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. 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 12h post-application in vitro and in vivo at 6h 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.
Vicentini
Fabiana T M C
FT
Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, São Paulo, Brazil.
Simi
Thaís R M
TR
Del Ciampo
José O
JO
Wolga
Nilce O
NO
Pitol
Dimitrius L
DL
Iyomasa
Mamie M
MM
Bentley
M Vitória L B
MV
Fonseca
Maria J V
MJ
D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers; D016503:Drug Delivery Systems; D004591:Electrophoresis, Polyacrylamide Gel; D004655:Emulsions; D005978:Glutathione / Q000378:metabolism; D007509:Irritants / Q000633:toxicity; D051379:Mice; D008812:Mice, Hairless; D009821:Oils; D010447:Peptide Hydrolases / Q000737:chemistry / Q000378:metabolism; D011794:Quercetin / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology*; D011837:Radiation-Protective Agents / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology*; D012867:Skin / Q000187:drug effects / Q000201:enzymology; D012869:Skin Absorption; D014466:Ultraviolet Rays; D014867:Water
D000975:Antioxidants; D004337:Drug Carriers; D004655:Emulsions; D007509:Irritants; D009821:Oils; D011837:Radiation-Protective Agents; D014867:Water; D011794:Quercetin; D010447:Peptide Hydrolases; D005978:Glutathione