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直链淀粉纳米粒经口服给药传递生物活性物质:离体和在体研究。

Gliadin nanoparticles for oral administration of bioactives: Ex vivo and in vivo investigations.

机构信息

Department of Health Sciences, University "Magna Græcia" of Catanzaro, Campus Universitario "S. Venuta", 88100 Catanzaro, Italy.

Department of Chemistry and Pharmaceutical Technology, University of Navarra, C/Irunlarrea 1, 31008 Pamplona, Spain.

出版信息

Int J Biol Macromol. 2023 Sep 30;249:126111. doi: 10.1016/j.ijbiomac.2023.126111. Epub 2023 Aug 2.

Abstract

This study aims to provide a thorough characterization of Brij O2-stabilized gliadin nanoparticles to be used for the potential oral administration of various compounds. Different techniques were used in order to evaluate their physico-chemical features and then in vivo studies in rats were performed for the investigation of their biodistribution and gastrointestinal transit profiles. The results showed that the gliadin nanoparticles accumulated in the mucus layer of the bowel mucosa and evidenced their ability to move along the digestive systems of the animals. The incubation of the nanosystems with Caenorhabditis elegans, used as an additional in vivo model, confirmed the intake of the particles and evidenced their presence along the entire gastrointestinal tract of these nematodes. The gliadin nanoparticles influenced neither the egg-laying activity of the worms nor their metabolism of lipids up to 10 μg/mL of nanoformulation. The systems decreased the content of the age-related lipofuscin pigment in the nematodes in a dose-dependent manner, demonstrating a certain antioxidant activity. Lastly, dihydroethidium staining showed the absence of oxidative stress upon incubation of the worms together with the formulations, confirming their safe profile. This data paves the way for the future application of the proposed nanosystems regarding the oral delivery of various bioactives.

摘要

本研究旨在对 Brij O2 稳定的醇溶蛋白纳米粒进行全面表征,以期将各种化合物经口服递送至体内。我们采用了不同的技术来评估其物理化学特性,随后在大鼠体内进行了研究,以考察其体内分布和胃肠道转运特征。结果表明,醇溶蛋白纳米粒在肠黏膜的黏液层中聚集,并证明了它们在动物消化系统中迁移的能力。将纳米系统与秀丽隐杆线虫孵育,作为另一种体内模型,进一步证实了这些粒子的摄入,并证明了它们在这些线虫整个胃肠道中的存在。醇溶蛋白纳米粒在 10μg/mL 纳米制剂浓度下,既不影响线虫的产卵活性,也不影响其脂质代谢。该系统以剂量依赖的方式降低了线虫中与年龄相关的脂褐素色素的含量,表现出一定的抗氧化活性。最后,二氢乙锭染色显示,在与制剂共同孵育的情况下,蠕虫不存在氧化应激,这证实了其安全特性。这些数据为未来应用所提出的纳米系统来口服递送至体内各种生物活性物质铺平了道路。

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