Article

Download article 		Title: Injectable in situ forming nanogel: A hybrid Alginate-NLC formulation extends bupivacaine anesthetic effect
Author: Ribeiro, Lígia N. M.; Alcântara, Ana C. S.; Rodrigues Da Silva, Gustavo H.; Franz-montan, Michelle; Nista, Silvia V. G.; Castro, Simone R.; Couto, Verônica M.; Guilherme, Viviane A.; De Paula, Eneida
Year: 2017
Is part of: International Journal of Polymer Science, v. 2017, p. 1 - 16
DOI: https://doi.org/10.1155/2017/1231464

Citation: Ribeiro, Lígia N. M.; Alcântara, Ana C. S.; Rodrigues Da Silva, Gustavo H.; Franz-montan, Michelle; Nista, Silvia V. G.; Castro, Simone R.; Couto, Verônica M.; Guilherme, Viviane A.; De Paula, Eneida; Injectable in situ forming nanogel: A hybrid Alginate-NLC formulation extends bupivacaine anesthetic effect. International Journal of Polymer Science, v.2017, p. 1-16, 2017

Abstract: Finding an ideal anesthetic agent for postoperative pain control, with long action and low side effects, is still a challenge. Local anesthetics have potential for such application if their time of action is improved. This work introduces a new hybrid formulation formed by the association of a nanostructured lipid carrier with a biopolymeric system to encapsulate bupivacaine (BVC). The hybrid formulation was physicochemical and structurally characterized by DLS, TEM, DSC, XRD and FTIR-ATR, and it remained stable for 12 months at room temperature. In vivo analgesia and imaging tests showed that the hybrid system was able to modulate the release, and to increase the concentration of BVC at the site of action, by forming a nanogel in situ. Such nanogel improved over 5 times ( > 24 h) the anesthesia duration, when compared to free BVC at clinical (0.5%) doses. Therefore, this novel in situ-forming nanogel shows great potential to be used in postsurgical pain control, improving the action of BVC, without losing its versatility of (infiltrative) application.

Keywords: drug delivery systems; hybrid hydrogel;
Subjects: CIENCIAS_BIOLOGICAS; Farmacologia Bioquímica e Molecular;

Funding: The authors thank FAPESP (#14/14457-5) and INCT-Bioanalitica for research grants, and the fellowships from FAPESP (#17/15174-5, #14/25372-0, #18/07100-4 - G.H.R.S., L.N.M.R and G.G.), CAPES (L.D.M.) and CNPq (J.D.O, E.P.). We are also grateful to Cristalia Prod. Quim. Farm. Ltda. for kindly providing Novabupi (R); Dhaymer Ind. Com. Prod. Quim Ltda for the donation of cetyl palmitate; Gatefosse do Brasil for providing Capryol 90 (R), and Nervous Regeneration Laboratory/Unicamp for the in vivo imaging analyzer. 		Financed by: