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Miltiadis K Tsilimbaris, Stella Blazaki, Chrysanthi Tsika, Konstantions Pachis, Irini Naoumidi, Christos Tsatsanis, Manolis Tzatzarakis, Sofia Antimisiaris; INTRAOCULAR SUSTAINED DELIVERY SYSTEM OF FLURBIPROFEN; EFFICACY AND PHARMACOKINETICS. Invest. Ophthalmol. Vis. Sci. 201657(12):.
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© ARVO (1962-2015); The Authors (2016-present)
The use of NSAIDS intraocularly remains a difficult task due to the short half-life time in the vitreous cavity.This study evaluates the intravitreal bioavailability and anti-inflammatory effects of sustained release flurbiprofen.
We evaluated a liposomal nanoformulation of flurbiprofen that is being explored in our laboratories. For pharmacokinetics we used two forms of flurbiprofen with concentrations of 7.66mg/ml and 15mg/ml. The kinetics of the slow release flurbiprofen were compared with the flurbiprofen alone. 3 eyes were analyzed per time point with means of HLPC/MS method. For efficacy, 100ng lipopolysaccharide (LPS) of E.coli were injected intravitreally to induce inflammation; the right eyes received 7.66mg/ml free flurbiprofen or 7.66mg/ml slow release flurbiprofen and the left eyes PBS. Clinical signs of inflammation were evaluated after 24h of LPS and aqueous humor was removed to determine the total cell count.
No adverse events were observed concerning the pharmacokinetics of the drug. No signs of inflammation, hemorrhage or detachment were detected. The recovery of the method was 92.6%. The half-life of the slow release flurbiprofen solution of 7.66mg/ml and 15mg/ml was 24.75 hours and 23.90 hours respectively while the half-life of the flurbiprofen alone was 16.12 hours. The elimination constant rate (K) was 0.028, 0.029 and 0.043 respectively. Treatment with free flurbiprofen and slow release flurbiprofen reduced significantly total cell count by 51% and 80.5% respectively. Signs of inflammation were also reduced compared to control eyes.
We managed to extend the presence of the drug into the vitreous cavity. This is crucial for drugs such as the NSAIDs that have a very short intravitreal half-life time. Flurbiprofen demonstrated potent anti-inflammatory effects. However, the need for greater prolongation in the vitreous demands further experimentation with the system’s structure and the substance’s dosage.
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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