The effect of several antimicrobial agents, active against Gram-positive cocci, anaerobes or fungi on the intracellular penetration of ofloxacin and its optically active isomer (-)-ofloxacin into human polymorphonuclear leucocytes (PMNs) was studied. In the presence of therapeutic extracellular concentrations of these drugs, both ofloxacin and (-)-ofloxacin reached high intracellular concentrations (cellular to extracellular ratio (C/E greater than 3). Ofloxacin and (-)-ofloxacin uptake by PMNs was higher when cells were stimulated with opsonized zymosan (C/E greater than 5). It is concluded that none of the antimicrobial agents studied significantly affected the uptake of both quinolones by human PMNs.