MgAl monolayer hydrotalcite increases the hypoglycemic effect of berberine by enhancing its oral bioavailability

MgAl monolayer hydrotalcite increases the hypoglycemic effect of berberine by enhancing its oral bioavailability

Berberine (BBR) is a potential novel agent to treat diabetes, but its oral bioavailability is restricted by the poor solubility, which greatly limits its clinical application. Here, a new drug delivery system of BBR-MgAl monolayer hydrotalcite (BBR/MLDH) was prepared to increase the solubility and b...

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Main Authors: Aiting Wang, Wei Yang, Xinyu Yang, Xuan Mei, Tingting Hu, Ruizheng Liang, Dali Meng, Dan Yan
Format: Article
Language:English
Published: Elsevier 2020-07-01
Series:Biomedicine & Pharmacotherapy
Subjects:
Berberine
Layered double hydroxide
Monolayer nanosheets
Pharmacokinetics
Hypoglycemic effect
Online Access:http://www.sciencedirect.com/science/article/pii/S0753332220303322
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spelling doaj-67e26bbd7b574d03978f6a14bcbb22112021-05-20T07:41:37ZengElsevierBiomedicine & Pharmacotherapy0753-33222020-07-01127110140MgAl monolayer hydrotalcite increases the hypoglycemic effect of berberine by enhancing its oral bioavailabilityAiting Wang0Wei Yang1Xinyu Yang2Xuan Mei3Tingting Hu4Ruizheng Liang5Dali Meng6Dan Yan7Beijing Shijitan Hospital, Capital Medical University, Beijing, 100038, China; Beijing Key Laboratory of Bio-characteristic Profiling for Evaluation of Clinical Rational Drug Use, Beijing, 100038, ChinaBeijing Shijitan Hospital, Capital Medical University, Beijing, 100038, China; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang, 110016, ChinaBeijing Shijitan Hospital, Capital Medical University, Beijing, 100038, China; Beijing Key Laboratory of Bio-characteristic Profiling for Evaluation of Clinical Rational Drug Use, Beijing, 100038, ChinaState Key Laboratory of Chemical Resource Engineering, Beijing Advanced Innovation Center for Soft Matter Science and Engineering, Beijing University of Chemical Technology, Beijing, 100029, ChinaState Key Laboratory of Chemical Resource Engineering, Beijing Advanced Innovation Center for Soft Matter Science and Engineering, Beijing University of Chemical Technology, Beijing, 100029, ChinaState Key Laboratory of Chemical Resource Engineering, Beijing Advanced Innovation Center for Soft Matter Science and Engineering, Beijing University of Chemical Technology, Beijing, 100029, China; Corresponding authors at: Beijing Key Laboratory of Bio-characteristic Profiling for Evaluation of Clinical Rational Drug Use, Beijing, 100038, China.Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang, 110016, China; Beijing Key Laboratory of Bio-characteristic Profiling for Evaluation of Clinical Rational Drug Use, Beijing, 100038, China; Corresponding authors at: Beijing Key Laboratory of Bio-characteristic Profiling for Evaluation of Clinical Rational Drug Use, Beijing, 100038, China.Beijing Shijitan Hospital, Capital Medical University, Beijing, 100038, China; Beijing Key Laboratory of Bio-characteristic Profiling for Evaluation of Clinical Rational Drug Use, Beijing, 100038, China; Corresponding authors at: Beijing Key Laboratory of Bio-characteristic Profiling for Evaluation of Clinical Rational Drug Use, Beijing, 100038, China.Berberine (BBR) is a potential novel agent to treat diabetes, but its oral bioavailability is restricted by the poor solubility, which greatly limits its clinical application. Here, a new drug delivery system of BBR-MgAl monolayer hydrotalcite (BBR/MLDH) was prepared to increase the solubility and bioavailability of BBR. The results