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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 and the aqueous humor of the noninjected left eye after intravitreal injection of 1.25 mg/0.05 mL bevacizumab into the fellow eye. Values at day 0 indicate background levels of bevacizumab detection in control animals.
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f3-opth-5-697: Bevacizumab concentration in the vitreous and the aqueous humor of the noninjected left eye after intravitreal injection of 1.25 mg/0.05 mL bevacizumab into the fellow eye. Values at day 0 indicate background levels of bevacizumab detection in control animals.

Mentions: Very low concentrations of the drug were detected in the fellow noninjected eye. The levels of bevacizumab in the aqueous humor of the noninjected eye peaked at 8 days after intravitreal injection with a concentration of 1.61 ng/mL and declined to 0.11 ng/mL at 29 days. For the vitreous of the noninjected eye, the levels of bevacizumab ranged from 0.245 ng/mL at 1 day after injection to a maximum of 0.335 ng/mL at 8 days and then declined to 0.218 ng/mL at 29 days. Figure 3 shows the change in concentration of bevacizumab in the aqueous and vitreous humor of the fellow noninjected eye.


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 and the aqueous humor of the noninjected left eye after intravitreal injection of 1.25 mg/0.05 mL bevacizumab into the fellow 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

f3-opth-5-697: Bevacizumab concentration in the vitreous and the aqueous humor of the noninjected left eye after intravitreal injection of 1.25 mg/0.05 mL bevacizumab into the fellow eye. Values at day 0 indicate background levels of bevacizumab detection in control animals.
Mentions: Very low concentrations of the drug were detected in the fellow noninjected eye. The levels of bevacizumab in the aqueous humor of the noninjected eye peaked at 8 days after intravitreal injection with a concentration of 1.61 ng/mL and declined to 0.11 ng/mL at 29 days. For the vitreous of the noninjected eye, the levels of bevacizumab ranged from 0.245 ng/mL at 1 day after injection to a maximum of 0.335 ng/mL at 8 days and then declined to 0.218 ng/mL at 29 days. Figure 3 shows the change in concentration of bevacizumab in the aqueous and vitreous humor of the fellow noninjected eye.

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.