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一种含有槲皮素负载微胶囊的局部制剂可预防 UVB 照射引发的氧化和炎症性皮肤改变:微囊化增强其活性。

A topical formulation containing quercetin-loaded microcapsules protects against oxidative and inflammatory skin alterations triggered by UVB irradiation: enhancement of activity by microencapsulation.

机构信息

Departamento de Ciências Farmacêuticas, Universidade Estadual de Londrina-UEL, Avenida Robert Koch, 60, Hospital Universitário, Londrina, Brazil.

Departamento de Ciências Patológicas, Centro de Ciências Biológicas, Universidade Estadual de Londrina-UEL, Londrina, Brazil.

出版信息

J Drug Target. 2021 Nov;29(9):983-997. doi: 10.1080/1061186X.2021.1898621. Epub 2021 Mar 15.

DOI:10.1080/1061186X.2021.1898621
PMID:33685319
Abstract

Ultraviolet B (UVB) irradiation causes free radical production, increase inflammation and oxidative stress, thus, supporting the use of antioxidants by topical administration as therapeutic approaches. Quercetin (QC) is a flavonoid with antioxidant activity, however, high liposolubility makes it difficult to remain in the viable skin layer. Thus, this study evaluated whether microencapsulation of QC would enhance its activity in comparison with the same dose of free QC (non-active dose) and unloaded-microcapsules added in formulation for topical administration in a mouse model of UVB irradiation targeting the skin. Topical formulation containing Quercetin-loaded microcapsules (TFcQCMC) presents physico-chemical (colour, consistence, phase separation and pH) and functional antioxidant stability at 4 °C, room temperature and 40 °C for 6 months. TFcQCMC inhibited the UVB-triggered depletion of antioxidants observed by GSH (reduced glutathione), ability to reduce iron, ability to scavenge 2,2'-azinobis radical and catalase activity. TFcQCMC also inhibited markers of oxidation (lipid hydroperoxides and superoxide anion production). Concerning inflammation, TFcQCMC reduced the production of inflammatory cytokines, matrix metalloproteinase-9 activity, skin edoema, collagen fibre damage, myeloperoxidase activity/neutrophil recruitment, mast cell and sunburn cell counts. The pharmacological activity of TFcQCMC was not shared by the same pharmaceutical form containing the same dose of free QC or unloaded control microcapsules.

摘要

中波紫外线(UVB)照射会导致自由基产生、炎症和氧化应激增加,因此,支持通过局部给药使用抗氧化剂作为治疗方法。槲皮素(QC)是一种具有抗氧化活性的类黄酮,但是,高脂溶性使其难以留在有活力的皮肤层中。因此,本研究评估了 QC 的微胶囊化是否会增强其活性,与相同剂量的游离 QC(非活性剂量)和添加到局部给药制剂中的未载药微胶囊相比,在针对皮肤的 UVB 照射的小鼠模型中。含有载有槲皮素的微胶囊的局部制剂(TFcQCMC)在 4°C、室温以及 40°C 下具有 6 个月的物理化学(颜色、稠度、相分离和 pH)和功能性抗氧化稳定性。TFcQCMC 抑制了 GSH(还原型谷胱甘肽)、还原铁能力、清除 2,2'-联氮双自由基能力和过氧化氢酶活性观察到的由 UVB 触发的抗氧化剂耗竭。TFcQCMC 还抑制了氧化标志物(脂质过氧化物和超氧阴离子的产生)。关于炎症,TFcQCMC 降低了促炎细胞因子的产生、基质金属蛋白酶-9 活性、皮肤水肿、胶原纤维损伤、髓过氧化物酶活性/中性粒细胞募集、肥大细胞和晒伤细胞计数。TFcQCMC 的药理学活性与含有相同剂量游离 QC 或未载药对照微胶囊的相同药物形式不共享。

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