Hybrid Nanoemulsions for Migraine Treatment

RIBEIRO, LÍGIA N.M.; COUTO, VERONICA M.; CASTRO, SIMONE R.; RODRIGUEZ DA SILVA, GUSTAVO H.; BREITKREITZ, MÁRCIA C.; MARTINEZ, CAROLINA SOLEDAD; IGARTÚA, DANIELA EDITH; PRIETO, MARIA JIMENA; DE PAULA, ENEIDA

Congreso; 20th IUPAB Congress, 45th Annual SBBf Meeting, and 50th Annual SBBq Meeting; 2021

INTRODUCTION: Migraine is a painful, disabling and often chronic disease, with no descriptions of cure so far. Intranasal sumatriptan succinate (SMT) is the gold standard drug in the treatment of migraine symptoms. Conversely, its efficacy by intranasal route is restrained by poor mucoadhesion. OBJECTIVES: The preparation of hybrid nanoemulsions (NE) with copaiba oil nanoparticles and xanthan, pectin or alginate biopolymers, for the intranasal sustained release of SMT (2%; w/v). MATERIALS AND METHODS: The blend of SMT and biopolymer matrices were encapsulated in copaiba oil nanoparticles, providing different hybrid NE. Structural characterization was performed by FTIR-ATR, DSC and TEM and the physicochemical stability was followed up a year (25 °C). The efficiency of encapsulation and SMT in vitro release profile were carried out. The nanotoxicity ofthe alginate-based NE (ALG-NE/SMT) was evaluated in vivo by measuring the mortality, spontaneous movement, morphological changes and cardiotoxicity of Zebrafish larvae. RESULTS AND DISCUSSION: The hybrid NE exhibited physicochemical stability over a year of storage at 25 °C, with size in the range of 120 nm, low polydispersity (~ 0.2), zeta potential around -25 mV, and concentration of ca. 2.1014 part/mL. The hybrid systems showed excellent SMT encapsulation (41-69 %), prolonging the in vitro SMT release for ca. 24 h, at 37 o C. The structuralanalyses confirmed the morphology of the particles and details on the molecular arrangements of the hybrid systems. The most suitable formulation (ALG-NE/SMT) was tested in Zebrafish larvae, showing no nanotoxicity in any of the evaluated parameters, after 48 h of treatment. CONCLUSIONS: These assays point out the ALG-NE/SMT system as a promising candidate for the treatment of migraine.