title: Dermal quercetin lipid nanocapsules: Influence of the formulation on antioxidant activity and cellular protection against hydrogen peroxide.
abstract: Quercetin is a plant flavonoid with strong antioxidant and antiinflammatory properties interesting for skin protection. However, its poor water solubility limits its penetration and so its efficiency on skin. For this purpose, quercetin lipid nanocapsules were formulated implementing phase inversion technique wherein several modifications were introduced to enhance quercetin loading. Quercetin lipid nanocapsules were formulated with two particle size range, (50nm and 20nm) allowing a drug loading of 18.6 and 32mM respectively. The successful encapsulation of quercetin within lipid nanocapsules increased its apparent water solubility by more than 5000 fold (from 0.5μg/ml to about 5mg/ml). The physicochemical properties of these formulations such as surface charge, stability and morphology were characterized. Lipid nanocapsules had spherical shape and were stable for 28days at 25°C. Quercetin release from lipid nanocapsules was studied and revealed a prolonged release kinetics during 24h. Using DPPH assay, we demonstrated that the formulation process of lipid nanocapsules did not modify the antioxidant activity of quercetin in vitro (92.3%). With the goal of a future dermal application, quercetin lipid nanocapsules were applied to THP-1 monocytes and proved the cellular safety of the formulation up to 2μg/ml of quercetin. Finally, formulated quercetin was as efficient as the crude form in the protection of THP-1 cells from oxidative stress by exogenous hydrogen peroxide. With its lipophilic nature and occlusive effect on skin, lipid nanocapsules present a promising strategy to deliver quercetin to skin tissue and can be of value for other poorly water soluble drug candidates.
authors.affiliation: Institut Charles Gerhardt Montpellier, UMR 5253 CNRS-ENSCM-UM, Equipe Matériaux Avancés pour la Catalyse et la Santé, 8 rue de l'Ecole Normale, 34296 Montpellier Cedex 5, France. Electronic address: taher.hatahet90@gmail.com.
authors.forename: T
authors.initials: T
authors.lastname: Hatahet
authors.affiliation: Institut Charles Gerhardt Montpellier, UMR 5253 CNRS-ENSCM-UM, Equipe Matériaux Avancés pour la Catalyse et la Santé, 8 rue de l'Ecole Normale, 34296 Montpellier Cedex 5, France.
authors.forename: M
authors.initials: M
authors.lastname: Morille
authors.affiliation: Comparative Molecular Immuno-Physiopathology, IRD Laboratory, UMR-MD3, Faculty of Pharmacy, Montpellier University, 15 Avenue Charles Flahault, 34093 Montpellier Cedex 5, France.
authors.forename: A
authors.initials: A
authors.lastname: Shamseddin
authors.affiliation: Institut Charles Gerhardt Montpellier, UMR 5253 CNRS-ENSCM-UM, Equipe Matériaux Avancés pour la Catalyse et la Santé, 8 rue de l'Ecole Normale, 34296 Montpellier Cedex 5, France.
authors.forename: A
authors.initials: A
authors.lastname: Aubert-Pouëssel
authors.affiliation: Institut Charles Gerhardt Montpellier, UMR 5253 CNRS-ENSCM-UM, Equipe Matériaux Avancés pour la Catalyse et la Santé, 8 rue de l'Ecole Normale, 34296 Montpellier Cedex 5, France.
authors.forename: J M
authors.initials: JM
authors.lastname: Devoisselle
authors.affiliation: Institut Charles Gerhardt Montpellier, UMR 5253 CNRS-ENSCM-UM, Equipe Matériaux Avancés pour la Catalyse et la Santé, 8 rue de l'Ecole Normale, 34296 Montpellier Cedex 5, France.
authors.forename: S
authors.initials: S
authors.lastname: Bégu
mesh_terms: D000279:Administration, Cutaneous; D000975:Antioxidants / Q000008:administration & dosage / Q000737:chemistry; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D004339:Drug Compounding; D065546:Drug Liberation; D006801:Humans; D006861:Hydrogen Peroxide / Q000494:pharmacology; D008055:Lipids / Q000737:chemistry; D053769:Nanocapsules / Q000008:administration & dosage / Q000737:chemistry; D018384:Oxidative Stress / Q000187:drug effects; D011794:Quercetin / Q000008:administration & dosage / Q000737:chemistry
chemical_list: D000975:Antioxidants; D004337:Drug Carriers; D008055:Lipids; D053769:Nanocapsules; D011794:Quercetin; D006861:Hydrogen Peroxide
keywords: Cellular protection; DPPH assay; Hydrogen peroxide induced toxicity; Lipid nanocapsules; Quercetin; Sustained release; THP-1 cells