An Overview of in Vitro, Ex Vivo and in Vivo Models for Studying the Transport of Drugs Across Intestinal Barriers

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.