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Evaluation of Drug Efflux Transporter Liabilities of Darifenacin in Cell Culture Models of the Blood–brain and Blood–ocular Barriers by Donald W. Miller; Martha Hinton; Fang Chen is a Medicine article available to read on EtoBox.

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## Abstract ## Aims The objective of the present study was to evaluate drug efflux transporter interactions of darifenacin and examine the impact of such transporter interactions on darifenacin permeability in an __in vitro__ model of the blood–brain barrier (BBB) and blood–ocular barrier (BOB). ## Methods Cell membranes expressing human P‐glycoprotein (P‐gp), multidrug resistance‐associated protein (MRP), and breast cancer resistance protein (BCRP) were examined for ATPase activity following darifenacin exposure (0–10 μM). Primary cultured bovine brain microvessel endothelial cells (BBMEC) and P‐gp transfected Manin–Darby canine kidney epithelial cells (MDCK__MDR1__) were used to examine darifenacin permeability and drug efflux transporter responses. ## Results Concentration‐dependent increases in ATPase activity was observed in P‐gp membranes following darifenacin exposure. Both MRP and BCRP membrane preparations were unresponsive to darifenacin. Studies in both BBMEC and MDCK__MDR1__ monolayers confirmed a P‐gp interaction for darifenacin and significantly greater efflux (basolateral to apical) permeability for darifenacin that was reduced by the P‐gp inhibitor, elacridar. ## Co

Who reads Evaluation of Drug Efflux Transporter Liabilities of Darifenacin in Cell Culture Models of the Blood–brain and Blood–ocular Barriers?

Author

Donald W. Miller; Martha Hinton; Fang Chen

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 0733-2467)

Published

2011

Language

EN

Field

Medicine (Health Sciences)