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Open AccessArticle

Organic Cation Transporters (OCTs) in EpiAirway™, a Cellular Model of Normal Human Bronchial Epithelium

1
Laboratory of General Pathology, Department of Medicine and Surgery, University of Parma, 43125 Parma, Italy
2
Preclinical Pharmacokinetics, Biochemistry & Metabolism Department, Chiesi Farmaceutici, 43122 Parma, Italy
*
Author to whom correspondence should be addressed.
Biomedicines 2020, 8(5), 127; https://doi.org/10.3390/biomedicines8050127
Received: 9 April 2020 / Revised: 14 May 2020 / Accepted: 18 May 2020 / Published: 19 May 2020
(This article belongs to the Special Issue Drug Transporters)
Organic cation transporters (OCTs) and novel organic cation transporters (OCTNs) are responsible for drug delivery in the intestine and kidney; in the lung, OCTs mediate inhaled drugs’ transport, although their physiological role in airways remains poorly understood. The studies addressing OCTs/OCTNs in human airways were mostly performed in immortal or transformed cell lines; here, we studied OCTs in EpiAirway™, a recently developed in vitro model of normal bronchial epithelium. Calu-3 monolayers were used for comparison. The activity of OCTs was evaluated by measuring the uptake of 1-methyl-4-phenylpyridinium (MPP+) at the apical and basolateral side of monolayers and protein expression through Western Blot analysis. OCTs and OCTNs expression, along with that of Amino acid Transporter B0,+ (ATB0,+)transporter, was determined by measuring the number of mRNA molecules through quantitative Polymerase Chain Reaction (qPCR). The interaction of the transporters with bronchodilators was also assessed. Results highlight significant differences between Calu-3 cells and EpiAirway™, since, in the latter, OCTs are active only on the basolateral membrane where they interact with the bronchodilator ipratropium. No activity of OCTs is detectable at the apical side; there, the most abundant carrier is, instead, SLC6A14/ATB0,+, that can thus be potentially listed among organic cation transporters responsible for drug delivery in the lung. View Full-Text
Keywords: bronchial epithelium; organic cation transporters; pulmonary drug delivery; SLC22A1 (OCT1); SLC22A3 (OCT3); SLC6A14 (ATB0,+) bronchial epithelium; organic cation transporters; pulmonary drug delivery; SLC22A1 (OCT1); SLC22A3 (OCT3); SLC6A14 (ATB0,+)
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MDPI and ACS Style

Barilli, A.; Visigalli, R.; Ferrari, F.; Di Lascia, M.; Riccardi, B.; Puccini, P.; Dall’Asta, V.; Rotoli, B.M. Organic Cation Transporters (OCTs) in EpiAirway™, a Cellular Model of Normal Human Bronchial Epithelium. Biomedicines 2020, 8, 127.

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