Quercetin-loaded solid lipid nanoparticles exhibit antitumor activity and suppress the proliferation of triple-negative MDA-MB 231 breast cancer cells: implications for invasive breast cancer treatment

Mol Biol Rep. 2023 Nov;50(11):9417-9430. doi: 10.1007/s11033-023-08848-w. Epub 2023 Oct 13.

Abstract

Background: Quercetin (QC) is a naturally occurring flavonoid found in abundance in fruits and vegetables. Its anti-cancer and anti-inflammatory properties have been previously demonstrated, but its low bioavailability hampers its clinical use. Triple-negative breast cancer is a subtype of breast cancer with a poor response to chemotherapy. This study investigates the anti-cancer effects of quercetin-solid lipid nanoparticles (QC-SLN) on the triple-negative breast cancer cell line MDA-MB231.

Materials and methods: MCF-7 and MDA-MB231 cells were treated with 18.9 µM of QC and QC-SLN for 48 h. Cell viability, apoptosis, colony formation assay, and the anti-angiogenic effects of the treatment were evaluated.

Results: QC-SLN displayed optimal properties (particle size of 154 nm, zeta potential of -27.7 mV, encapsulation efficiency of 99.6%, and drug loading of 1.81%) and exhibited sustained release of QC over 72 h. Compared to the QC group, the QC-SLN group showed a significant decrease in cell viability, colony formation, angiogenesis, and a substantial increase in apoptosis through the modulation of Bax and Bcl-2 at both gene and protein levels. The augmentation in the proportion of cleaved-to-pro caspases 3 and 9, as well as poly (ADP-ribose) polymerase (PARP), under the influence of QC-SLN, was conspicuously observed in both cancer cell lines.

Conclusions: This study showcases quercetin-solid lipid nanoparticles (QC-SLN) as a promising therapy for triple-negative breast cancer. The optimized QC-SLN formulation improved physicochemical properties and sustained quercetin release, resulting in reduced cell viability, colony formation, angiogenesis, and increased apoptosis in the MDA-MB231 cell line. These effects were driven by modulating Bax and Bcl-2 expression, activating caspases 3 and 9, and poly (ADP-ribose) polymerase (PARP). Further in vivo studies are needed to confirm QC-SLN's efficacy and safety.

Keywords: Apoptosis; Breast cancer; Invasive; Quercetin; Solid lipid nanoparticles (SLN).

MeSH terms

  • Antineoplastic Agents* / chemistry
  • Apoptosis
  • Breast Neoplasms* / metabolism
  • Caspases
  • Cell Line, Tumor
  • Cell Proliferation
  • Female
  • Humans
  • Nanoparticles* / chemistry
  • Poly(ADP-ribose) Polymerase Inhibitors / pharmacology
  • Poly(ADP-ribose) Polymerase Inhibitors / therapeutic use
  • Quercetin
  • Ribose
  • Triple Negative Breast Neoplasms* / drug therapy
  • bcl-2-Associated X Protein

Substances

  • Lipid Nanoparticles
  • Quercetin
  • bcl-2-Associated X Protein
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Ribose
  • Caspases
  • Antineoplastic Agents