Characterization, pharmacokinetics, and hypoglycemic effect of berberine loaded solid lipid nanoparticles

Mei Xue, Ming-xing Yang, Wei Zhang, Xiu-min Li, De-hong Gao, Zhi-min Ou, Zhi-peng Li, Su-huan Liu, Xue-jun Li, Shu-yu Yang Xiamen Diabetes Institute, The First Affiliated Hospital of Xiamen University, Xiamen, People’s Republic of China Abstract: The high aqueous solubility, poor permeabil...

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Autores principales:	Xue M, Yang MX, Zhang W, Li XM, Gao DH, Ou ZM, Li ZP, Liu SH, Li XJ, Yang SY
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/e30d2def10da4efab80bd562edd90dd5
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spelling	oai:doaj.org-article:e30d2def10da4efab80bd562edd90dd52021-12-02T02:44:06ZCharacterization, pharmacokinetics, and hypoglycemic effect of berberine loaded solid lipid nanoparticles1176-91141178-2013https://doaj.org/article/e30d2def10da4efab80bd562edd90dd52013-12-01T00:00:00Zhttp://www.dovepress.com/characterization-pharmacokinetics-and-hypoglycemic-effect-of-berberine-a15184https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Mei Xue, Ming-xing Yang, Wei Zhang, Xiu-min Li, De-hong Gao, Zhi-min Ou, Zhi-peng Li, Su-huan Liu, Xue-jun Li, Shu-yu Yang Xiamen Diabetes Institute, The First Affiliated Hospital of Xiamen University, Xiamen, People’s Republic of China Abstract: The high aqueous solubility, poor permeability, and absorption of berberine (BBR) result in its low plasma level after oral administration, which greatly limits its clinical application. BBR solid lipid nanoparticles (SLNs) were prepared to achieve improved bioavailability and prolonged effect. Developed SLNs showed homogeneous spherical shapes, small size (76.8 nm), zeta potential (7.87 mV), encapsulation efficiency (58%), and drug loading (4.2%). The power of X-ray diffraction combined with 1H nuclear magnetic resonance spectroscopy was employed to analyze chemical functional groups and the microstructure of BBR-SLNs, and indicated that the drug was wrapped in a lipid carrier. Single dose (50 mg/kg) oral pharmacokinetic studies in rats showed significant improvement (P<0.05) in the peak plasma concentration, area under the curve, and variance of mean residence time of BBR-SLNs when compared to BBR alone (P<0.05), suggesting improved bioavailability. Furthermore, oral administration of both BBR and BBR-SLNs significantly suppressed body weight gain, fasting blood glucose levels, and homeostasis assessment of insulin resistance, and ameliorated impaired glucose tolerance and insulin tolerance in db/db diabetic mice. BBR-SLNs at high dose (100 mg/kg) showed more potent effects when compared to an equivalent dose of BBR. Morphologic analysis demonstrated that BBR-SLNs potentially promoted islet function and protected the islet from regeneration. In conclusion, our study demonstrates that by entrapping BBR into SLNs the absorption of BBR and its anti-diabetic action were effectively enhanced. Keywords: berberine, solid lipid nanoparticles, pharmacokinetic, hypoglycemic effectXue MYang MXZhang WLi XMGao DHOu ZMLi ZPLiu SHLi XJYang SYDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss Issue 1, Pp 4677-4687 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Xue M Yang MX Zhang W Li XM Gao DH Ou ZM Li ZP Liu SH Li XJ Yang SY Characterization, pharmacokinetics, and hypoglycemic effect of berberine loaded solid lipid nanoparticles
description	Mei Xue, Ming-xing Yang, Wei Zhang, Xiu-min Li, De-hong Gao, Zhi-min Ou, Zhi-peng Li, Su-huan Liu, Xue-jun Li, Shu-yu Yang Xiamen Diabetes Institute, The First Affiliated Hospital of Xiamen University, Xiamen, People’s Republic of China Abstract: The high aqueous solubility, poor permeability, and absorption of berberine (BBR) result in its low plasma level after oral administration, which greatly limits its clinical application. BBR solid lipid nanoparticles (SLNs) were prepared to achieve improved bioavailability and prolonged effect. Developed SLNs showed homogeneous spherical shapes, small size (76.8 nm), zeta potential (7.87 mV), encapsulation efficiency (58%), and drug loading (4.2%). The power of X-ray diffraction combined with 1H nuclear magnetic resonance spectroscopy was employed to analyze chemical functional groups and the microstructure of BBR-SLNs, and indicated that the drug was wrapped in a lipid carrier. Single dose (50 mg/kg) oral pharmacokinetic studies in rats showed significant improvement (P<0.05) in the peak plasma concentration, area under the curve, and variance of mean residence time of BBR-SLNs when compared to BBR alone (P<0.05), suggesting improved bioavailability. Furthermore, oral administration of both BBR and BBR-SLNs significantly suppressed body weight gain, fasting blood glucose levels, and homeostasis assessment of insulin resistance, and ameliorated impaired glucose tolerance and insulin tolerance in db/db diabetic mice. BBR-SLNs at high dose (100 mg/kg) showed more potent effects when compared to an equivalent dose of BBR. Morphologic analysis demonstrated that BBR-SLNs potentially promoted islet function and protected the islet from regeneration. In conclusion, our study demonstrates that by entrapping BBR into SLNs the absorption of BBR and its anti-diabetic action were effectively enhanced. Keywords: berberine, solid lipid nanoparticles, pharmacokinetic, hypoglycemic effect
format	article
author	Xue M Yang MX Zhang W Li XM Gao DH Ou ZM Li ZP Liu SH Li XJ Yang SY
author_facet	Xue M Yang MX Zhang W Li XM Gao DH Ou ZM Li ZP Liu SH Li XJ Yang SY
author_sort	Xue M
title	Characterization, pharmacokinetics, and hypoglycemic effect of berberine loaded solid lipid nanoparticles
title_short	Characterization, pharmacokinetics, and hypoglycemic effect of berberine loaded solid lipid nanoparticles
title_full	Characterization, pharmacokinetics, and hypoglycemic effect of berberine loaded solid lipid nanoparticles
title_fullStr	Characterization, pharmacokinetics, and hypoglycemic effect of berberine loaded solid lipid nanoparticles
title_full_unstemmed	Characterization, pharmacokinetics, and hypoglycemic effect of berberine loaded solid lipid nanoparticles
title_sort	characterization, pharmacokinetics, and hypoglycemic effect of berberine loaded solid lipid nanoparticles
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/e30d2def10da4efab80bd562edd90dd5
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Characterization, pharmacokinetics, and hypoglycemic effect of berberine loaded solid lipid nanoparticles

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