Design and Ocular Tolerance of Flurbiprofen Loaded Nanosuspension

Background: Nanosuspension applicability in ocular drug delivery. Objective: Development of efficient nano-based ocular delivery is a major challenge. The purpose of this work was to design and evaluate the sustained release flurbiprofen (FB) loaded nanosuspensions for improving the drug availability at the corneal surface. Methods: Polymeric nanosuspensions were prepared by solvent displacement method using process variables such as drug to polymer ratio and solvent to non solvent ratio and their influence on particle size, polydispersity index, zeta potential, entrapment efficiency, in vitro release and ocular tolerance was investigated. Results: The prepared nanoparticles were predominantly spherical in shape having average particle diameter ranging from 107.7±3.8 to 245.0±4.6 nm, with positive zeta potential values from +6.6±2.2 to +19.0±3.1 mV and entrapment efficiency values from 54.67±3.4 to 90.32±3.2%. Drug release from optimized nanosuspension was sustained with approximately 60 % over 12 hrs period, when compared with marketed formulation, Flur eye drops. The release profile of nanoparticles followed zero-order release kinetics. Stability studies revealed that there were no significant change in particle size, entrapment efficiency and drug release even after 6 months storage. In vivo experiments showed that, topical instillation of prepared nanosuspension to rabbit’s eye found to be non-irritant by Draize’s test and also considered safe by hispathological study. Conclusion: The above results clearly indicated Eudragit RL 100 loaded FB nanosupension was found to be stable, sustained its drug release and suitability for ocular application.