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Absorption properties of baicalin-berberine complex and nanocrystals in Caco-2 monolayer model
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DOI   10.11656/j.issn.1673-9043.2023.01.17
Key Words   baicalin;berberine;Caco-2 cell monolayer model;cumulative amount transported;Papp
Author NameAffiliationE-mail
WANG Jilin State Key Laboratory of Component-based 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 
 
FENG Xiaojiao State Key Laboratory of Component-based 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 
 
DANG Wenli State Key Laboratory of Component-based 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 
 
LI Ziwei State Key Laboratory of Component-based 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 
 
LIU Zhidong State Key Laboratory of Component-based 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 State Key Laboratory of Component-based 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] The absorption properties of Baicalin (BA)-Berberine (BBR) complex and nanocrystals were studied,and the improvement of nanocrystals technology on the absorption properties of BA-BBR complex was discussed.[Methods] The concentration of the BA-BBR complex and nanocrystals on Caco-2 cell-line were selected by CCK-8 method. The Caco-2 cell monolayer model was constructed to explore the membrane transport of BA-BBR complex and nanocrystals. The influence of P-gp inhibitor verapamil on the cumulative transport volume and apparent permeability coefficient (Papp) was further studied.[Results] Papp values of BA and BBR in the complex group were lower than those in the physical mixture group. Compared with the complex group,the cumulative amount transported and Papp values of BA and BBR in nanocrystals group were significantly increased. Papp values of BA and BBR in nanocrystals were 1.3 and 2.3 times than those in the complex group,respectively. After verapamil addition,Papp values of BA and BBR were increased by 1.5 and 2.0 times separately in BA-BBR complex,while not significantly increased in nanocrystals.[Conclusion] Unlike physical mixtures,BA-BBR complex exhibited low permeability and high susceptibility on P-gp efflux. Nanocrystals could achieve the significantly permeability improvement and efflux reduction of BA-BBR complex.

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