Research Paper

Pharmaceutical Research

, Volume 31, Issue 4, pp 959-968

Topical Anti-Inflammatory Potential of Quercetin in Lipid-Based Nanosystems: In Vivo and In Vitro Evaluation

  • Carla CaddeoAffiliated withDepartment of Scienze della Vita e dell’Ambiente Sezione di Scienze del Farmaco, University of Cagliari Email author 
  • , Octavio Díez-SalesAffiliated withDepartment of Pharmacy and Pharmaceutical Technology, University of ValenciaInstituto de Reconocimiento Molecular y Desarrollo Tecnológico, Centro Mixto Universidad Politécnica de Valencia Universidad de Valencia
  • , Ramon PonsAffiliated withDepartment of Tecnologia Química i de Tensioactius, Institut de Química Avançada de Catalunya (IQAC-CSIC)
  • , Xavier Fernàndez-BusquetsAffiliated withNanobioengineering Group, Institute for Bioengineering of CataloniaBarcelona Centre for International Health Research, CRESIB Hospital Clínic-Universitat de BarcelonaBiomolecular Interactions Team Nanoscience and Nanotechnology Institute (IN2UB), University of Barcelona
  • , Anna Maria FaddaAffiliated withDepartment of Scienze della Vita e dell’Ambiente Sezione di Scienze del Farmaco, University of Cagliari
  • , Maria ManconiAffiliated withDepartment of Scienze della Vita e dell’Ambiente Sezione di Scienze del Farmaco, University of Cagliari

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ABSTRACT

Purpose

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.

KEY WORDS

dermal fibroblasts mice quercetin skin inflammation vesicles