Abstract
Quercetin (3,3′,4′,5,7-pentahydroxyflavone) exerts multiple pharmacological effects: anti-oxidant activity, induction of apoptosis, modulation of cell cycle, anti-mutagenesis, and anti-inflammatory effect. In topical formulations quercetin inhibits oxidative skin damage and the inflammatory processes induced by solar UV radiation. In this work, quercetin (2 mg/mL) was loaded in vesicular Penetration Enhancer containing Vesicles (PEVs), prepared using a mixture of lipids (Phospholipon® 50, P50) and one of four selected hydrophilic penetration enhancers: Transcutol® P, propylene glycol, polyethylene glycol 400, and Labrasol® at the same concentration (40% of water phase). Photon Correlation Spectroscopy results showed a mean diameter of drug loaded vesicles in the range 80–220 nm. All formulations showed a negative surface charge and incorporation efficiency in the range 48–75%. Transmission Electron Microscopy confirmed that size and morphology varied as a function of the used penetration enhancer. The influence of PEVs on ex vivo quercetin (trans)dermal delivery was evaluated using Franz-type diffusion cells, new born pig skin and Confocal Laser Scanning Microscopy. Results showed that drug delivery is affected by the penetration enhancer used in the PEVs' formulation.
Highlights
Quercetin (3,3′,4′,5,7-pentahydroxyflavone, QUE) is a bioflavonoid, profuse in nature in plant food sources
It has been reported that the topical application of quercetin inhibits oxidative skin damage and the inflammatory processes induced by solar UV radiation [1]
We prepared and characterized phospholipid vesicles containing high quantities of different penetration enhancers (PEs) (40%) in the water phase, which is required to avoid quercetin (2 mg/mL) precipitation
Summary
Quercetin (3,3′,4′,5,7-pentahydroxyflavone, QUE) is a bioflavonoid, profuse in nature in plant food sources. Topical use of quercetin is frequently hampered by its low skin permeability and poor solubility in aqueous media, which make the development of pharmaceutical formulations difficult. Different strategies, such as prodrug [2] and microemulsion [3], have been used to improve quercetin topical delivery. Previous findings demonstrated that PEVs are powerful enhancers for dermal delivery, due to the synergistic effect of phospholipid vesicles and PE [4,5,6,7,8] The latter may increase fluidity of the lipid portion of the stratum corneum, facilitating the delivery of the vesicle loaded-drug, and its diffusion through the skin. Their penetration capability and distribution through pig skin were assessed by Franz diffusion experiments and confocal microscopy, to give further evidence of the superior performances of PEVs
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