Using liposomes as carriers for polyphenolic compounds: the case of trans-resveratrol

PLoS One. 2012;7(8):e41438. doi: 10.1371/journal.pone.0041438. Epub 2012 Aug 22.

Abstract

Resveratrol (3,5,4'-trihydroxy-trans-stilbene) is a polyphenol found in various plants, especially in the skin of red grapes. The effect of resveratrol on human health is the topic of numerous studies. In fact this molecule has shown anti-cancer, anti-inflammatory, blood-sugar-lowering ability and beneficial cardiovascular effects. However, for many polyphenol compounds of natural origin bioavailability is limited by low solubility in biological fluids, as well as by rapid metabolization in vivo. Therefore, appropriate carriers are required to obtain efficient therapeutics along with low administration doses.Liposomes are excellent candidates for drug delivery purposes, due to their biocompatibility, wide choice of physico-chemical properties and easy preparation.In this paper liposome formulations made by a saturated phosphatidyl-choline (DPPC) and cholesterol (or its positively charged derivative DC-CHOL) were chosen to optimize the loading of a rigid hydrophobic molecule such as resveratrol.Plain and resveratrol loaded liposomes were characterized for size, surface charge and structural details by complementary techniques, i.e. Dynamic Light Scattering (DLS), Zeta potential and Small Angle X-ray Scattering (SAXS). Nuclear and Electron Spin magnetic resonances (NMR and ESR, respectively) were also used to gain information at the molecular scale.The obtained results allowed to give an account of loaded liposomes in which resveratrol interacted with the bilayer, being more deeply inserted in cationic liposomes than in zwitterionic liposomes. Relevant properties such as the mean size and the presence of oligolamellar structures were influenced by the loading of RESV guest molecules.The toxicity of all these systems was tested on stabilized cell lines (mouse fibroblast NIH-3T3 and human astrocytes U373-MG), showing that cell viability was not affected by the administration of liposomial resveratrol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line
  • Drug Delivery Systems / methods*
  • Electron Spin Resonance Spectroscopy
  • Humans
  • Liposomes / administration & dosage
  • Liposomes / chemistry*
  • Magnetic Resonance Spectroscopy
  • Mice
  • Models, Theoretical
  • NIH 3T3 Cells
  • Polyphenols / administration & dosage
  • Polyphenols / chemistry
  • Resveratrol
  • Stilbenes / administration & dosage
  • Stilbenes / chemistry*

Substances

  • Liposomes
  • Polyphenols
  • Stilbenes
  • Resveratrol

Grants and funding

This study was conducted in the framework of a Phospholipids Research Center (Heidelberg, Germany) funded research project. Dr. Herbert Rebmann, a member of the Phospholipids Research Center, took part to the work and co-authored this manuscript. Apart from Dr. Rebmann, who contributed as co-author, the funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.