Design, Development and Optimization of Solid Lipid Nanoparticles for Ocular Delivery of an Antifungal Agent

Abstract

Oral and intravenous dosing of the second-generation antifungal drug voriconazole (VCZ), with its wide range of antifungal action, is commercially accessible. Visual and hepatic problems might occur when VCZ is used in large doses. Voriconazole SLNs were prepared in this study with the goal of increasing corneal penetration and drug release. The thin fi lm hydration approach was used to make VCZ SLNs. The central composite experimental design was used to maximize the impacts of independent processing factors on vesicle size (R1), drug entrapment effi ciency (%EE) and zeta potential (ZP; R3) responses on lipid concentration (X1), surfactant concentration (X2), and sonication duration (X3). An evaluation of the drug release profi le, corneal penetration, antifungal susceptibility, and cytotoxicity of the improved formula was conducted. The improved recipe achieved the best results with a ZP of -39.6 ± 0.28 mV, an average particle size of 156 ± 3.84 nm, and an EE% of 89.2 ± 2.01. When compared to the unformulated drug solution, the VCZ-SLNs had a prolonged 10 hours drug release profi le with improved corneal penetration, with Papp and Jss measuring 14.35×10-2 cm h-1 and 4.61 mol h-1, respectively, instead of 7.28×10-2 cm h-1 and 2.48 mol h-1. Non-irritating VCZ-SLNs were determined to be corneal tissue, according to the study. Improved corneal penetration and higher antifungal activity without harmful eff ects on ocular tissues were achieved by VCZ-SLNs