Dept. of Scienze della Vita e dell'Ambiente, University of Cagliari, via Ospedale 72, 09124 Cagliari, Italy.
Dept. of Scienze della Vita e dell'Ambiente, University of Cagliari, via Ospedale 72, 09124 Cagliari, Italy.
Int J Pharm. 2019 Feb 10;556:82-88. doi: 10.1016/j.ijpharm.2018.11.073. Epub 2018 Dec 7.
In this paper, nutriosomes (phospholipid vesicles associated with Nutriose® FM06) were modified to obtain new systems aimed at enhancing the efficacy of curcumin in counteracting malaria infection upon oral administration. Eudragit® L100, a pH-sensitive co-polymer, was added to these vesicles, thus obtaining eudragit-nutriosomes, to improve their in vivo performances. Liposomes without eudragit and nutriose were also prepared as a reference. Cryo-TEM images showed the formation of multicompartment vesicles, with mean diameter around 300 nm and highly negative zeta potential. Vesicles were stable in fluids mimicking the gastro-intestinal content due to the high phospholipid concentration and the presence of gastro-resistant eudragit and digestion-resistant nutriose. Eudragit-nutriosomes disclosed promising performances in vitro and in vivo: they maximized the ability of curcumin to counteract oxidative stress in intestinal cells (Caco-2), which presumably reinforced its systemic efficacy. Orally-administered curcumin-loaded eudragit-nutriosomes increased significantly the survival of malaria-infected mice relative to free curcumin-treated controls.
本文中，我们对 nutriosomes（与 Nutriose® FM06 相关的磷脂囊泡）进行了修饰，以期获得新的系统，以提高姜黄素在口服抵抗疟疾感染方面的功效。向这些囊泡中添加了 pH 敏感的共聚物 Eudragit® L100，从而获得了 eudragit-nutriosomes，以改善其体内性能。还制备了不含 eudragit 和 nutriose 的脂质体作为对照。低温透射电镜图像显示形成了多室囊泡，平均直径约为 300nm，且具有高度负的 Zeta 电位。由于高磷脂浓度以及存在耐胃酸的 eudragit 和耐消化的 nutriose，囊泡在模拟胃肠内容物的液体中稳定。Eudragit-nutriosomes 在体外和体内均表现出良好的性能：它们使姜黄素抵抗肠细胞（Caco-2）氧化应激的能力最大化，这可能增强了其全身功效。与游离姜黄素处理的对照组相比，口服给予载有姜黄素的 eudragit-nutriosomes 显著提高了感染疟疾的小鼠的存活率。
