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Assessment of Macrolide Transport Using PAMPA, Caco-2 and MDCKII-hMDR1 Assays

Nožinić, Danijela; Milić, Astrid; Mikac, Lara; Ralić, Jovica; Padovan, Jasna; Antolović, Roberto (2010) Assessment of Macrolide Transport Using PAMPA, Caco-2 and MDCKII-hMDR1 Assays. Croatica Chemica Acta, 83 (3). pp. 323-331. ISSN 0011-1643

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The transport of commercially available macrolide antibiotics erythromycin, clarithromycin, roxithromycin, azithromycin, and telithromycin was studied by PAMPA, a model of passive diffusion, and by two models of active transport, Caco-2 and MDCKII-hMDR1. An involvement of efflux pump P-glycoprotein (P-gp) in macrolide transport was also examined. Generally, in Caco-2 and MDCKII-hMDR1 assays without P-gp inhibition, a significantly lower apparent permeability (P(app)) in apical-to-basolateral (AB) than basolateral-to-apical (BA) direction was observed [efflux ratio, P(app)ratio(BA/AB) > 4.2]. Upon P-gp inhibition, P(app)(AB) was increased and P(app)(BA) was decreased. The observed P(app) values, their efflux ratios, as well as a significant decrease in efflux ratios caused by P-gp inhibition (> 50 %) qualify all tested macrolides as P-gp substrates. Results obtained with PAMPA suggest that this assay is not a method of choice for screening of macrolide permeability due to the lack of P-gp efflux pump and/or other transporters potentially involved in macrolide transport.

Item Type: Article
Uncontrolled Keywords: macrolides; permeability; P-glycoprotein; PAMPA; Caco-2; MDCK; membrane-permeability assay; drug-drug interactions; p-glycoprotein; in-vitro; antimicrobial agents; mediated transport; cell monolayer; protein mrp2; absorption; azithromycin
Subjects: NATURAL SCIENCES > Chemistry
Divisions: Division of Materials Physics
Depositing User: Lara Mikac
Date Deposited: 16 Oct 2013 13:45

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