Effect of quercetin and resveratrol co-incorporated in liposomes against inflammatory/oxidative response associated with skin cancer
Effect of quercetin and resveratrol co-incorporated in liposomes against inflammatory/oxidative response associated with skin cancer
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DOI：
10.1016/j.ijpharm.2016.09.014
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发表时间：
2016-11-20
影响因子：
5.8
通讯作者：
Manconi, Maria
中科院分区：
文献类型：
--
作者：
Caddeo, Carla;Nacher, Amparo;Manconi, Maria
本研究报道了脂质体的发展，用于共同递送天然存在的多酚，即槲皮素和白藜芦醇。通过光散射、低温透射电镜、SAXS等观察发现，制备出小的球形单/双层囊泡。槲皮素和白藜芦醇在脂质体中的掺入不影响其内在的抗氧化活性，因为DPPH自由基几乎完全被抑制。当它们在脂质体中配制时，细胞对多酚的摄取更高，特别是当它们共载而不是作为单一试剂时，这导致了成纤维细胞中清除ROS的卓越能力。在小鼠皮肤损伤模型中评估脂质体中多酚的体内功效。局部给药脂质体可显著改善组织损伤，显著减少水肿和白细胞浸润。因此，基于多酚囊泡配方的建议方法可能在治疗与癌前/癌性皮肤病变相关的炎症/氧化应激方面具有价值。(C) 2016 Elsevier B.V.版权所有
The present investigation reports the development of liposomes for the co-delivery of naturally occurring polyphenols, namely quercetin and resveratrol. Small, spherical, uni/bilamellar vesicles were produced, as demonstrated by light scattering, cryo-TEM, SAXS. The incorporation of quercetin and resveratrol in liposomes did not affect their intrinsic antioxidant activity, as DPPH radical was almost completely inhibited. The cellular uptake of the polyphenols was higher when they were formulated in liposomes, and especially when co-loaded rather than as single agents, which resulted in a superior ability to scavenge ROS in fibroblasts. The in vivo efficacy of the polyphenols in liposomes was assessed in a mouse model of skin lesion. The topical administration of liposomes led to a remarkable amelioration of the tissue damage, with a significant reduction of oedema and leukocyte infiltration. Therefore, the proposed approach based on polyphenol vesicular formulation may be of value in the treatment of inflammation/oxidative stress associated with pre-cancerous/cancerous skin lesions. (C) 2016 Elsevier B.V. All rights reserved.