Caco-2 cells are commonly used to test which of the following?

Caco-2 cells are commonly used to test which of the following?

• A. Human intestinal permeability and bioavailability of orally administered drugs
• B. Metabolic rate in the liver
• C. Renal excretion in humans
• D. Neuronal transport across the blood-brain barrier

Answer: (A)

Caco-2 cells are used as a model of the human intestinal barrier to study drug permeability and oral bioavailability. When they differentiate into polarized, enterocyte-like monolayers with tight junctions and brush-border enzymes, they allow measurement of how readily a drug crosses the intestinal lining, typically as apparent permeability, and they help reveal transporter effects such as efflux by P-glycoprotein. This setup provides a functional readout that can predict how much of an orally administered drug will reach the systemic circulation. They aren’t the right model for liver metabolism, renal excretion, or neuronal transport across the blood–brain barrier, which require hepatocytes or liver microsomes, kidney models, or brain endothelial cell models, respectively.

Caco-2 cells are used as a model of the human intestinal barrier to study drug permeability and oral bioavailability. When they differentiate into polarized, enterocyte-like monolayers with tight junctions and brush-border enzymes, they allow measurement of how readily a drug crosses the intestinal lining, typically as apparent permeability, and they help reveal transporter effects such as efflux by P-glycoprotein. This setup provides a functional readout that can predict how much of an orally administered drug will reach the systemic circulation. They aren’t the right model for liver metabolism, renal excretion, or neuronal transport across the blood–brain barrier, which require hepatocytes or liver microsomes, kidney models, or brain endothelial cell models, respectively.