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 Caddeo
  • Octavio Díez-Sales
  • Ramon Pons
  • Xavier Fernàndez-Busquets
  • Anna Maria Fadda
  • Maria Manconi
Research Paper

DOI: 10.1007/s11095-013-1215-0

Cite this article as:
Caddeo, C., Díez-Sales, O., Pons, R. et al. Pharm Res (2014) 31: 959. doi:10.1007/s11095-013-1215-0

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 fibroblastsmicequercetinskin inflammationvesicles

Copyright information

© Springer Science+Business Media New York 2013

Authors and Affiliations

  • Carla Caddeo
    • 1
  • Octavio Díez-Sales
    • 2
    • 3
  • Ramon Pons
    • 4
  • Xavier Fernàndez-Busquets
    • 5
    • 6
    • 7
  • Anna Maria Fadda
    • 1
  • Maria Manconi
    • 1
  1. 1.Department of Scienze della Vita e dell’Ambiente Sezione di Scienze del FarmacoUniversity of CagliariCagliariItaly
  2. 2.Department of Pharmacy and Pharmaceutical TechnologyUniversity of ValenciaBurjassotSpain
  3. 3.Instituto de Reconocimiento Molecular y Desarrollo TecnológicoCentro Mixto Universidad Politécnica de Valencia Universidad de ValenciaValenciaSpain
  4. 4.Department of Tecnologia Química i de TensioactiusInstitut de Química Avançada de Catalunya (IQAC-CSIC)BarcelonaSpain
  5. 5.Nanobioengineering GroupInstitute for Bioengineering of CataloniaBarcelonaSpain
  6. 6.Barcelona Centre for International Health ResearchCRESIB Hospital Clínic-Universitat de BarcelonaBarcelonaSpain
  7. 7.Biomolecular Interactions Team Nanoscience and Nanotechnology Institute (IN2UB)University of BarcelonaBarcelonaSpain