Abstract
Objective:
To determine the efficacy of pazopanib eye drops in the streptozotocin induced diabetic retinopathy rat model.
Methods:
A 0.5% w/v pazopanib suspension was prepared in phosphate buffered saline (PBS, pH 7.4) in the presence of 0.5% w/v sodium carboxymethyl cellulose. Brown Norway rats were divided into three groups (n=4) - (1) healthy, (2) diabetic, and (3) diabetic with treatment. The drug suspension was administered twice daily as eye drops to group 3 for 30 days. Efficacy parameters including the number of adherent leukocytes in the retinal vasculature (leukostasis), blood-retinal FITC-dextran leakage, and vitreous-to-plasma protein ratio were measured.
Results:
Pazopanib suspension in the form of eye drops significantly reduced leukostasis (32%), FITC-dextran leakage (39%), and the vitreous-to-plasma protein ratio (64%) in diabetic animals compared to untreated diabetic group.
Conclusion:
Pazopanib eye drops can alleviate retinal complications of diabetic retinopathy.
Copyright © 2011 Elsevier Inc. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Administration, Ophthalmic
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Animals
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Blood Glucose / metabolism
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Blood Proteins / metabolism
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Blood-Retinal Barrier / drug effects*
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Blood-Retinal Barrier / enzymology
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Body Weight
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Capillary Permeability / drug effects*
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Diabetes Mellitus, Experimental / complications
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Diabetes Mellitus, Experimental / drug therapy*
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Diabetes Mellitus, Experimental / enzymology
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Diabetic Retinopathy / enzymology
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Diabetic Retinopathy / etiology
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Diabetic Retinopathy / prevention & control*
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Indazoles
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Leukocytes / drug effects
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Leukocytes / enzymology
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Leukostasis / enzymology
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Leukostasis / etiology
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Leukostasis / prevention & control*
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Macular Edema / enzymology
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Macular Edema / etiology
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Macular Edema / prevention & control*
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Male
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Molecular Targeted Therapy
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Ophthalmic Solutions
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Protein Kinase Inhibitors / administration & dosage
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Protein Kinase Inhibitors / pharmacology*
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Protein-Tyrosine Kinases / antagonists & inhibitors*
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Protein-Tyrosine Kinases / metabolism
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Pyrimidines / administration & dosage
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Pyrimidines / pharmacology*
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Rats
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Rats, Inbred BN
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Sulfonamides / administration & dosage
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Sulfonamides / pharmacology*
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Time Factors
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Vitreous Body / metabolism
Substances
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Blood Glucose
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Blood Proteins
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Indazoles
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Ophthalmic Solutions
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Protein Kinase Inhibitors
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Pyrimidines
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Sulfonamides
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pazopanib
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Protein-Tyrosine Kinases