Development, characterization, and molecular dynamics simulation of resveratrol-loaded nanostructured lipid carriers for enhanced anti-oxidant and antityrosinase activity

Objective(s): This study aimed to develop and characterize resveratrol-loaded nanostructured lipid carriers (Res-NLCs) to assess their preliminary potential as topical delivery systems, with a focus on antioxidant and antityrosinase properties.Materials and Methods: Ten Res-NLC formulations (F۱–F۱۰) were prepared by high-shear homogenization combined with ultrasound. The formulations underwent comprehensive evaluation of morphology, particle size, long-term stability, and entrapment efficiency (EE%). Experimental findings were correlated with molecular dynamics (MD) simulations. In vitro performance was assessed by drug-release profiling (dialysis-bag diffusion), cytotoxicity and protective effects (MTT assay), reactive oxygen species (ROS) reduction (DCFH-DA), and anti-tyrosinase activity (L-DOPA assay).Results: Formulation F۱۰ exhibited excellent surface characteristics, including a z-average particle size of ۱۴۴.۰ nm, a narrow polydispersity index (PDI) of ۰.۱۱۷, a high negative zeta potential of -۲۲.۶ mV, favorable stability at lower temperatures, and optimal EE%. MD simulations confirmed superior molecular stability for F۱۰ through compact cluster formation, consistent with its sustained long-term stability at ۴ °C and ۲۵ °C. In contrast, structural fragmentation observed in F۲ accounted for its large particle size (>۵۰۰ nm). The NLC systems exhibited a sustained-release profile, delivering ۸۴% of the resveratrol over ۴۸ hr. Furthermore, F۱۰ significantly inhibited tyrosinase activity and effectively reduced intracellular ROS levels following hydrogen peroxide-induced stress.Conclusion: The newly developed Res-NLC (F۱۰) formulation serves as a promising, stable carrier for the sustained topical delivery of resveratrol, demonstrating notable antioxidant and antityrosinase performance, which warrants subsequent biological validation.

کلیدواژه ها:

Anti-oxidant ، nanostructured lipid carriers ، Resveratrol ، Reactive oxygen species inhibition ، Tyrosinase inhibitor