Using Liposomes as Carriers for Polyphenolic Compounds: The Case of Trans-Resveratrol
News Sep 04, 2012
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.
This article is published online in PLoS One and is free to access.
Scientists Develop a Synthetic Solution to Combat Dwindling Supply of Cancer and HIV DrugNews
Supplies of a promising drug for cancer, HIV and possibly other diseases is dwindling, and scientists have struggled to extract more from the marine creatures who produce it. Now, chemists have a synthetic solution.READ MORE
Arsenic Trioxide Could Extend Lives of Patients with Aggressive Brain CancerNews
Arsenic trioxide could be a powerful therapy that could extend the lives of certain glioblastoma patients by as much as three to four times the median expectation.READ MORE
XenoGesis and Juniper Pharma Services Strengthen AllianceNews
Campanies extend strategic alliance in early drug development services.READ MORE
Comments | 0 ADD COMMENT
Annual Conference on Antimicrobials and Drug Resistance
Sep 24 - Sep 25, 2018
1st Alpine Winter Conference on Medicinal and Synthetic Chemistry
Jan 28 - Feb 01, 2018