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Organic cation transporters in the blood-air barrier: Expression and implications for pulmonary drug delivery

机译:血气屏障中的有机阳离子转运蛋白:表达和对肺部药物输送的影响

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摘要

Studies concerning the impact that hepatic, renal and intestinal transporters have on drug disposition have been frequently reported in the literature. Surprisingly, however, little is known regarding the distribution and function of drug-transporter proteins of the lung epithelium. Many drugs (delivered to the lung) have a net positive charge and, thus, are potential substrates of organic cation transporters; currently marketed compounds (e.g., ronchodilators), as well as novel drug candidates in development, are such substrates. It is the aim of this review to summarize the current state of organic cation-transporter expression analysis in the lung and in in vitro models of bronchial and alveolar barriers. Moreover, activity of selected transporters in lung epithelium in situ and in vitro will be highlighted, and their potential role in pulmonary drug disposition will be addressed. One example included here is the transporter-dependent absorption of 2-agonists in respiratory epithelial cells.
机译:关于肝,肾和肠转运蛋白对药物处置的影响的研究已在文献中频繁报道。然而,令人惊讶的是,关于肺上皮的药物转运蛋白的分布和功能知之甚少。许多药物(输送到肺部)具有净正电荷,因此是有机阳离子转运蛋白的潜在底物。这样的底物是目前市售的化合物(例如,ronchodilator),以及正在开发的新型药物候选物。这篇综述的目的是总结在肺以及支气管和肺泡屏障的体外模型中有机阳离子转运蛋白表达分析的当前状态。此外,将突出显示所选转运蛋白在肺上皮原位和体外的活性,并将探讨其在肺部药物处置中的潜在作用。这里包括的一个例子是呼吸道上皮细胞中2-激动剂的转运蛋白依赖性吸收。

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