PAMAM树状大分子磁共振成像造影剂的研究进展_刘晶莹.docVIP

PAMAM树状大分子磁共振成像造影剂的研究进展/刘晶莹等#69# PAMAM树状大分子磁共振成像造影剂的研究进展 刘晶莹,郑玉峰1,21,3 (1 哈尔滨工程大学生物医学材料与工程研究中心,哈尔滨150001;2 沈阳药科大学制药工程学院,沈阳110016; 3 北京大学工学院先进材料与纳米技术系,北京100871) 摘要 树状大分子磁共振成像造影剂与小分子造影剂相比具有很高的质子弛豫增强及摩尔弛豫率,成像清晰度更好,有更长的血液循环时间等,因而具有十分乐观的应用前景。着重介绍了聚酰胺-胺(PAMAM)树状大分子钆螯合物造影剂的性质及应用研究情况。低代数(PAMAM-G2、G3、G4)树状大分子钆螯合物造影剂分子尺寸较小(小于6nm),相对而言可以迅速从肾排泄,能够作为肾功能性造影剂。高代数(PAMAM-G7、G8)树状大分子钆螯合物造影剂分子尺寸较大(大于12nm),可静脉注射用于血池造影剂,而PAMAM-G6大分子试剂可用于淋巴成像造影剂。对PAMAM树状大分子钆螯合物进行化学或生物学修饰,还可以使其具有肿瘤靶向性,并能作为钆中子捕获治疗(Gd-NCT)试剂。 关键词 PAMAM树状大分子 磁共振成像造影剂 钆螯合物 弛豫率 DevelopmentofMagneticResonanceImagingContrastAgentswith PAMAMDendrimerCores LIUJingying1,2,ZHENGYufeng1,3 (1 CenterforBiomedicalMaterialsandEngineering,HarbinEngineeringUniversity,Harbin150001; 2 CollegeofPharmaceuticalEngineering,ShenyangPharmaceuticalUniversity,Shenyang110016; 3 DepartmentofAdvancedMaterialsandNanotechnology,CollegeofEngineering,PekingUniversity,Beijing100871) Abstract Magneticresonanceimaging(MRI)contrastagentswithdendrimercoreshavelargerprotonrelaxa- tionenhancementsandhighermolarrelaxivities,betterimagingvisualizationandlongerbloodretentioncomparedtothoseagentswithsmallmolecularweight.Itsuggeststhatthisnewclassofcontrastagenthasthepotentialfordiverseandextensiveapplications.Thepropertiesandapplicationofpolyamidoamine(PAMAM)dendrimer-basedgadoliniumcomplexcontrastagentsarereviewedbrieflyinthepresentpaper.Thisentireseriesofdendrimer-basedmacromolecularMRIcontrastagentshaveasphericalshape,andchangesinmolecularsizealtertherouteofexcretion.Smallersizedcontrastagents(PAMAM-G2,G3,G4)areexcretedthroughthekidneyresultingintheseagentsbeingsuitableasfunc-tionalrenalcontrastagents.Largersizedcontrastagents(PAMAM-G7,G8)arefoundbettersuitedforuseasbloodpoolcontrastagents,andlargercontrastagents(PAMAM-G6)arealsousefulforlymphaticimaging.Finally,macromolecu-larMRIcontrastagentsconjugatedwitheitherfolateorwithavidinareabletofunctionastumor-specificcontrastagentsandmightalsobeemployedastherapeuticdrugsforgadoliniumneutroncapturetherapy(Gd-NCT). Keyw