Development of topical nanoemulsions containing quercetin and 3-O-methylquercetin.
This study describes the physico-chemical properties and the skin permeation profile of quercetin (Q) and 3-O-methylquercetin (MQ) from lipid nanoemulsions. Formulations composed of octyldodecanol, egg lecithin, water (NE) and cetyl trimethyl ammonium bromide (CNE) were obtained by spontaneous emulsification. This procedure yielded monodisperse nanoemulsions exhibiting a mean droplet size of approximately 200-300 nm. Nanoemulsions were further characterized in terms of zeta-potential, surface tension, and morphology by transmission electron microscopy. The amount of flavonoids incorporated into nanoemulsions reached nearly 100% (at 1 mg/mL). The permeation studies were carried out using ear pig skin mounted in Franz diffusion cells. The overall results have shown a slow permeation profile of both Q and MQ from nanoemulsions. However, a higher permeation flux rate of flavonoids from CNE (approximately 0.2 microg/cm2/h) as compared to NE (approximately 0.08 microg/cm2/h) was observed, showing the effect of the positively charged surface of CNE on this parameter. Such results open interesting perspectives for the topical administration of the flavonoids Q and MQ.
Fasolo
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Programa de Pós-graduação em Ciências Farmacêuticas da Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Brazil.
Bassani
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VL
Teixeira
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HF
D000287:Administration, Topical; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D015194:Diffusion Chambers, Culture; D004563:Electrochemistry; D004655:Emulsions; D005419:Flavonoids / Q000032:analysis; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D010316:Particle Size; D011794:Quercetin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D012869:Skin Absorption; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D013552:Swine
D004655:Emulsions; D005419:Flavonoids; D007202:Indicators and Reagents; C047368:3-methylquercetin; D011794:Quercetin