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Caco-2 Cell Conditions Enabling Studies of Drug Absorptionfrom Digestible Lipid-Based Formulations
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy. (Drug Delivery, Department of Pharmacy)
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy. (Drug Delivery, Department of Pharmacy)ORCID iD: 0000-0002-8917-2612
2018 (English)In: Pharmaceutical research, ISSN 0724-8741, E-ISSN 1573-904X, Vol. 35, no 4, article id 74Article in journal (Refereed) Published
Abstract [en]

Purpose To identify conditions allowing the use of cell-based models for studies of drug absorption during in vitro lipolysis of lipid-based formulations (LBFs). Methods Caco-2 was selected as the cell-based model system. Monolayer integrity was evaluated by measuring mannitol permeability after incubating Caco-2 cells in the presence of components available during lipolysis. Pure excipients and formulations representing the lipid formulation classification system (LFCS) were evaluated before and after digestion. Porcine mucin was evaluated for its capacity to protect the cell monolayer. Results Most undigested formulations were compatible with the cells (II-LC, IIIB-LC, and IV) although some needed mucin to protect against damaging effects (II-MC, IIIB-MC, LC, and IIIA-LC). The pancreatic extract commonly used in digestion studies was incompatible with the cells but the Caco-2 monolayers could withstand immobilized recombinant lipase. Upon digestion, long chain formulations caused more damage to Caco-2 cells than their undigested counterparts whereas medium chain formulations showed better tolerability after digestion. Conclusions Most LBFs and components thereof (undigested and digested) are compatible with Caco-2 cells. Pancreatic enzyme is not tolerated by the cells but immobilized lipase can be used in combination with the cell monolayer. Mucin is beneficial for critical formulations and digestion products.

Place, publisher, year, edition, pages
Springer, 2018. Vol. 35, no 4, article id 74
Keywords [en]
Caco-2 cells, digestion, intestinal absorption, lipid-based formulation
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-342749DOI: 10.1007/s11095-017-2327-8ISI: 000441807000003PubMedID: 29484506OAI: oai:DiVA.org:uu-342749DiVA, id: diva2:1185045
Funder
EU, European Research Council, 638965Swedish Research Council, 2014-3309Available from: 2018-02-23 Created: 2018-02-23 Last updated: 2018-11-05Bibliographically approved

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Keemink, JannekeBergström, Christel

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