Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model.
The transport characteristics of six fluoroquinolones (FQs) with various lipophilicities were compared in a Calu-3 cell model. For each FQ, an active polarized transport was observed in the direction of the apical side. However, the apparent permeability of FQs resulted from active transport and passive diffusion that were highly variable between compounds and mainly governed by lipophilicity. Therefore, active transport was predominant for compounds with relatively low lipophilicity but minor for FQs with higher lipophilicity.
Brillault
Julien
J
INSERM, ERI-23, Pôle Biologie Santé, 40 avenue du Recteur Pineau, 86000 Poitiers, France.
De Castro
Whocely Victor
WV
Couet
William
W
D018435:ATP Binding Cassette Transporter, Subfamily B / Q000037:antagonists & inhibitors / Q000378:metabolism; D000042:Absorption; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000378:metabolism*; D001693:Biological Transport, Active; D002460:Cell Line; D002463:Cell Membrane Permeability; D003524:Cyclosporins / Q000494:pharmacology; D004058:Diffusion; D004347:Drug Interactions; D024881:Drug Resistance, Bacterial / Q000187:drug effects; D004847:Epithelial Cells / Q000187:drug effects / Q000378:metabolism*; D024841:Fluoroquinolones / Q000737:chemistry / Q000378:metabolism*; D007700:Kinetics; D008055:Lipids / Q000737:chemistry; D008168:Lung / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*
D018435:ATP Binding Cassette Transporter, Subfamily B; D000900:Anti-Bacterial Agents; D003524:Cyclosporins; D024841:Fluoroquinolones; D008055:Lipids; C070272:valspodar