Nanoparticle-based topical ophthalmic formulations for sustained celecoxib release

Area of Science:

• Ophthalmic Drug Delivery
• Nanotechnology in Pharmaceuticals
• Biomaterials Science

Background:

• Ophthalmic drug delivery faces challenges with poor bioavailability and frequent administration.
• Biodegradable polymers offer potential for sustained drug release and improved ocular drug targeting.
• Celecoxib is a non-steroidal anti-inflammatory drug with potential applications in treating ocular inflammatory conditions.

Purpose of the Study:

• To develop and characterize celecoxib-loaded nanoparticles (NPs) using biodegradable polymers for ophthalmic applications.
• To evaluate the suitability of these NPs when incorporated into various ophthalmic formulations like eye drops and gels.
• To assess the safety and release kinetics of the developed drug delivery systems.

Main Methods:

• Celecoxib-loaded NPs were prepared using poly-ε-caprolactone (PCL), poly(L-lactide) (PLA), and poly(D,L-lactide-co-glycolide) (PLGA) via spontaneous emulsification solvent diffusion.
• Nanoparticles were characterized for size, PDI, zeta potential, morphology (TEM), and drug content.
• Formulations (eye drops, in situ gelling system, gel) containing NPs were assessed for pH, viscosity, drug uniformity, in vitro release, and cytotoxicity.

Main Results:

• Optimized NPs exhibited favorable characteristics: PCL NPs (119 nm, -22.43 mV), PLGA NPs (126.67 nm, -25.46 mV), PLA NPs (135.33 nm, -31.81 mV) with high encapsulation efficiencies (up to 93.44%).
• TEM confirmed spherical NPs with a dense core and distinct coat.
• Formulations showed good ocular compatibility (pH, viscosity), sustained drug release via Higuchi non-fickian diffusion, and were found to be non-toxic.
• The methodology allows tuning of NP size and zeta potential for specific needs.

Conclusions:

• Biodegradable polymer-based celecoxib-loaded NPs are successfully prepared and formulated for ophthalmic use.
• These NP formulations offer sustained release, good ocular compatibility, and are non-toxic.
• The scalable and robust methodologies provide flexibility, positioning these formulations as promising drug delivery systems for anterior and posterior eye diseases.