An overview of in vitro, ex vivo and in vivo models for studying the transport of drugs across intestinal barriers

[Display omitted] •Oral absorption depends on drug, formulation and gastrointestinal tract.•Different preclinical models are used to evaluate the intestinal drug transport.•Preclinical models greatly impact development and translation of oral formulations.•Advanced preclinical models with better cor...

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Bibliographic Details
Published in:Advanced drug delivery reviews 2021-08, Vol.175, p.113795-113795, Article 113795
Main Authors: Xu, Yining, Shrestha, Neha, Préat, Véronique, Beloqui, Ana
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Ex vivo models
Humans
In vitro models
In vivo models
Intestinal Absorption
Intestinal barriers
Intestinal Mucosa - metabolism
Oral delivery
Pharmacokinetics
Transport
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Summary:[Display omitted] •Oral absorption depends on drug, formulation and gastrointestinal tract.•Different preclinical models are used to evaluate the intestinal drug transport.•Preclinical models greatly impact development and translation of oral formulations.•Advanced preclinical models with better correlation to clinical data are needed. Oral administration is the most commonly used route for drug delivery owing to its cost-effectiveness, ease of administration, and high patient compliance. However, the absorption of orally delivered compounds is a complex process that greatly depends on the interplay between the characteristics of the drug/formulation and the gastrointestinal tract. In this contribution, we review the different preclinical models (in vitro, ex vivo and in vivo) from their development to application for studying the transport of drugs across intestinal barriers. This review also discusses the advantages and disadvantages of each model. Furthermore, the authors have reviewed the selection and validation of these models and how the limitations of the models can be addressed in future investigations. The correlation and predictability of the intestinal transport data from the preclinical models and human data are also explored. With the increasing popularity and prevalence of orally delivered drugs/formulations, sophisticated preclinical models with higher predictive capacity for absorption of oral formulations used in clinical studies will be needed.
ISSN:0169-409X
1872-8294
DOI:10.1016/j.addr.2021.05.005