Pharmacokinetic parameters determination

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Apparent Permeability Determination (Papp) – Caco-2 cell line
Absorption is defined as a drug’s ability to cross epithelial and endothelial cell barriers from the point of administration to the site of action. The most common method used to study the absorption of a chemical compound use the immortalized Caco-2 cell line of the intestinal epithelium. Caco-2 cells method predicts human intestinal absorption. These in vitro models provide more predictive permeability information than artificial membrane systems (i.e., PAMPA) based on the cells’ ability to promote (active transport) or resist (efflux) transport. Caco-2 cells exhibit many features of absorptive intestinal cells. The intestinal permeability is evaluated by measuring the flux of the test compound from the apical (A) to the basolateral (B) side and is measured in order to predict the absorption from the lumen of the gut. The interaction with the active transporter P-glycoprotein (P-gp) can also be investigated. According to the apparent permeability (Papp) value obtained, test compounds can be classified as follows:
Papp > 50 nm/s: high absorption
Papp 10-50 nm/s: medium absorption
Papp < 10 nm/s: low absorption