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

紫外线 B (UVB) 照射会导致自由基产生、增加炎症和氧化应激，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黄酮类化合物，但是，高脂溶性使其难以留在有活力的皮肤层中。因此，本研究评估了与相同剂量的游离 QC（非活性剂量）和添加到配方中用于局部给药的未加载微胶囊在针对皮肤的 UVB 照射的小鼠模型中相比，QC 的微胶囊化是否会增强其活性。含有槲皮素负载微胶囊 (TFcQCMC) 的局部制剂在 4 °C、室温和 40 °C 下 6 个月具有物理化学（颜色、稠度、相分离和 pH 值）和功能性抗氧化稳定性。TFcQCMC 抑制由 GSH（还原型谷胱甘肽）观察到的 UVB 引发的抗氧化剂消耗、还原铁的能力、清除 2,2'-azinobis 自由基的能力和过氧化氢酶活性。TFcQCMC 还抑制氧化标志物（脂质氢过氧化物和超氧阴离子产生）。关于炎症，TFcQCMC 减少了炎症细胞因子的产生、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 的药理活性不与含有相同剂量游离 QC 或未加载对照微胶囊的相同药物形式共享。2'-azinobis 自由基和过氧化氢酶活性。TFcQCMC 还抑制氧化标志物（脂质氢过氧化物和超氧阴离子产生）。关于炎症，TFcQCMC 减少了炎症细胞因子的产生、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 的药理活性不与含有相同剂量游离 QC 或未加载对照微胶囊的相同药物形式共享。2'-azinobis 自由基和过氧化氢酶活性。TFcQCMC 还抑制氧化标志物（脂质氢过氧化物和超氧阴离子产生）。关于炎症，TFcQCMC 减少了炎症细胞因子的产生、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 的药理活性不与含有相同剂量游离 QC 或未加载对照微胶囊的相同药物形式共享。肥大细胞和晒伤细胞计数。TFcQCMC 的药理活性不与含有相同剂量游离 QC 或未加载对照微胶囊的相同药物形式共享。肥大细胞和晒伤细胞计数。TFcQCMC 的药理活性不与含有相同剂量游离 QC 或未加载对照微胶囊的相同药物形式共享。