title: Usefulness of Caco-2/HT29-MTX and Caco-2/HT29-MTX/Raji B Coculture Models To Predict Intestinal and Colonic Permeability Compared to Caco-2 Monoculture.
abstract: The Caco-2 cellular monolayer is a widely accepted in vitro model to predict human permeability but suffering from several and critical limitations. Therefore, some alternative cell cultures to mimic the human intestinal epithelium, as closely as possible, have been developed to achieve more physiological conditions, as the Caco-2/HT29-MTX coculture and the triple Caco-2/HT29-MTX/Raji B models. In this work the permeability of 12 model drugs of different Biopharmaceutical Classification System (BCS) characteristics, in the coculture and triple coculture models was assessed. Additionally, the utility of both models to classify compounds according to the BCS criteria was scrutinized. The obtained results suggested that the coculture of Caco-2/HT29-MTX and the triple coculture of Caco-2/HT29-MTX/Raji B were useful models to predict intestinal permeability and to classify the drugs in high or low permeability according to BCS. Moreover, to study thoroughly the transport mechanism of a specific drug, using a more complex model than Caco-2 monocultures is more suitable because coculture and triple coculture are more physiological models, so the results obtained with them will be closer to those obtained in the human intestine.
authors.affiliation: Department of Pharmacokinetics and Pharmaceutical Technology, Miguel Hernandez University , San Juan de Alicante, 03550 Alicante, Spain.|Department of Pharmacokinetics and Pharmaceutical Technology, University of Valencia , Av. de Blasco Ibáñez, 13, 46010 Valencia, Spain.
authors.forename: Isabel
authors.initials: I
authors.lastname: Lozoya-Agullo
authors.affiliation: i3S-Instituto de Investigação e Inovação em Saúde, University of Porto , Rua Alfredo Allen 208, 4200-135 Porto, Portugal.|INEB-Instituto de Engenharia Biomédica, University of Porto , Rua Alfredo Allen 208, 4200-135 Porto, Portugal.
authors.forename: Francisca
authors.initials: F
authors.lastname: Araújo
authors.affiliation: Department of Pharmacokinetics and Pharmaceutical Technology, Miguel Hernandez University , San Juan de Alicante, 03550 Alicante, Spain.
authors.forename: Isabel
authors.initials: I
authors.lastname: González-Álvarez
authors.affiliation: Department of Pharmacokinetics and Pharmaceutical Technology, University of Valencia , Av. de Blasco Ibáñez, 13, 46010 Valencia, Spain.|Molecular Recognition and Technological Development, Polytechnic University-University of Valencia , Camí de Vera, s/n, 46022 Valencia, Spain.
authors.forename: Matilde
authors.initials: M
authors.lastname: Merino-Sanjuán
authors.affiliation: Department of Pharmacokinetics and Pharmaceutical Technology, Miguel Hernandez University , San Juan de Alicante, 03550 Alicante, Spain.
authors.forename: Marta
authors.initials: M
authors.lastname: González-Álvarez
authors.affiliation: Department of Pharmacokinetics and Pharmaceutical Technology, Miguel Hernandez University , San Juan de Alicante, 03550 Alicante, Spain.
authors.forename: Marival
authors.initials: M
authors.lastname: Bermejo
authors.affiliation: i3S-Instituto de Investigação e Inovação em Saúde, University of Porto , Rua Alfredo Allen 208, 4200-135 Porto, Portugal.|INEB-Instituto de Engenharia Biomédica, University of Porto , Rua Alfredo Allen 208, 4200-135 Porto, Portugal.|CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde , Rua Central da Gandra 1317, 4585-116 Gandra, Portugal.
authors.forename: Bruno
authors.identifier: 0000-0001-5763-7553
authors.initials: B
authors.lastname: Sarmento
mesh_terms: D018938:Caco-2 Cells; D045744:Cell Line, Tumor; D018920:Coculture Techniques / Q000379:methods; D003106:Colon / Q000378:metabolism*; D019073:HT29 Cells; D006801:Humans; D007408:Intestinal Absorption / Q000502:physiology*; D007413:Intestinal Mucosa / Q000378:metabolism*; D010539:Permeability
keywords: Caco-2; coculture; in vitro models; permeability; triple coculture