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Pharmaceutics 2011, 3(3), 497-509; doi:10.3390/pharmaceutics3030497
Article

Effect of Penetration Enhancer Containing Vesicles on the Percutaneous Delivery of Quercetin through New Born Pig Skin

, , , * ,  and
Dipartimento Farmaco Chimico Tecnologico, University of Cagliari, Via Ospedale 72, Cagliari, Italy
* Author to whom correspondence should be addressed.
Received: 1 July 2011 / Revised: 4 August 2011 / Accepted: 10 August 2011 / Published: 12 August 2011
(This article belongs to the Special Issue Transdermal Drug Delivery)
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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.
Keywords: liposome; quercetin; penetration enhancer; skin permeation; rheology; confocal laser scanning microscopy; bioflavonoid liposome; quercetin; penetration enhancer; skin permeation; rheology; confocal laser scanning microscopy; bioflavonoid
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Chessa, M.; Caddeo, C.; Valenti, D.; Manconi, M.; Sinico, C.; Fadda, A.M. Effect of Penetration Enhancer Containing Vesicles on the Percutaneous Delivery of Quercetin through New Born Pig Skin. Pharmaceutics 2011, 3, 497-509.

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