title: Monodisperse microparticles loaded with the self-assembled berberine-phospholipid complex-based phytosomes for improving oral bioavailability and enhancing hypoglycemic efficiency.
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.
authors.affiliation: Department of Chemical and Biochemical Engineering, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen 361005, China.
authors.forename: Fei
authors.initials: F
authors.lastname: Yu
authors.affiliation: College of Materials, Xiamen University, Xiamen 361005, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Li
authors.affiliation: Department of Pharmacy, College of Pharmaceutical Science, Soochow University, Suzhou 215123, China.
authors.forename: Qin
authors.initials: Q
authors.lastname: Chen
authors.affiliation: College of Materials, Xiamen University, Xiamen 361005, China.
authors.forename: Yuan
authors.initials: Y
authors.lastname: He
authors.affiliation: Department of Pharmacy, Jining Medical College, Sunshine City 276826, China.
authors.forename: Huiyun
authors.initials: H
authors.lastname: Wang
authors.affiliation: Medical College, Xiamen University, Xiamen 361005, China.
authors.forename: Liu
authors.initials: L
authors.lastname: Yang
authors.affiliation: School of Pharmacy, Liaocheng University, Liaocheng 252059, China.
authors.forename: Shangjing
authors.initials: S
authors.lastname: Guo
authors.affiliation: College of Materials, Xiamen University, Xiamen 361005, China.
authors.forename: Zhaohui
authors.initials: Z
authors.lastname: Meng
authors.affiliation: Department of Pharmacy, College of Pharmaceutical Science, Soochow University, Suzhou 215123, China. Electronic address: jhcui@suda.edu.cn.
authors.forename: Jinghao
authors.initials: J
authors.lastname: Cui
authors.affiliation: Department of Pharmacology, Nanjing University of Chinese Medicine, Nanjing 210046, China. Electronic address: xuemeibox@126.com.
authors.forename: Mei
authors.initials: M
authors.lastname: Xue
authors.affiliation: 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.
authors.forename: Xiao Dong
authors.initials: XD
authors.lastname: Chen
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001599:Berberine / Q000737:chemistry*; D001682:Biological Availability; D018938:Caco-2 Cells; D002152:Calorimetry, Differential Scanning; D006801:Humans; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000737:chemistry; D010316:Particle Size; D010743:Phospholipids / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
chemical_list: D007004:Hypoglycemic Agents; D010743:Phospholipids; D001599:Berberine
keywords: Berberine; Microparticles; Oral; Phospholipid complex; Phytosomes; Spray drying