Chitosan Nanoparticles for Meloxicam Ocular Delivery: Development, In Vitro Characterization, and In Vivo Evaluation in a Rabbit Eye Model

Abstract

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 anti-inflammatory 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.

Chitosan Encapsulated Meloxicam Nanoparticles for Sustained Drug Delivery Applications: Preparation, Characterization, and Pharmacokinetics in Wistar Rats

“…The hydrodynamic diameter of the CEMNPs was measured in 0.1% carboxymethyl cellulose (CMC), which yielded 138.5 nm ( Figure 3 a). The previous studies with chitosan nanoparticles reported the size range of 90–690 nm [ 33 , 36 , 37 , 38 ].…”

“…Due to the presence of free amine groups on the polymer, the positive zeta potential value of CEMNPs shows that the nanoparticle surface has positively charged [ 41 , 42 ]. In the previous studies, the zeta potential for chitosan nanoparticles was reported as positively charged [ 33 , 36 , 37 , 38 ].…”

“…Chitosan-based nanomaterials exhibit superior drug absorption due to their GI luminal protection, mucoadhesive nature, permeability enhancement, controlled drug release, and efflux inhibition [ 30 ]. In recent times, few attempts have been made to synthesize MLX nanoparticles for effective delivery [ 17 , 18 , 32 , 33 ]. After a thorough review of the literature, and with the available information regarding chitosan-encapsulated meloxicam nanoparticles, the current investigation was carried out to explore the beneficial effects of chitosan-encapsulated meloxicam nanoparticles with respect to their pharmacokinetic behavior in male Wistar rats.…”

In Vitro Preparation and Evaluation of Chitosan/Pluronic F-127 Hydrogel as a Local Delivery of Crude Extract of Phycocyanin for Treating Gingivitis

“…The chitosan/pluronic F-127 hydrogel was spontaneously formed when pluronic F-127 was added to the chitosan solution. Pluronic F -127 acted as a nontoxic cross-linker between chitosan cationic polymers using an electrostatic interaction between different polar of those polymers (Mohamed et al, 2022). Our finding has shown that over 15% (w/v) of pluronic F -127 in the mixture could form the hydrogel.…”

Ciprofloxacin-Loaded Zein/Hyaluronic Acid Nanoparticles for Ocular Mucosa Delivery

“…Ocular drug delivery is challenging due to physiological barriers, limitations associated with conventional ocular therapy (i.e., blurred vision and frequent administration), and NPs’ properties, such as Dh, charge, and hydrophilicity. It is extremely important to overcome the challenges mentioned above [ 59 , 60 , 61 ]. The Dh of the fresh NPs suffered a significant increase upon the encapsulation of CPX from 86 ± 14 nm to 109 ± 10.2 nm, as shown in Figure 4 .…”