Natural lipids-based NLC containing lidocaine: from pre-formulation to in vivo studies

Author(s)

Ribeiro, Ligia N. M. ; Breitkreitz, Marcia C. ; Guilherme, Viviane A. ; da Silva, Gustavo H. R. ; Couto, Veronica M. ; Castro, Simone R. ; de Paula, Barbara O. ; Machado, Daisy ; de Paula, Eneida

• Document type: Journal article
• Source: European Journal of Pharmaceutical Sciences; v. 106, p. 102-112, AUG 30 2017.
• Web of Science Citations: 18

Abstract

In a nanotechnological approach we have investigated the use of natural lipids in the preparation of nanostructured lipid carriers (NLC). Three different NLC composed of copaiba oil and beeswax, sweet almond oil and shea butter, and sesame oil and cocoa butter as structural matrices were optimized using factorial analysis; Pluronic (R) 68 and lidocaine (LDC) were used as the colloidal stabilizer and model encapsulated drug, respectively. The optimal formulations were characterized by different techniques (IR-ATR, DSC, and TEM), and their safety and efficacy were also tested. These nanocarriers were able to upload high amounts of the anesthetic with a sustained in vitro release profile for 24 h. The physicochemical stability in terms of size (nm), PDI, zeta potential (mV), pH, nanoparticle concentration (particles/mL), and visual inspection was followed during 12 months of storage at 25 degrees C. The formulations exhibited excellent structural properties and stability. They proved to be nontoxic in vitro (cell viability tests with Balb/c 3T3 fibroblasts) and significantly improved the in vivo effects of LDC, over the heart rate of zebra fish larvae and in the blockage of sciatic nerve in mice. The results from this study support that the proper combination of natural excipients is promising in DDS, taking advantage of the biocompatibility, low cost, and diversity of lipids. (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
• 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