Penetration of topically applied ciprofloxacin and ofloxacin into the aqueous humor and vitreous

• Published in: Journal of cataract and refractive surgery Vol. 29; no. 3; p. 487
• Main Authors: Yalvac, Ilgaz Sagdic, Basci, Nursabah E, Bozkurt, Atila, Duman, Sunay
• Format: Journal Article
• Language: English
• Published: United States 01-03-2003
• Subjects: Administration, Topical; Aged; Anti-Infective Agents - pharmacokinetics; Aqueous Humor - metabolism; Bacteria - drug effects; Biological Availability; Cataract Extraction; Chromatography, High Pressure Liquid; Ciprofloxacin - pharmacokinetics; Cornea - metabolism; Female; Humans; Male; Microbial Sensitivity Tests; Middle Aged; Ofloxacin - pharmacokinetics; Prospective Studies; Vitreous Body - metabolism
• ISSN: 0886-3350
• DOI: 10.1016/S0886-3350(02)01538-9

To determine the intraocular penetration of topical drops of 2 antibiotics, ciprofloxacin 0.3% and ofloxacin 0.3%, into the aqueous humor and vitreous and to relate these levels to the miminum inhibitory concentration (MIC(90)) for organisms associated with ocular bacterial infections.
Department of Ophthalmology, Ankara Hospital, and Department of Pharmacology, Faculty of Medicine, Hacettepe University, Ankara, Turkey.
This prospective randomized clinical trial comprised 18 patients having cataract surgery, all with an intact corneal epithelium. The patients were randomly assigned to receive topical ciprofloxacin 0.3% (n = 10) or topical ofloxacin 0.3% (n = 8) 1 drop every 15 minutes 5 times and every 30 minutes 3 times before surgery. Aqueous and vitreous samples (if vitreous loss occurred during the cataract surgery) were collected 30 minutes after the administration of the last dose. Drug concentrations were determined by high-performance liquid chromatography (HPLC) fluorescence.
All patients had detectable drug concentrations in the aqueous humor and vitreous measurable by HPLC. The mean aqueous humor concentration of ciprofloxacin was 1.13 microg/mL +/- 1.90 (SD) and the mean vitreous concentration, 0.23 +/- 0.06 microg/mL. Topical administration of ciprofloxacin yielded 4.9 times more drug concentration in the anterior chamber than in the vitreous. The mean aqueous concentration of ofloxacin was 2.06 +/- 1.06 microg/mL and the mean vitreous concentration, 0.46 +/- 0.10 microg/mL. Topical administration of ofloxacin yielded 4.7 times more drug concentration in the anterior chamber than in the vitreous. Aqueous humor concentrations of ofloxacin and ciprofloxacin were not statistically significantly different (P =.353). Intravitreal concentrations of ofloxacin were statistically significantly higher than those of ciprofloxacin (P =.001).
Topical ofloxacin 0.3% penetrated better than topical ciprofloxacin 0.3% into the anterior chamber and vitreous in noninflamed eyes. Both drugs were above the MIC(90) for most ocular pathogens in the anterior chamber. The mean concentration in the vitreous of topically applied ofloxacin 0.3% was statistically significantly higher than that of ciprofloxacin 0.3%, but it was not sufficiently above the MIC(90) for most ocular pathogens in terms of empirical endopthalmitis therapy.