Quercetin in w/o microemulsion: In vitro and in vivo skin penetration and efficacy against UVB-induced skin damages evaluated in vivo

The present study evaluated the potential of a w/o microemulsion as a topical carrier system for delivery of the antioxidant quercetin. Topical and transdermal delivery of quercetin were evaluated in vitro using porcine ear skin mounted on a Franz diffusion cell and in vivo on hairless-skin mice. Sk...

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Bibliographic Details
Published in:	European journal of pharmaceutics and biopharmaceutics Vol. 69; no. 3; pp. 948 - 957
Main Authors:	Vicentini, Fabiana T.M.C., Simi, Thaís R.M., Del Ciampo, José O., Wolga, Nilce O., Pitol, Dimitrius L., Iyomasa, Mamie M., Bentley, M. Vitória L.B., Fonseca, Maria J.V.
Format:	Journal Article
Language:	English
Published:	Amsterdam Elsevier B.V 01-08-2008 Elsevier Science
Subjects:	Animals Antioxidants - administration & dosage Antioxidants - pharmacokinetics Antioxidants - pharmacology Biological and medical sciences Chemistry, Pharmaceutical Chromatography, High Pressure Liquid Drug Carriers Drug Delivery Systems Electrophoresis, Polyacrylamide Gel Emulsions General pharmacology Glutathione - metabolism Irritants - toxicity Medical sciences Mice Mice, Hairless Microemulsion Oils Peptide Hydrolases - chemistry Peptide Hydrolases - metabolism Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Quercetin Quercetin - administration & dosage Quercetin - pharmacokinetics Quercetin - pharmacology Radiation-Protective Agents - administration & dosage Radiation-Protective Agents - pharmacokinetics Radiation-Protective Agents - pharmacology Skin - drug effects Skin - enzymology Skin Absorption Skin irritation Skin penetration Ultraviolet Rays UVB radiation Water Skin penetration Skin irritation Microemulsion UVB radiation Quercetin Pharmaceutical technology Toxicity Flavonoid In vitro In vivo Polyphenol Penetration Water oil microemulsion Efficiency Phenols Skin Irritation
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Summary:	The present study evaluated the potential of a w/o microemulsion as a topical carrier system for delivery of the antioxidant quercetin. Topical and transdermal delivery of quercetin were evaluated in vitro using porcine ear skin mounted on a Franz diffusion cell and in vivo on hairless-skin mice. Skin irritation by topical application of the microemulsion containing quercetin, and the protective effect of the formulation on UVB-induced decrease of endogenous reduced glutathione levels and increase of cutaneous proteinase secretion/activity were also investigated. The w/o microemulsion increased the penetration of quercetin into the stratum corneum and epidermis plus dermis at 3, 6, 9 and 12 h post-application in vitro and in vivo at 6 h post-application. No transdermal delivery of quercetin occurred. By evaluating established endpoints of skin irritation (erythema formation, epidermis thickening and infiltration of inflammatory cells), the study demonstrated that the daily application of the w/o microemulsion for up to 2 days did not cause skin irritation. W/o microemulsion containing quercetin significantly prevented the UVB irradiation-induced GSH depletion and secretion/activity of metalloproteinases.
ISSN:	0939-6411 1873-3441
DOI:	10.1016/j.ejpb.2008.01.012