In Vitro Permeability and Transporters

Creative Bioarray provides a number of in vitro permeability and transporter assays to evaluate drug permeability and predict drug absorption and distribution, including Caco-2 permeability assay, MDCK permeability assay, Parallel artificial membrane permeability assay (PAMPA), and a panel of transporter assays on several of the most relevant transporters such as canine P-glycoprotein (P-gp), BCRP, BSEP, OAT1, OAT3, OATP1B1, OATP1B3, OCT1, and OCT2.

Prediction of drug absorption is an important goal in the design, optimization, and selection of drugs. Drug permeability across biological membranes is a key factor in the absorption of drugs across gastrointestinal mucosa and the distribution of drugs to tissues through blood circulation. Poor permeability can lead to poor absorption (for orally administered drugs) or poor distribution throughout the body. The permeability of a drug across a membrane depends on both the passive diffusion and the active transport of the drug.

There are a number of in vitro cell-based or cell-free methods to study drug permeability and transporter interactions:

Caco-2 permeability assay is the gold standard method to evaluate both the passive and active transport and the absorption of orally taken drugs. The method can be used to assess the bidirectional permeability of a test compound (from the apical to the basolateral side or vice versa).

MDCK permeability assay is a useful tool for the identification of substrates and inhibitors of efflux transporters P-gp, and for the calculation of net flux ratio.

PAMPA, a cell-free method that uses a lipid-infused artificial membrane to determine the passive permeability of substances from a donor compartment to an acceptor compartment, is a widely used assay to predict oral absorption that exhibit a high degree of correlation with Caco-2 assay. Mechanism of drug absorption can be better estimated combining the results of PAMPA and of Caco-2 assay.

Other related assays and transporter assays are also available. We provide assays on a variety of transporters, including but not limited to P-gp, BCRP, BSEP, OAT1, OAT3, OATP1B1, OATP1B3, OCT1, and OCT2. Contact us for more information.

Creative Bioarray is staffed with experienced experts in the field of drug development. We are dedicated to serving our customers with well-developed assays and high quality data, helping our customers achieve a trouble-free drug screening and optimizing experience. We are capable of tailoring the assays in order to meet your needs. If you have any questions, please feel free to contact us. We look forward to working with you in the future.

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