Uptake of quinolones by in-vitro human monocyte derived macrophages

  • Dorian M
  • Grellet J
  • Saux M
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Abstract

We have developed an in-vitro model of monocyte-derived macrophage (MDMØ) to compare fluoroquinolone uptake in monocytes and derived macrophages. Monocyte-derived macrophages were obtained in-vitro by cultivating freshly isolated monocytes for seven days in RPMI 1640 medium, containing foetal calf serum and Rhu granulocyte-macrophage colony stimulating factor. Final suspensions contained 95% viable cells and 63% macrophages. Intra-macrophagic accumulation of ciprofloxacin, ofloxacin or sparfloxacin was measured at equilibrium after 30-min incubation in the presence of 16–18 μg mL−1 antibiotic. The results revealed low intra-cellular accumulation of ofloxacin in MDMØ (intracellular/extracellular ratio: IC/EC = 1.7). Ciprofloxacin and sparfloxacin uptake was significantly higher. The IC/EC ratios were only slightly increased in macrophages when compared with monocytes under the same experimental conditions. These results suggest that maturation of monocyte to macrophage has only a limited effect on basal quinolone uptake. Monocytic maturation cannot explain the important differences between fluoroquinolone accumulation in monocytes and tissue macrophages. Cell activation may be a greater determinant.

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Dorian, M., Grellet, J., & Saux, M. C. (2010). Uptake of quinolones by in-vitro human monocyte derived macrophages. Journal of Pharmacy and Pharmacology, 53(5), 735–741. https://doi.org/10.1211/0022357011775866

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