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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.


Bevacizumab concentration in the vitreous, aqueous humor, and serum after intravitreal injection of 1.25 mg/0.05 mL of bevacizumab in rabbits. Samples were taken from the aqueous humor and vitreous of the injected right eye. Values at day 0 indicate background levels of bevacizumab detection in control animals.
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f2-opth-5-697: Bevacizumab concentration in the vitreous, aqueous humor, and serum after intravitreal injection of 1.25 mg/0.05 mL of bevacizumab in rabbits. Samples were taken from the aqueous humor and vitreous of the injected right eye. Values at day 0 indicate background levels of bevacizumab detection in control animals.

Mentions: Data were obtained from the 48 eyes of 24 rabbits. There were no signs of ocular inflammation or other adverse events. The change in concentration over time for bevacizumab in the vitreous and aqueous humor of injected eye and in serum after intravitreal injection is illustrated in Figure 2. A peak concentration of 406.25 μg/mL was achieved in the vitreous 1 day after intravitreal injection of 1.25 mg/0.05 mL bevacizumab. Half-life of bevacizumab in the right vitreous was 6.61 days (Table 1). A concentration of 5.17 μg/mL was maintained in the vitreous 29 days after injection. Bevacizumab concentrations in the aqueous humor of the injected eye reached a peak concentration of 5.835 μg/mL 1 day after drug administration as well. A concentration of 0.225 μg/mL was maintained in aqueous humor 29 days after injection. In serum, a maximum concentration of 0.413 μg/mL was achieved 8 days after drug injection and the concentration fell to 0.032 μg/mL 29 days after drug administration. Half-life of bevacizumab in the right aqueous humor and serum were 6.51 and 5.87 days, respectively (Table 1).


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)

Bevacizumab concentration in the vitreous, aqueous humor, and serum after intravitreal injection of 1.25 mg/0.05 mL of bevacizumab in rabbits. Samples were taken from the aqueous humor and vitreous of the injected right eye. Values at day 0 indicate background levels of bevacizumab detection in control animals.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3104800&req=5

f2-opth-5-697: Bevacizumab concentration in the vitreous, aqueous humor, and serum after intravitreal injection of 1.25 mg/0.05 mL of bevacizumab in rabbits. Samples were taken from the aqueous humor and vitreous of the injected right eye. Values at day 0 indicate background levels of bevacizumab detection in control animals.
Mentions: Data were obtained from the 48 eyes of 24 rabbits. There were no signs of ocular inflammation or other adverse events. The change in concentration over time for bevacizumab in the vitreous and aqueous humor of injected eye and in serum after intravitreal injection is illustrated in Figure 2. A peak concentration of 406.25 μg/mL was achieved in the vitreous 1 day after intravitreal injection of 1.25 mg/0.05 mL bevacizumab. Half-life of bevacizumab in the right vitreous was 6.61 days (Table 1). A concentration of 5.17 μg/mL was maintained in the vitreous 29 days after injection. Bevacizumab concentrations in the aqueous humor of the injected eye reached a peak concentration of 5.835 μg/mL 1 day after drug administration as well. A concentration of 0.225 μg/mL was maintained in aqueous humor 29 days after injection. In serum, a maximum concentration of 0.413 μg/mL was achieved 8 days after drug injection and the concentration fell to 0.032 μg/mL 29 days after drug administration. Half-life of bevacizumab in the right aqueous humor and serum were 6.51 and 5.87 days, respectively (Table 1).

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.