Intracellular penetration of 5 quinolones into non-phagocytic cells
García, I.; Pascual, A.; Conejo, M.C.; Perea, E.J.
Enfermedades Infecciosas y Microbiologia Clinica 14(3): 167-170
1996
ISSN/ISBN: 0213-005X PMID: 8695686 Document Number: 467534
The intracellular penetration and activity of antimicrobial agents can be an important factor in the treatment of infections caused by intracellular pathogens. The new quinolones are able to penetrate into phagocytes, but only a few studies have evaluated other types of cells. The purpose of this study is to evaluate the intracellular penetration of ofloxacin, levofloxacin, lomefloxacin, sparfloxacin and BAY Y 3118 into human polymorphonuclear leukocytes and tissue cultured epithelial cells. Intracellular penetration was evaluated by a fluorometric assay for all the quinolones evaluated except for sparfloxacin, which was evaluated by a radiometric assay. All the quinolones evaluated reached intracellular concentrations higher than extracellular ones. The penetration of sparfloxacin and BAY Y 3118 into the epithelial cells was similar to those observed for PMNs (cellular to extracellular concentration ratio; C/E > or = 4). The C/E values of ofloxacin, levofloxacin and lomefloxacin for epithelial cells were lower than those observed in PMN, but still yielding C/E values > or = 2.