Abstract

Background: Blepharitis is considered one of the most common ocular surface conditions in optometry and ophthalmology practice. While azithromycin and dexamethasone have been used successfully to treat blepharitis, they are generally formulated as eye drops requiring frequent administration. Ocular inserts based on biodegradable polymers may overcome some of the problems associated with conventional eye drops such as the fast nasolacrimal drainage.

Methods: Inserts with different β-glucan and hydroxypropyl methycellulose (HPMC) compositions were prepared using the solvent-casting method and evaluated in terms of their appearance, thickness, weight, pH, mechanical strength, bioadhesive properties and drug-polymer interactions. The ability of the ocular inserts to provide controlled release of the drugs was assessed through an in vitro release study of dexamethasone and an antibacterial assay for azithromycin.

Results: All parameters were found acceptable for ocular use, with the film laminate exhibiting the highest tensile strength and mucoadhesion. Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared Spectroscopy (FTIR) revealed that the drugs were molecularly dispersed within the polymer films with no obvious interactions. Dexamethasone release was fast with 100% released within 1 hr. Azithromycin also showed a high burst release achieving the minimum inhibitory concentration after only 5 min; however, antibacterial activity was maintained for 24 hrs.

Conclusion: Ocular inserts were successfully prepared and delivered both drugs over prolonged periods compared to conventional eye drops. However, additional coating may be required to further control the drug release.

Keywords: Azithromycin, blepharitis, β-glucan, dexamethasone, hydroxypropyl methycellulose, ocular inserts.

Graphical Abstract