Amphotericin-B entrapped lecithin/chitosan nanoparticles for prolonged ocular application

Area of Science:

• Ophthalmology
• Nanotechnology
• Mycology

Background:

• Fungal keratitis is a leading cause of global vision loss.
• Amphotericin-B is the preferred antifungal but faces challenges in ophthalmic delivery due to rapid clearance.
• Blinking, tear turnover, and drainage limit drug residence time on the ocular surface.

Purpose of the Study:

• To develop Amphotericin-B loaded lecithin/chitosan nanoparticles for sustained ocular drug delivery.
• To evaluate the physicochemical properties, antifungal efficacy, and in-vivo performance of these nanoparticles.

Main Methods:

• Preparation and characterization of Amphotericin-B loaded lecithin/chitosan nanoparticles (size, entrapment efficiency, drug loading, zeta potential).
• Antifungal susceptibility testing against Candida albicans and Aspergillus fumigatus.
• In-vivo pharmacokinetic studies in rabbit eyes to assess bioavailability and precorneal residence time.

Main Results:

• Nanoparticles ranged from 161.9-230.5 nm with 70-75% entrapment efficiency and 5.71% drug loading.
• Positive zeta potential (26.6-38.3 mV) indicated stability.
• Nanoparticles demonstrated superior antifungal activity and mucoadhesion compared to the marketed formulation.
• In-vivo studies showed a ~2.04-fold increase in bioavailability and a ~3.36-fold increase in precorneal residence time.

Conclusions:

• Lecithin/chitosan nanoparticles effectively encapsulate Amphotericin-B for ophthalmic use.
• The developed nanoparticles improve drug bioavailability and residence time, offering a superior alternative for fungal keratitis treatment.
• This formulation holds potential for enhanced management of fungal eye infections.