Chitosan Nanoparticles for Meloxicam Ocular Delivery: Development, In Vitro Characterization, and In Vivo Evaluation in a Rabbit Eye Model
Eye inflammation is considered one of the most common co-morbidities associated with
ocular disorders and surgeries. Conventional management of this condition with non-steroidal antiinflammatory
drugs as eye drops is associated with low corneal bioavailability and ocular irritancy.
In the current study, we first investigated the capacity of different solvent systems to enhance the
solubility of Meloxicam (MLX). Then, we prepared chitosan nanoparticles loaded with meloxicam
(MLX-CS-NPs) through electrostatic interaction between the cationic chitosan and the anionic MLX
using either 100% v/v polyethylene glycol 400 or 0.25% w/v tripolyphosphate solution as solvents
based on the MLX solubility data. In further studies, MLX-CS-NPs were characterized in vitro and
assessed for their ex vivo corneal and scleral permeability. The morphology, average particle size
(195–597 nm), zeta potential (25–54 mV), and percent entrapment efficiencies (70–96%) of the prepared
MLX-CS-NPs were evaluated. The in vitro release study of MLX from the selected MLX-CS-NPs
showed a sustained drug release for 72 h with accepted flux and permeation through the cornea
and sclera of rabbits. In the in vivo studies, MLX-CS-NPs eye drop dispersion showed enhanced
anti-inflammatory activity and no ocular irritancy compared to MLX-eye drop solution. Our findings
suggest the potential for using chitosan nanotechnology for ocular delivery of MLX with high contact
time and activity.
