ABSTRACT
Within the pharmaceutical industry, the assessment of a compound’s intestinal permeability remains one of the key determinants in the drug development process. Bioavailability measurements are determined by measuring the drug in the blood, hours following oral administration to an animal. How well the drug is absorbed across the intestinal epithelia is difficult to determine with these in vivo measurements. With the advancement of new and improved cell culture systems, intestinal cell lines are available to study the transport of therapeutics across the epithelia, although these cell culture systems can also be a very time-consuming, labor-intensive process. Due to the logarithmic increase in pharmaceutical leads from the drug discovery stages of the pipeline, there is, in turn, a serious demand to increase throughput of in vitro cell-based assays for evaluating intestinal permeability. A significant number of pharmaceutical companies have altered their drug development testing strategy, such that they are now conducting primary screens of compounds for various ADME (absorption, distribution, metabolism, excretion) parameters to decrease the amount of compounds advancing into traditional, more time-consuming secondary assays. The goal is to rank order drug-permeability into groups, so that only the more ‘drug-like’ compounds will continue in the drug development pipeline, minimizing the bottleneck of excessive number of compounds in the drug development phase.
