title: Development of self-microemulsifying drug delivery system for oral bioavailability enhancement of berberine hydrochloride.
abstract: The purpose of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) to improve the oral bioavailability of Berberine hydrochloride (BBH), an important bioactive compound from Chinese Medicines with poor water solubility. Pseudoternary phase diagrams were constructed using oil, surfactant and co-surfactant types to identify the efficient self-microemulsification region. SMEDDS was characterized by morphological observation, droplet size, zeta-potential determination, stability, in vitro release and in vivo bioavailability study. The optimal formulation with the best self-microemulsifying and solubilization ability consisted of 40% (w/w) of ethyl linoleate and oleic acid (2:1), 35% (w/w) Tween-80 and 25% (w/w) glycerol. The SMEDDS of BBH could exhibit good stability. In vitro release test showed a complete release of BBH from SMEDDS was in 5 h. In vivo results indicated that the peak plasma concentration (C(max)) and the area under the curve (AUC(0→12 h)) of SMEDDS of BBH were higher than the commercial tablet by 163.4% and 154.2%, respectively. The relative bioavailability of SMEDDS of BBH was enhanced about 2.42-fold compared with the commercial tablet in rats. The study confirmed that the SMEDDS formulation could be used as a possible alternative to traditional oral formulations of BBH to improve its bioavailability.
authors.affiliation: State Key Laboratory for Quality Research in Chinese Medicine, Faculty of Chinese Medicine, Macau University of Science and Technology, Macau, PR China.
authors.forename: Jia-Xiao
authors.initials: JX
authors.lastname: Zhu
authors.forename: Dan
authors.initials: D
authors.lastname: Tang
authors.forename: Liang
authors.initials: L
authors.lastname: Feng
authors.forename: Zhao-Guang
authors.initials: ZG
authors.lastname: Zheng
authors.forename: Ru-Shang
authors.initials: RS
authors.lastname: Wang
authors.forename: An-Guo
authors.initials: AG
authors.lastname: Wu
authors.forename: Ting-Ting
authors.initials: TT
authors.lastname: Duan
authors.forename: Bao
authors.initials: B
authors.lastname: He
authors.forename: Quan
authors.initials: Q
authors.lastname: Zhu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001599:Berberine / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000493:pharmacokinetics*; D004655:Emulsions / Q000737:chemistry*; D010316:Particle Size; D051381:Rats; D012995:Solubility
chemical_list: D004365:Drugs, Chinese Herbal; D004655:Emulsions; D001599:Berberine