Journal of Drug Delivery Science and Technology, cilt.92, 2024 (SCI-Expanded)
As a bioactive flavonoid in Citrus seeds, hesperidin exerts significant antioxidant, free radical scavenging, and anticancer activity with limited bioavailability. To enhance the stability and improve the bioactive potential of hesperidin, an electrospun nanofiber formulation was developed. Electrospinning solution was characterized by surface tension, viscosity, and conductivity measurements, and these values were found to be 25.18 ± 0.04 mN/m 145 ± 2 cPs and 9.0 ± 0.4 μS/cm, respectively. Electrospun hesperidin nanofiber was tested in a coincubation with the cytotoxic agent sodium fluoride (NaF) in Caco-2 cells. Inhibitory concentration-50 (IC50) values of hesperidin nanofiber in Caco-2 cells alone were as low as 30 μM, indicating its potential anticancer effect, while coincubation with 10 and 20 μM of hesperidin nanofibers was found to alleviate the cytotoxic effect induced by NaF at 2.1, 1.05 and 0.525 mM concentrations. This effect was in accordance with cellular antioxidant mechanisms; where malondialdehyde (MDA) levels at 10 μM hesperidin nanofiber were found to be decreased by 55.60% in the thiobarbituric acid reactive substances (TBARS) assay, and the mRNA expression of Thioredoxin1 (TRX1) and Superoxide dismutase-1 (SOD1) were decreased in qPCR. The results revealed that electrospun nanofiber of hesperidin was developed for the first time with useful implications against cellular toxicity by alleviating the cellular antioxidant defense mechanisms, including MDA, SOD1, and TRX1.