Preparation of uniform-sized exenatide-loaded PLGA microspheres as long-effective release system with high encapsulation efficiency and bio-stability | |
Qi, Feng1,2; Wu, Jie1; Fan, Qingze1,2; He, Fan1,2; Tian, Guifang1,3; Yang, Tingyuan1; Ma, Guanghui1; Su, Zhiguo1 | |
刊名 | COLLOIDS AND SURFACES B-BIOINTERFACES
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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. |
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