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Pharmacokinetics of intravitreal bevacizumab (Avastin®) in rabbits.

Sinapis CI, Routsias JG, Sinapis AI, Sinapis DI, Agrogiannis GD, Pantopoulou A, Theocharis SE, Baltatzis S, Patsouris E, Perrea D - Clin Ophthalmol (2011)

Bottom Line: In the aqueous humor of the noninjected eye, maximum concentration of bevacizumab was achieved at day 8 (1.6125 ng/mL) and declined (to 0.11 ng/mL) at 4 weeks.The vitreous half-life of 1.25 mg/0.05 mL intravitreal bevacizumab was 6.61 days in this rabbit model.Very low concentrations of bevacizumab were measured in the fellow noninjected eye.

View Article: PubMed Central - PubMed

Affiliation: Laboratory for Experimental Surgery and Surgical Research 'N.S.Christeas', School of Medicine, National and Kapodistrian University of Athens, 15b AgiouThoma Street, 11527, Athens, Greece. csinapis@yahoo.gr

ABSTRACT

Purpose: To describe the pharmacokinetics of intravitreal bevacizumab (Avastin®) in rabbits.

Methods: The right eye of 20 rabbits was injected intravitreally with 1.25 mg/0.05 mL bevacizumab. Both eyes of four rabbits each time were enucleated at days 1, 3, 8, 15, and 29. Bevacizumab concentrations were measured in serum, aqueous humor, and vitreous.

Results: Maximum vitreous (406.25 μg/mL) and aqueous humor (5.83 μg/mL) concentrations of bevacizumab in the right eye were measured at day 1. Serum bevacizumab concentration peaked at day 8 (0.413 μg/mL) and declined to 0.032 μg/mL at 4 weeks. Half-life values in right vitreous, right aqueous humor, and serum were 6.61, 6.51, and 5.87 days, respectively. Concentration of bevacizumab in the vitreous of the noninjected eye peaked at day 8 (0.335 ng/mL) and declined to 0.218 ng/mL at 4 weeks. In the aqueous humor of the noninjected eye, maximum concentration of bevacizumab was achieved at day 8 (1.6125 ng/mL) and declined (to 0.11 ng/mL) at 4 weeks.

Conclusion: The vitreous half-life of 1.25 mg/0.05 mL intravitreal bevacizumab was 6.61 days in this rabbit model. Maximum concentrations of bevacizumab were reached at day 1 in both vitreous and aqueous humor of the right eye and at day 8 in the serum. Very low concentrations of bevacizumab were measured in the fellow noninjected eye.

No MeSH data available.


Related in: MedlinePlus

Light micrographs of 4μm thick sections stained with hematoxylin-eosin revealed chronic inflammatory infiltrations (A) especially in the nerve fiber layer of the retina around the optic disc (B) and in iris (C) in a few specimens. No other histological differences were evident between injected and noninjected eyes in the rest of the specimens (D).
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f5-opth-5-697: Light micrographs of 4μm thick sections stained with hematoxylin-eosin revealed chronic inflammatory infiltrations (A) especially in the nerve fiber layer of the retina around the optic disc (B) and in iris (C) in a few specimens. No other histological differences were evident between injected and noninjected eyes in the rest of the specimens (D).

Mentions: The cytotoxicity of the drug is currently under investigation in our laboratory. Our preliminary results show no important histological changes in all the anatomical parts that were examined by light microscopy (Figure 5). In both injected and noninjected eyes, no signs of necrosis or degeneration of the retina were noticed and the retinal thickness was unchanged. Only some specimens of the right injected eyes revealed chronic inflammatory infiltrations (indicated by arrows in Figure 5) consisting of lymphocytes, plasma cells, and rarely eosinophils. The left noninjected eyes had no histological changes as seen by light microscopy.


Pharmacokinetics of intravitreal bevacizumab (Avastin®) in rabbits.

Sinapis CI, Routsias JG, Sinapis AI, Sinapis DI, Agrogiannis GD, Pantopoulou A, Theocharis SE, Baltatzis S, Patsouris E, Perrea D - Clin Ophthalmol (2011)

Light micrographs of 4μm thick sections stained with hematoxylin-eosin revealed chronic inflammatory infiltrations (A) especially in the nerve fiber layer of the retina around the optic disc (B) and in iris (C) in a few specimens. No other histological differences were evident between injected and noninjected eyes in the rest of the specimens (D).
© Copyright Policy
Related In: Results  -  Collection

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getmorefigures.php?uid=PMC3104800&req=5

f5-opth-5-697: Light micrographs of 4μm thick sections stained with hematoxylin-eosin revealed chronic inflammatory infiltrations (A) especially in the nerve fiber layer of the retina around the optic disc (B) and in iris (C) in a few specimens. No other histological differences were evident between injected and noninjected eyes in the rest of the specimens (D).
Mentions: The cytotoxicity of the drug is currently under investigation in our laboratory. Our preliminary results show no important histological changes in all the anatomical parts that were examined by light microscopy (Figure 5). In both injected and noninjected eyes, no signs of necrosis or degeneration of the retina were noticed and the retinal thickness was unchanged. Only some specimens of the right injected eyes revealed chronic inflammatory infiltrations (indicated by arrows in Figure 5) consisting of lymphocytes, plasma cells, and rarely eosinophils. The left noninjected eyes had no histological changes as seen by light microscopy.

Bottom Line: In the aqueous humor of the noninjected eye, maximum concentration of bevacizumab was achieved at day 8 (1.6125 ng/mL) and declined (to 0.11 ng/mL) at 4 weeks.The vitreous half-life of 1.25 mg/0.05 mL intravitreal bevacizumab was 6.61 days in this rabbit model.Very low concentrations of bevacizumab were measured in the fellow noninjected eye.

View Article: PubMed Central - PubMed

Affiliation: Laboratory for Experimental Surgery and Surgical Research 'N.S.Christeas', School of Medicine, National and Kapodistrian University of Athens, 15b AgiouThoma Street, 11527, Athens, Greece. csinapis@yahoo.gr

ABSTRACT

Purpose: To describe the pharmacokinetics of intravitreal bevacizumab (Avastin®) in rabbits.

Methods: The right eye of 20 rabbits was injected intravitreally with 1.25 mg/0.05 mL bevacizumab. Both eyes of four rabbits each time were enucleated at days 1, 3, 8, 15, and 29. Bevacizumab concentrations were measured in serum, aqueous humor, and vitreous.

Results: Maximum vitreous (406.25 μg/mL) and aqueous humor (5.83 μg/mL) concentrations of bevacizumab in the right eye were measured at day 1. Serum bevacizumab concentration peaked at day 8 (0.413 μg/mL) and declined to 0.032 μg/mL at 4 weeks. Half-life values in right vitreous, right aqueous humor, and serum were 6.61, 6.51, and 5.87 days, respectively. Concentration of bevacizumab in the vitreous of the noninjected eye peaked at day 8 (0.335 ng/mL) and declined to 0.218 ng/mL at 4 weeks. In the aqueous humor of the noninjected eye, maximum concentration of bevacizumab was achieved at day 8 (1.6125 ng/mL) and declined (to 0.11 ng/mL) at 4 weeks.

Conclusion: The vitreous half-life of 1.25 mg/0.05 mL intravitreal bevacizumab was 6.61 days in this rabbit model. Maximum concentrations of bevacizumab were reached at day 1 in both vitreous and aqueous humor of the right eye and at day 8 in the serum. Very low concentrations of bevacizumab were measured in the fellow noninjected eye.

No MeSH data available.


Related in: MedlinePlus