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Sufentanil-2-hydroxypropyl-β-cyclodextrin Inclusion Complex For Pain Treatment: Physicochemical, Cytotoxicity, And Pharmacological Evaluation

dc.creatorVolobuef C.
dc.creatorMoraes C.M.
dc.creatorNunes L.A.S.
dc.creatorCereda C.M.S.
dc.creatorYokaichiya F.
dc.creatorFranco M.K.K.D.
dc.creatorBraga A.F.A.
dc.creatorde Paula E.
dc.creatorTofoli G.R.
dc.creatorFraceto L.F.
dc.creatorde Araujo D.R.
dc.date2012
dc.date2015-06-25T20:24:27Z
dc.date2015-11-26T15:19:57Z
dc.date2015-06-25T20:24:27Z
dc.date2015-11-26T15:19:57Z
dc.date.accessioned2018-03-28T22:29:27Z
dc.date.available2018-03-28T22:29:27Z
dc.identifier
dc.identifierJournal Of Pharmaceutical Sciences. , v. 101, n. 10, p. 3698 - 3707, 2012.
dc.identifier223549
dc.identifier10.1002/jps.23234
dc.identifierhttp://www.scopus.com/inward/record.url?eid=2-s2.0-84865384414&partnerID=40&md5=ebd7beef1569df0e41ab79de5046ed9b
dc.identifierhttp://www.repositorio.unicamp.br/handle/REPOSIP/90226
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/90226
dc.identifier2-s2.0-84865384414
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1259858
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-β-cyclodextrin (HP-β-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 ± 1.2M-1 between SUF and HP-β-CD. Complexation with HP-β-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 ± 0.39min-1/2 for SUF-HP-β-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 ± 34.6min) was significantly increased (p < 0.001) after complexation with HP-β-CD (355.7 ± 47.2min) when injected at the same dose (1μg 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. © 2012 Wiley Periodicals, Inc.
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dc.languageen
dc.publisher
dc.relationJournal of Pharmaceutical Sciences
dc.rightsfechado
dc.sourceScopus
dc.titleSufentanil-2-hydroxypropyl-β-cyclodextrin Inclusion Complex For Pain Treatment: Physicochemical, Cytotoxicity, And Pharmacological Evaluation
dc.typeArtículos de revistas


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