Preparation of uniform-sized exenatide-loaded PLGA microspheres as long-effective release system with high encapsulation efficiency and bio-stability

CORC > 过程工程研究所 > 中国科学院过程工程研究所 > 研究所（批量导入）

	Preparation of uniform-sized exenatide-loaded PLGA microspheres as long-effective release system with high encapsulation efficiency and bio-stability
	Qi, Feng 1,2; Wu, Jie 1; Fan, Qingze 1,2; He, Fan 1,2; Tian, Guifang 1,3; Yang, Tingyuan 1; Ma, Guanghui 1; Su, Zhiguo 1
刊名	COLLOIDS AND SURFACES B-BIOINTERFACES
	2013-12-01
卷号	112 期号:0 页码:492-498
关键词	Exenatide PLGA microspheres Narrow size distribution Premix membrane emulsification In vitro release
英文摘要	Exenatide-loaded poly(D-L-lactic-co-glycolic acid) (PLGA) microspheres hold great potential as a drug delivery system to treat type 2 diabetes mellitus (T2DM) because they can overcome the shortcoming of exenatide's short half-life and realize sustained efficacy. However, conventional preparation methods often lead to microspheres with a broad size distribution, which in turn would cause poor preparation repeatability, drug efficacy and so forth. In this study, we used Shirasu Porous Glass (SPG) premix membrane emulsification technique characterized with high trans-membrane flux and size controllability to prepare uniform-sized PLGA microspheres. By optimizing trans-membrane pressure and PVA concentration in external aqueous phase, uniform-sized PLGA microspheres with large size (around 20 mu m) were successfully obtained. To achieve high encapsulation efficiency (EE) and improve in vitro release behavior, we have carefully examined the process parameters. Our results show that using ultrasonication to form primary emulsion, microspheres with high EE were easily obtained, but the rate of in vitro release was very slow. Instead, high EE and appropriate in vitro release were achieved when homogenization with optimized time and speed were employed. Besides, we also systematically investigated the effect of formulations on loading efficiency (LE) as well as the relationship between the resultant size of the microspheres and pore size of the membrane. Finally, through RP-HPLC and CD spectra analysis, we have demonstrated that the bio-stability of exenatide in microspheres was preserved during the preparation process. (C) 2013 Elsevier B.V. All rights reserved.
WOS标题词	Science & Technology ; Life Sciences & Biomedicine ; Physical Sciences ; Technology
类目[WOS]	Biophysics ; Chemistry, Physical ; Materials Science, Biomaterials
研究领域[WOS]	Biophysics ; Chemistry ; Materials Science
关键词[WOS]	MEMBRANE EMULSIFICATION TECHNIQUE ; BIODEGRADABLE POLYMERIC MICROSPHERES ; SOLVENT EVAPORATION METHOD ; POLY(LACTIDE-CO-GLYCOLIDE) MICROPARTICLES ; PLA MICROCAPSULES ; DRUG-DELIVERY ; IN-VITRO ; EMULSION ; MORPHOLOGY ; BURST
收录类别	SCI
语种	英语
WOS记录号	WOS:000328593100070
公开日期	2015-05-27
内容类型	期刊论文
源URL	[http://ir.ipe.ac.cn/handle/122111/13573]
专题	过程工程研究所_研究所（批量导入）
作者单位	1.Chinese Acad Sci, Inst Proc Engn, PM Key Lab Biopharmaceut Prod & Formulat Engn, Natl Key Lab Biochem Engn, Beijing 100190, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Beijing Univ Chem Technol, State Key Lab Chem Resource Engn, Beijing 100029, Peoples R China
推荐引用方式 GB/T 7714	Qi, Feng,Wu, Jie,Fan, Qingze,et al. Preparation of uniform-sized exenatide-loaded PLGA microspheres as long-effective release system with high encapsulation efficiency and bio-stability[J]. COLLOIDS AND SURFACES B-BIOINTERFACES,2013,112(0):492-498.
APA	Qi, Feng.,Wu, Jie.,Fan, Qingze.,He, Fan.,Tian, Guifang.,...&Su, Zhiguo.(2013).Preparation of uniform-sized exenatide-loaded PLGA microspheres as long-effective release system with high encapsulation efficiency and bio-stability.COLLOIDS AND SURFACES B-BIOINTERFACES,112(0),492-498.
MLA	Qi, Feng,et al."Preparation of uniform-sized exenatide-loaded PLGA microspheres as long-effective release system with high encapsulation efficiency and bio-stability".COLLOIDS AND SURFACES B-BIOINTERFACES 112.0(2013):492-498.