Quercetin Loaded Nanoparticles for the Treatment of Dry Eye Disease

Dry eye disease (DED) is a common condition that affects the eye\u27s anterior surface due to tear deficiency or excessive evaporation. The lack of tears leads to dryness and initiation of an inflammatory response which can irritate the eye and interfere with daily activities. Current treatment depends mainly on artificial tears eye drops which offer temporary relief and require repetitive administration due to frequent blinking. Prescription medications are also available but need around three months to relieve dry eye symptoms. Quercetin is a flavonoid that has an anti-inflammatory and antioxidant effect. However, it suffers from low water solubility and low bioavailability, which prevent its effectiveness when administrated topically to the eye. Therefore, it is crucial to improve quercetin solubility to use it for ocular drug delivery. In this study, quercetin-loaded chitosan nanoparticles were successfully prepared using the ionic gelation method. The QCNPs had a size of 248 ± 8.43 nm, PDI of 0.244 ± 0.23, and zeta potential of 25.5 ± 1.15 mV. TEM images of QCNPs showed particle size ranging from 178 nm to 378 nm. The entrapment efficiency (%EE) of the optimized formulation was 83% ± 2.54. The in vitro drug release of quercetin from the QCNPs showed a sustained release effect compared to quercetin solution, which reduces the need for frequent ocular administration. Cytotoxicity of QCNPs performed using rabbit corneal cell line (SIRC) showed that the nanoparticles were 66% and 78% less toxic than the drug solution after 24 and 48 hours of treatment, respectively. Also, the QCNPs were uptake by SIRC cells in a time-dependent manner. IL-6 ELISA assay showed that QCNPs could decrease IL-6 expression by 36.2% after 48 hours of treatment compared to the positive control. Therefore, the prepared QCNPs can be an alternative potential treatment for DED