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N-三甲基壳聚糖包覆靶向纳米粒提高牡荆素的口服生物利用度和抗氧化活性。

N-trimethyl chitosan coated targeting nanoparticles improve the oral bioavailability and antioxidant activity of vitexin.

机构信息

School of Health Science and Engineering, University of Shanghai for Science and Technology, Shanghai 200093, China; National Grain Industry (Urban Grain and Oil Security) Technology Innovation Center, Shanghai 200093, China.

School of Health Science and Engineering, University of Shanghai for Science and Technology, Shanghai 200093, China; National Grain Industry (Urban Grain and Oil Security) Technology Innovation Center, Shanghai 200093, China.

出版信息

Carbohydr Polym. 2022 Jun 15;286:119273. doi: 10.1016/j.carbpol.2022.119273. Epub 2022 Feb 23.

Abstract

Vitexin is a flavonoid which exerted many protective activities. However, the low bioavailability discounts the in vivo effects of vitexin. This study designed vitexin loaded bilayer nanoparticles by the assembly of soybean peptides and the coating of goblet cell targeting peptide CSKSSDYQC (CSK) coupled N-trimethyl chitosan (TMC), to improve the bioavailability of vitexin. The results showed that the bilayer nanoparticles could protect vitexin from being released in stomach and promote sustained release in intestine. Ex vivo experiments confirmed that nanoparticles promoted absorption of vitexin through tight junctions. Further in vivo studies suggested that the embedding of vitexin by nanoparticles increased the bioavailability and antioxidant activity of vitexin. Our results indicated that the nanoparticles could not only promote the absorption of vitexin, but also improve its in vivo antioxidant activity. Therefore, the reported nanoparticles could be effective delivery platforms to improve the bioavailability of vitexin.

摘要

牡荆素是一种黄酮类化合物,具有多种保护活性。然而,其生物利用度低,限制了牡荆素的体内作用。本研究通过大豆肽的组装和粘蛋白靶向肽 CSKSSDYQC(CSK)偶联的三甲基壳聚糖(TMC)的涂层,设计了牡荆素双层纳米粒,以提高牡荆素的生物利用度。结果表明,双层纳米粒可以防止牡荆素在胃中释放,并促进其在肠道中的持续释放。离体实验证实,纳米粒通过紧密连接促进牡荆素的吸收。进一步的体内研究表明,纳米粒将牡荆素包埋后增加了牡荆素的生物利用度和抗氧化活性。我们的结果表明,纳米粒不仅可以促进牡荆素的吸收,还可以提高其体内抗氧化活性。因此,所报道的纳米粒可以作为有效的递送平台,以提高牡荆素的生物利用度。

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