作者：jiaolu,mengshi,andmollys.shoichet
departmentofchemistry,departmentofchemicalengineeringandappliedchemistry,andinstituteforbiomaterialsandbiomedicalengineering,terrencedonnellycenterforcellularandbiomolecularresearch,universityoftoronto
摘要：self-assembledpolymericnanoparticlesmodifiedwithtargetingligandsonthesurfaceprovideameansforlocalizedcelldelivery.togaingreaterinsightintothepossibilityofderivatizingpoly(2-methyl-2-carboxytrimethylenecarbonate-co-d,l-lactide)(poly(tmcc-co-la))nanoparticlesusingthehuisgen’s1,3dipolarcycloadditionreaction,wesynthesizedamphiphiliccopolymerscomprisingahydrophobicpoly(tmcc-co-la)backboneandahydrophilicpoly(ethyleneglycol)(peg)pendantchain.bycouplingamine-terminatedpeg-azidetothecarboxylicacidgroupofthepoly(tmcc-co-la)viaedcchemistry,anamphiphiliccopolymerwasformed.thepoly(tmcc-co-la)-g-peg-n3self-assembledinaqueoussolutionandpresentedazidegroupsonthesurfaceofthenanoparticles.alkyne-modifiedkgrgdspeptidesweresynthesizedandcoupledtotheazide-functionalizednanoparticlesviahuisgen’s1,3dipolarcycloaddition,whichwascatalyzedbycoppersulfateandsodiumascorbateinaqueoussolution.usingcoumarin-modifiedlysine(k)ofthekgrgdspeptide,fluorescencewasusedtodeterminethattherewereapproximay400peptidesboundtoeachnanoparticle.thebioactivityofthegrgdsnanoparticlewasconfirmedwithacompetitivecellattachmentassayusingrabbitcornealepithelialcells.thisgrgdsnanoparticlesystemmaybesuitablefortargeteddrugdelivery.