Topical Anti-Inflammatory Potential of Quercetin in Lipid-Based Nanosystems: In Vivo and In Vitro Evaluation
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To develop quercetin-loaded phospholipid vesicles, namely liposomes and PEVs (Penetration Enhancer-containing Vesicles), and to investigate their efficacy on TPA-induced skin inflammation.
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.
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.
The proposed approach based on quercetin vesicular formulations may be of value in the treatment of inflammatory skin disorders.
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- Topical Anti-Inflammatory Potential of Quercetin in Lipid-Based Nanosystems: In Vivo and In Vitro Evaluation
Volume 31, Issue 4 , pp 959-968
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- dermal fibroblasts
- skin inflammation
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- Author Affiliations
- 1. Department of Scienze della Vita e dell’Ambiente Sezione di Scienze del Farmaco, University of Cagliari, Via Ospedale 72, 09124, Cagliari, Italy
- 2. Department of Pharmacy and Pharmaceutical Technology, University of Valencia, Avda Vicente Andrés Estellés s/n, 46100, Burjassot, Valencia, Spain
- 3. Instituto de Reconocimiento Molecular y Desarrollo Tecnológico, Centro Mixto Universidad Politécnica de Valencia Universidad de Valencia, Valencia, Spain
- 4. Department of Tecnologia Química i de Tensioactius, Institut de Química Avançada de Catalunya (IQAC-CSIC), 08034, Barcelona, Spain
- 5. Nanobioengineering Group, Institute for Bioengineering of Catalonia, Baldiri Reixac 10-12, Barcelona, 08028, Spain
- 6. Barcelona Centre for International Health Research, CRESIB Hospital Clínic-Universitat de Barcelona, Rosselló 149-153, Barcelona, 08036, Spain
- 7. Biomolecular Interactions Team Nanoscience and Nanotechnology Institute (IN2UB), University of Barcelona, Martí i Franquès 1, Barcelona, 08028, Spain