Manca Maria Letizia, Castangia Ines, Caddeo Carla, Pando Daniel, Escribano Elvira, Valenti Donatella, Lampis Sandrina, Zaru Marco, Fadda Anna Maria, Manconi Maria
Dept. Scienze della Vita e dell'Ambiente, CNBS, University of Cagliari, Cagliari, Italy.
Dept. Scienze della Vita e dell'Ambiente, CNBS, University of Cagliari, Cagliari, Italy.
Colloids Surf B Biointerfaces. 2014 Nov 1;123:566-74. doi: 10.1016/j.colsurfb.2014.09.059. Epub 2014 Oct 7.
Quercetin was incorporated in glycerosomes, new phospholipid-glycerol vesicles, and their protective effect against oxidative stress skin damages was extensively evaluated. In particular, the concentration-dependent effect of glycerol (from 10 to 50%) on vesicle suitability as cutaneous carriers of quercetin was carefully assessed. All vesicles were unilamellar and small in size (∼80-110 nm), as confirmed by cryo-TEM observation, with a drug incorporation efficiency ranging between 81 and 91%. SAXS studies, performed to investigate the bilayer arrangement, indicated a strong, dose-dependent interaction of glycerol with the polar portions of the phospholipid molecules, while quercetin did not significantly change the bilayer packing. In vitro studies on newborn pig skin underlined the concentration-dependent ability of glycerosomes to promote quercetin accumulation in the different layers, also confirmed by confocal microscopic observation of skin treated with fluorescent vesicles. Quercetin incorporated into liposomal and glycerosomal nanoformulations showed a strong ability to scavenge free radicals (DPPH test) and protect human keratinocytes in vitro against hydrogen peroxide damage. Moreover, quercetin-loaded vesicles were avidly taken up by keratinocytes in vitro. Overall, results indicate 40 and 50% glycerosomes as promising nanosystems for the improvement of cutaneous quercetin delivery and keratinocyte protection against oxidative stress damage.
槲皮素被包裹于甘油脂质体（一种新型磷脂 - 甘油囊泡）中，并对其对氧化应激性皮肤损伤的保护作用进行了广泛评估。特别地，仔细评估了甘油（10%至50%）对囊泡作为槲皮素皮肤载体适用性的浓度依赖性影响。经冷冻透射电子显微镜观察证实，所有囊泡均为单层且尺寸较小（约80 - 110纳米），药物包封效率在81%至91%之间。为研究双层排列而进行的小角X射线散射研究表明，甘油与磷脂分子的极性部分存在强烈的剂量依赖性相互作用，而槲皮素并未显著改变双层堆积。对新生猪皮肤的体外研究强调了甘油脂质体促进槲皮素在不同层中积累的浓度依赖性能力，用荧光囊泡处理皮肤的共聚焦显微镜观察也证实了这一点。包裹于脂质体和甘油脂质体纳米制剂中的槲皮素在体外表现出强大的清除自由基能力（DPPH测试），并能保护人角质形成细胞免受过氧化氢损伤。此外，载有槲皮素的囊泡在体外能被角质形成细胞大量摄取。总体而言，结果表明40%和50%的甘油脂质体是用于改善皮肤槲皮素递送以及角质形成细胞免受氧化应激损伤的有前景的纳米系统。
