Novel self-nanoemulsifying self-nanosuspension (SNESNS) for enhancing oral bioavailability of diacerein: Simultaneous portal blood absorption and lymphatic delivery

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dc.AffiliationOctober University for modern sciences and Arts (MSA)
dc.contributor.authorEl-Laithy H.M.
dc.contributor.authorBasalious E.B.
dc.contributor.authorEl-Hoseiny B.M.
dc.contributor.authorAdel M.M.
dc.contributor.otherDepartment of Pharmaceutics and Industrial Pharmacy
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherCairo University
dc.contributor.otherCairo
dc.contributor.otherEgypt; Department of Pharmaceutics and Industrial Pharmacy
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherOctober University for Modern Sciences and Arts (MSA)
dc.contributor.otherCairo
dc.contributor.otherEgypt; Duuepartment of Pharmaceutics
dc.contributor.otherNational Organization for Drug Control and Research
dc.contributor.otherCairo
dc.contributor.otherEgypt
dc.date.accessioned2020-01-09T20:41:50Z
dc.date.available2020-01-09T20:41:50Z
dc.date.issued2015
dc.descriptionScopus
dc.description.abstractThe application of self-nanoemulsified drug delivery system (SNEDDS) to improve bioavailability of diacerein (D) has been hampered by its large dose and limited solubility. This work aimed to prepare diacerein loaded self nanoemulsifying self nanosuspension (D-SNESNS) containing high drug load. D-SNESNS was prepared by homogenizing D into Maisine-based SNEDDS that gave the highest drug solubility. D-SNESNS was evaluated for particle size, zeta potential and in vitro dissolution. Significant increase of D solubility was observed from D-SNESNS (?309 ?g/mL) than traditional SNEDDS (?162 ?g/mL) due to the spontaneous simultaneous formation of nanoemulsion and nanosuspension (top-down approach). When exposed to water with mild agitation, the drug microparticles in D-SNESNS are temporarily surrounded by unsaturated aqueous layer (containing optimum concentrations of surfactant and co-solvent) that facilitates the erosion of the suspended drug particles into nanosized ones. Nanoemulsion-based nanosuspension (NENS) was confirmed using transmission electron microscopy and particle size analysis. D-SNESNS equivalent to 50 mg D exhibited complete and very rapid dissolution after 15 min in phosphate buffer pH 6.8 due to the existence of D as solubilized molecules inside nanoemulsion globules and nanosized suspended drug particles forming D-NENS. The relative bioavailabilities of rhein from D-SNESNS in rats with normal and blocked chylomicron flow were about 210% and 164%, respectively in comparison to aqueous D suspension. The significant increase in the dissolution, portal absorption and lymphatic delivery of D propose that SNESNS could be promising to improve oral bioavailability of poorly water soluble drugs that have limited drug load in SNEDDS. 2015 Elsevier B.V. All rights reserved.en_US
dc.description.urihttps://www.scimagojr.com/journalsearch.php?q=22454&tip=sid&clean=0
dc.identifier.doihttps://doi.org/10.1016/j.ijpharm.2015.05.039
dc.identifier.doiPubMed ID 26002566
dc.identifier.issn3785173
dc.identifier.otherhttps://doi.org/10.1016/j.ijpharm.2015.05.039
dc.identifier.otherPubMed ID 26002566
dc.identifier.urihttps://t.ly/1VM95
dc.language.isoEnglishen_US
dc.publisherElsevieren_US
dc.relation.ispartofseriesInternational Journal of Pharmaceutics
dc.relation.ispartofseries490
dc.subjectBlocked chylomicron flowen_US
dc.subjectDiacereinen_US
dc.subjectLymphatic deliveryen_US
dc.subjectPortal absorptionen_US
dc.subjectSelf-nanoemulsifying self-nanosuspensionen_US
dc.subjectSNESNSen_US
dc.subjectchylomicronen_US
dc.subjectdiacereinen_US
dc.subjectphosphate buffered salineen_US
dc.subjectrheinen_US
dc.subjectsurfactanten_US
dc.subjectwateren_US
dc.subjectanthraquinone derivativeen_US
dc.subjectdiacereinen_US
dc.subjectdrug carrieren_US
dc.subjectemulsionen_US
dc.subjectnanoparticleen_US
dc.subjectrheinen_US
dc.subjectsurfactanten_US
dc.subjectsuspensionen_US
dc.subjectagitationen_US
dc.subjectArticleen_US
dc.subjectdrug absorptionen_US
dc.subjectdrug bioavailabilityen_US
dc.subjectdrug blood levelen_US
dc.subjectdrug delivery systemen_US
dc.subjectdrug eliminationen_US
dc.subjectdrug half lifeen_US
dc.subjectdrug solubilityen_US
dc.subjectdrug synthesisen_US
dc.subjectelimination rate constanten_US
dc.subjecterosionen_US
dc.subjectin vitro studyen_US
dc.subjectin vivo studyen_US
dc.subjectlymph vesselen_US
dc.subjectmaximum plasma concentrationen_US
dc.subjectnanoemulsionen_US
dc.subjectparticle sizeen_US
dc.subjectpHen_US
dc.subjectpriority journalen_US
dc.subjectsuspensionen_US
dc.subjecttime to maximum plasma concentrationen_US
dc.subjecttransmission electron microscopyen_US
dc.subjectzeta potentialen_US
dc.subjectadministration and dosageen_US
dc.subjectanimalen_US
dc.subjectbioavailabilityen_US
dc.subjectchemistryen_US
dc.subjectclassificationen_US
dc.subjectdrug delivery systemen_US
dc.subjectemulsionen_US
dc.subjectmaleen_US
dc.subjectmedicinal chemistryen_US
dc.subjectoral drug administrationen_US
dc.subjectpharmacokineticsen_US
dc.subjectproceduresen_US
dc.subjectraten_US
dc.subjectsolubilityen_US
dc.subjectsuspensionen_US
dc.subjectWistar raten_US
dc.subjectAdministration, Oralen_US
dc.subjectAnimalsen_US
dc.subjectAnthraquinonesen_US
dc.subjectBiological Availabilityen_US
dc.subjectChemistry, Pharmaceuticalen_US
dc.subjectDrug Carriersen_US
dc.subjectDrug Delivery Systemsen_US
dc.subjectEmulsionsen_US
dc.subjectMaleen_US
dc.subjectNanoparticlesen_US
dc.subjectParticle Sizeen_US
dc.subjectRatsen_US
dc.subjectRats, Wistaren_US
dc.subjectSolubilityen_US
dc.subjectSurface-Active Agentsen_US
dc.subjectSuspensionsen_US
dc.titleNovel self-nanoemulsifying self-nanosuspension (SNESNS) for enhancing oral bioavailability of diacerein: Simultaneous portal blood absorption and lymphatic deliveryen_US
dc.typeArticleen_US
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