Uptake and intracellular activity of ofloxacin isomers in human phagocytic and non-phagocytic cells

The penetration and intracellular activity of ofloxacin and its isomers (levofloxacin and D-ofloxacin) into human polymorphonuclear leucocytes (PMN), human peritoneal macrophages (PMphi) and tissue cultured epithelial cells (McCoy) were evaluated. The cellular to extracellular concentration (C/E) values of the three fluoroquinolones were higher than 3.6 and 2.6 in PMN and PMphi, respectively. The C/E ratios in McCoy cells were lower than those in PMN, but still higher than 2.0. The uptake of ofloxacin and its isomers was rapid, non-saturable and reversible. All quinolones (extracellular concentrations: 2, 5 and 10 mg/l) produced a significant reduction of viable intraphagocytic Staphylococcus aureus in phagocytic cells. We concluded that ofloxacin and its isomers reach high intracellular concentrations in phagocytic and non phagocytic cells while remaining active in the former.