Formulation Development, Optimization, and In Vitro–In Vivo Characterization of Natamycin-Loaded PEGylated Nano-Lipid Carriers for Ocular Applications

Abstract Current study aimed at formulating and optimizing natamycin (NT) loaded PEGylated NLCs (NT-PEG-NLCs) using Box-Behnken Design and investigating their potential in ocular applications. Response surface methodology (RSM) computations and plots for optimization were performed using Design Expert ® software, to obtain optimum values for response variables based on the criteria of desirability. Optimized NT-PEG-NLCs had predicted values for the dependent variables not significantly different from the experimental values. NT-PEG-NLCs were characterized for their physicochemical parameters; NT's rate of permeation and flux across rabbit cornea was evaluated, in vitro ; ocular tissue distribution was assessed in rabbits, in vivo . NT-PEG-NLCs were found to have optimum particle size ( In vitro transcorneal permeability and flux of NT from NT-PEG-NLCs was significantly higher than Natacyn ® . NT-PEG-NLC (0.3%) showed improved delivery of NT across the intact cornea and provided concentrations statistically similar to the marketed suspension (5%) in inner ocular tissues, in vivo , indicating that it could be a potential alternative to the conventional suspension during the course of fungal keratitis therapy.