MgAl monolayer hydrotalcite increases the hypoglycemic effect of berberine by enhancing its oral bioavailability - 30/05/20
, Dali Meng b, c, ⁎ , Dan Yan a, c, ⁎ Bienvenue sur EM-consulte, la référence des professionnels de santé.
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Graphical abstract |
Highlights |
• | Berberine (BBR) was immobilized onto MgAl monolayer hydrotalcite (MLDH) by ion-exchange method. |
• | BBR-MgAl monolayer hydrotalcite (BBR/MLDH) could increase the solubility and bioavailability of BBR. |
• | BBR/MLDH showed stronger hypoglycemic effect than free BBR in diabetic mice. |
Abstract |
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.
Le texte complet de cet article est disponible en PDF.Abbreviations : BBR, MLDH, BBR/MLDH, AUC, T2DM, LDHs, MET, CMC-Na, HFD, XRD, FT-IR, TEM, AFM, LC, EE, PBS, STZ, FBG, ESI, MRM, OGTT, ITT, TC, TG, FFAs, HOMA-IR
Keywords : Berberine, Layered double hydroxide, Monolayer nanosheets, Pharmacokinetics, Hypoglycemic effect
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Vol 127
Article 110140- juillet 2020 Retour au numéro
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