Best practices in current models mimicking drug permeability in the gastrointestinal tract - An UNGAP review

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Title: Best practices in current models mimicking drug permeability in the gastrointestinal tract - An UNGAP review
Authors: O'Shea, Joseph P.Augustijns, PatrickBrandl, MartinBrayden, David Jameset al.
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Date: 1-Mar-2022
Online since: 2022-06-03T15:57:42Z
Abstract: The absorption of orally administered drug products is a complex, dynamic process, dependant on a range of biopharmaceutical properties; notably the aqueous solubility of a molecule, stability within the gastrointestinal tract (GIT) and permeability. From a regulatory perspective, the concept of high intestinal permeability is intrinsically linked to the fraction of the oral dose absorbed. The relationship between permeability and the extent of absorption means that experimental models of permeability have regularly been used as a surrogate measure to estimate the fraction absorbed. Accurate assessment of a molecule's intestinal permeability is of critical importance during the pharmaceutical development process of oral drug products, and the current review provides a critique of in vivo, in vitro and ex vivo approaches. The usefulness of in silico models to predict drug permeability is also discussed and an overview of solvent systems used in permeability assessments is provided. Studies of drug absorption in humans are an indirect indicator of intestinal permeability, but both in vitro and ex vivo tools provide initial screening approaches and are important tools for assessment of permeability in drug development. Continued refinement of the accuracy of in silico approaches and their validation with human in vivo data will facilitate more efficient characterisation of permeability earlier in the drug development process and will provide useful inputs for integrated, end-to-end absorption modelling.
Funding Details: European Commission Horizon 2020
Science Foundation Ireland
Funding Details: CÚRAM Centre for Medical Devices
AMBER Centre for Advanced Materials and BioEngineering Research
Type of material: Journal Article
Publisher: Elsevier
Journal: European Journal of Pharmaceutical Sciences
Volume: 170
Start page: 1
End page: 35
Copyright (published version): 2021 The Authors
Keywords: Intestinal permeabilityOral absorptionIn vitro modelsIn vivo modelsIn silico modelsOral biopharmaceutics
DOI: 10.1016/j.ejps.2021.106098
Language: en
Status of Item: Peer reviewed
ISSN: 0928-0987
This item is made available under a Creative Commons License:
Appears in Collections:Conway Institute Research Collection
Veterinary Medicine Research Collection

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