title: Enhanced antioxidant effect of trans-resveratrol: potential of binary systems with polyethylene glycol and cyclodextrin.
abstract: Trans-resveratrol, a polyphenol extracted from Vitis vinifera, has different beneficial effects following its administration on the skin. Here the potential use of binary systems to enhance in vitro and in vivo activity of trans-resveratrol was investigated. Thus the aqueous solubility of trans-resveratrol was investigated in the presence of growing concentrations of polyethylene glycol (PEG) or β-cyclodextrin (βCD) as solubilizing excipients. Then, the solid dispersion of trans-resveratrol with PEG or inclusion complexes trans-resveratrol/βCD were prepared and characterised by different methods. Cytotoxicity and inhibition of reactive oxygen species (ROS) following H2O2 challenge in the presence of trans-resveratrol, alone or associated to the excipients, was evaluated on human keratinocyte HaCaT cell line. Both the trans-resveratrol-containing binary systems induced significant reduction of H2O2-induced ROS production, especially in the case of βCD that was selected for the following phase of the study. Thus, the effect of a cream containing trans-resveratrol, alone or associated to βCD, on different skin parameters such as corneometry, colorimetry and elastometry, was evaluated on human volunteers. All patients showed a visible improvement of clinical conditions with a remarkable decrease of aging signs, but this effect was higher of the hemi face treated with the βCD-containing formulation versus formulation containing trans-resveratrol alone.
authors.affiliation: Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Seville , Seville , Spain .
authors.forename: Josè Ramon
authors.initials: JR
authors.lastname: Moyano-Mendez
authors.forename: Gabriella
authors.initials: G
authors.lastname: Fabbrocini
authors.forename: Daniela
authors.initials: D
authors.lastname: De Stefano
authors.forename: Caterina
authors.initials: C
authors.lastname: Mazzella
authors.forename: Laura
authors.initials: L
authors.lastname: Mayol
authors.forename: Immacolata
authors.initials: I
authors.lastname: Scognamiglio
authors.forename: Rosa
authors.initials: R
authors.lastname: Carnuccio
authors.forename: Fabio
authors.initials: F
authors.lastname: Ayala
authors.forename: Maria Immacolata
authors.initials: MI
authors.lastname: La Rotonda
authors.forename: Giuseppe
authors.initials: G
authors.lastname: De Rosa
mesh_terms: D000368:Aged; D000975:Antioxidants / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003124:Colorimetry; D005079:Excipients / Q000737:chemistry; D005260:Female; D006801:Humans; D006861:Hydrogen Peroxide / Q000494:pharmacology; D015603:Keratinocytes / Q000187:drug effects / Q000378:metabolism; D008875:Middle Aged; D011092:Polyethylene Glycols / Q000737:chemistry*; D017382:Reactive Oxygen Species / Q000378:metabolism; D000077185:Resveratrol; D016037:Single-Blind Method; D015595:Skin Aging / Q000187:drug effects; D012995:Solubility; D013267:Stilbenes / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D000975:Antioxidants; D005079:Excipients; D017382:Reactive Oxygen Species; D013267:Stilbenes; D047392:beta-Cyclodextrins; D011092:Polyethylene Glycols; D006861:Hydrogen Peroxide; C031215:betadex; D000077185:Resveratrol
keywords: Anti-aging; human keratinocyte; polyethylene glycol; trans-resveratrol; β-cyclodextrin