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Comparative Study
. 2010 Jan;54(1):543-5.
doi: 10.1128/AAC.00733-09. Epub 2009 Oct 12.

Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model

Julien Brillault  1 , Whocely Victor De Castro, William Couet
Affiliations
Comparative Study

Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model

Julien Brillault et al. Antimicrob Agents Chemother. 2010 Jan.

Abstract

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.

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Figures

FIG. 1.
FIG. 1.
Linear relationship between the apparent permeability of FQs in the presence of PSC-833 and the log D. The linear regression fitted the data with the following equation: Papp = 6.1 log D + 7.5. Data are expressed as mean ± SEM (n = 6).
See this image and copyright information in PMC

References

    1. Alvarez, A. I., M. Perez, J. G. Prieto, A. J. Molina, R. Real, and G. Merino. 2008. Fluoroquinolone efflux mediated by ABC transporters. J. Pharm. Sci. 97:3483-3493. - PubMed
    1. Brillault, J., W. V. De Castro, T. Harnois, A. Kitzis, J. C. Olivier, and W. Couet. 2009. P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model. Antimicrob. Agents Chemother. 53:1457-1462. - PMC - PubMed
    1. Endter, S., U. Becker, N. Daum, H. Huwer, C. M. Lehr, M. Gumbleton, and C. Ehrhardt. 2007. P-glycoprotein (MDR1) functional activity in human alveolar epithelial cell monolayers. Cell Tissue Res. 328:77-84. - PubMed
    1. Hamilton, K. O., E. Topp, I. Makagiansar, T. Siahaan, M. Yazdanian, and K. L. Audus. 2001. Multidrug resistance-associated protein-1 functional activity in Calu-3 cells. J. Pharmacol. Exp. Ther. 298:1199-1205. - PubMed
    1. Langlois, M.-H., M. Montagut, J.-P. Dubost, J. Grellet, and M.-C. Saux. 2005. Protonation equilibrium and lipophilicity of moxifloxacin. J. Pharm. Biomed. Anal. 37:389-393. - PubMed

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