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.
Keywords: Nanosuspensions, flurbiprofen, ocular tolerance, sustained release, draize test.
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