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Gerhard Garhofer, Robert Klaus, Alexandra Maier-Salamon, Walter Jäger, Markus Zeitlinger, Sybilla Richter-Mueksch, Leopold Schmetterer; An exploratory microdialysis study to assess the ocular pharmacokinetics of ciprofloxacin eye drops in rabbits. Invest. Ophthalmol. Vis. Sci. 2015;56(7 ):5723.
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Topical drug delivery is the most widely used drug administration route for the treatment of ocular diseases. However, studies regarding the intraocular in-vivo pharmacokinetics of topically applied drugs are technically demanding and consequently pharmacokinetic data are sparse. The purpose of the study was to gain a robust in-vivo pharmacokinetic profile of the widely used topical antibiotic ciprofloxacin. For this purpose, in-vivo microdialysis of the anterior chamber and the vitreous was performed in a rabbit model.
8 Female New Zealand White rabbits (Charles River, Germany) weighing 2.3 - 4.1 kg were included in the experiments. Under general anesthesia, a linear microdialysis probe (30 kDa molecular weight cut off [MWCO]) was implanted in the anterior chamber, a concentric microdialysis probe (0.5x 10 mm, 20 kDa MWCO) in the posterior segment of the same eye. After a run-in period of 2 hours, one single drop (30µl) of ciprofloxacin eye drops (0.09mg in 30ml) was administered on the ocular surface. Microdialysis samples of the anterior chamber and the vitreous were collected every 30 min for 6h. Finally, relative recovery was assessed by retro-dialysis to calculate absolute concentration values. Samples were analyzed using HPCL.
In the anterior chamber, the maximum free drug concentration (Cmax) amounted to 0.373±0.281 µg/ml and was reached (Tmax) after 116±36 minutes. Calculated AUC (0-n) for ciprofloxacin in the anterior chamber was 78.8±47.1 mg min/ml. For the vitreous, Cmax was 0.002±0.003 µg/ml and maximum drug concentration was reached 106±60min after topical administration. AUC (0-n) for ciprofloxacin in the vitreous was 0.268±0.370 mg min/ml.
Microdialysis is a suitable method to assess in-vivo pharmacokinetic profiles in the anterior chamber and in the vitreous. In the anterior chamber maximum drug concentration was reached approximately 2 hours after single drug administration. Although the drug concentration in the vitreous was considerably lower, time course of drug concentration was comparable.
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