Abstract

Dry eye syndrome poses a therapeutic challenge due to the limited residence time of traditional treatments on the ocular surface. The commercially available rebamipide (REB) ophthalmic suspension, though approved for clinical use in dry eye patients, suffers from rapid drainage through the nasolacrimal duct, limiting its effectiveness. In this study, rebamipide nanosuspension was successfully developed by solvent-diffusion methodology and investigated for measurement of particle size, shape, surface charge, fourier-transform infrared (FTIR), differential scanning calorimetry (DSC), percentage entrapment efficiency, dissolution studies and release kinetics, ex-vivo permeability study. Results demonstrate that the optimized formulation has 196 nm particle size, surface charge of +32.5 mV, and low polydispersity. FTIR studies revealed that the drug exhibits compatibility with the excipients integrated into the formulation. DSC and X-ray diffraction (XRD) analysis revealed a decrease in the crystalline nature of the drug. Transmission electron microscope (TEM) findings indicate that rebamipide nanosuspension possesses a spherical shape, and in-vitro studies demonstrate a slower and sustained release of REB. Ex-vivo studies performed on excised goat corneas demonstrated significantly improved drug permeation compared to the suspension without inducing corneal damage.

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