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首页> 外文期刊>International Journal of Pharmaceutics >Ipratropium is ‘luminally recycled’ by an inter-play between apical uptake and efflux transporters in Calu-3 bronchial epithelial cell layers
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Ipratropium is ‘luminally recycled’ by an inter-play between apical uptake and efflux transporters in Calu-3 bronchial epithelial cell layers

机译：在Calu-3支气管上皮细胞层的顶端摄取和流出转运蛋白之间的间隙之间的间隙，IPratropium是“Lumintly回收”

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Graphical abstract Display Omitted Abstract The mechanism by which quaternized anticholinergic bronchodilators permeate the airway epithelium remains controversial to date. In order to elucidate the role of drug transporters, ipratropium bidirectional transport as well as accumulation and release studies were performed in layers of the broncho-epithelial cell line Calu-3 grown at an air-liquid interface, in presence or absence of a range of transporter inhibitors. Unexpectedly, a higher transepithelial permeability was observed in the secretory direction, with an apparent efflux ratio of > 4. Concentration-dependent and inhibitor studies demonstrated the drug intracellular uptake was carrier-mediated. Interestingly, monitoring drug release post cell loading revealed the presence of an efficient efflux system on the apical side of the cell layers. Acting in concert, apical transporters seem to promote the ‘luminal recycling’ of the drug and hence, limit its transcellular transport. The data are in agreement with an apical Organic Cation Transporter (OCT) being involved in this process but also suggest the participation of unknown uptake and efflux transporters sensitive to probenecid. This study suggests the absorption of ipratropium across the pulmonary barrier is primarily governed by paracellular passive diffusion but transporters might play a significant role in controlling the drug local concentrations in the lungs. ]]>
机译：图形抽象显示省略了季铵化抗胆碱能支气管扩张剂渗透的机制迄今仍然存在争议。为了阐明药物转运蛋白的作用，在空气液界面生长的支气管上皮细胞系Calu-3层中，在支气管上皮细胞系Calu-3层中进行综合双向运输以及积累和释放研究。在存在或不存在范围内转运抑制剂。出乎意料地，在分泌方向上观察到更高的Transepithelial渗透率，表观抑制和抑制剂研究表明浓缩的抑制作用和抑制剂研究表明载体介导的药物介导的药物吸收。有趣的是，监测药物释放后细胞载荷显示在细胞层的顶端侧存在有效的渗透系统。在音乐会中行事，顶端运输师似乎促进了药物的“腔回收”，因此限制了其型造粒。该数据与Apical有机阳离子转运蛋白（OCT）一致，参与了该过程，而且还表明了未知摄取和流出转运蛋白对丙烯酸的转运蛋白的参与。本研究表明，肺屏屏障中的IPratropium的吸收主要由肺膜无源扩散治理，但运输递转运蛋白可能在控制肺部中的药物局部浓度方面发挥重要作用。 ]]>

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