Injectable in situ forming nanogel: A hybrid Alginate-NLC formulation extends bupivacaine anesthetic effect

Author(s)

Rodrigues da Silva, Gustavo H. ^[1] ; Geronimo, Gabriela ^[1] ; Ribeiro, Ligia N. M. ^[1] ; Guilherme, Viviane A. ^[1] ; de Moura, Ludmilla David ^[1] ; Bombeiro, Andre L. ^[2] ; Oliveira, Juliana Damasceno ^[1] ; Breitkreitz, Marcia C. ^[3] ; de Paula, Eneida ^[1]

Affiliation

^[1] Univ Estadual Campinas, Inst Biol, Dept Biochem & Tissue Biol, UNICAMP, Rua Monteiro Lobato 255, BR-13083862 Campinas, SP - Brazil

^[2] Univ Estadual Campinas, Inst Biol, Dept Struct & Funct Biol, UNICAMP, Campinas, SP - Brazil

^[3] Univ Estadual Campinas, Dept Analyt Chem, Inst Chem, Campinas, SP - Brazil

• Document type: Journal article
• Source: Materials Science & Engineering C-Materials for Biological Applications; v. 109, APR 2020.
• Web of Science Citations: 0

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. (AU)

• FAPESP's process: 18/07100-4 - Citotoxicity and in vivo anesthesia effect of functional nanostructured lipid carriers loaded with S75:R25 bupivacaine, designed for burn treatment
• Grantee: Gabriela Geronimo
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• FAPESP's process: 14/25372-0 - Development of nanostructured lipid carriers encapsulating local anesthetics processed biopolymeric matrices for topical application at oral mucosa
• Grantee: Lígia Nunes de Morais Ribeiro
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 17/15174-5 - Development of functional lipid nanoparticles for the improvement of the anesthetic potency at inflamed tissues
• Grantee: Gustavo Henrique Rodrigues da Silva
• Support Opportunities: Scholarships in Brazil - Doctorate
• 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