Dermal quercetin lipid nanocapsules: Influence of the formulation on antioxidant activity and cellular protection against hydrogen peroxide

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• 作者：T. Hatahet^a ; ^{taher.hatahet90@gmail.com} ; M. Morille^a ; A. Shamseddin^b ; A. Aubert-Pouë ; ssel^a ; J.M. Devoisselle^a ; S. Bé ; gu^a
• 关键词：Quercetin ; Lipid nanocapsules ; DPPH assay ; Sustained release ; Cellular protection ; Hydrogen peroxide induced toxicity ; THP-1 cells
• 刊名：International Journal of Pharmaceutics
• 出版年：2017
• 出版时间：25 February 2017
• 年：2017
• 卷：518
• 期：1-2
• 页码：167-176
• 全文大小：1487 K
• 卷排序：518

文摘

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, (50 nm and 20 nm) allowing a drug loading of 18.6 and 32 mM respectively. The successful encapsulation of quercetin within lipid nanocapsules increased its apparent water solubility by more than 5000 fold (from 0.5 μg/ml to about 5 mg/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 28 days at 25 °C. Quercetin release from lipid nanocapsules was studied and revealed a prolonged release kinetics during 24 h. 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 2 μg/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.