Stabilizing excipients for engineered clopidogrel bisulfate procubosome derived in situ cubosomes for enhanced intestinal dissolution: Stability and bioavailability considerations

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dc.AffiliationOctober University for modern sciences and Arts (MSA)
dc.contributor.authorEl-Laithy H.M.
dc.contributor.authorBadawi A.
dc.contributor.authorAbdelmalak N.S.
dc.contributor.authorElsayyad N.M.E.
dc.contributor.otherDepartment of Pharmaceutics and Industrial Pharmacy
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherCairo University
dc.contributor.otherEgypt; Department of Pharmaceutics and Industrial Pharmacy
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherOctober University for Modern Sciences and Arts (MSA University)
dc.contributor.otherEgypt
dc.date.accessioned2020-01-09T20:40:35Z
dc.date.available2020-01-09T20:40:35Z
dc.date.issued2019
dc.descriptionScopus
dc.description.abstractClopidogrel bisulfate (CB) is a golden antiplatelet treatment, yet its benefits are limited by its low bioavailability (<50%) caused by poor intestinal solubility and absorption. The present study aims to improve CB intestinal solubility and absorption through developing a novel stable dry CB procubosomes tablets ready to disintegrate and re-disperse upon dilution in the GIT forming in situ CB cubosome nanoparticles while simultaneously overcome the poor stability of conventional cubosome dispersion at room temperature. Glyceryl monooleate based CB cubosome dispersion was prepared using Poloxamer 407 as surfactant, freeze dried using different stabilizing excipients (dextrose, mannitol and avicel) then compressed into procubosome tablets. The effect of excipient's physicochemical properties on the flowability, in vitro dissolution and stability at accelerated conditions (40 � 2 �C/75 � 5% RH) were evaluated. The prepared procubosomes exhibited an excipient type dependent dissolution profile where Avicel based procubosome tablet CF2 showed the highest in vitro dissolution profile among other excipients used during the freeze drying process. Upon transition to intestinal pH of 6.8 to mimic the drug absorption site, CF2 procubosome Avicel tablet, was able to preserve the enhanced CB release profile (99.6 � 6.92%) compared to commercial Plavix� where, CB dissolved % dropped dramatically to 79.1 � 2.45%. After storage for six months, CF2 retained the fresh tablet drug content of 98.5 � 5.82% and dissolution properties. Moreover, following oral administration in rabbits, CF2 showed higher relative bioavailability (153%) compared to commercial Plavix� with significant higher Cmax,shorter tmax, as well as enhanced antiplatelet activity. � 2019 Elsevier B.V.en_US
dc.description.urihttps://www.scimagojr.com/journalsearch.php?q=21331&tip=sid&clean=0
dc.identifier.doihttps://doi.org/10.1016/j.ejps.2019.06.008
dc.identifier.doiPubMed ID 31189083
dc.identifier.issn9280987
dc.identifier.otherhttps://doi.org/10.1016/j.ejps.2019.06.008
dc.identifier.otherPubMed ID 31189083
dc.identifier.urihttps://t.ly/7OM2E
dc.language.isoEnglishen_US
dc.publisherElsevier B.V.en_US
dc.relation.ispartofseriesEuropean Journal of Pharmaceutical Sciences
dc.relation.ispartofseries136
dc.subjectBioavailabilityen_US
dc.subjectClopidogrel bisulfateen_US
dc.subjectCubosomesen_US
dc.subjectFreeze dryingen_US
dc.subjectProcubosomesen_US
dc.subjectStabilityen_US
dc.subjectStabilizing excipientsen_US
dc.subjectclopidogrelen_US
dc.subjectglucoseen_US
dc.subjectglycerol oleateen_US
dc.subjectmannitolen_US
dc.subjectmicrocrystalline celluloseen_US
dc.subjectpoloxameren_US
dc.subjectclopidogrelen_US
dc.subjectexcipienten_US
dc.subjectnanoparticleen_US
dc.subjectanimal experimenten_US
dc.subjectantiplatelet activityen_US
dc.subjectArticleen_US
dc.subjectdilutionen_US
dc.subjectdrug absorptionen_US
dc.subjectdrug bioavailabilityen_US
dc.subjectdrug delivery systemen_US
dc.subjectdrug solubilityen_US
dc.subjectdrug stabilityen_US
dc.subjectfreeze dryingen_US
dc.subjectin vitro studyen_US
dc.subjectmaximum concentrationen_US
dc.subjectnanoengineeringen_US
dc.subjectnonhumanen_US
dc.subjectpHen_US
dc.subjectphysical chemistryen_US
dc.subjectpriority journalen_US
dc.subjectroom temperatureen_US
dc.subjecttablet compressionen_US
dc.subjecttablet porosityen_US
dc.subjectanimalen_US
dc.subjectbioavailabilityen_US
dc.subjectchemistryen_US
dc.subjectdrug effecten_US
dc.subjectintestineen_US
dc.subjectLeporidaeen_US
dc.subjectmaleen_US
dc.subjectmetabolismen_US
dc.subjectoral drug administrationen_US
dc.subjectparticle sizeen_US
dc.subjectproceduresen_US
dc.subjectsolubilityen_US
dc.subjecttableten_US
dc.subjectAdministration, Oralen_US
dc.subjectAnimalsen_US
dc.subjectBiological Availabilityen_US
dc.subjectClopidogrelen_US
dc.subjectDrug Delivery Systemsen_US
dc.subjectExcipientsen_US
dc.subjectFreeze Dryingen_US
dc.subjectIntestinesen_US
dc.subjectMaleen_US
dc.subjectNanoparticlesen_US
dc.subjectParticle Sizeen_US
dc.subjectPoloxameren_US
dc.subjectRabbitsen_US
dc.subjectSolubilityen_US
dc.subjectTabletsen_US
dc.titleStabilizing excipients for engineered clopidogrel bisulfate procubosome derived in situ cubosomes for enhanced intestinal dissolution: Stability and bioavailability considerationsen_US
dc.typeArticleen_US
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