Preparation and in vitro evaluation of quercetin cyclodextrin nanoparticles

Quercetin (Qu), a polyphenolic flavonoid, is one of the most effective plant originated antioxidants. Despite the potential use of Qu in clinical trials, low water solubility, stability problems and the scarcity of cellular bioavailability limit its applications. The purpose of thesis study was to enhance aqueous solubility, dissolution rate, antioxidant and anticancer activity of Qu by complexation with Methyl-- cyclodextrin (M--CD). Complexes were prepared by freeze-drying and evaporation method. The characteristics of the complexes were evaluated by DSC, XRD, 1H-NMR, FT-IR, SEM, encapsulation efficacy, in-vitro dissolution rate analyses. Antioxidant activity studies on complexes carried out with DPPH tests. Cytotoxicity assay of the complexes was performed by cervical adenocarcinoma cell line (HeLa) and ovary carcinoma cell line (SKOV-3). Hoechst staining and flow cytometry analysis were performed by HeLa cells line. Analyses results showed that the aqueous solubility, dissolution rate and antioxidant activity of the complex were increased 254-fold, ~3-fold and 10 % respectively compared to the pure Qu. Cytotoxic point of view, it was determined to vary the prepared formulations according to the type of cell line. Although the formulation of L3 showed high cytotoxic effects at low concentrations according to other formulations by HeLa cell line, it was found to be cytotoxic L4 formulations by SKOV-3 cell line. The results of the analysis obtained were analysed statistically and the meaningfulness was found according to each other and duration. L3 formulation stability was found to be stable at different storage conditions during the three months of storage.