Cyclosporine A Loaded PLGA Nanoparticles for Dry Eye Disease: In Vitro Characterization Studies

Abstract

Dry eye disease is a common disease of the tear film caused by decreased tear production or increased evaporation. The objective of this study was to develop and evaluate poly (dl-lactide-co-glycolide) (PLGA) nanoparticles for CsA (CsA) ophthalmic delivery, for the treatment of dry eye disease. Topical CsA is currently the only and safe pharmacologic treatment of severe dry eye symptoms. Nanoparticles (NPs) were prepared by W/O solvent evaporation technique followed by probe sonicator and characterized for various properties such as particle size, entrapment efficiency, zeta potential, in vitro drug release, in vitro permeation studies by Franz diffusion cells, XRD, DSC, SEM, and stability studies. The developed nanosuspension showed a mean particle size in the range from 128 to 253.50 nm before freeze drying and after freeze drying 145.60 to 260.0 nm. The drug entrapment efficiency was from 58.35 to 95.69% and production yield was found between 52.29±2.4 and 85.30±2.1% in all preparations. The zeta potential of the Eudragit RL containing nanoparticles was positive, that is, 20.3 mV to 34.5 mV. The NPs formulations exhibited a biphasic drug release with initial burst followed by a very slow drug release and total cumulative release up to 24 h ranged from 69.83 to 91.92%. Kinetically, the release profiles of CsA from NPs appeared to fit best with the Higuchi model. The change of surface characteristics of NPs represents a useful approach for improvement of ocular retention and drug availability.