Catanionic lipid nanosystems improve pharmacokinetics and anti-lung cancer activity of curcumin

Nanomedicine. 2016 Aug;12(6):1567-79. doi: 10.1016/j.nano.2016.02.007. Epub 2016 Mar 17.

Abstract

Novel catanionic lipid nanosystems (CLNs) incorporating curcumin (CCM) were developed, and improvements in pharmacokinetics and enhanced anti-lung cancer activity were observed. CCM was present in a lipid matrix surrounded by cationic, anionic and zwitterionic surfactants, forming the core-shell nanosystems. Compared with free CCM, the CCM-CLNs had much higher oral and intravenous bioavailabilities due to enhanced absorption and reduced clearance. The CCM-CLNs exhibited greater cytotoxicity in Lewis lung cancer (LLC) cells, which might have been due to increased antiproliferative, proapoptotic and anti-invasive activities and induction of cell cycle arrest. The CCM-CLNs increased the antitumor efficacy of CCM and decreased the tumor growth rate in tumor-bearing mice. This is the first report of induction of apoptosis in LLC cells by CCM through the PI3K/Akt/FoxO1/Bim signaling pathway. Catanionic lipid nanocarriers show promise for the therapeutic delivery of insoluble anti-tumor drugs.

Keywords: Anti-lung cancer activity; Bioavailabilities; Catanionic lipid nanosystems; Curcumin; Signaling pathway.

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / pharmacokinetics
  • Apoptosis
  • Cell Line, Tumor
  • Curcumin / administration & dosage*
  • Curcumin / pharmacokinetics
  • Humans
  • Lipids / therapeutic use
  • Lung Neoplasms / drug therapy*
  • Mice
  • Nanoparticles
  • Phosphatidylinositol 3-Kinases
  • Signal Transduction / drug effects

Substances

  • Antineoplastic Agents
  • Lipids
  • Phosphatidylinositol 3-Kinases
  • Curcumin