的释放机制有利于向酸性瘤微环境.
  • 这些发现支持CFZ载入tPNPs在药物耐药固体瘤的组合疗法中的潜力.