Active secretion of the fluoroquinolone ciprofloxacin by human intestinal epithelial Caco-2 cell layers. |
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| Authors: | N. M. Griffiths B. H. Hirst N. L. Simmons |
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| Affiliation: | Gastrointestinal Drug Delivery Research Centre, Medical School, University of Newcastle upon Tyne. |
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| Abstract: | The bidirectional transepithelial fluxes of ciprofloxacin, an antibacterial fluoroquinolone, across the human intestinal epithelial Caco-2 cell-line show marked asymmetry. Basal-to-apical flux of ciprofloxacin (10 microM) exceeds apical-to-basal flux indicating net secretion. Net ciprofloxacin secretion is abolished by azide/2-deoxy-D-glucose treatment, displays saturation kinetics (Km = 0.89 +/- 0.23 mM, Vmax 44.3 +/- 4.9 nmol cm-2.h) and competition by other fluoroquinolones. A specific, active secretion in Caco-2 epithelia may explain the transintestinal elimination of ciprofloxacin observed in pharmacokinetic studies in man. |
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