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C. Sinapis, J. Routsias, D. Sinapis, A. Sinapis, V. Sinapi, A. Pantopoulou, S. Baltatzis, E. Patsouris, D. Perrea; Pharmacokinetics of Intravitreal Bevacizumab (Avastin) in Rabbits. Invest. Ophthalmol. Vis. Sci. 2010;51(13):2440.
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To describe the pharmacokinetics of 1.25 mg of intravitreal bevacizumab (Avastin) in rabbits.
The right eye of each of 20 rabbits was injected with 1.25 mg of intravitreal bevacizumab. Both eyes of each of 4 rabbits were enucleated at days 1, 3, 8, 15 and 29. Bevacizumab concentrations were measured in aqueous humor, vitreous and serum using two enzyme-linked immunosorbent assays (ELISA), one of low sensitivity (5ng/ml - 0.1 µg/ml) and one of high sensitivity (10pg/ml - 5ng/ml).
Maximum vitreous (406.25 µg/ml) and aqueous humor (5.83 µg/ml) concentrations of bevacizumab in the right eye were measured 1 day after drug administration. Concentrations of >5 µg/ml bevacizumab were maintained in the vitreous 29 days after injection. A maximum serum concentration of 0.412 µg/ml was achieved 8 days after intravitreal injection and the concentration fell at 0.032 µg/ml 29 days after injection. Very low concentrations of bevacizumab were detected in the fellow uninjected eye. Concentrations of bevacizumab in the vitreous of the fellow eye reached their peak 8 days after injection, at 0.335 ng/ml, and declined to 0.2175 ng/ml at 4 weeks. Concentrations of bevacizumab in the aqueous humor of the fellow eye reached their peak 8 days after injection, at 1.6125 ng/ml, and declined to 0.105ng/ml at 4 weeks.
The maximum concentrations of bevacizumab in both vitreous and aqueous humor of right eye were reached at 1 day after injection while in the serum at 8 days after injection. Very small amounts of bevacizumab were detected in the fellow uninjected eye with the maximum concentrations measured at 8 days after injection for both the aqueous humor and vitreous.
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