Development, Optimization and Characterization of Ocular Nanoemulsion of an Antifungal Agent using Design of Experiments

Abstract

Antifungal agents of the echinocandin family act on the fungal cell wall by inhibition of synthesis of β (1, 3)-D-glucan. Currently no market formulation is available for ocular delivery of new antifungal agents from the echinocandin family. Further, currently available eye drops in market have the limitations due to high lacrimal drainage and low corneal permeability. The aim of the present work is to optimize and characterize nanoemulsion of an antifungal agent form echinocandin family for ocular delivery. Nanoemulsion was prepared using high shear homogenization followed by high pressure homogenizer. Solubility studies were carried out to identify suitable oil and surfactant. A three level three factor Box-Behnken design was used to optimize nanoemulsion. Prepared formulation was characterized for globule size, zeta potential, polydispersity index and in vitro drug release study by dialysis method using bottle apparatus. Eye irritation study was carried out by Hen’s egg chorioallantoic Membrane test. Stability study of the prepared formulation was performed as per ICH guidelines. Prepared nanoemulsion is transparent with a blue tinge. Optimized batch of nanoemulsion showed average globule size of 108.5 nm with a polydispersity index of 0.108. The results of in vitro drug release study suggest more than 90% drug release over a period of 24 h. Developed formulation was found to be non-irritant and stable when stored at 40°C and can be used for ophthalmic delivery.