In vitro characterization and in vivo evaluation of nanostructured lipid curcumin carriers for intragastric administration

Min Fang, Yilin Jin, Wei Bao, Hui Gao, Mengjin Xu, Di Wang, Xia Wang, Ping Yao, Liegang LiuDepartment of Nutrition and Food Hygiene, Hubei Key Laboratory of Food Nutrition and Safety, and Ministry of Education Key Laboratory of Environment and Health, School of Public Health, Tongji Medical College,...

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Autores principales:	Fang M, Jin Y, Bao W, Gao H, Xu M, Wang D, Wang X, Yao P, Liu L
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/cb3c19473d2243cd93c3e145d6dea2be
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spelling	oai:doaj.org-article:cb3c19473d2243cd93c3e145d6dea2be2021-12-02T05:09:45ZIn vitro characterization and in vivo evaluation of nanostructured lipid curcumin carriers for intragastric administration1176-91141178-2013https://doaj.org/article/cb3c19473d2243cd93c3e145d6dea2be2012-10-01T00:00:00Zhttp://www.dovepress.com/in-vitro-characterization-and-in-vivo-evaluation-of-nanostructured-lip-a11219https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Min Fang, Yilin Jin, Wei Bao, Hui Gao, Mengjin Xu, Di Wang, Xia Wang, Ping Yao, Liegang LiuDepartment of Nutrition and Food Hygiene, Hubei Key Laboratory of Food Nutrition and Safety, and Ministry of Education Key Laboratory of Environment and Health, School of Public Health, Tongji Medical College, Huazhong University of Science and Technology, 13 Hangkong Road, Wuhan, People&rsquo;s Republic of ChinaBackground: Curcumin has a variety of pharmacological effects. However, poor water solubility and low oral bioavailability limit its clinical utility. A delivery system for nanostructured lipid carriers has been reported to be a promising approach to enhancing the oral absorption of curcumin. The aim of the present study was to investigate the pharmacokinetics, tissue distribution, and relative bioavailability of curcumin in rats after a single intragastric dose of a nanostructured lipid curcumin carrier formulation.Methods: Nanostructured lipid curcumin carriers were prepared using the ethanol dripping method and characterized in terms of the particle size, polydispersity index, zeta potential, differential scanning calorimetry, drug-loading capacity, encapsulation efficiency, and in vitro release. The pharmacokinetics and tissue distribution of nanostructured lipid curcumin carriers and curcumin suspension were compared after intragastric administration.Results: Nanostructured lipid curcumin carriers showed a significantly higher peak plasma concentration (564.94 &plusmn; 14.98 ng/mL versus 279.43 &plusmn; 7.21 ng/mL, P &lt; 0.01), a shorter time taken to reach peak plasma concentration (0.5 &plusmn; 0.01 hour versus 1.0 &plusmn; 0.12 hour, P &lt; 0.01), and a greater AUC0&ndash;&infin; (820.36 &plusmn; 25.11 mg &times; hour/L versus 344.11 &plusmn; 10.01 mg &times; hour/L, P &lt; 0.05) compared with curcumin suspension. In the tissue distribution studies, curcumin could be detected in the spleen, heart, liver, kidneys, lungs, and brain. Following intragastric administration of the nanostructured lipid curcumin carrier formulation, tissue concentrations of curcumin also increased, especially in the brain. The nanostructured lipid curcumin carrier formulation improved the ability of curcumin to cross the blood&ndash;brain barrier, with an 11.93-fold increase in the area under the curve achieved in the brain when compared with curcumin suspension.Conclusion: The nanostructured lipid carrier formulation significantly improved the oral bioavailability of curcumin and represents a promising method for its oral delivery.Keywords: curcumin, oral bioavailability, tissue distributionFang MJin YBao WGao HXu MWang DWang XYao PLiu LDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 5395-5404 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Fang M Jin Y Bao W Gao H Xu M Wang D Wang X Yao P Liu L In vitro characterization and in vivo evaluation of nanostructured lipid curcumin carriers for intragastric administration
description	Min Fang, Yilin Jin, Wei Bao, Hui Gao, Mengjin Xu, Di Wang, Xia Wang, Ping Yao, Liegang LiuDepartment of Nutrition and Food Hygiene, Hubei Key Laboratory of Food Nutrition and Safety, and Ministry of Education Key Laboratory of Environment and Health, School of Public Health, Tongji Medical College, Huazhong University of Science and Technology, 13 Hangkong Road, Wuhan, People&rsquo;s Republic of ChinaBackground: Curcumin has a variety of pharmacological effects. However, poor water solubility and low oral bioavailability limit its clinical utility. A delivery system for nanostructured lipid carriers has been reported to be a promising approach to enhancing the oral absorption of curcumin. The aim of the present study was to investigate the pharmacokinetics, tissue distribution, and relative bioavailability of curcumin in rats after a single intragastric dose of a nanostructured lipid curcumin carrier formulation.Methods: Nanostructured lipid curcumin carriers were prepared using the ethanol dripping method and characterized in terms of the particle size, polydispersity index, zeta potential, differential scanning calorimetry, drug-loading capacity, encapsulation efficiency, and in vitro release. The pharmacokinetics and tissue distribution of nanostructured lipid curcumin carriers and curcumin suspension were compared after intragastric administration.Results: Nanostructured lipid curcumin carriers showed a significantly higher peak plasma concentration (564.94 &plusmn; 14.98 ng/mL versus 279.43 &plusmn; 7.21 ng/mL, P &lt; 0.01), a shorter time taken to reach peak plasma concentration (0.5 &plusmn; 0.01 hour versus 1.0 &plusmn; 0.12 hour, P &lt; 0.01), and a greater AUC0&ndash;&infin; (820.36 &plusmn; 25.11 mg &times; hour/L versus 344.11 &plusmn; 10.01 mg &times; hour/L, P &lt; 0.05) compared with curcumin suspension. In the tissue distribution studies, curcumin could be detected in the spleen, heart, liver, kidneys, lungs, and brain. Following intragastric administration of the nanostructured lipid curcumin carrier formulation, tissue concentrations of curcumin also increased, especially in the brain. The nanostructured lipid curcumin carrier formulation improved the ability of curcumin to cross the blood&ndash;brain barrier, with an 11.93-fold increase in the area under the curve achieved in the brain when compared with curcumin suspension.Conclusion: The nanostructured lipid carrier formulation significantly improved the oral bioavailability of curcumin and represents a promising method for its oral delivery.Keywords: curcumin, oral bioavailability, tissue distribution
format	article
author	Fang M Jin Y Bao W Gao H Xu M Wang D Wang X Yao P Liu L
author_facet	Fang M Jin Y Bao W Gao H Xu M Wang D Wang X Yao P Liu L
author_sort	Fang M
title	In vitro characterization and in vivo evaluation of nanostructured lipid curcumin carriers for intragastric administration
title_short	In vitro characterization and in vivo evaluation of nanostructured lipid curcumin carriers for intragastric administration
title_full	In vitro characterization and in vivo evaluation of nanostructured lipid curcumin carriers for intragastric administration
title_fullStr	In vitro characterization and in vivo evaluation of nanostructured lipid curcumin carriers for intragastric administration
title_full_unstemmed	In vitro characterization and in vivo evaluation of nanostructured lipid curcumin carriers for intragastric administration
title_sort	in vitro characterization and in vivo evaluation of nanostructured lipid curcumin carriers for intragastric administration
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/cb3c19473d2243cd93c3e145d6dea2be
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In vitro characterization and in vivo evaluation of nanostructured lipid curcumin carriers for intragastric administration

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