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用于葛根素口服递送以缓解糖尿病发病的金属-多酚微凝胶

Metal-polyphenol microgels for oral delivery of puerarin to alleviate the onset of diabetes.

作者信息

Li Si-Hui, Li Yan-Fei, Wu Di, Xu Yu, Yan Hui-Jia, Hu Jiang-Ning

机构信息

Research Group of Nutrition and Health, National Engineering Research Center of Seafood, Dalian Polytechnic University, Dalian, 116034, China.

出版信息

Drug Deliv Transl Res. 2024 Mar;14(3):757-772. doi: 10.1007/s13346-023-01428-2. Epub 2023 Sep 28.

Abstract

Puerarin (Pue) is a naturally bioactive compound with many potential functions in regulating blood glucose and lipid metabolism. However, the low bioavailability and rapid elimination in vivo limit the application of Pue in diabetic treatment. Here, we developed a metal-polyphenol-functionalized microgel to effectively deliver Pue in vivo and eventually alleviate the onset of diabetes. Pue was initially encapsulated in alginate beads through electrospray technology, and further immersed in Fe and tannic acid solution from tannic acid (TA)-iron (Fe) coatings (TF). These constructed Pue@SA-TF microgels exhibited uniform spheres with an average size of 367.89 ± 18.74 µm and high encapsulation efficiency of Pue with 61.16 ± 1.39%. In vivo experiments proved that compared with free Pue and microgels without TF coatings, the biological distribution of Pue@SA-TF microgels specifically accumulated in the small intestine, prolonged the retention time of Pue, and achieved a high effectiveness in vivo. Anti-diabetic experimental results showed that Pue@SA-TF microgels significantly improved the levels of blood glucose, blood lipid, and oxidative stress in diabetic mice. Meanwhile, histopathological observations indicated that Pue@SA-TF microgels could significantly alleviate the damage to the liver, kidney, and pancreas in diabetic mice. Our study provided an effective strategy for oral delivery of Pue and achieved high anti-diabetic efficacy.

摘要

葛根素(Pue)是一种天然生物活性化合物,在调节血糖和脂质代谢方面具有多种潜在功能。然而,其低生物利用度和在体内的快速消除限制了葛根素在糖尿病治疗中的应用。在此,我们开发了一种金属-多酚功能化微凝胶,以有效地在体内递送葛根素,并最终缓解糖尿病的发病。葛根素最初通过电喷雾技术包裹在藻酸盐珠中,然后进一步浸入由单宁酸(TA)-铁(Fe)涂层(TF)形成的铁和单宁酸溶液中。这些构建的Pue@SA-TF微凝胶呈现出平均尺寸为367.89±18.74 µm的均匀球体,对葛根素的包封效率高,为61.16±1.39%。体内实验证明,与游离葛根素和没有TF涂层的微凝胶相比,Pue@SA-TF微凝胶的生物分布特异性地在小肠中积累,延长了葛根素的保留时间,并在体内实现了高效能。抗糖尿病实验结果表明,Pue@SA-TF微凝胶显著改善了糖尿病小鼠的血糖、血脂和氧化应激水平。同时,组织病理学观察表明,Pue@SA-TF微凝胶可显著减轻糖尿病小鼠肝脏、肾脏和胰腺的损伤。我们的研究为葛根素的口服递送提供了一种有效策略,并实现了高抗糖尿病疗效。

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