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Title

Topical anti-inflammatory potential of quercetin in lipid-based nanosystems: In vivo and in vitro evaluation

AuthorsCaddeo, Carla; Díez-Sales, Octavio; Pons Pons, Ramon; Fernàndez-Busquets, Xavier; Fadda, Anna Maria; Manconi, Maria
Keywordsdermal fibroblasts
mice
quercetin
skin inflammation
vesicles
Issue DateApr-2014
PublisherSpringer
CitationPharmaceutical Research
AbstractPurpose: To develop quercetin-loaded phospholipid vesicles, namely liposomes and PEVs (Penetration Enhancer-containing Vesicles), and to investigate their efficacy on TPA-induced skin inflammation. Methods: Vesicles were made from a mixture of phospholipids, quercetin and polyethylene glycol 400 (PEG), specifically added to increase drug solubility and penetration through the skin. Vesicle morphology and self-assembly were probed by Cryo-Transmission Electron Microscopy and Small/Wide Angle X-ray Scattering, as well as the main physico-chemical features by Light Scattering. The anti-inflammatory efficacy of quercetin nanovesicles was assessed in vivo on TPA-treated mice dorsal skin by the determination of two biomarkers: oedema formation and myeloperoxidase activity. The uptake of vesicles by 3T3 fibroblasts was also evaluated. Results: Small spherical vesicles were produced. Their size and lamellarity was strongly influenced by the PEG content (0%, 5%, 10% v/v). The administration of vesicular quercetin on TPA-inflamed skin resulted in an amelioration of the tissue damage, with a noticeable attenuation of oedema and leukocyte infiltration, especially using 5% PEG-PEVs, as also confirmed by confocal microscopy. In vitro studies disclosed a massive uptake and diffusion of PEVs in dermal fibroblasts. Conclusions: The proposed approach based on quercetin vesicular formulations may be of value in the treatment of inflammatory skin disorders.
Publisher version (URL)10.1007/s11095-013-1215-0
URIhttp://hdl.handle.net/10261/128714
DOI10.1007/s11095-013-1215-0
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