Posaconazole loaded ocular inserts for antifungal activity

Abstract

Corneal and conjunctival infections are common ocular diseases; however, sometimes lead to blindness when neglected. Despite most of the ocular drug delivery systems are in eye drop form, they suffer from poor retention on the ocular surface and low ocular bioavailability leading to unsatisfactory results even with repeated treatment. Therefore, there is a need for more effective drug delivery systems for the ocular application. The present study was carried out to demonstrate that ocular inserts effectively delivers a significant concentration of drug with topical administration for the treatment of fungal infections with the help of extended residence time on the ocular surface. Chitosan-based inserts were prepared by the freeze-drying method. The prepared inserts were evaluated for various parameters. Layered structures were revealed with scanning electron microscopy analyses. Thermal and structural behaviors were analyzed by differential scanning calorimetry and Fourier-transform infrared spectroscopy with nuclear magnetic resonance analyses, respectively. Drug contents were evaluated by a validated HPLC method. In vitro release studies were also performed in simulated tear fluid at 34±1°C for 48 hours. Analyses results revealed that chitosan-based ocular inserts were suitable systems for posaconazole delivery for the treatment of severe ocular fungal infections.