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Eur J Pharm Biopharm. 2016 Jun;103:136-148. doi: 10.1016/j.ejpb.2016.03.019. Epub 2016 Mar 25.

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

Author information

1
Department of Chemical and Biochemical Engineering, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen 361005, China.
2
College of Materials, Xiamen University, Xiamen 361005, China.
3
Department of Pharmacy, College of Pharmaceutical Science, Soochow University, Suzhou 215123, China.
4
Department of Pharmacy, Jining Medical College, Sunshine City 276826, China.
5
Medical College, Xiamen University, Xiamen 361005, China.
6
School of Pharmacy, Liaocheng University, Liaocheng 252059, China.
7
Department of Pharmacy, College of Pharmaceutical Science, Soochow University, Suzhou 215123, China. Electronic address: jhcui@suda.edu.cn.
8
Department of Pharmacology, Nanjing University of Chinese Medicine, Nanjing 210046, China. Electronic address: xuemeibox@126.com.
9
Department of Chemical and Biochemical Engineering, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen 361005, China; Suzhou Key Lab of Green Chemical Engineering, School of Chemical and Environmental Engineering, College of Chemistry, Chemical Engineering and Material Science, Soochow University, Suzhou 215123, China. Electronic address: xdc@xmu.edu.cn.

Abstract

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.

KEYWORDS:

Berberine; Microparticles; Oral; Phospholipid complex; Phytosomes; Spray drying

PMID:
27020531
DOI:
10.1016/j.ejpb.2016.03.019
[Indexed for MEDLINE]

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