Omega-3 PUFA Loaded in Resveratrol-Based Solid Lipid Nanoparticles: Physicochemical Properties and Antineoplastic Activities in Human Colorectal Cancer Cells In Vitro

Int J Mol Sci. 2018 Feb 16;19(2):586. doi: 10.3390/ijms19020586.

Abstract

New strategies are being investigated to ameliorate the efficacy and reduce the toxicity of the drugs currently used in colorectal cancer (CRC), one of the most common malignancies in the Western world. Data have been accumulated demonstrating that the antineoplastic therapies with either conventional or single-targeted drugs could take advantage from a combined treatment with omega-3 polyunsaturated fatty acids (omega-3 PUFA). These nutrients, shown to be safe at the dosage generally used in human trials, are able to modulate molecules involved in colon cancer cell growth and survival. They have also the potential to act against inflammation, which plays a critical role in CRC development, and to increase the anti-cancer immune response. In the present study, omega-3 PUFA were encapsulated in solid lipid nanoparticles (SLN) having a lipid matrix containing resveratrol esterified to stearic acid. Our aim was to increase the efficiency of the incorporation of these fatty acids into the cells and prevent their peroxidation and degradation. The Resveratrol-based SLN were characterized and investigated for their antioxidant activity. It was observed that the encapsulation of omega-3 PUFA into the SLN enhanced significantly their incorporation in human HT-29 CRC cells in vitro, and their growth inhibitory effects in these cancer cells, mainly by reducing cell proliferation.

Keywords: colon cancer cells; delivery; encapsulation; nanoparticles; omega-3; resveratrol.

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / pharmacology
  • Antioxidants / administration & dosage*
  • Antioxidants / pharmacology
  • Cell Proliferation / drug effects
  • Colorectal Neoplasms / metabolism
  • Fatty Acids, Omega-3 / administration & dosage*
  • Fatty Acids, Omega-3 / pharmacology
  • HCT116 Cells
  • HT29 Cells
  • Humans
  • Nanoparticles / chemistry*
  • Nanoparticles / metabolism
  • Rats
  • Resveratrol
  • Stearic Acids / chemistry
  • Stilbenes / chemistry*

Substances

  • Antineoplastic Agents
  • Antioxidants
  • Fatty Acids, Omega-3
  • Stearic Acids
  • Stilbenes
  • stearic acid
  • Resveratrol