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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
2013-12-01
Source PublicationCOLLOIDS AND SURFACES B-BIOINTERFACES
Volume112Issue:0Pages:492-498
AbstractExenatide-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.
KeywordExenatide Plga Microspheres Narrow Size Distribution Premix Membrane Emulsification In Vitro Release
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine ; Physical Sciences ; Technology
Indexed BySCI
Language英语
WOS KeywordMEMBRANE EMULSIFICATION TECHNIQUE ; BIODEGRADABLE POLYMERIC MICROSPHERES ; SOLVENT EVAPORATION METHOD ; POLY(LACTIDE-CO-GLYCOLIDE) MICROPARTICLES ; PLA MICROCAPSULES ; DRUG-DELIVERY ; IN-VITRO ; EMULSION ; MORPHOLOGY ; BURST
WOS Research AreaBiophysics ; Chemistry ; Materials Science
WOS SubjectBiophysics ; Chemistry, Physical ; Materials Science, Biomaterials
WOS IDWOS:000328593100070
Citation statistics
Cited Times:62[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.ipe.ac.cn/handle/122111/13573
Collection研究所(批量导入)
Affiliation1.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
Recommended Citation
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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