Retinal Delivery of Celecoxib Is Several-Fold Higher Following Subconjunctival Administration Compared to Systemic Administration

@article{Ayalasomayajula2004RetinalDO,
  title={Retinal Delivery of Celecoxib Is Several-Fold Higher Following Subconjunctival Administration Compared to Systemic Administration},
  author={Surya P. Ayalasomayajula and Uday B. Kompella},
  journal={Pharmaceutical Research},
  year={2004},
  volume={21},
  pages={1797-1804}
}
Purpose. We have previously demonstrated that celecoxib, a selective COX-2 inhibitor, reaches the retina following repeated oral administrations and inhibits diabetes-induced vascular endothelial growth factor (VEGF) mRNA expression and vascular leakage in a rat model. The aim of this study was to quantify the relative retinal bioavailability of celecoxib from the subconjunctival route compared to a systemic route. Methods. The plasma and ocular tissue distribution of celecoxib was determined… CONTINUE READING

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RetinaNo subtypeSclera
For the subconjunctivally dosed ( ipsilateral ) eye , the AUC0-≈ ratios between subconjunctival and intraperitoneal groups were 0.8 ± 0.1 , 53 ± 4 , 54 ± 8 , 145 ± 21 , 61 ± 16 , and 52 ± 6 for plasma , sclera , retina , vitreous , lens , and cornea , respectively .
For the contralateral ocular tissues , the AUC0-≈ ratios were 1.2 ± 0.3 , 1.1 ± 0.3 , 1.1 ± 0.4 , 1.0 ± 0.3 , and 1.2 ± 0.3 in the sclera , retina , vitreous , lens , and the cornea , respectively , between the subconjunctival and the intraperitoneal groups .
The plasma , sclera , retina , vitreous , lens , and the cornea were isolated and celecoxib levels were determined using an HPLC method .
ScleraNo subtypeRetina
The plasma , sclera , retina , vitreous , lens , and the cornea were isolated and celecoxib levels were determined using an HPLC method .
For the subconjunctivally dosed ( ipsilateral ) eye , the AUC0-≈ ratios between subconjunctival and intraperitoneal groups were 0.8 ± 0.1 , 53 ± 4 , 54 ± 8 , 145 ± 21 , 61 ± 16 , and 52 ± 6 for plasma , sclera , retina , vitreous , lens , and cornea , respectively .
For the contralateral ocular tissues , the AUC0-≈ ratios were 1.2 ± 0.3 , 1.1 ± 0.3 , 1.1 ± 0.4 , 1.0 ± 0.3 , and 1.2 ± 0.3 in the sclera , retina , vitreous , lens , and the cornea , respectively , between the subconjunctival and the intraperitoneal groups .
RetinaSibling in part ofSclera
For the subconjunctivally dosed ( ipsilateral ) eye , the AUC0-≈ ratios between subconjunctival and intraperitoneal groups were 0.8 ± 0.1 , 53 ± 4 , 54 ± 8 , 145 ± 21 , 61 ± 16 , and 52 ± 6 for plasma , sclera , retina , vitreous , lens , and cornea , respectively .
For the contralateral ocular tissues , the AUC0-≈ ratios were 1.2 ± 0.3 , 1.1 ± 0.3 , 1.1 ± 0.4 , 1.0 ± 0.3 , and 1.2 ± 0.3 in the sclera , retina , vitreous , lens , and the cornea , respectively , between the subconjunctival and the intraperitoneal groups .
The plasma , sclera , retina , vitreous , lens , and the cornea were isolated and celecoxib levels were determined using an HPLC method .
ScleraSibling in part ofRetina
The plasma , sclera , retina , vitreous , lens , and the cornea were isolated and celecoxib levels were determined using an HPLC method .
For the subconjunctivally dosed ( ipsilateral ) eye , the AUC0-≈ ratios between subconjunctival and intraperitoneal groups were 0.8 ± 0.1 , 53 ± 4 , 54 ± 8 , 145 ± 21 , 61 ± 16 , and 52 ± 6 for plasma , sclera , retina , vitreous , lens , and cornea , respectively .
For the contralateral ocular tissues , the AUC0-≈ ratios were 1.2 ± 0.3 , 1.1 ± 0.3 , 1.1 ± 0.4 , 1.0 ± 0.3 , and 1.2 ± 0.3 in the sclera , retina , vitreous , lens , and the cornea , respectively , between the subconjunctival and the intraperitoneal groups .
We have previously demonstrated that celecoxib , a selective COX-2 inhibitor , reaches the retina following repeated oral administrations and inhibits diabetes - induced vascular endothelial growth factor ( VEGF ) mRNA expression and vascular leakage in a rat model .
We have previously demonstrated that celecoxib , a selective COX-2 inhibitor , reaches the retina following repeated oral administrations and inhibits diabetes - induced vascular endothelial growth factor ( VEGF ) mRNA expression and vascular leakage in a rat model .
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