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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Optimised NLC: a nanotechnological approach to improve the anaesthetic effect of bupivacaine

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Author(s):
Rodrigues da Silva, Gustavo H. ; Ribeiro, Ligia N. M. ; Mitsutake, Hery ; Guilherme, Viviane A. ; Castro, Simone R. ; Poppi, Ronei J. ; Breitkreitz, Marcia C. ; de Paula, Eneida
Total Authors: 8
Document type: Journal article
Source: International Journal of Pharmaceutics; v. 529, n. 1-2, p. 253-263, AUG 30 2017.
Web of Science Citations: 11
Abstract

The short time of action and systemic toxicity of local anaesthetics limit their clinical application. Bupivacaine is the most frequently used local anaesthetic in surgical procedures worldwide. The discovery that its S(-) enantiomeric form is less toxic than the R(+) form led to the introduction of products with enantiomeric excess (S75:R25 bupivacaine) in the market. Nevertheless, the time of action of bupivacaine is still short; to overcome that, bupivacaine S75: R25 (BVCS75) was encapsulated in nanostructured lipid carriers (NLC). In this work, we present the development of the formulation using chemometric tools of experimental design to study the formulation factors and Raman mapping associated with Classical Least Squares (CLS) to study the miscibility of the solid and the liquid lipids. The selected formulation of the nanostructured lipid carrier containing bupivacaine S75: R25 (NLCBVC) was observed to be stable for 12 months under room conditions regarding particle size, polydispersion, Zeta potential and encapsulation efficiency. The characterisation by DSC, XDR and TEM confirmed the encapsulation of BVCS75 in the lipid matrix, with no changes in the structure of the nanoparticles. The in vivo analgesic effect elicited by NLCBVC was twice that of free BVCS75. Besides improving the time of action, no statistical difference in the blockage of the sciatic nerve of rats was found between 0.125% NLCBVC and 0.5% free BVCS75. Therefore, the formulation allows a reduction in the required anaesthesia dose, decreasing the systemic toxicity of bupivacaine, and opening up new possibilities for different clinical applications. (C) 2017 Elsevier B.V. All rights reserved. (AU)

FAPESP's process: 14/14457-5 - Lipid-based nanocarriers (SLN/NLC and remote-loading liposomes) used to improve the upload and potency of local anesthetics
Grantee:Eneida de Paula
Support Opportunities: Research Projects - Thematic Grants