Development of S75:R25 bupivacaine‐loaded lipid nanoparticles functionalized with essential oils for treating melanoma

• DOI: 10.1002/jctb.6715
• Publication Date: 2021-03-02T07:57:14Z
• Authors: Gabriela Geronimo; Gustavo H Rodrigu...; Ludmilla D de Moura; Lígia NM Ribeiro; Viviane A Guilherme; Talita C Mendonça; Simone R Castro; Márcia C Breitkreitz; Eneida de Paula
• Keywords: 0303 health sciences; 03 medical and health sciences; 12. Responsible consumption; 3. Good health

Abstract BACKGROUND A new role as an antitumoral agent has been proposed for the local anesthetic bupivacaine (BVC), considering its toxic effects on cancer cells. However, such drug repositioning requires improvement in available concentrations and sustained release profiles to surpass BVC short action narrow therapeutic window. Nanostructured lipid carriers (NLC) may provide with release, they can be formulated essential oils, whose intrinsic properties act synergistically BVC. This study reports development of two NLC formulations prepared lavender or melaleuca oils enantiomeric excess S (−)75: R (+)25 (BVC S75 ). The nanoparticles were characterized by dynamic light scattering, nanotracking analysis, transmission electron microscopy, differential scanning calorimetry X‐ray diffraction, their stability was followed 1 year. Encapsulation efficiency vitro profile also measured. Additionally, effect viability mice (B16‐F10) human (SK‐MEL‐25) melanoma cells determined, vivo anesthesia assessed tail flick test mice. RESULTS optimized factorial design (NLC‐L‐B NLC‐M‐B) showed robust physical chemical properties, 1‐year . Cytotoxicity tests revealed a decrease IC 50 values, relative free , ~80% 62% (NLC‐L‐B) 80% 25% (NLC‐M‐B) cells, respectively. both doubled time CONCLUSION Combining excipients, containing interesting nanosystems treatment melanomas after further tests. © 2021 Society Chemical Industry (SCI).