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Transport study of different proportions of puerarin-glycyrrhizic acid self-assembled nanoparticles in a Caco-2 cell monolayer model
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DOI   10.11656/j.issn.1673-9043.2026.04.07
Key Words   puerarin;glycyrrhizic acid;self-assembly;nanoparticle;Caco-2 cell model;transport characteristics
Author NameAffiliationE-mail
HOU Xiaotong National Key Laboratory of Innovative Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China 
 
SHEN Pengyu National Key Laboratory of Innovative Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China 
 
HUANG Xiaochao National Key Laboratory of Innovative Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China 
 
ZHANG Linhui National Key Laboratory of Innovative Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China 
 
HU Yiwen National Key Laboratory of Innovative Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China 
 
JIAN Ruihong National Key Laboratory of Innovative Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China 
 
PI Jiaxin National Key Laboratory of Innovative Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China 
pijiaxin@tjutcm.edu.cn 
Abstract
    [Objective] To enhance the solubility and intestinal absorption of puerarin(Pue),the study investigated the absorption and transport characteristics of self-assembled puerarin-glycyrrhizic acid nanoparticles(Pue-GA NPs) prepared at different molar ratios using a Caco-2 cell monolayer model. The research was inspired by the component interactions occurring during the decoction of the traditional Chinese herbal pair Radix Puerariae-Radix Glycyrrhizae. [Methods] Pue-GA NPs were prepared via a solvent evaporation method,and their particle size and morphology were characterized. The interactions between Pue and glycyrrhizic acid(GA) were evaluated through UV-visible spectroscopy and molecular docking. Transwell assays were employed to compare the transmembrane transport of physical mixtures versus self-assembled nanoparticles at different molar ratios. Additionally,four endocytic inhibitors were applied to elucidate the underlying absorption mechanisms. [Results] Pue-GA NPs with different molar ratios formed stable spherical nanoparticles,and hydrogen bonding was involved in their self-assembly. Caco-2 transport studies revealed that Pue-GA NPs at a 1∶1 molar ratio exhibited the highest transmembrane transport efficiency,which was significantly greater than that of the physical mixture. All four endocytic inhibitors reduced nanoparticle transport,with chlorpromazine showing the most pronounced inhibitory effect. [Conclusion] Glycyrrhizic acid and puerarin can efficiently self-assemble into stable nanoparticles. The Pue-GA NPs notably improved the transport efficiency of Pue across the Caco-2 cell monolayer,with the 1∶1 molar ratio formulation exhibiting the best performance. The enhanced absorption was primarily mediated via a clathrin-dependent endocytic pathway.

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