Research progress on berberine with a special focus on its oral bioavailability

Liu, Chang-Shun; Zheng, Yurong; Zhang, Yingfeng; Long, Xiao-ying

doi:10.1016/j.fitote.2016.02.001

Cited by 282 publications

(223 citation statements)

References 117 publications

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“…D‐α‐tocopheryl polyethylene glycol 1,000 succinate at a concentration of 2.5% could improve AUC (0–36) of berberine by 1.9 times, probably via inhibition of the activity of P‐gps (Chen et al, ). Chitosan also enhances the absorption of berberine via regulating tight junctions shows mucoadhesive properties and enhances drug maintenance at the mucosal surface (Liu et al, ). The oral administration of berberine at 100 mg/kg plus 50 mg/kg sodium caprate also increased the AUC of berberine by 28%, in comparison with administration of berberine alone in rats.…”

Section: Clinical Pharmacokineticmentioning

confidence: 99%

“…Previously, we presented a table that lists the applications of the different parts of barberry (root, bark, leaf, and fruit) in folk medicine of Iran and other countries (Imenshahidi & Hosseinzadeh, ). Berberine is a quaternary benzylisoquinoline alkaloid from the structural class of protoberberines and present in the roots, rhizomes, stem, and bark of B. vulgaris and many other plants, including other species of Berberis ( Berberis aristata L., Berberis croatica L. , Berberis aquifolium L.), Coptis ( Coptis chinensis L., Coptis japonica L.), and Hydrastis ( Hydrastis Canadensis L.; Aggarwal, Prasad, Sung, Krishnan, & Guha, ; Liu, Zheng, Zhang, & Long, ).…”

Section: Introductionmentioning

confidence: 99%

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Berberine and barberry (Berberis vulgaris): A clinical review

Imenshahidi

Hosseinzadeh

2019

Phytotherapy Research

254

134

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Barberry (Berberis vulgaris L.) has different medicinal applications in folk medicine of Iran. Berberine, an alkaloid constituent of this plant, is present in the roots, rhizomes, stem, and bark of B. vulgaris and many other plants. There have been many clinical trials conducted that suggested a wide range of therapeutic applications. Here, we investigated the clinical uses of berberine and B. vulgaris in the treatment of different diseases in humans. An extensive search in electronic databases (PubMed, Scopus, Embase, Web of Sciences and Science Direct) was used to identify the clinical trials on B. vulgaris and berberine. Lipid‐lowering and insulin‐resistance improving actions are the most studied properties of berberine in numerous randomized clinical trials. There are also clinical trials regarding cardiovascular, anticancer, gastrointestinal, CNS, endocrine, and so on. Berberine has very low toxicity in usual doses and reveals clinical benefits without major side effects. Only mild gastrointestinal reactions may occur in some patients. The purpose of this review is to provide a summary concerning the clinical trials conducted on berberine to improve the clinical application of this nutraceutical in different diseases. In this review article, we used 77 clinical studies on human subjects.

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Section: Clinical Pharmacokineticmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Berberine and barberry (Berberis vulgaris): A clinical review

Imenshahidi

Hosseinzadeh

2019

Phytotherapy Research

254

134

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“…14,15 However, the clinical use of berberine is largely limited because of its poor intestinal absorption and inadequate plasma level after oral administration. 16 Besides, oral administration, especially at a high dose, often causes gastrointestinal discomfort due to considerable exposure to free berberine. 17 Therefore, it is necessary to develop advanced formulations of berberine to improve the oral delivery efficacy, thereby enhancing the in vivo antidiabetic effect.…”

Section: Introductionmentioning

confidence: 99%

Selenium-coated nanostructured lipid carriers used for oral delivery of berberine to accomplish a synergic hypoglycemic effect

Yin¹,

Hou²,

Yin³

et al. 2017

IJN

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Diabetes mellitus is an incurable metabolic disorder that seriously threatens human health. At present, there is no effective medication available to defeat it. This work intended to develop selenium-coated nanostructured lipid carriers (SeNLCs) for enhancing the oral bioavailability and the curative effect of berberine, an antidiabetic phytomedicine. Berberine-loaded SeNLCs (BB-SeNLCs) were prepared by hot-melt dispersion/homogenization procedure followed by in situ reduction. BB-SeNLCs were characterized by particle size, morphology, entrapment efficiency (EE) and in vitro release. Pharmacokinetics of berberine solution, berberine-loaded NLCs (BB-NLCs) and BB-SeNLCs were studied in Sprague Dawley rats administered by oral gavage. The prepared BB-SeNLCs were around 160 nm in particle size with an EE of 90%. In addition, BB-SeNLCs exhibited a better sustained release of berberine compared to the plain NLCs. After oral administration, BB-SeNLCs greatly enhanced the oral bioavailability of berberine, which was approximately 6.63 times as much as that of berberine solution. The hypoglycemic effect of BB-SeNLCs was also significantly superior to that of BB-NLCs and berberine solution. It turned out that sustained drug release and good intestinal absorption, plus the synergy of selenium, were basically responsible for enhanced oral bioavailability and hypoglycemic effect. Our findings show that SeNLCs are promising nanocarriers for oral delivery of berberine to strengthen the antidiabetic action.

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“…However, although oral intake of BBR has a good safety record, BBR administration via the intravenous route has been found to elicit some acute adverse reactions, such as cardiac suppression, hypotension and vasodilation . In accordance with this toxicological effect, pharmacokinetic studies have shown that BBR has a quick and wide distribution to major organs after intravenous injection . Circumvention of these potential adverse reactions, potentially by modifying the biological exposure, is of significance in the medicinal application of BBR injections.…”

Section: Introductionmentioning

confidence: 99%