Cell-Based Intestinal In Vitro Models for Drug Absorption Screening

Despite major innovations in drug administration, oral intake remains the preferred route for drug delivery, mainly due to ease of administration and high patient compliance. Therefore, intestinal permeability of molecules lasts to be critical during oral pharmaceutical research, and the prediction of drug absorption is of major importance in the design, optimization, and selection of drugs and pharmaceutical formulations for oral delivery. There are various in vitro methods to assess the extent of drug absorption across different phases of drug development research. Further to a brief description of the physiology of gastrointestinal mucosa and the absorption mechanisms across the intestinal barrier, this chapter focuses on the different in vitro cell models currently used to predict human permeability. It is given a thorough discussion on their suitability and pros and cons considering the study objectives to evaluate passive, efflux, or uptake carriers mediated absorption, metabolism, and drug–drug interaction. It also intended a critical assessment and clarification about the add value of these models in the absorption-related prediction.