Design and Evaluation of Solid Lipid Nanoparticle Eye Drops Containing VRN for Ocular Drug Delivery

Abstract

As a well-known oral and intravenous antifungal, voriconazole (VRN) has an extensive history of usage in the medical field. Solid lipid nanoparticles (SLNs) have been produced to treat ocular fungal keratitis in the eye. A 32Box-behnken design was used to produce a variety of new formulas for hot-melt extrusion. The SLNs were evaluated by entrapment efficiency (EE percent), particle size (PS), polydispersity index (PDI), and zeta potential (ZP). A series of in-vitro and in-vivo studies were carried out on the new formula. The produced vesicles’ EE, PS, PDI, and ZP values were all good. SLNs eye drops were numerically adjusted to include carbopol, a stabilizer, lipids, and a surfactant, among other substances. ZP of -36.5 ± 0.20 mV, 80.9 ± 1.02 % EE, 205 ± 9.1 nm PS, and 0.015 PDI were all included in the data. For example, by differential scanning calorimetry (DSC) and fourier-transform infrared (FTIR), it was discovered that the crystallinity of the drug had been reduced. The in-vitro release study and the SLNs and carbopol-based eye drops prepared with ultrasonication method demonstrated sustained release up to 48 hours. Comparing VRN-SLNs pharmacokinetics to that of pure drug solution, researchers discovered an area under the curve (AUC) and Cmax three times higher and a factor of five times higher, respectively (both P 0.01). By functioning as a carrier, SLNs may increase the bioavailability of VRN in the eye. The in-vivo studies were performed by infecting the rats with candida species. It was observed that VRN-loaded SLNs eye drops were more efficient in treating candidiasis. Results indicate that VRN-loaded SLNs eye drops provide a sustaining VRN topical effect and quick relief from fungal infection.