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

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...

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Autores principales: Claudia Bonechi, Silvia Martini, Laura Ciani, Stefania Lamponi, Herbert Rebmann, Claudio Rossi, Sandra Ristori
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Publicado: Public Library of Science (PLoS) 2012
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spelling oai:doaj.org-article:6b5f77c159b941599c8cd32f57cf50fb2021-11-18T07:07:56ZUsing liposomes as carriers for polyphenolic compounds: the case of trans-resveratrol.1932-620310.1371/journal.pone.0041438https://doaj.org/article/6b5f77c159b941599c8cd32f57cf50fb2012-01-01T00:00:00Zhttps://www.ncbi.nlm.nih.gov/pmc/articles/pmid/22936976/pdf/?tool=EBIhttps://doaj.org/toc/1932-6203Resveratrol (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.Claudia BonechiSilvia MartiniLaura CianiStefania LamponiHerbert RebmannClaudio RossiSandra RistoriPublic Library of Science (PLoS)articleMedicineRScienceQENPLoS ONE, Vol 7, Iss 8, p e41438 (2012)
institution DOAJ
collection DOAJ
language EN
topic Medicine
R
Science
Q
spellingShingle Medicine
R
Science
Q
Claudia Bonechi
Silvia Martini
Laura Ciani
Stefania Lamponi
Herbert Rebmann
Claudio Rossi
Sandra Ristori
Using liposomes as carriers for polyphenolic compounds: the case of trans-resveratrol.
description 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.
format article
author Claudia Bonechi
Silvia Martini
Laura Ciani
Stefania Lamponi
Herbert Rebmann
Claudio Rossi
Sandra Ristori
author_facet Claudia Bonechi
Silvia Martini
Laura Ciani
Stefania Lamponi
Herbert Rebmann
Claudio Rossi
Sandra Ristori
author_sort Claudia Bonechi
title Using liposomes as carriers for polyphenolic compounds: the case of trans-resveratrol.
title_short Using liposomes as carriers for polyphenolic compounds: the case of trans-resveratrol.
title_full Using liposomes as carriers for polyphenolic compounds: the case of trans-resveratrol.
title_fullStr Using liposomes as carriers for polyphenolic compounds: the case of trans-resveratrol.
title_full_unstemmed Using liposomes as carriers for polyphenolic compounds: the case of trans-resveratrol.
title_sort using liposomes as carriers for polyphenolic compounds: the case of trans-resveratrol.
publisher Public Library of Science (PLoS)
publishDate 2012
url https://doaj.org/article/6b5f77c159b941599c8cd32f57cf50fb
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