showed that BBR/MLDH presented as a uniform hexagonal plate-like particle with a loading capacity of 28.61 %, a diameter of ∼70 nm and a thickness of ∼1.5 nm. The solubility and dissolution of BBR increased when loading onto MLDH. Compared with BBR, pharmacokinetics of BBR/MLDH in rats showed significant enhancement (P < 0.01) in area under the curve (AUC) and the peak plasma concentration (Cmax), suggesting the bioavailability of BBR was improved. Furthermore, BBR/MLDH showed more potent effects in reducing fasting blood glucose, ameliorating glucose tolerance and insulin resistance comparing to the equivalent dose of BBR. In a word, the solubility, oral bioavailability and hypoglycemic effect of BBR could be improved by loading onto MLDH.http://www.sciencedirect.com/science/article/pii/S0753332220303322BerberineLayered double hydroxideMonolayer nanosheetsPharmacokineticsHypoglycemic effect
collection DOAJ
language English
format Article
sources DOAJ
author Aiting Wang
Wei Yang
Xinyu Yang
Xuan Mei
Tingting Hu
Ruizheng Liang
Dali Meng
Dan Yan
spellingShingle Aiting Wang
Wei Yang
Xinyu Yang
Xuan Mei
Tingting Hu
Ruizheng Liang
Dali Meng
Dan Yan
MgAl monolayer hydrotalcite increases the hypoglycemic effect of berberine by enhancing its oral bioavailability
Biomedicine & Pharmacotherapy
Berberine
Layered double hydroxide
Monolayer nanosheets
Pharmacokinetics
Hypoglycemic effect
author_facet Aiting Wang
Wei Yang
Xinyu Yang
Xuan Mei
Tingting Hu
Ruizheng Liang
Dali Meng
Dan Yan
author_sort Aiting Wang
title MgAl monolayer hydrotalcite increases the hypoglycemic effect of berberine by enhancing its oral bioavailability
title_short MgAl monolayer hydrotalcite increases the hypoglycemic effect of berberine by enhancing its oral bioavailability
title_full MgAl monolayer hydrotalcite increases the hypoglycemic effect of berberine by enhancing its oral bioavailability
title_fullStr MgAl monolayer hydrotalcite increases the hypoglycemic effect of berberine by enhancing its oral bioavailability
title_full_unstemmed MgAl monolayer hydrotalcite increases the hypoglycemic effect of berberine by enhancing its oral bioavailability
title_sort mgal monolayer hydrotalcite increases the hypoglycemic effect of berberine by enhancing its oral bioavailability
publisher Elsevier
series Biomedicine & Pharmacotherapy
issn 0753-3322
publishDate 2020-07-01
description Berberine (BBR) is a potential novel agent to treat diabetes, but its oral bioavailability is restricted by the poor solubility, which greatly limits its clinical application. Here, a new drug delivery system of BBR-MgAl monolayer hydrotalcite (BBR/MLDH) was prepared to increase the solubility and bioavailability of BBR. The results showed that BBR/MLDH presented as a uniform hexagonal plate-like particle with a loading capacity of 28.61 %, a diameter of ∼70 nm and a thickness of ∼1.5 nm. The solubility and dissolution of BBR increased when loading onto MLDH. Compared with BBR, pharmacokinetics of BBR/MLDH in rats showed significant enhancement (P < 0.01) in area under the curve (AUC) and the peak plasma concentration (Cmax), suggesting the bioavailability of BBR was improved. Furthermore, BBR/MLDH showed more potent effects in reducing fasting blood glucose, ameliorating glucose tolerance and insulin resistance comparing to the equivalent dose of BBR. In a word, the solubility, oral bioavailability and hypoglycemic effect of BBR could be improved by loading onto MLDH.
topic Berberine
Layered double hydroxide
Monolayer nanosheets
Pharmacokinetics
Hypoglycemic effect
url http://www.sciencedirect.com/science/article/pii/S0753332220303322
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