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Blazaki Styliani, Chrysanthi Tsika, Eirini Tsiapa, Irini Naoumidi, Manolis Tzatzarakis, Christos Tsatsanis, Miltiadis K Tsilimbaris; THE EFFICACY AND PHARMACOKINETICS OF INTRAVITREAL FLURBIPROFEN. Invest. Ophthalmol. Vis. Sci. 2016;57(12):87. doi: https://doi.org/.
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© ARVO (1962-2015); The Authors (2016-present)
Intravitreal delivelry of non-steroidal anti-inflammatory drugs could be an effective way to treat age-related macular degeneration, diabetic macular edema and other causes of posterior segment inflammation. In this study we evaluated the intravitreal bioavailability and anti-inflammatory effects of intravitreal flurbiprofen in rabbit eyes.
For pharmacokinetics, 7.66mg/ml flurbiprofen was injected and vitreous drug levels were analyzed at specific time points. 3 eyes were analyzed per time point with means of HLPC/MS method. For efficacy, 100ng lipopolysaccharide (LPS) of E.coli was injected intravitreally to induce inflammation; the right eyes received flurbiprofen or dexamethasone and the left eyes PBS. Total cell count was determined after aqueous fluid remove at specific time points. Seven days after LPS injection eyes were enucleated for histopathologic analysis. The effect of drugs in the uveitis model was determined by clinical signs of inflammation, total leukocyte count and histology findings.
No adverse events were observed during pharmacokinetics assesment. No signs of inflammation, hemorrhage or detachment were detected. The recovery of the method was 92.6%. The clearance of flurbiprofen follows first order kinetics. The half-life of slow release flurbiprofen solution estimated 16.12 hours with an elimination constant rate (K) of 0.043. Treatment with flurbiprofen and dexamethasone reduced significantly total cell count by 51.1% and 86.2% respectively. Histologic studies demonstrated less signs of ocular inflammation after flurbiprofen and dexamethasone intraocular injection compared to control eyes.
Flurbiprofen is effective in inflammatory ocular diseases. Intravitreal flurbiprofen and dexamethasone seem to have similar therapeutic results. However, the half-life of the drug remains short and so there is a need for greater prolongation in the vitreous.
This is an abstract that was submitted for the 2016 ARVO Annual Meeting, held in Seattle, Wash., May 1-5, 2016.
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