Monodisperse microparticles loaded with the self-assembled berberine-phospholipid complex-based phytosomes for improving oral bioavailability and enhancing hypoglycemic efficiency

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• 作者：Fei Yu^a ; Yang Li^g ; Qin Chen^c ; Yuan He^g ; Huiyun Wang^h ; Liu Yang^f ; Shangjing Guo^e ; Zhaohui Meng^g ; Jinghao Cui^c ; ^{jhcui@suda.edu.cn" class="auth_mail" title="E-mail the corresponding author} ; Mei Xue^d ; ^{xuemeibox@126.com" class="auth_mail" title="E-mail the corresponding author} ; Xiao Dong Chen^a ; ^b ; ^{xdc@xmu.edu.cn" class="auth_mail" title="E-mail the corresponding author} ; ^{xdchen@mail.suda.edu.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Berberine ; Phospholipid complex ; Phytosomes ; Microparticles ; Oral ; Spray drying
• 刊名：European Journal of Pharmaceutics and Biopharmaceutics
• 出版年：2016
• 出版时间：June 2016
• 年：2016
• 卷：103
• 期：Complete
• 页码：136-148
• 全文大小：3434 K

文摘

Berberine (BER), possessing a variety of pharmacological functions, has caused a growing interest in recent years. More importantly, BER is a potential natural alternative to other synthetic antidiabetic drugs. However, poor gastrointestinal absorption and low oral bioavailability have limited its development for further clinical application. In this study, for the first time, the phytosomes loaded with berberine-phospholipid complex (P-BER) were prepared by a rapid solvent evaporation method followed by a self-assembly technique for developing a more efficient BER drug delivery system. The P-BER showed a nanoscale particle size, a negative surface charge, and excellent drug entrapment efficiency (∼85%). Compared to the orally administrated BER in previous pharmacokinetic studies, the oral bioavailability of the P-BER was significantly improved by 3-fold. More importantly, the oral administration of P-BER could suppress the fasting glucose levels and improve the ability of systematic hyperlipidemia metabolism of db/db diabetic mice. All results have demonstrated that the P-BER could be a promising oral drug delivery system.