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

dc.creatorVolobuef, Cristiane
dc.creatorMoraes, Carolina M.
dc.creatorNunes, Lazaro A. S.
dc.creatorCereda, Cintia M. S.
dc.creatorYokaichiya, Fabiano
dc.creatorFranco, Margareth K. K. D.
dc.creatorBraga, Angelica F. A.
dc.creatorDe Paula, Eneida
dc.creatorTofoli, Giovana Radomille
dc.creatorFraceto, Leonardo F.
dc.creatorDe Araujo, Daniele R.
dc.date2012
dc.date2013-09-19T18:06:36Z
dc.date2016-07-01T14:42:02Z
dc.date2013-09-19T18:06:36Z
dc.date2016-07-01T14:42:02Z
dc.date.accessioned2018-03-29T01:54:42Z
dc.date.available2018-03-29T01:54:42Z
dc.identifierJournal of Pharmaceutical Sciences. Wiley-Blackwell, v.101, n.10, p.3698-3707, 2012
dc.identifier0022-3549
dc.identifierWOS:000307966600017
dc.identifier10.1002/jps.23234
dc.identifierhttp://www.repositorio.unicamp.br/jspui/handle/REPOSIP/2288
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/2288
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1308612
dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.descriptionConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.descriptionSufentanil (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, 2012
dc.description101
dc.description10
dc.description3698
dc.description3707
dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.descriptionConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.descriptionConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.languageeng
dc.publisherWiley-Blackwell
dc.publisherHoboken
dc.relationJournal of Pharmaceutical Sciences
dc.rightsfechado
dc.sourceWOS
dc.subjectSufentanil
dc.subjectcyclodextrins
dc.subjectanalgesia
dc.subjectcontrolled release
dc.subjectcomplexation
dc.subjectinjectables
dc.subjectsolubility
dc.subjectHYDROXYPROPYL-BETA-CYCLODEXTRIN
dc.subjectDRUG-DELIVERY SYSTEMS
dc.subjectPHARMACEUTICAL APPLICATIONS
dc.subjectLOCAL-ANESTHETICS
dc.subjectNMR DIFFUSION
dc.subject2-HYDROXYPROPYL-BETA-CYCLODEXTRIN
dc.subjectSUFENTANIL
dc.subjectFENTANYL
dc.subjectANALGESIA
dc.subjectVEHICLE
dc.titleSufentanil-2-hydroxypropyl-beta-cyclodextrin inclusion complex for pain treatment: Physicochemical, cytotoxicity, and pharmacological evaluation
dc.typeArtículos de revistas


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