Flurbiprofen loaded biodegradable nanoparticles for ophtalmic administration

Area of Science:

• Materials Science
• Pharmaceutical Sciences
• Ophthalmology

Background:

• Ocular inflammation following surgery poses a significant clinical challenge.
• Effective drug delivery systems are crucial for improving therapeutic outcomes in ophthalmic treatments.
• Flurbiprofen (FB) is a non-steroidal anti-inflammatory drug with potential for ocular applications.

Purpose of the Study:

• To develop and characterize poly(lactic/glycolic) acid nanoparticles (NPs) encapsulating flurbiprofen (FB).
• To optimize NP formulation for enhanced drug availability and efficacy in preventing post-surgical ocular inflammation.
• To evaluate the physicochemical properties, in vitro release, ocular toxicity, and in vivo anti-inflammatory activity of FB-loaded NPs.

Main Methods:

• Solvent displacement technique using poloxamer 188 as a stabilizer.
• A 2(3) + star experimental design to optimize formulation parameters (pH, stabilizer concentration, drug concentration).
• Physicochemical characterization (particle size, zeta potential, drug loading efficiency), in vitro drug release studies, ocular toxicity tests, and in vivo anti-inflammatory assessment in rabbits.

Main Results:

• Optimized NPs prepared at pH 3.5 with 1.5 mg/mL FB and 10 or 20 mg/mL poloxamer 188 showed particle sizes of 232.8 nm and 277.6 nm, respectively.
• High entrapment efficiencies (94.60% and 93.55%) were achieved.
• Complete, biphasic release of FB from NPs was observed. Formulations were non-toxic to ocular tissues.
• Significant reduction in sodium arachidonate-induced ocular inflammation in rabbits was demonstrated by NP formulations.

Conclusions:

• Poly(lactic/glycolic) acid nanoparticles effectively encapsulate flurbiprofen for ophthalmic use.
• Optimized FB-loaded NPs exhibit favorable physicochemical properties, good entrapment, and controlled release.
• The developed nanoparticles demonstrate promising in vivo anti-inflammatory efficacy and ocular safety, suggesting potential for managing post-surgical ocular inflammation.