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Type: Artigo de periódico
Title: Sufentanil-2-hydroxypropyl-β-cyclodextrin Inclusion Complex For Pain Treatment: Physicochemical, Cytotoxicity, And Pharmacological Evaluation
Author: Volobuef C.
Moraes C.M.
Nunes L.A.S.
Cereda C.M.S.
Yokaichiya F.
Franco M.K.K.D.
Braga A.F.A.
de Paula E.
Tofoli G.R.
Fraceto L.F.
de Araujo D.R.
Abstract: Sufentanil (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.
Citation: Journal Of Pharmaceutical Sciences. , v. 101, n. 10, p. 3698 - 3707, 2012.
Rights: fechado
Identifier DOI: 10.1002/jps.23234
Date Issue: 2012
Appears in Collections:Unicamp - Artigos e Outros Documentos

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