| Full text | |
| Author(s): Show less - |
Araujo, Daniele R. de
;
Tsuneda, Simone S.
;
Cereda, Cíntia M. S.
;
Carvalho, Fernanda Del G. F.
;
Preté, Paulo S. C.
;
Fernandes, Sergio A.
;
Yokaichiya, Fabiano
;
Franco, Margareth K. K. D.
;
Mazzaro, Irineu
;
Fraceto, Leonardo F.
;
et al
Total Authors: 11
|
| Document type: | Journal article |
| Source: | European Journal of Pharmaceutical Sciences; v. 33, n. 1, p. 60-71, Jan. 2008. |
| Field of knowledge: | Health Sciences - Dentistry |
| Abstract | |
Ropivacaine (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-beta-cyclodextrin (HP-P-CD) inclusion complex. Phase-solubility diagrams allowed the determination of the association constant between RVC and HP-beta-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-beta-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-beta-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-beta-CD complex as an effective novel approach to enhance the pharmacological effects of RVC, presenting it as a promising new anesthetic formulation. (AU) | |