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Oral absorption of peptides and nanoparticles across the human intestine: Opportunities, limitations and studies in human tissues
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
2016 (English)In: Advanced Drug Delivery Reviews, ISSN 0169-409X, E-ISSN 1872-8294, Vol. 106, p. 256-276Article, review/survey (Refereed) Published
Abstract [en]

In this contribution, we review the molecular and physiological barriers to oral delivery of peptides and nanoparticles. We discuss the opportunities and predictivity of various in vitro systems with special emphasis on human intestine in Ussing chambers. First, the molecular constraints to peptide absorption are discussed. Then the physiological barriers to peptide delivery are examined. These include the gastric and intestinal environment, the mucus barrier, tight junctions between epithelial cells, the enterocytes of the intestinal epithelium, and the subepithelial tissue. Recent data from human proteome studies are used to provide information about the protein expression profiles of the different physiological barriers to peptide and nanoparticle absorption. Strategies that have been employed to increase peptide absorption across each of the barriers are discussed. Special consideration is given to attempts at utilizing endogenous transcytotic pathways. To reliably translate in vitro data on peptide or nanoparticle permeability to the in vivo situation in a human subject, the in vitro experimental system needs to realistically capture the central aspects of the mentioned barriers. Therefore, characteristics of common in vitro cell culture systems are discussed and compared to those of human intestinal tissues. Attempts to use the cell and tissue models for in vitro-in vivo extrapolation are reviewed.

Place, publisher, year, edition, pages
2016. Vol. 106, p. 256-276
Keywords [en]
Oral drug delivery, Peptide drugs, Nanoparticles, Ussing chamber, Peptide permeability, Bioavailability, Human intestinal tissue, Human Protein Atla, Transcytosis, Transepithelial transport
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-311768DOI: 10.1016/j.addr.2016.07.007ISI: 000389097600005PubMedID: 27496705OAI: oai:DiVA.org:uu-311768DiVA, id: diva2:1061365
Funder
EU, European Research Council, NMP4-LA-2012-281035Swedish Research Council, 2822Available from: 2017-01-02 Created: 2017-01-02 Last updated: 2018-01-13Bibliographically approved

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