Formulation and Evaluation of Econazole loaded Solid Lipid Nanoparticles based Ocular Film for Treatment of Fungal Infection

Abstract

This study evaluated the viability of using solid lipid nanoparticles for the ocular delivery of Econazole, adopting stearic acid as lipidic material, tween 80 as a stabilizer, and carbopol 934 as a controlled release agent and for increasing the precorneal residence time in the eye. The systems were prepared using two different methods, that is, the ultrasonication method and the microemulsion technique. The results showed that the larger particle size of SLNs was found with the microemulsion technique (309 ± 3.53 nm to 344 ± 3.52) compared to SLN prepared with the ultrasonication method (235 ± 3.53 nm to 289 ± 4.59 nm). All of the formulations had polydispersity index values less than 0.3, and the formulations made using these two procedures had zeta potentials ranging from -23.72 ± 0.64 mV to -29.87 ± 0.59 mV. The drug's crystallinity decreased, as shown by differential scanning calorimetry and powder X-ray diffraction. The SLN formulations made using the ultrasonication method and the in vitro release research both showed sustained release for a maximum of 12 hours. This investigation showed that, without significantly altering the amount of corneal moisture, SLN prepared using the ultrasonication method is more appropriate than that made using the microemulsion approach. The goal of the solid lipid nanoparticle-loaded ocular film of Econazole, an antifungal medication used to treat fungal keratitis, was to improve patient compliance by reducing the need for repeated dosage, lengthening the retention period, and providing sustained release. Using the retarding polymers chitosan, PVA, and ethyl cellulose, the optimal solid dispersion formulation was first created by the solvent evaporation method and then added to films made by the solvent casting method. Plasticizer PEG-400 was utilized. The films were assessed for antimicrobial activity, in-vitro and ex-vivo permeation investigations, thickness, surface pH, drug content, weight uniformity, tensile strength, and in-vitro antifungal research. The films were within an acceptable range and showed good mechanical properties with promising results. In vitro tests using the improved formulation F6 demonstrate more drug release than in vivo experiments. This results from disruption of other tissues and the cornea's variable pore size. The developed formulation proved not to irritate the eyes, according to an ocular irritation test. Therefore, it appears that the ophthalmic film formulation holds promise for the safe and efficient administration of Econazole via the ocular route in the management of fungal keratitis.