Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles

Yike Huang,* Suya Deng,* Xinxin Luo, Yi Liu, Wanjun Xu, Jingmiao Pan, Min Wang, Zhining Xia School of Pharmaceutical Sciences and Innovative Drug Research Centre, Chongqing University, Chongqing 401331, People’s Republic of China*These authors contributed equally to this workCorrespondence...

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Autores principales:	Huang Y, Deng S, Luo X, Liu Y, Xu W, Pan J, Wang M, Xia Z
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	intestinal absorption galactosylated nanoparticles oral bioavailability absorption mechanism curcumin Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/878603e0b0794bfe88205d7bde3518ad
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spelling	oai:doaj.org-article:878603e0b0794bfe88205d7bde3518ad2021-12-02T09:16:28ZEvaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles1178-2013https://doaj.org/article/878603e0b0794bfe88205d7bde3518ad2019-12-01T00:00:00Zhttps://www.dovepress.com/evaluation-of-intestinal-absorption-mechanism-and-pharmacokinetics-of--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Yike Huang,* Suya Deng,* Xinxin Luo, Yi Liu, Wanjun Xu, Jingmiao Pan, Min Wang, Zhining Xia School of Pharmaceutical Sciences and Innovative Drug Research Centre, Chongqing University, Chongqing 401331, People’s Republic of China*These authors contributed equally to this workCorrespondence: Zhining XiaSchool of Pharmaceutical Sciences and Innovative Drug Research Centre, Chongqing University, Huxi Campus, No.55 Daxuecheng South Road, Shapingba, Chongqing 401331, People’s Republic of ChinaTel +86-13883077188Email znxia@cqu.edu.cnBackground: Most of the oral drugs have the properties of weak intestinal absorption and low bioavailability, which leads to little treatment to diseases. By nanotechnology, these drugs can be efficiently delivered to pass biological barriers and promote the cell uptake ability for the enhancement of the oral bioavailability.Methods: The present work chose the prepared curcumin-loaded galactosylated albumin nanoparticles (Gal-BSA NPs) as the nano-drug samples to study the intestinal capacity and the oral bioavailability.Results: The cell uptake assay showed that the Gal-BSA NPs could promote the internalization of more curcumin into the Caco-2 cells. Moreover, the cell uptake mechanism of Gal-BSA-Cur NPs depended on the clathrin-mediated endocytosis transport. The intestinal permeation assay using one Ussing chamber exhibited that the absorptive amounts of curcumin in Gal-BSA-Cur NPs group were 1.5-fold of pure curcumin group. Meanwhile, the permeation mechanism of Gal-BSA-Cur NPs across the intestine mainly depended on the passive transport. The pharmacokinetics study in vivo suggested that the oral bioavailability of Gal-BSA-Cur NPs was improved by 1.4-fold compared with pure curcumin.Conclusion: All results demonstrated that Gal-BSA NPs could improve the intestinal absorption capacity and oral bioavailability of curcumin through the double absorption mechanisms of the clathrin-mediated endocytosis and the passive transport.Keywords: intestinal absorption, galactosylated nanoparticles, oral bioavailability, absorption mechanism, curcumin  Huang YDeng SLuo XLiu YXu WPan JWang MXia ZDove Medical Pressarticleintestinal absorptiongalactosylated nanoparticlesoral bioavailabilityabsorption mechanismcurcuminMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 9721-9730 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	intestinal absorption galactosylated nanoparticles oral bioavailability absorption mechanism curcumin Medicine (General) R5-920
spellingShingle	intestinal absorption galactosylated nanoparticles oral bioavailability absorption mechanism curcumin Medicine (General) R5-920 Huang Y Deng S Luo X Liu Y Xu W Pan J Wang M Xia Z Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles
description	Yike Huang,* Suya Deng,* Xinxin Luo, Yi Liu, Wanjun Xu, Jingmiao Pan, Min Wang, Zhining Xia School of Pharmaceutical Sciences and Innovative Drug Research Centre, Chongqing University, Chongqing 401331, People’s Republic of China*These authors contributed equally to this workCorrespondence: Zhining XiaSchool of Pharmaceutical Sciences and Innovative Drug Research Centre, Chongqing University, Huxi Campus, No.55 Daxuecheng South Road, Shapingba, Chongqing 401331, People’s Republic of ChinaTel +86-13883077188Email znxia@cqu.edu.cnBackground: Most of the oral drugs have the properties of weak intestinal absorption and low bioavailability, which leads to little treatment to diseases. By nanotechnology, these drugs can be efficiently delivered to pass biological barriers and promote the cell uptake ability for the enhancement of the oral bioavailability.Methods: The present work chose the prepared curcumin-loaded galactosylated albumin nanoparticles (Gal-BSA NPs) as the nano-drug samples to study the intestinal capacity and the oral bioavailability.Results: The cell uptake assay showed that the Gal-BSA NPs could promote the internalization of more curcumin into the Caco-2 cells. Moreover, the cell uptake mechanism of Gal-BSA-Cur NPs depended on the clathrin-mediated endocytosis transport. The intestinal permeation assay using one Ussing chamber exhibited that the absorptive amounts of curcumin in Gal-BSA-Cur NPs group were 1.5-fold of pure curcumin group. Meanwhile, the permeation mechanism of Gal-BSA-Cur NPs across the intestine mainly depended on the passive transport. The pharmacokinetics study in vivo suggested that the oral bioavailability of Gal-BSA-Cur NPs was improved by 1.4-fold compared with pure curcumin.Conclusion: All results demonstrated that Gal-BSA NPs could improve the intestinal absorption capacity and oral bioavailability of curcumin through the double absorption mechanisms of the clathrin-mediated endocytosis and the passive transport.Keywords: intestinal absorption, galactosylated nanoparticles, oral bioavailability, absorption mechanism, curcumin
format	article
author	Huang Y Deng S Luo X Liu Y Xu W Pan J Wang M Xia Z
author_facet	Huang Y Deng S Luo X Liu Y Xu W Pan J Wang M Xia Z
author_sort	Huang Y
title	Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles
title_short	Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles
title_full	Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles
title_fullStr	Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles
title_full_unstemmed	Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles
title_sort	evaluation of intestinal absorption mechanism and pharmacokinetics of curcumin-loaded galactosylated albumin nanoparticles
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/878603e0b0794bfe88205d7bde3518ad
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Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles

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