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Sidney Sousa, Gleilton Mendonça; Penetration of Eye Drop Solutions of Fluoroquinolones into the Cornea and Anterior Chamber of Human Enucleated Eyes. Invest. Ophthalmol. Vis. Sci. 2013;54(15):4303.
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Many Eye-banks decontaminate the donated eyeballs by fully immersing them, for ten minutes, into commercial eye-drop solutions of antibiotics. The purpose of this study was to compare the penetration of ciprofloxacin 0.3%, ofloxacin 0.3%, and moxifloxacin 0.5% into the cornea and aqueous humor of enucleated human eyes immersed into these solutions.
Three groups of 30 enucleated human eyes, inappropriate for corneal transplantation, were immersed, for ten minutes, into commercial eye drop solutions of ciprofloxacin 0.3%, ofloxacin 0.3% and moxifloxacin 0.5%, respectively. Samples of the cornea and the aqueous humor were stocked under -70 C in liquid nitrogen until the time of analysis with high performance chromatography (HPLC).
The 95% CI of the average concentration within the corneal stroma ranged from 2.50 to 4.78 µg/g for ciprofloxacin 0,3%, from 5.42 to 7.87 µg/g for ofloxacin 0,3% and from 10.81 to 19.16 µg/g for moxifloxacin 0.5%. The differences among the three antibiotics were statistically significant. The 95% CI of the average concentration in the aqueous humor ranged from 0.80 to 1.30 µg/g for ciprofloxacin 0.3% , from 1.20 to 1.59 µg/g for ofloxacin 0.3% and from 3.38 to 5.75 µg/g for moxifloxacin 0.5%. The advantage of the moxifloxacin over the other antibiotics was statistically significant. However, it was impossible to demonstrate a significant difference in the aqueous concentration of ofloxacin and ciprofloxacin.
The corneal concentration expected for moxifloxacin is almost twice as much as for ofloxacin and five times greater than for ciprofloxacin, under the conditions of the experiment. The concentration expected for moxifloxacin in the aqueous humor is about 3.5 times bigger than for ciprofloxacin or for ofloxacin. In summary the superiority of the moxifloxacin penetration into the eye seems to be remarkable, albeit not so intense to rise concerns with the endothelial toxicity. Ofloxacin seems to penetrate better than ciprofloxacin into the cornea. However, in the aqueous humor we could not tell if the difference found in favor of the former was real our fortuitous. Since most of the intraocular penetration of drugs is due to passive diffusion (Healy et al. 2004) this method seems to be a promising tool for comparing relative drug penetration into the cornea and anterior chamber.
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