Sufentanil-2-hydroxypropyl-beta-cyclodextrin inclusion complex for pain treatment: Physicochemical, cytotoxicity, and pharmacological evaluation

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dc.contributor.authorVolobuef, Cristiane
dc.contributor.authorMoraes, Carolina M.
dc.contributor.authorNunes, Lazaro A. S.
dc.contributor.authorCereda, Cintia M. S.
dc.contributor.authorYokaichiya, Fabiano
dc.contributor.authorFranco, Margareth K. K. D.
dc.contributor.authorBraga, Angelica F. A.
dc.contributor.authorDe Paula, Eneida
dc.contributor.authorTofoli, Giovana Radomille
dc.contributor.authorFraceto, Leonardo F. [UNESP]
dc.contributor.authorDe Araujo, Daniele R.
dc.contributor.institutionUniversidade Estadual de Campinas (UNICAMP)
dc.contributor.institutionLab Nacl Luz Sincrotron
dc.contributor.institutionUniv Sao Francisco
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionUniversidade Federal do ABC (UFABC)
dc.date.accessioned2014-05-20T15:30:22Z
dc.date.available2014-05-20T15:30:22Z
dc.date.issued2012-10-01
dc.description.abstractSufentanil (SUF) is a synthetic analgesic opioid widely used for the management of acute and chronic pain. This drug was complexed with 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and the physicochemical characterization, in vitro/ex vivo toxicity assays, and pharmacological evaluation were performed. Differential scanning calorimetry, Fourier transform infrared spectroscopy (FTIR) analysis, and X-ray powder diffraction showed the formation and the morphology of the complex. Nuclear magnetic resonance afforded data regarding inclusion complex stoichiometry (1:1) with an association binding constant (Ka) value of 515.2 +/- 1.2?M-1 between SUF and HP-beta-CD. Complexation with HP-beta-CD protected SUF from light exposure and increased its photostability. Release kinetics revealed a decrease in SUF release rate (Krel = 7.05 +/- 0.52 and 5.61 +/- 0.39?min-1/2 for SUFHP-beta-CD and SUF, respectively) and reduced hemolytic or myotoxic effects after complexation. Time course of tail-flick test showed that the duration of analgesia induced by SUF (150.0 +/- 34.6?min) was significantly increased (p < 0.001) after complexation with HP-beta-CD (355.7 +/- 47.2?min) when injected at the same dose (1 mu g kg-1), prolonging the duration of analgesia after intramuscular administration and representing an alternative on the development of effective and safe drug-delivery system for opioid analgesics. (C) 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:36983707, 2012en
dc.description.affiliationUniv Estadual Campinas, Dept Bioquim, Inst Biol, São Paulo, Brazil
dc.description.affiliationLab Nacl Luz Sincrotron, São Paulo, Brazil
dc.description.affiliationUniv Estadual Campinas, Dept Anestesiol, Fac Ciencias Med, São Paulo, Brazil
dc.description.affiliationUniv Sao Francisco, Unidade Gastroenterol & Farmacol Clin, São Paulo, Brazil
dc.description.affiliationUniv Estadual Julio de Mesquita Filho UNESP, Dept Engn Ambiental, São Paulo, Brazil
dc.description.affiliationUniversidade Federal do ABC (UFABC), Ctr Ciencias Nat & Humanas, UFABC, BR-09210170 São Paulo, Brazil
dc.description.affiliationUnespUniv Estadual Julio de Mesquita Filho UNESP, Dept Engn Ambiental, São Paulo, Brazil
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorshipIdFAPESP: 06/00121-9
dc.description.sponsorshipIdFAPESP: 10/11475-1
dc.description.sponsorshipIdCNPq: 300952/2010-4
dc.format.extent3698-3707
dc.identifierhttp://dx.doi.org/10.1002/jps.23234
dc.identifier.citationJournal of Pharmaceutical Sciences. Hoboken: Wiley-blackwell, v. 101, n. 10, p. 3698-3707, 2012.
dc.identifier.doi10.1002/jps.23234
dc.identifier.issn0022-3549
dc.identifier.urihttp://hdl.handle.net/11449/39771
dc.identifier.wosWOS:000307966600017
dc.language.isoeng
dc.publisherWiley-Blackwell
dc.relation.ispartofJournal of Pharmaceutical Sciences
dc.relation.ispartofjcr3.075
dc.relation.ispartofsjr0,984
dc.rights.accessRightsAcesso restrito
dc.sourceWeb of Science
dc.subjectSufentanilen
dc.subjectcyclodextrinsen
dc.subjectanalgesiaen
dc.subjectcontrolled releaseen
dc.subjectcomplexationen
dc.subjectinjectablesen
dc.subjectsolubilityen
dc.titleSufentanil-2-hydroxypropyl-beta-cyclodextrin inclusion complex for pain treatment: Physicochemical, cytotoxicity, and pharmacological evaluationen
dc.typeArtigo
dcterms.licensehttp://olabout.wiley.com/WileyCDA/Section/id-406071.html
dcterms.rightsHolderWiley-blackwell
unesp.author.orcid0000-0002-9289-4229[11]
unesp.author.orcid0000-0001-5934-1609[3]
unesp.author.orcid0000-0002-2827-2038[10]
unesp.campusUniversidade Estadual Paulista (Unesp), Instituto de Ciência e Tecnologia, Sorocabapt

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