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In vitro toxicity of lomefloxacin in rabbit corneal epithelial cell cultures
1Laboratorios cusi, Barcelona, Spain.
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.
Insights
Lomefloxacin (LFLX), a new 4-quinolone antimicrobial, shows no cytotoxicity to corneal cells at concentrations relevant to ophthalmic applications. This suggests LFLX is a promising candidate for topical eye treatments.
Area of Science:
- Ophthalmology
- Microbiology
- Toxicology
Background:
- Lomefloxacin (LFLX) is a novel 4-quinolone antimicrobial with potential for ophthalmic use.
- Understanding its ocular toxicity is crucial for developing safe topical treatments.
Purpose of the Study:
- To evaluate the oculotoxicity of Lomefloxacin (LFLX).
- To determine the safety of LFLX for topical ophthalmic applications.
Main Methods:
- Tested four concentrations of LFLX (10-300 µg/ml) on rabbit corneal epithelial cells.
- Assessed cell number, protein content, neutral red uptake, and wound healing.
- Compared LFLX concentrations with pharmacokinetic and MIC data.
Main Results:
- Low LFLX concentrations (10 & 30 µg/ml) showed no cytotoxic effects.
- High LFLX concentrations (≥100 µg/ml) exhibited significant cytotoxicity.
- Achieved corneal LFLX levels and relevant MIC values were below cytotoxic thresholds.
Conclusions:
- Lomefloxacin demonstrates a favorable safety profile at concentrations relevant to topical ophthalmic use.
- LFLX is a potentially useful agent for developing new ophthalmic antimicrobial therapies.