艾塞那肽长效缓释微球的制备及体内药效学研究

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1、艾塞那肽长效缓释微球的制备及体内药效学研究刘斌1,2，董庆光1，王梦舒1，李纯1，孔维1,2，陈妍1*(1.吉林大学生命科学学院，长春130012；2.吉林大学超分子结构与材料国家重点实验室，长春130012.)摘要：目的制备艾塞那肽长效缓释微球，并考察其理化性质、体外释放特性及体内药效学。方法采用复乳－溶剂挥发法（W/O/W）制备包裹艾塞那肽的聚乳酸－羟基乙酸嵌段共聚物（PLGA）微球；考察微球的粒径分布、表面形态、载药量和包封率；用micro－BCA试剂盒测定微球的体外释放速率；考察了微球在糖尿病模型小鼠体内的降血糖作

2、用。结果微球外观光滑圆整，分散性好，艾塞那肽载药量为3％，包封率为75％；微球40d之内体外累积释放达到88％，其体外释放曲线近似零级释放模式；体内药效学实验结果显示，40d内微球组小鼠与模型对照组小鼠血糖相比具有显著性差异（P<0.05）。结论采用复乳－溶剂挥发法成功制备了可以缓释40d的艾塞那肽长效微球，且40d之内在糖尿病小鼠体内具有明显的降血糖作用。关键词：艾塞那肽；聚乳酸－羟基乙酸嵌段共聚物；微球；血糖中图文类号：文献标识码：文章编号：PreparationofLong-actingReleaseMicrosph

3、eresofExenatideandStudiesonTheirinvivoPharmacodynamicsLIUBin1,2，DONGQing-Guang1，WANGMeng-Shu1，LIChun1，KONGWei1,2，CHENYan1*（1.CollegeofLifeScience,JilinUniversity,Changchun130012,China；2.StateKeyLaboratoryofSupramolecularStructure&Materials,JilinUniversity,Changchu

4、n130012.,China.）ABSTRACT:OBJECTIVEToprapereExenatideloadedlong-actingreleasemicrospheres,andtoevaluatetheirphysicalandchemicalcharacteristics、invitroreleasebehavioraswellasinvivopharmacodynamics.METHODExenatideloadedPLGAmicrosphereswerepreparedbydoubleemulsion(W/O

5、/W)method.Themeandiameter、morphology、drugloadingandencapsulationefficiencywereevaluated.Themicro-BCAproteinassaywasusedfortheinvitroreleasebehavior.Theeffectofreducingplasmaglucosewereevaluatedonthediabetesmice.RESULTSThemicrospherespossessedsmoothandroundappearan

6、ceaswellasgooddispersivequality.Thedrugloadingandencapsulationefficiencywas3%and75%.Theinvitroaccumulatedreleasewithin40dreachedupto88%,andthereleaseprofileisconsistentwithzero-classreleasemodel.Theresultsofinvivopharmacodynamicsindicatedthattheplasmaglucoseofmice

7、injectedwithExenatidemicrosphereswasdifferentsignificantlyfromtheplasmaglucoseofthediabetesmodelmicewithin40d(P<0.05).CONCLUSIONTheExenatideloadedlong-actingreleasemicrosphereswhichcouldyield40dcontinuousreleasewerepreparedsuccessfullybydoubleemulsionmethod.Themic

8、rospheresdisplayedsignificantappearanceofdecreasingplasmaglucoseinthediabetesmicewithin40d.KEYWORDS:Exenatide；poly(lactide-co-glycolicacid)；microspheres