Polymeric Inserts Containing Eudragit^® L100 Nanoparticle for Improved Ocular Delivery of Azithromycin

Area of Science:

• Ophthalmology
• Nanotechnology
• Materials Science

Background:

• Ocular drug delivery faces challenges like rapid clearance and poor bioavailability.
• Sustained release systems are needed to improve therapeutic efficacy and patient compliance for ocular infections.

Purpose of the Study:

• To develop and characterize azithromycin-loaded Eudragit L100 nanoparticles for enhanced ocular delivery.
• To formulate mucoadhesive ocular inserts using these nanoparticles for sustained drug release and improved ocular performance.

Main Methods:

• Nanoparticles were prepared using the solvent diffusion technique.
• Azithromycin ocular inserts were fabricated via solvent casting incorporating nanoparticles into polyvinyl alcohol solutions with cellulose derivatives.
• Nanoparticles and inserts were characterized for particle size, zeta potential, entrapment efficiency, and drug release kinetics.

Main Results:

• Optimized nanoparticles exhibited a size of 78.06 nm, zeta potential of -2.45 mV, and 62.17% entrapment efficiency.
• The prepared inserts demonstrated antibacterial activity against Staphylococcus aureus and Escherichia coli.
• Ex-vivo studies showed enhanced corneal permeation and in-vivo studies in rabbit eyes revealed a prolonged release of azithromycin for up to 121 hours.

Conclusions:

• Mucoadhesive ocular inserts containing azithromycin-loaded Eudragit L100 nanoparticles provide a promising sustained drug delivery system.
• This approach enhances ocular bioavailability and offers a potential new treatment strategy for bacterial ocular infections requiring prolonged drug exposure.