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Comparative Studies on the Influences of Primary Emulsion Preparation on Properties of Uniform-Sized Exenatide-Loaded PLGA Microspheres
Alternative TitlePharm. Res.
Qi, Feng1,2; Wu, Jie1; Hao, Dongxia1; Yang, Tingyuan1; Ren, Yu1; Ma, Guanghui1; Su, Zhiguo1
2014-06-01
Source PublicationPHARMACEUTICAL RESEARCH
ISSN0724-8741
Volume31Issue:6Pages:1566-1574
AbstractIt is well known that primary emulsion (W-1/O) preparation process (by ultrasonication or homogenization) plays an important role in the properties of drug-loaded microspheres, such as encapsulation efficiency, release behavior and pharmacodynamics. However, its involved mechanism has not been intensively and systematically studied, partly because that broad size distribution of the resultant particles prepared by conventional preparation can greatly disturb the analysis and reliability of the results. Here, we focused on the relevant studies. In order to eliminate the disturbance caused by broad size distribution, uniform-sized exenatide-loaded poly(DL-lactic-co-glycolic acid) (PLGA) microspheres were prepared by Shirasu Porous Glass (SPG) premix membrane emulsification. The properties of microspheres whose W-1/O was formed by ultrasonication (UMS) and homogenization (HMS) were compared including in vitro release, pharmacology and so forth. HMS exhibited fast release rate and hyperglycemic efficacy within first 14 days, but declined afterwards. Comparatively, UMS showed slower polymer degradation, more acidic microclimate pH (mu pH) in vitro, and stable drug release with sustained efficacy during 1 month in vivo. HMS was desirable for the 2-week-sustained release in vivo, while UMS was more appropriate for the longer time release (about 1 month). These comparative researches can provide guidance for emulsion-microsphere preparation routs in pharmaceutics.; It is well known that primary emulsion (W-1/O) preparation process (by ultrasonication or homogenization) plays an important role in the properties of drug-loaded microspheres, such as encapsulation efficiency, release behavior and pharmacodynamics. However, its involved mechanism has not been intensively and systematically studied, partly because that broad size distribution of the resultant particles prepared by conventional preparation can greatly disturb the analysis and reliability of the results. Here, we focused on the relevant studies.
KeywordControlled Release Homogenization Primary Emulsion Ultrasonication Uniform-sized
SubtypeArticle
WOS HeadingsScience & Technology ; Physical Sciences ; Life Sciences & Biomedicine
DOI10.1007/s11095-013-1262-6
URL查看原文
Indexed BySCI
Language英语
WOS KeywordMEMBRANE EMULSIFICATION TECHNIQUE ; HIGH ENCAPSULATION EFFICIENCY ; MICROCLIMATE PH DISTRIBUTION ; SOLVENT EVAPORATION METHOD ; LASER-SCANNING MICROSCOPY ; POLY(LACTIDE-CO-GLYCOLIDE) MICROSPHERES ; PROCESS PARAMETERS ; PLA MICROCAPSULES ; RELEASE PROFILES ; IN-VITRO
WOS Research AreaChemistry ; Pharmacology & Pharmacy
WOS SubjectChemistry, Multidisciplinary ; Pharmacology & Pharmacy
WOS IDWOS:000336745800019
Citation statistics
Cited Times:27[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Version出版稿
Identifierhttp://ir.ipe.ac.cn/handle/122111/10950
Collection研究所(批量导入)
Affiliation1.Chinese Acad Sci, Inst Proc Engn, Natl Key Lab Biochem Engn, PLA Key Lab Biopharmaceut Prod & Formulat Engn, Beijing 100190, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
Recommended Citation
GB/T 7714
Qi, Feng,Wu, Jie,Hao, Dongxia,et al. Comparative Studies on the Influences of Primary Emulsion Preparation on Properties of Uniform-Sized Exenatide-Loaded PLGA Microspheres[J]. PHARMACEUTICAL RESEARCH,2014,31(6):1566-1574.
APA Qi, Feng.,Wu, Jie.,Hao, Dongxia.,Yang, Tingyuan.,Ren, Yu.,...&Su, Zhiguo.(2014).Comparative Studies on the Influences of Primary Emulsion Preparation on Properties of Uniform-Sized Exenatide-Loaded PLGA Microspheres.PHARMACEUTICAL RESEARCH,31(6),1566-1574.
MLA Qi, Feng,et al."Comparative Studies on the Influences of Primary Emulsion Preparation on Properties of Uniform-Sized Exenatide-Loaded PLGA Microspheres".PHARMACEUTICAL RESEARCH 31.6(2014):1566-1574.
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