A topical formulation containing quercetin-loaded microcapsules protects against oxidative and inflammatory skin alterations triggered by UVB irradiation: enhancement of activity by microencapsulation. (21st October 2021)

• Record Type: Journal Article
• Authors: Vale, David L.; Martinez, Renata M.; Medeiros, Daniela C.; da Rocha, Camila; Sfeir, Natália; Lopez, Renata F. V.; Vicentini, Fabiana T. M. C.; Verri, Waldiceu A.; Georgetti, Sandra R.; Baracat, Marcela M.; Casagrande, Rúbia
• Is Part Of: Journal of drug targeting. Volume 29:Number 9(2021)
• Page Start: 983
• Page End: 997
• Publication Date: 2021-10-21
• Subjects: Quercetin -- microcapsule -- inflammation -- oxidative stress -- ultraviolet B; Drug delivery systems -- Periodicals; Drug Delivery Systems; Vehicles; Drug Administration Routes; Drug Evaluation; 615.7
• DOI: 10.1080/1061186X.2021.1898621
• Languages: English
• ISSNs: 1061-186X

Abstract

Abstract: Ultraviolet B (UVB) irradiation causes free radical production, increase inflammation and oxidative stress, thus, supporting the use of antioxidants by topical administration as therapeutic approaches. Quercetin (QC) is a flavonoid with antioxidant activity, however, high liposolubility makes it difficult to remain in the viable skin layer. Thus, this study evaluated whether microencapsulation of QC would enhance its activity in comparison with the same dose of free QC (non-active dose) and unloaded-microcapsules added in formulation for topical administration in a mouse model of UVB irradiation targeting the skin. Topical formulation containing Quercetin-loaded microcapsules (TFcQCMC) presents physico-chemical (colour, consistence, phase separation and pH) and functional antioxidant stability at 4 °C, room temperature and 40 °C for 6 months. TFcQCMC inhibited the UVB-triggered depletion of antioxidants observed by GSH (reduced glutathione), ability to reduce iron, ability to scavenge 2, 2'-azinobis radical and catalase activity. TFcQCMC also inhibited markers of oxidation (lipid hydroperoxides and superoxide anion production). Concerning inflammation, TFcQCMC reduced the production of inflammatory cytokines, matrix metalloproteinase-9 activity, skin edoema, collagen fibre damage, myeloperoxidase activity/neutrophil recruitment, mast cell and sunburn cell counts. The pharmacological activity of TFcQCMC was not shared by the same pharmaceutical form containing the same dose of free QC or unloaded control microcapsules.