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评估β₂ -agonists作为肺表面活性剂涂层纳米凝吸入疗法的siRNA输送辅助剂

Pieterjan Merckx¹, Griet Conickx², Evy Blomme²

¹Ghent Research Group on Nanomedicines, Laboratory of General Biochemistry and Physical Pharmacy, Faculty of Pharmaceutical Sciences, Department of Pharmaceutics, Ghent University, Ottergemsesteenweg 460, 9000 Ghent, Belgium.

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V

|February 17, 2024

概括

某些喘药物,如沙米特醇和因达卡特罗尔,可以增强小干扰RNA (siRNA) 治疗药物向肺细胞的传递. 这种支气管扩展剂的重新定位可能会改善基于RNA的肺部疾病治疗方法.

科学领域:

纳米医学和RNA疗法
肺部药物输送肺部药物输送
药理学药理学是指药理学的学科.

背景情况:

肺是RNA治疗的关键目标,如小干扰RNA (siRNA),但临床使用受到传递障碍的限制.
之前的工作开发了混合纳米粒子,其中含有siRNA载荷的纳米凝芯,涂有肺表面活性剂 (Curosurf®),以提高稳定性和传递性.
一个主要的挑战仍然存在:siRNA纳米载体通常在 lysosomes 中降解,限制细胞质的访问和治疗疗效.

研究的目的:

评估皮质两性药物 (CADs),特别是β2-激动剂,作为通过纳米载体向肺细胞传递siRNA的增强剂.
评估重新使用的支气管扩展剂 (沙布塔摩尔,福莫特醇,沙米特醇,因达卡特醇) 提高细胞内siRNA运输的潜力.

主要方法:

在肺上皮和巨细胞系中评估了四种β2-激动剂的siRNA递送增强能力.
测试了未涂层和表面活性剂涂层的siRNA装载纳米凝.
相关的药物疏水性与促进siRNA释放到细胞细胞醇的能力.

主要成果:

更多的疏水性长效β2-激动剂 (LABAs),沙米特醇和因达卡特醇,显示出显著的siRNA递送增强.
对于两种纳米凝类型的肺上皮细胞和巨细胞,萨尔米特促进了siRNA的递送.
伊达卡特罗尔增强了siRNA传递,特别是在肺上皮细胞中.

结论:

萨尔米特醇和因达卡特罗尔作为纳米载体介导siRNA向肺部传递的辅助剂具有前景.
重新利用这些β2-激动剂可以克服细胞内障碍,并使肺部疾病的组合疗法成为可能.
药物疏水性是CAD作为siRNA递送增强剂有效性的关键因素.

关键词:

阴阳性两性药物阴阳性两性药物药物重新定位是药物重新定位.细胞内体逃脱是什么?吸入治疗是一种吸入疗法.纳米医学是一种纳米医学.肺部表面活性剂的使用方法对于RNA疗法来说,它是非常重要的.

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