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Paula Garcia
Christine Prosser Paula Garcia John Comer Shenaz Nunhuck Darren Edwards Toni Llinās


Permeability: Transporting drugs through (lipid) membranes

Paula Garcia, Organon, NL

The absorption of orally administered substances is largely determined by their ability to cross the gastrointestinal tract (GI-tract). Up to now, the Caco-2 assay is used to measure permeability. This assay uses a cancer cell line as a membrane and therefore includes all types of membrane transport mechanisms. Attending to the fact that between 80-95% of the commercial drugs are absorbed by passive diffusion, it is of utmost interest to implement a high throughput and inexpensive permeability assay which delivers data on passive diffusion rates. At Organon we have implemented a high throughput screening assay (PAMPA) to measure permeability of drugs in order to predict/estimate their permeability in the Human Intestinal Tract. In this talk, I would like to show and discuss the effect of the pH, incubation time, lipophilicity and solubility on permeability. The PAMPA assay was designed and implemented to measure passive diffusion permeability of compounds in early drug discovery.

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Last modified: 28 April 2008