Caddeo Carla, Nacher Amparo, Vassallo Antonio, Armentano Maria Francesca, Pons Ramon, Fernàndez-Busquets Xavier, Carbone Claudia, Valenti Donatella, Fadda Anna Maria, Manconi Maria
Dept. of Science della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, University of Cagliari, Via Ospedale 72, 09124 Cagliari, Italy.
Dept. of Pharmacy and Pharmaceutical Technology, University of Valencia, Avda Vicente Andrés Estellés s/n, 46100 Burjassot, Valencia, Spain; Institute of Molecular Recognition and Technological Development, Inter-Universitary Institute from Polytechnic University of Valencia and University of Valencia, Spain.
Int J Pharm. 2016 Nov 20;513(1-2):153-163. doi: 10.1016/j.ijpharm.2016.09.014. Epub 2016 Sep 5.
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.
本研究报告了用于共同递送天然存在的多酚(即槲皮素和白藜芦醇)的脂质体的开发情况。通过光散射、冷冻透射电子显微镜(cryo-TEM)、小角X射线散射(SAXS)证明,制备出了小的球形单/双分子层囊泡。槲皮素和白藜芦醇掺入脂质体中并未影响其内在抗氧化活性,因为二苯基苦味酰基自由基(DPPH)几乎被完全抑制。当多酚以脂质体制剂形式存在时,其细胞摄取量更高,尤其是当它们共负载而非单独使用时,这导致在成纤维细胞中清除活性氧(ROS)的能力更强。在皮肤损伤小鼠模型中评估了脂质体中多酚的体内疗效。脂质体的局部给药导致组织损伤显著改善,水肿和白细胞浸润明显减少。因此,基于多酚囊泡制剂的所提出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。