DESIGN, OPTIMIZATION AND CHARACTERIZATION OF ITRACONAZOLE LOADED SELF-NANOEMULSIFYING SYSTEM FOR THE OPHTHALMIC DELIVERY

Abstract

The triazole medication is an active medicinal ingredient that is highly effective against the dermatophyte, Candida, and Aspergillus species. Being a BCS II medication, responsible for most of its poor bioavailability in ocular region. The present study focuses on the development of a self-nanoemulsifying drug delivery system (SNEDDS) designed to improve the solubility and ophthalmic bioavailability of itraconazole. Screening of appropriate oils, surfactants, and co-surfactants was carried out through solubility profiling. A water dilution method was applied to evaluate emulsification capacity. The formulation was optimized using a 3² factorial design. The optimized batch demonstrated a droplet size of 60.6 nm, PDI of 0.46, and zeta potential of -11.2 mV. Drug content was found to be 93.25%. In vitro drug release followed anomalous transport with an 'n' value ≥0.85, indicating release pattern was controlled by a combined interaction of diffusion and polymer swelling mechanisms. An antifungal assay revealed significantly enhanced inhibition of Candida albicans growth by the optimized SNEDDS. In comparison to its marketed eye drop (ITRAL 1% w/v), an improved property of Itraconazole loaded self-nanoemulsifying system was noticed, and in vitro data suggest it is an alternative to eye drop. Assessment of different parameters -: such as minimal droplet size, optimal surfactant concentration, desired viscosity, excellent in vitro drug release, shorter self-emulsification time, and appropriate drug content -: revealed that the optimized batch was the most suitable formulation for further in vivo and ex vivo studies to establish its potential as an effective and efficient ophthalmic delivery system.