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

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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 Fe3+ 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.

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Acknowledgements

The authors appreciate the staff from the National Engineering Research Center of Seafood of Dalian Polytechnic University for their technical assistance.

Funding

This work was supported by the National Natural Science Foundation of China (32172208) and Central Funds Guiding the Local Science and Technology Development of China (2020JH6/10500002).

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

    Si-hui Li, Yan-fei Li, Di Wu, Yu Xu, Hui-jia Yan & Jiang-Ning Hu

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Contributions

Conceptualization, methodology, and writing—original draft, S H Li; methodology and investigation, Y F Li; writing review and editing, D Wu; data curation and writing editing, Y Xu; methodology and investigation, H J Yan; funding acquisition and writing editing, J N Hu. All authors read and approved the final manuscript.

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Correspondence to Jiang-Ning Hu.

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All procedures of this investigation were approved by the Experimental Animal Ethics Committee of National Engineering Research Center of Seafood of Dalian Polytechnic University (Dalian, China, Animal JN. No DLPU2022010).

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13346_2023_1428_MOESM1_ESM.docx

The characterization images of SA and SA-TF microgels, Fig. S1. Microscopy images of SA microgels in simulated digestive solutions at various stages, Fig. S2A. Swelling indexes of SA microgels and SA-TF microgels, Fig. S2B and C. The synthesis process and biocompatibility of Pue@SA-TF microgels, results of protein expression by Western blotting, Fig S3. (DOCX 1379 KB)

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Li, Sh., Li, Yf., Wu, D. et al. Metal-polyphenol microgels for oral delivery of puerarin to alleviate the onset of diabetes. Drug Deliv. and Transl. Res. 14, 757–772 (2024). https://doi.org/10.1007/s13346-023-01428-2

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