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Int J Pharm. 2016 Nov 20;513(1-2):153-163. doi: 10.1016/j.ijpharm.2016.09.014. Epub 2016 Sep 5.

Effect of quercetin and resveratrol co-incorporated in liposomes against inflammatory/oxidative response associated with skin cancer.

Author information

1
Dept. of Science della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, University of Cagliari, Via Ospedale 72, 09124 Cagliari, Italy. Electronic address: caddeoc@unica.it.
2
Dept. of Pharmacy and Pharmaceutical Technology, University of Valencia, Avda Vicente Andrés Estellés s/n, 46100 Burjassot, Valencia, Spain; Institute of Molecular Recognition and Technological Development, Inter-Universitary Institute from Polytechnic University of Valencia and University of Valencia, Spain.
3
Dept. of Science, University of Basilicata, Viale dell'Ateneo Lucano 10, 85100 Potenza, Italy.
4
Dept. of Tecnologia Química i de Tensioactius, Institut de Química Avançada de Catalunya (IQAC-CSIC), 08034 Barcelona, Spain.
5
Nanomalaria Group, Institute for Bioengineering of Catalonia (IBEC), Baldiri Reixac 10-12, Barcelona E08028, Spain; Barcelona Institute for Global Health (ISGlobal), Barcelona Centre for International Health Research (CRESIB, Hospital Clínic-Universitat de Barcelona), Rosselló 149-153, Barcelona E08036, Spain.
6
Dept. of Scienze del Farmaco, University of Catania, Viale A. Doria 6, 95125 Catania, Italy.
7
Dept. of Science della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, University of Cagliari, Via Ospedale 72, 09124 Cagliari, Italy.

Abstract

The present investigation reports the development of liposomes for the co-delivery of naturally occurring polyphenols, namely quercetin and resveratrol. Small, spherical, uni/bilamellar vesicles were produced, as demonstrated by light scattering, cryo-TEM, SAXS. The incorporation of quercetin and resveratrol in liposomes did not affect their intrinsic antioxidant activity, as DPPH radical was almost completely inhibited. The cellular uptake of the polyphenols was higher when they were formulated in liposomes, and especially when co-loaded rather than as single agents, which resulted in a superior ability to scavenge ROS in fibroblasts. The in vivo efficacy of the polyphenols in liposomes was assessed in a mouse model of skin lesion. The topical administration of liposomes led to a remarkable amelioration of the tissue damage, with a significant reduction of oedema and leukocyte infiltration. Therefore, the proposed approach based on polyphenol vesicular formulation may be of value in the treatment of inflammation/oxidative stress associated with pre-cancerous/cancerous skin lesions.

KEYWORDS:

Antioxidant; Fibroblast; Liposome; Quercetin; Resveratrol; Skin lesion

PMID:
27609664
DOI:
10.1016/j.ijpharm.2016.09.014
[Indexed for MEDLINE]

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