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Histone deacetylase inhibitor-polymer conjugate nanoparticles for acid-responsive drug delivery

dc.rights.licenseopen
hal.structure.identifierCentre de Recherche en Cancérologie Nantes-Angers [CRCNA]
hal.structure.identifierUniversité de Nantes [UN]
dc.contributor.authorDENIS, Iza
hal.structure.identifierInstitut de chimie des milieux et matériaux de Poitiers [UMR 7285] [IC2MP [Poitiers]]
dc.contributor.authorEL BAHHAJ, Fatima
hal.structure.identifierLaboratoire de Chimie des Polymères Organiques [LCPO]
hal.structure.identifierTeam 1 LCPO : Polymerization Catalyses & Engineering
dc.contributor.authorCOLLETTE, Floraine
hal.structure.identifierInstitut de chimie des milieux et matériaux de Poitiers [UMR 7285] [IC2MP [Poitiers]]
dc.contributor.authorDELATOUCHE, Régis
hal.structure.identifierCentre de Recherche en Cancérologie Nantes-Angers [CRCNA]
hal.structure.identifierUniversité de Nantes [UN]
dc.contributor.authorGUEUGNON, Fabien
hal.structure.identifierCentre de Recherche en Cancérologie Nantes-Angers [CRCNA]
hal.structure.identifierUniversité de Nantes [UN]
dc.contributor.authorPOULIQUEN, Daniel
hal.structure.identifierLaboratoire de Chimie des Polymères Organiques [LCPO]
hal.structure.identifierTeam 1 LCPO : Polymerization Catalyses & Engineering
dc.contributor.authorPICHAVANT, Loïc
hal.structure.identifierLaboratoire de Chimie des Polymères Organiques [LCPO]
hal.structure.identifierTeam 1 LCPO : Polymerization Catalyses & Engineering
dc.contributor.authorHÉROGUEZ, Valérie
hal.structure.identifierCentre de Recherche en Cancérologie Nantes-Angers [CRCNA]
hal.structure.identifierUniversité de Nantes [UN]
dc.contributor.authorGREGOIRE, Marc
hal.structure.identifierInstitut de chimie des milieux et matériaux de Poitiers [UMR 7285] [IC2MP [Poitiers]]
dc.contributor.authorPHILIPPE, Bertrand
hal.structure.identifierCentre de Recherche en Cancérologie Nantes-Angers [CRCNA]
hal.structure.identifierUniversité de Nantes [UN]
dc.contributor.authorBLANQUART, Christophe
dc.date.accessioned2020
dc.date.available2020
dc.date.issued2015
dc.identifier.issn0223-5234
dc.identifier.urihttps://oskar-bordeaux.fr/handle/20.500.12278/20235
dc.description.abstractEnWe report the synthesis of acid responsive polymeric nanoparticles (NPs) consisting of a polymerhistone deacetylase inhibitor conjugate. An innovative aspect of this drug delivery particle lies in the NP conjugation of a histone deacetylase (HDAC) inhibitor, CI-994 (Tacedinaline), introduced with a clickable acid-responsive prodrug during monomer synthesis, prior to polymerization. Another novelty lies in the selected norbornene (NB)-polyethylene oxide (PEO) macromonomer allowing standardization of the polymerization process by Ring-Opening Metathesis Polymerization (ROMP) and functionalization through azide-allcyne click chemistry. Herein we demonstrate that the synthesized polymer gave 300 nm core-shell spherical nanoparticles with low dispersity (0.04), high water dispersability thanks to the PEO shell and well controlled HDAC inhibitor prodrug loading. Bioluminescence Resonance Energy Transfer (BRET) assay in living cells and viability experiments demonstrated efficient cellular internalization without additional chemistry, drug release inside cells with restoration of the HDAC inhibition and induction of apoptosis. Such NPs should minimize drug release in vivo during blood circulation and trigger intracellular delivery after endocytosis, holding promises for improved efficacy of this class of epigenetic inhibitors. This standardized synthesis paves the way for multifunctional nanoparticles synthesis.
dc.language.isoen
dc.publisherElsevier
dc.subject.enCI-994
dc.subject.enCANCER
dc.subject.enOXIDE)
dc.subject.enPolymeric nanoparticle
dc.subject.enEpigenetic inhibitor
dc.subject.enDrug delivery
dc.subject.enControlled release
dc.subject.enStimuli-responsive
dc.subject.enOPENING METATHESIS POLYMERIZATION
dc.subject.enHDAC
dc.title.enHistone deacetylase inhibitor-polymer conjugate nanoparticles for acid-responsive drug delivery
dc.typeArticle de revue
dc.identifier.doi10.1016/j.ejmech.2015.03.037
dc.subject.halChimie/Polymères
bordeaux.journalEuropean Journal of Medicinal Chemistry
bordeaux.page369-376
bordeaux.volume95
bordeaux.hal.laboratoriesLaboratoire de Chimie des Polymères Organiques (LCPO) - UMR 5629*
bordeaux.institutionBordeaux INP
bordeaux.institutionUniversité de Bordeaux
bordeaux.peerReviewedoui
hal.identifierhal-01368838
hal.version1
hal.origin.linkhttps://hal.archives-ouvertes.fr//hal-01368838v1
bordeaux.COinSctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=European%20Journal%20of%20Medicinal%20Chemistry&rft.date=2015&rft.volume=95&rft.spage=369-376&rft.epage=369-376&rft.eissn=0223-5234&rft.issn=0223-5234&rft.au=DENIS,%20Iza&EL%20BAHHAJ,%20Fatima&COLLETTE,%20Floraine&DELATOUCHE,%20R%C3%A9gis&GUEUGNON,%20Fabien&rft.genre=article


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