Caco‐2 Cell Culture Model for Oral Drug Absorption

Caco-2 cell model is recognized as the "gold standard" for studying intestinal absorption of orally administrated drugs. It is also a valuable tool in elucidating the intestinal absorption, excretion, transport, and metabolism mechanisms. Despite the wide acceptance of Caco-2 model, expression levels of certain efflux and uptake transporters and metabolic enzymes may vary among passages or laboratories, which limits the correlation between in vitro and in vivo data. In recent years, technologies, such as genetic modification and organ-on-a-chip, have been implemented in Caco-2 cell models to minimize the bias, improve the model accuracy, and extend the application. An example of a drug transport study using Caco-2 cell model and the relevant data analysis is presented and then discussed to guide the readers who are interested in practicing the model.