Effects of fluoroquinolone eye solutions without preservatives on human corneal epithelial cells in vitro

To evaluate the biologic effects of fluoroquinolone eye solutions without preservatives on cultured human corneal epithelial cells in vitro.

We studied the effect of diverse generations of topical fluoroquinolones such as ofloxacin 0.3%, levofloxacin 0.5%, tosufloxacin 0.3%, moxifloxacin 0.5% and gatifloxacin 0.3% on cultured human corneal epithelial cells. MTT-based calorimetric assay, lactate dehydrogenase leakage (LDH) assay and scratch wound test were performed. Corneal epithelial cell morphologies were examined by performing inverted light microscopy and transmission electron microscopy.

In all topical fluoroquinolones, the metabolic activity of the corneal epithelial cells decreased in a time-dependent fashion and the LDH titer increased with longer exposure times. Especially, the LDH titers significantly increased after exposure to moxifloxacin 0.5% and gatifloxacin 0.3% compared with controls. The migration rates of the corneal epithelial cells were faster in ofloxacin 0.3% or levofloxacin 0.5% than other fluoroquinolones. Severe cellular morphological damage was observed after exposure to moxifloxacin 0.5% and gatifloxacin 0.3%.

As moxifloxacin 0.5% and gatifloxacin 0.3% induced the toxic effect to the corneal epithelial cells, compared with other fluoroquinolones, the 4th fluoroquinolone eye solutions should be carefully used in case of the corneal epithelium is damaged by long duration of treatment or overdosage.