{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,26]],"date-time":"2026-09-26T10:31:13Z","timestamp":1790418673078,"version":"4.1.0"},"reference-count":102,"publisher":"MDPI AG","issue":"9","license":[{"start":{"date-parts":[[2020,9,10]],"date-time":"2020-09-10T00:00:00Z","timestamp":1599696000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Biomedicines"],"abstract":"<jats:p>Robust, predictive ex vivo\/in vitro models to study intestinal drug absorption by passive and active transport mechanisms are scarce. Membrane transporters can significantly impact drug uptake and transporter-mediated drug\u2013drug interactions can play a pivotal role in determining the drug safety profile. Here, the presence and activity of seven clinically relevant apical\/basolateral drug transporters found in human jejunum were tested using ex vivo porcine intestine in a Ussing chamber system. Experiments using known substrates of peptide transporter 1 (PEPT1), organic anion transporting polypeptide (OATP2B1), organic cation transporter 1 (OCT1), P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), multi drug resistance-associated protein 2 and 3 (MRP2 and MRP3), in the absence and presence of potent inhibitors, showed that there was a statistically significant change in apparent intestinal permeability Papp,pig (cm\/s) in the presence of the corresponding inhibitor. For MRP2, a transporter reportedly present at relatively low concentration, although Papp,pig did not significantly change in the presence of the inhibitor, substrate deposition (QDEP) in the intestinal tissue was significantly increased. The activity of the seven transport proteins was successfully demonstrated and the results provided insight into their apical\/basolateral localization. In conclusion, the results suggest that studies using the porcine intestine\/Ussing chamber system, which could easily be integrated into the drug development process, might enable the early-stage identification of new molecular entities that are substrates of membrane transporters.<\/jats:p>","DOI":"10.3390\/biomedicines8090340","type":"journal-article","created":{"date-parts":[[2020,9,10]],"date-time":"2020-09-10T09:10:09Z","timestamp":1599729009000},"page":"340","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["Using Ex Vivo Porcine Jejunum to Identify Membrane Transporter Substrates: A Screening Tool for Early\u2014Stage Drug Development"],"prefix":"10.3390","volume":"8","author":[{"given":"Yvonne E.","family":"Arnold","sequence":"first","affiliation":[{"name":"School of Pharmaceutical Sciences, University of Geneva, Centre M\u00e9dical Universitaire, 1 rue Michel Servet, 1211 Geneva, Switzerland"},{"name":"Institute of Pharmaceutical Sciences of Western Switzerland, University of Geneva, Centre M\u00e9dical Universitaire, 1 rue Michel Servet, 1211 Geneva, Switzerland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9049-5489","authenticated-orcid":false,"given":"Yogeshvar N.","family":"Kalia","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Sciences, University of Geneva, Centre M\u00e9dical Universitaire, 1 rue Michel Servet, 1211 Geneva, Switzerland"},{"name":"Institute of Pharmaceutical Sciences of Western Switzerland, University of Geneva, Centre M\u00e9dical Universitaire, 1 rue Michel Servet, 1211 Geneva, Switzerland"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2020,9,10]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"799","DOI":"10.1038\/nri2653","article-title":"Intestinal mucosal barrier function in health and disease","volume":"9","author":"Turner","year":"2009","journal-title":"Nat. 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