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1、JournalofControlledRelease143(2010)136–142ContentslistsavailableatScienceDirectJournalofControlledReleasejournalhomepage:www.elsevier.com/locate/jconrelNANOMEDICINECyclicRGDconjugatedpoly(ethyleneglycol)-co-poly(lacticacid)micelleenhancespaclitaxelanti-gl
2、ioblastomaeffectChangyouZhan,BingGu,CaoXie,JinLi,YuLiu,WeiyueLu⁎DepartmentofPharmaceutics,SchoolofPharmacy,FudanUniversity,Shanghai,201203,PRChinaarticleinfoabstractArticlehistory:Theuseofglioblastoma-targeteddrugdeliverysystemfacilitatesefficientdeliveryo
3、fchemotherapeuticReceived30August2009agentstomalignantgliomasinthecentralnervoussystemwhileminimizinghighsystemicdosesassociatedAccepted18December2009withdebilitatingtoxicities.ToemploythehighbindingaffinityofacyclicRGDpeptide(c(RGDyK),cyclicAvailableonlin
4、e7January2010Arginine–Glycine–Asparticacid-D-Tyrosine-Lysine)withintegrinαvβ3over-expressedontumorneovascu-latureandU87MGglioblastomacells,wepreparedpaclitaxel-loadedc(RGDyK)-Poly(ethyleneglycol)-block-Keywords:poly(lacticacid)micelle(c(RGDyK)-PEG-PLA-PTX
5、).Invitrophysicochemicalcharacterizationofthesenovelc(RGDyK)PEG-PLAmicellemicellesshowedsatisfactoryencapsulatedefficiency,loadingcapacityandsizedistribution.InvitroGlioblastomacytotoxicitystudiesprovedthatthepresenceofc(RGDyK)enhancedtheanti-glioblastomac
6、ellcytotoxicPaclitaxelefficacyby2.5folds.Thebindingaffinityofc(RGDyK)-PEG-PLAmicellewithU87MGcellswasalsoinvestigated.ThecompetitivebindingIC50valueofc(RGDyK)-PEG-PLAmicellewas26.30nM,evenlower125thanthatofc(RGDyK)(56.23nM).InU87MGglioblastoma-bearingnudemi
7、cemodel,biodistributionofI-radiolabeledc(RGDyK)-PEG-PLAorDiRencapsulatedmicellesandanti-glioblastomapharmacologicaleffectwasinvestigatedafterintravenousadministration.c(RGDyK)-PEG-PLAmicelleaccumulatedinthesubcutaneousandintracranialtumortissue,andwhenloa
8、dedwithPTX(c(RGDyK)-PEG-PLA-PTX),exhibitedthestrongesttumorgrowthinhibitionamongthestudiedpaclitaxelformulations.Theanti-glioblastomaeffectofc(RGDyK)-PEG-PLA-PTXmicellewasalsoreflectedinthemediansurvivaltimeofmicebea
