The presence of the superfamily members of the ATP binding cassette (ABC) transporters is well established as the main cause of multidrug resistance, since they efflux therapeutic compounds from cells and reduce the intracellular drug levels.
An investigation led by the researcher Nicoló Milani was published in the prestigious analytical journal Lab on a Chip. The CacoGoblet kit was employed to investigate the permeability and the metabolism of the compound in a gut-liver-organ-on-a-chip (OoC).
OATP1B1 and OATP1B3 are two influx transporters of the SLCO gene family that are primarily expressed in the sinusoidal membrane of hepatocytes.
Understanding the role of these transporters in the clearance of new molecular entities (NME) is normally performed in-vitro at the early stages of drug development.
It is well known that food intake changes luminal conditions (e.g. pH, motility, microbiota,…) in the stomach and the small intestine, modifying drugs bioavailability. Food-drug interactions are one of the major challenges for oral-administered drugs, even more so if considering the growing use of food supplements and functional foods.
The endothelial cells that conform the BBB limit the passage of blood circulating endogenous substrates and larger molecules to the brain. This intrinsic protective role is also a major hurdle for reasearchers developing drugs for Central Nervous System (CNS) disorders.
