Cyclodextrin-enabled nepafenac eye drops with improved absorption open a new therapeutic window

Nepafenac is a highly effective NSAID used for treating postoperative ocular inflammation and pain after cataract surgery and its advantage over conventional topical NSAIDs has been proved many times. However, Nevanac® is a suspension eye drop, which clearly lacks patient compliance causing irritation, blurred vision, foreign body sensation along with problematic dosage due to its sticky, inhomogeneous consistence. In this study, nepafenac containing eye drops were prepared using hydroxypropyl-β-cyclodextrin to ensure complete dissolution of nepafenac, sodium hyaluronate to provide mucoadhesion and adequate viscosity and a preservative-free officinal formula, Oculogutta Carbomerae containing carbomer (just like Nevanac®), therefore providing a similar base for the new formulations.

According to an experimental design, 11 formulations were tested in vitro including two reference formulations by measuring their viscosity, mucoadhesion, drug release and corneal permeability. Finally, two formulations were found promising and investigated further on porcine eyes ex vivo and corneal distribution of nepafenac was determined by RAMAN mapping. The results showed that one formulation possessed better bioavailability ex vivo than Nevanac® 0.1 % suspension, while the other formulation containing only 60 % of the original dose were ex vivo equivalent with Nevanac® opening the way to nepafenac-containing eye drops with better patient compliance in the future.

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Anna Vincze, Réka Facskó, Mária Budai-Szűcs, Gábor Katona, Benjámin Gyarmati, Anita Csorba, Romána Zelkó, Zoltán Zsolt Nagy, Lajos Szente, György T. Balogh, Cyclodextrin-enabled nepafenac eye drops with improved absorption open a new therapeutic window, Carbohydrate Polymers, Volume 310, 2023, 120717, ISSN 0144-8617, https://doi.org/10.1016/j.carbpol.2023.120717.