title: Improvement of quercetin protective effect against oxidative stress skin damages by incorporation in nanovesicles.
abstract: Quercetin was incorporated in glycerosomes, new phospholipid-glycerol vesicles, and their protective effect against oxidative stress skin damages was extensively evaluated. In particular, the concentration-dependent effect of glycerol (from 10 to 50%) on vesicle suitability as cutaneous carriers of quercetin was carefully assessed. All vesicles were unilamellar and small in size (∼80-110 nm), as confirmed by cryo-TEM observation, with a drug incorporation efficiency ranging between 81 and 91%. SAXS studies, performed to investigate the bilayer arrangement, indicated a strong, dose-dependent interaction of glycerol with the polar portions of the phospholipid molecules, while quercetin did not significantly change the bilayer packing. In vitro studies on newborn pig skin underlined the concentration-dependent ability of glycerosomes to promote quercetin accumulation in the different layers, also confirmed by confocal microscopic observation of skin treated with fluorescent vesicles. Quercetin incorporated into liposomal and glycerosomal nanoformulations showed a strong ability to scavenge free radicals (DPPH test) and protect human keratinocytes in vitro against hydrogen peroxide damage. Moreover, quercetin-loaded vesicles were avidly taken up by keratinocytes in vitro. Overall, results indicate 40 and 50% glycerosomes as promising nanosystems for the improvement of cutaneous quercetin delivery and keratinocyte protection against oxidative stress damage.
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, CNBS, University of Cagliari, Cagliari, Italy. Electronic address: mlmanca@unica.it.
authors.forename: Maria Letizia
authors.initials: ML
authors.lastname: Manca
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, CNBS, University of Cagliari, Cagliari, Italy.
authors.forename: Ines
authors.initials: I
authors.lastname: Castangia
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, CNBS, University of Cagliari, Cagliari, Italy.
authors.forename: Carla
authors.initials: C
authors.lastname: Caddeo
authors.affiliation: Department Ingeniería Química y Tecnología del Medio Ambiente, University of Oviedo, Oviedo, Spain.
authors.forename: Daniel
authors.initials: D
authors.lastname: Pando
authors.affiliation: Biopharmaceutics and Pharmacokinetics Unit, Institute for Nanoscience and Nanotechnology, University of Barcelona, Barcelona, Spain.
authors.forename: Elvira
authors.initials: E
authors.lastname: Escribano
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, CNBS, University of Cagliari, Cagliari, Italy.
authors.forename: Donatella
authors.initials: D
authors.lastname: Valenti
authors.affiliation: Dept. Scienze Chimiche e Geologiche, CNBS and CSGI, University of Cagliari, Monserrato (CA), Italy.
authors.forename: Sandrina
authors.initials: S
authors.lastname: Lampis
authors.affiliation: Prigen srl, Sardegna Ricerche Ed. 3, Pula (Cagliari) 09010, Italy.
authors.forename: Marco
authors.initials: M
authors.lastname: Zaru
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, CNBS, University of Cagliari, Cagliari, Italy.
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Fadda
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, CNBS, University of Cagliari, Cagliari, Italy.
authors.forename: Maria
authors.initials: M
authors.lastname: Manconi
mesh_terms: D000975:Antioxidants / Q000737:chemistry / Q000494:pharmacology; D002478:Cells, Cultured; D005990:Glycerol / Q000737:chemistry*; D006801:Humans; D015603:Keratinocytes / Q000187:drug effects / Q000378:metabolism; D018613:Microscopy, Confocal; D018384:Oxidative Stress / Q000187:drug effects*; D011794:Quercetin / Q000737:chemistry* / Q000494:pharmacology; D012867:Skin / Q000187:drug effects*
chemical_list: D000975:Antioxidants; D011794:Quercetin; D005990:Glycerol
keywords: Confocal microscopy; Glycerol; Human keratinocytes; Hydrogen peroxide damage; Natural antioxidant; Phospholipid vesicles