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Abstract

Quercetin a natural flavonoid has been extensively investigated for its anti-cancer activity. However, the major disadvantage remained its poor aqueous solubility. In the present research, we investigated the efficacy of folate conjugated quercetin nanoparticles in vitro and further formulated its lotion and studied its skin permeation ability with in vivo activity. The in vitro cellular uptake and antiproliferative potentials of folate conjugated quercetin nanoparticles was evaluated using HaCaT, KB and A431 cell lines. The results showed robust cellular uptake of folate conjugated quercetin nanoparticles by cell lines. ROS study and intracellular GSH study revealed that folate conjugated QuNPs remarkably reduces the intracellular reactive oxygen species generation and release of GSH. Cells viability studies showed that folate conjugated quercetin nanoparticles were found to exert profound effect at a concentration of 20 μM on all three cell lines as compared to non-conjugated quercetin nanoparticles, in a shorter span of time. The skin permeability of the formulation was compared with the marketed drug and was estimated by CLSM study. In vivo studies supported the in vitro activity of folate conjugated quercetin nanoparticles by reducing the epidermal hyperplasia, inflammation and lesion formations.

Keywords: HaCaT cell lines; KB-cell lines; A431 cell lines; Reactive oxygen species; Intracellular GSH; CLSM