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dc.rights.licenseopenen_US
dc.contributor.authorREHMAN, Asad Ur
hal.structure.identifierInstitut de Mécanique et d'Ingénierie [I2M]
dc.contributor.authorBUSIGNIES, Virginie
IDREF: 07355247X
dc.contributor.authorCOELHO SILVA RIBEIRO, Marcela
dc.contributor.authorALMEIDA LAGE, Nayara
hal.structure.identifierInstitut de Mécanique et d'Ingénierie [I2M]
dc.contributor.authorTCHORELOFF, Pierre
IDREF: 069233624
dc.contributor.authorESCRIOU, Virginie
dc.contributor.authorCHARRUEAU, Christine
dc.date.accessioned2021-12-21T10:21:35Z
dc.date.available2021-12-21T10:21:35Z
dc.date.issued2021-10-28
dc.identifier.issn1999-4923en_US
dc.identifier.urioai:crossref.org:10.3390/pharmaceutics13111807
dc.identifier.urihttps://oskar-bordeaux.fr/handle/20.500.12278/124288
dc.description.abstractEnThe incorporation of siRNA into nanocarriers is mandatory to facilitate its intracellular delivery, as siRNA itself cannot enter cells. However, the incorporation of these nanocarriers into oral, solid dosage forms and their fate in the gastrointestinal environment is yet to be explored. In the present work, the fate of, (i) naked siRNA, (ii) freshly prepared siRNA lipoplexes, and (iii) tableted siRNA lipoplexes, in simulated gastric and intestinal fluids was studied. The siRNA, either released from or protected within the lipoplexes, was quantified by gel electrophoresis and siRNA efficacy was assessed in cell transfection. The freshly prepared lipoplexes kept their siRNA load and transfection efficiency totally preserved during 1 h of incubation in simulated gastric fluid at 37 °C. However, in simulated intestinal fluid, despite no release of siRNA from lipoplexes after 6 h of incubation, gene silencing efficacy was dramatically decreased even after 1 h of exposure. The lipoplexes obtained from tablets efficiently protected siRNA in simulated gastric fluid, thus preserving the gene silencing efficacy, whereas their incubation in simulated intestinal fluid resulted in a marked siRNA release and decreased gene silencing efficacy. These results provided a detailed explanation for understanding the fate of siRNA in gastrointestinal conditions, when simply loaded in lipoplexes or formulated in the form of tablets.
dc.language.isoENen_US
dc.rightsAttribution 3.0 United States*
dc.rights.urihttp://creativecommons.org/licenses/by/3.0/us/*
dc.sourcecrossref
dc.subject.enGel electrophoresis
dc.subject.enNanocarriers
dc.subject.enOral delivery
dc.subject.enRNA interference
dc.subject.enSolid dosage form
dc.title.enFate of Tableted Freeze-Dried siRNA Lipoplexes in Gastrointestinal Environment
dc.typeArticle de revueen_US
dc.identifier.doi10.3390/pharmaceutics13111807en_US
dc.subject.halSciences de l'ingénieur [physics]/Autreen_US
bordeaux.journalPharmaceuticsen_US
bordeaux.page1807en_US
bordeaux.volume13en_US
bordeaux.hal.laboratoriesInstitut de Mécanique et d’Ingénierie de Bordeaux (I2M) - UMR 5295en_US
bordeaux.issue11en_US
bordeaux.institutionUniversité de Bordeauxen_US
bordeaux.institutionBordeaux INPen_US
bordeaux.institutionCNRSen_US
bordeaux.institutionINRAEen_US
bordeaux.institutionArts et Métiersen_US
bordeaux.peerReviewedouien_US
bordeaux.inpressnonen_US
bordeaux.import.sourcedissemin
hal.identifierhal-03498858
hal.version1
hal.date.transferred2021-12-21T10:21:41Z
hal.exporttrue
workflow.import.sourcedissemin
dc.rights.ccPas de Licence CCen_US
bordeaux.COinSctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Pharmaceutics&rft.date=2021-10-28&rft.volume=13&rft.issue=11&rft.spage=1807&rft.epage=1807&rft.eissn=1999-4923&rft.issn=1999-4923&rft.au=REHMAN,%20Asad%20Ur&BUSIGNIES,%20Virginie&COELHO%20SILVA%20RIBEIRO,%20Marcela&ALMEIDA%20LAGE,%20Nayara&TCHORELOFF,%20Pierre&rft.genre=article


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