Effects of Quercetin-Loaded Nanoparticles on MCF-7 Human Breast Cancer Cells

Abstract

: Background and objectives: Previous studies have shown anti-tumor activity of quercetin (QT). However, the low bioavailability of QT has restricted its use. This study aimed to assess the toxic effect of QT encapsulated in solid lipid nanoparticles (QT-SLNs) on the growth of MCF-7 human breast cancer cells. Materials and Methods: MCF-7 and MCF-10A (non-tumorigenic cell line) cell lines treated with 25 µmol/mL of QT or QT-SLNs for 48 h. Cell viability, colony formation, oxidative stress, and apoptosis were evaluated to determine the toxic effects of the QT-SLNs. Results: The QT-SLNs with appropriate characteristics (particle size of 85.5 nm, a zeta potential of −22.5 and encapsulation efficiency of 97.6%) were prepared. The QT-SLNs showed sustained QT release until 48 h. Cytotoxicity assessments indicated that QT-SLNs inhibited MCF-7 cells growth with a low IC50 (50% inhibitory concentration) value, compared to the free QT. QT-SLNs induced a significant decrease in the viability and proliferation of MCF-7 cells, compared to the free QT. QT-SLN significantly increased reactive oxygen species (ROS) level and MDA contents and significantly decreased antioxidant enzyme activity in the MCF-7 cells. Following QT-SLNs treatment, the expression of the Bcl-2 protein significantly decreased, whereas Bx expression showed a significant increase in comparison with free QT-treated cells. Furthermore, The QT-SLNs significantly increased apoptotic and necrotic indexes in MCF-7 cells. Viability, proliferation, oxidative stress and apoptosis of MCF-10A cells were not affected by QT or QT-SLNs. Conclusion: According to the results of this study, SLN significantly enhanced the toxic effect of QT against human breast cancer cells.

Antitumor Effects of Quercetin in Hepatocarcinoma In Vitro and In Vivo Models: A Systematic Review

“…In the present work, six studies evaluated different nanoparticles and demonstrated higher cytotoxic effects of quercetin in both in vitro and in vivo HCC models [39][40][41][42][43][44]. This strategy has been recently arisen and numerous investigations have proved greater quercetin activities in other tumors than HCC, for example breast [75] and colon cancer [76], as well as with other compounds, such as doxorubicin and paclitaxel [77] in tumor hepatocytes. Within the included articles, some of them studied not only cytotoxicity of encapsulated quercetin but also its modulating effects on cancer-related processes and signaling pathways [42,43], providing greater information about quercetin properties.…”

Anticancer, Antioxidant and Antiangiogenic Activities of Nanoparticles of Bioactive Dietary Nutraceuticals

“…Recently, nutraceuticals have shown good cytotoxicity and selectivity in inhibition of various cancer cells in both in vitro assays and in vivo experiments . In view of this, NPs of 1–6 and corresponding bulk compounds were screened for their anticancer activity against hormone dependent human breast adenocarcinoma cell line MCF‐7 employing sulforhodamine B (SRB) assay method .…”

Berries polyphenols: Nano-delivery systems to improve their potential in cancer therapy

“…Both nano-delivery systems showed a sustained release pattern [15,32], and augmented QUE solubility up to ∼1000 folds [15]. QUE-NLC also decreased the colony formation capacity and the antioxidant enzyme activity, while increased ROS levels and malondialdehyde (MDA) content in MCF-7 cells [33].…”

“…However, therapeutic use of this flavonols is limited by its very low solubility in the upper GT [3,15,[32][33][34], intestinal permeability [3] and high instability [3,15]. In that sense, the recent use of nano-delivery systems has proven to be effective in increasing QUE bioavailability and efficacy.…”

“…In MCF-7 [15,33] and MDA-MB-231 [15] breast cancer cells, the use of biocompatible and biodegradable QUE-nanostructured lipid carriers (QUE-NLC) [15,33] or mixed polymeric micelles containing QUE (QUE-MPM) [32] increased cytotoxicity and induced apoptosis in a dose-dependent manner. These effects were correlated not only to an augmentation of Bax protein expression along with a diminution of Bcl-2 expression, but also to a better QUE uptake by the tumor cells [33]. Both nano-delivery systems showed a sustained release pattern [15,32], and augmented QUE solubility up to ∼1000 folds [15].…”