Dept. of Scienze della Vita e dell'Ambiente, University of Cagliari, Cagliari, Italy.
Nanoscale. 2018 Jan 25;10(4):1957-1969. doi: 10.1039/c7nr05929a.
Nutriosomes, new phospholipid nanovesicles specifically designed for intestinal protection were developed by simultaneously loading a water-soluble dextrin (Nutriose® FM06) and a natural antioxidant (curcumin). Nutriosomes were easily fabricated in a one-step, organic solvent-free procedure. The stability and delivery performances of the vesicles were improved by adding hydroxypropyl methylcellulose. All the vesicles were small in size (mean diameter ∼168 nm), negatively charged (zeta potential ∼-38 mV, irrespective of their composition), and self-assembled predominantly in unilamellar vesicles stabilized by the presence of Nutriose®, which was located in both the inter-lamellar and inter-vesicle media, as confirmed by cryo-TEM and SAXS investigation. The dextrin acted also as a cryo-protector, avoiding vesicle collapse during the lyophilization process, and as a protector against high ionic strength and pH changes encountered in the gastrointestinal environment. Thanks to the antioxidant properties of curcumin, nutriosomes provided an optimal protective effect against hydrogen peroxide-induced oxidative stress in Caco-2 cells. Moreover, these innovative vesicles showed promising efficacy in vivo, as they improved the bioavailability and the biodistribution of both curcumin and dextrin upon oral administration, which acted synergically in reducing colonic damage chemically induced in rats.
新型磷脂纳米囊泡 Nutriosomes 被专门设计用于肠道保护，它通过同时负载水溶性糊精（Nutriose® FM06）和天然抗氧化剂（姜黄素）而制成。Nutriosomes 可以通过一步、无有机溶剂的方法轻松制备。通过添加羟丙基甲基纤维素，可以提高囊泡的稳定性和传递性能。所有囊泡的粒径都较小（平均直径约为 168nm），带负电荷（zeta 电位约为-38mV，无论其组成如何），并且主要自组装成由 Nutriose®稳定的单层囊泡，这一点通过 cryo-TEM 和 SAXS 研究得到了证实。糊精还可以作为冷冻保护剂，避免在冷冻干燥过程中囊泡塌陷，并可以保护囊泡免受胃肠道环境中遇到的高离子强度和 pH 值变化的影响。由于姜黄素具有抗氧化性能，Nutriosomes 可以为 Caco-2 细胞提供对抗过氧化氢诱导的氧化应激的最佳保护作用。此外，这些创新的囊泡在体内表现出了有希望的疗效，因为它们可以提高姜黄素和糊精口服后的生物利用度和生物分布，从而协同作用减轻大鼠化学诱导的结肠损伤。
