Development and pharmacological evaluation of ropivacaine-2-hydroxypropyl-β-cyclodextrin inclusion complex

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Autor(es): dc.creatorAraujo, Daniele R. de-
Autor(es): dc.creatorTsuneda, Simone S.-
Autor(es): dc.creatorCereda, Cíntia M. S.-
Autor(es): dc.creatorCarvalho, Fernanda Del G. F.-
Autor(es): dc.creatorPreté, Paulo S. C.-
Autor(es): dc.creatorFernandes, Sergio A.-
Autor(es): dc.creatorYokaichiya, Fabiano-
Autor(es): dc.creatorFranco, Margareth K. K. D.-
Autor(es): dc.creatorMazzaro, Irineu-
Autor(es): dc.creatorFraceto, Leonardo F.-
Autor(es): dc.creatorBraga, Angélica de F. A.-
Autor(es): dc.creatorPaula, Eneida de-
Data de aceite: dc.date.accessioned2026-02-09T11:51:10Z-
Data de disponibilização: dc.date.available2026-02-09T11:51:10Z-
Data de envio: dc.date.issued2020-05-18-
Data de envio: dc.date.issued2020-05-18-
Data de envio: dc.date.issued2008-01-
Fonte completa do material: dc.identifierhttps://repositorio.ufla.br/handle/1/40973-
Fonte completa do material: dc.identifierhttps://www.sciencedirect.com/science/article/abs/pii/S092809870700365X-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/capes/1148872-
Descrição: dc.descriptionRopivacaine (RVC) is an enantiomerically pure local anesthetic (LA) largely used in surgical procedures, which presents physico-chemical and therapeutic properties similar to those of bupivacaine (BPV), but associated to less systemic toxicity. This study focuses on the development and pharmacological evaluation of a RVC in 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex. Phase-solubility diagrams allowed the determination of the association constant between RVC and HP-β-CD (9.46 M−1) and showed an increase on RVC solubility upon complexation. Release kinetics revealed a decrease on RVC release rate and reduced hemolytic effects after complexation (onset at 3.7 mM and 11.2 mM for RVC and RVCHP-β-CD, respectively) were observed. Differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and X-ray analysis (X-ray) showed the formation and the morphology of the complex. Nuclear magnetic resonance (NMR) and job-plot experiments afforded data regarding inclusion complex stoichiometry (1:1) and topology. Sciatic nerve blockade studies showed that RVCHP-β-CD was able to reduce the latency without increasing the duration of motor blockade, but prolonging the duration and intensity of the sensory blockade (p < 0.001) induced by the LA in mice. These results identify the RVCHP-β-CD complex as an effective novel approach to enhance the pharmacological effects of RVC, presenting it as a promising new anesthetic formulation.-
Idioma: dc.languageen-
Publicador: dc.publisherElsevier-
Direitos: dc.rightsrestrictAccess-
???dc.source???: dc.sourceEuropean Journal of Pharmaceutical Sciences-
Palavras-chave: dc.subjectLocal anesthetic-
Palavras-chave: dc.subjectRopivacaine-
Palavras-chave: dc.subjectCyclodextrin-
Palavras-chave: dc.subjectAnalgesia-
Palavras-chave: dc.subjectDrug-delivery-
Título: dc.titleDevelopment and pharmacological evaluation of ropivacaine-2-hydroxypropyl-β-cyclodextrin inclusion complex-
Tipo de arquivo: dc.typeArtigo-
Aparece nas coleções:Repositório Institucional da Universidade Federal de Lavras (RIUFLA)

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