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dc.creatorDordevic, Sanela M
dc.creatorCekic, Nebojsa
dc.creatorSavić, Miroslav M.
dc.creatorIsailovic, Tanja M
dc.creatorRanđelović, Danijela
dc.creatorMarković, Bojan D.
dc.creatorSavić, Saša R.
dc.creatorStamenic, Tamara Timic
dc.creatorDaniels, Rolf
dc.creatorSavić, Snežana D.
dc.date.accessioned2019-01-30T17:45:04Z
dc.date.available2019-01-30T17:45:04Z
dc.date.issued2015
dc.identifier.issn0378-5173
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/1697
dc.description.abstractThis paper describes design and evaluation of parenteral lecithin-based nanoemulsions intended for brain delivery of risperidone, a poorly water-soluble psychopharmacological drug. The nanoemulsions were prepared through cold/hot high pressure homogenization and characterized regarding droplet size, polydispersity, surface charge, morphology, drug-vehicle interactions, and physical stability. To estimate the simultaneous influence of nanoemulsion formulation and preparation parameters-co-emulsifier type, aqueous phase type, homogenization temperature-on the critical quality attributes of developed nanoemulsions, a general factorial experimental design was applied. From the established design space and stability data, promising risperidone-loaded nanoemulsions (mean size about 160 nm, size distribution LT 0.15, zeta potential around -50 mV), containing sodium oleate in the aqueous phase and polysorbate 80, poloxamer 188 or Solutol (R) HS15 as co-emulsifier, were produced by hot homogenization and their ability to improve risperidone delivery to the brain was assessed in rats. Pharmacokinetic study demonstrated erratic brain profiles of risperidone following intraperitoneal administration in selected nanoemulsions, most probably due to their different droplet surface properties (different composition of the stabilizing layer). Namely, polysorbate 80-costabilized nanoemulsion showed increased (1.4-7.4-fold higher) risperidone brain availability compared to other nanoemulsions and drug solution, suggesting this nanoemulsion as a promising carrier worth exploring further for brain targeting.en
dc.publisherElsevier Science Bv, Amsterdam
dc.relationinfo:eu-repo/grantAgreement/MESTD/Technological Development (TD or TR)/34031/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/175076/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Technological Development (TD or TR)/32008/RS//
dc.rightsrestrictedAccess
dc.sourceInternational Journal of Pharmaceutics
dc.subjectParenteral nanoemulsionsen
dc.subjectBrain targetingen
dc.subjectPoorly water-soluble drugsen
dc.subjectGeneral factorial designen
dc.subjectPhysical stabilityen
dc.subjectPharmacokineticsen
dc.titleParenteral nanoemulsions as promising carriers for brain delivery of risperidone: Design, characterization and in vivo pharmacokinetic evaluationen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractСтамениц, Тамара Тимиц; Савиц, Снезана Д; Дордевиц, Санела М; Савиц, Мирослав М; Цекиц, Небојса Д; Марковиц, Бојан Д; Исаиловиц, Тања М; Савиц, Саса Р; Даниелс, Ролф; Ранђеловић, Данијела;
dc.citation.volume493
dc.citation.issue1-2
dc.citation.spage40
dc.citation.epage54
dc.citation.other493(1-2): 40-54
dc.citation.rankM21
dc.description.otherAccepted version: [http://cer.ihtm.bg.ac.rs/handle/123456789/3201]
dc.identifier.pmid26209070
dc.identifier.doi10.1016/j.ijpharm.2015.07.007
dc.identifier.rcubConv_3394
dc.identifier.scopus2-s2.0-84938080952
dc.identifier.wos000360492000005
dc.type.versionpublishedVersion


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