title: Comparative penetration of lomefloxacin and other quinolones into human phagocytes.
abstract: The penetration of lomefloxacin into human polymorphonuclear leukocytes (PMNs) and peritoneal macrophages (PMphis) was evaluated using a fluorometric assay. Lomefloxacin reached high intracellular concentrations into PMNs at extracellular concentrations of 2 and 5 mg/L (cellular to extracellular concentration ratio [C/E] greater than 4). At the same conditions (20 minutes incubation; extracellular concentrations: 2 mg/L) lomefloxacin uptake by human PMNs (C/E: 7.9 +/- 2.6) was slightly higher than those of norfloxacin (C/E 5.1 +/- 1.8), ciprofloxacin (C/E: 6.2 +/- 2.0), and ofloxacin (C/E 7.1 +/- 2.6). Lomefloxacin penetration into human PMphis was significantly lower than PMNs but still with C/E ratios greater than 4. Entry of lomefloxacin into phagocytes was not affected by cell viability but was environmental-temperature dependent. It is concluded that lomefloxacin and the other quinolones evaluated reach high intracellular concentrations in human phagocytic cells.
authors.affiliation: Department of Microbiology, School of Medicine, Sevilla, Spain.
authors.forename: E J
authors.initials: EJ
authors.lastname: Perea
authors.forename: I
authors.initials: I
authors.lastname: García
authors.forename: A
authors.initials: A
authors.lastname: Pascual
mesh_terms: D000704:Analysis of Variance; D000890:Anti-Infective Agents / Q000493:pharmacokinetics*; D001202:Ascitic Fluid / Q000166:cytology; D002939:Ciprofloxacin / Q000493:pharmacokinetics; D024841:Fluoroquinolones; D006801:Humans; D066298:In Vitro Techniques; D008264:Macrophages / Q000378:metabolism*; D009504:Neutrophils / Q000378:metabolism*; D009643:Norfloxacin / Q000493:pharmacokinetics; D015242:Ofloxacin / Q000493:pharmacokinetics; D015363:Quinolones / Q000493:pharmacokinetics*
chemical_list: D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D015363:Quinolones; D002939:Ciprofloxacin; D015242:Ofloxacin; C053091:lomefloxacin; D009643:Norfloxacin