title: In vitro toxicity of lomefloxacin in rabbit corneal epithelial cell cultures.
abstract: Lomefloxacin (NY-198) is a chemotherapic agent from the new 4-quinolone group, acting on DNA gyrase system. Lomefloxacin (LFLX), as some other new 4-quinolone compounds are antimicrobials of potential use for ophthalmic application. A first approach on the oculotoxicity of LFLX is the main purpose of this study. Four concentrations of LFLX (10, 30, 100 and 300 micrograms/ml) were tested on the first subculture of pigmented rabbit corneal epithelial cells. Cell number, protein contents, neutral red stain and wound healing were evaluated. The results showed that the lower concentrations (10 & 30 micrograms/ml) had no effect while the highest one had a remarkable cytotoxic effect. Pharmacokinetic data show that peak values achieved in the cornea and other ocular structures are lower than 40 micrograms/g (0.3% topical application) and, on another hand, MIC values range from less than or equal to 0.05 to 16 micrograms/ml. So, these "critical" concentrations have no cytotoxic effects according to our results. Then, it is concluded that Lomefloxacin could be a useful drug for topical ophthalmic development.
authors.affiliation: Laboratorios cusi, Barcelona, Spain.
authors.forename: M
authors.initials: M
authors.lastname: Portolés
authors.forename: A
authors.initials: A
authors.lastname: Igual
authors.forename: A
authors.initials: A
authors.lastname: Jauch
authors.forename: S
authors.initials: S
authors.lastname: Nos-Barbéra
mesh_terms: D042462:4-Quinolones; D000818:Animals; D000890:Anti-Infective Agents / Q000633:toxicity*; D002452:Cell Count / Q000187:drug effects; D002470:Cell Survival; D002478:Cells, Cultured; D003315:Cornea / Q000737:chemistry / Q000166:cytology / Q000187:drug effects*; D004848:Epithelium / Q000187:drug effects; D005136:Eye Proteins / Q000032:analysis; D024841:Fluoroquinolones; D008928:Mitochondria / Q000201:enzymology; D015363:Quinolones; D011817:Rabbits; D013385:Succinate Dehydrogenase / Q000378:metabolism; D014945:Wound Healing / Q000187:drug effects
chemical_list: D042462:4-Quinolones; D000890:Anti-Infective Agents; D005136:Eye Proteins; D024841:Fluoroquinolones; D015363:Quinolones; D013385:Succinate Dehydrogenase; C053091:lomefloxacin