IngentaConnect Uptake of quinolones by in-vitro human monocyte derived macrophag...

Authors: Dorian M.¹; Grellet J.¹; Saux M.C.¹

Source: Journal of Pharmacy and Pharmacology, Volume 53, Number 5, 1 May 2001 , pp. 735-741(7)

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

g 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.

Document Type: Research article

DOI: 10.1211/0022357011775866

Affiliations: 1: Laboratory of Pharmacokinetics and Clinical Pharmacy, University Victor Ségalen-Bordeaux II, Rue Leo Saignat 33076, Bordeaux Cedex, France

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Uptake of quinolones by in-vitro human monocyte derived macrophages