Sistemas nano/microemulsionados como carreadores para derivado flavonoídico (FLAVONA)

Abstract

Infectious diseases are responsible for about 25% deaths worldwide and 45% in underdeveloped countries. Antimicrobials are usually used to fight an established infection, they aim either to eliminate or to impede bacterial growth without causing harm to the patient. Flavone, a molecule derived from flavonoids, has evidence of bactericidal activity, with LogP of 3.37 which indicates high lipophilicity. Therefore, it needs a carrier system with lipophilic characteristics, such as microemulsions (ME) and nanoemulsions (NE) O/A, that are systems indicated to its incorporation and use as a novel drug delivery system (NDDS). The aim of this work was to develop nano/microemulsion systems for the incorporation of flavone, aiming topical application, characterizing them physico-chemically, defining a methodology for drug dosing. For the development of the systems and for the choice of formulations to be studied, the construction of the pseudo-ternary phase diagram was performed, followed by incorporation of the drug (1 mg/mL). From this, the physicochemical characterization of the samples was initiated: macroscopic evaluation, isotropy, pH measurement, refractive index, differential scanning calorimetry (DSC), transmission electron microscopy (MET), Zeta potential, droplet size and polydispersity index. In addition, the validation of an analytical method for flavone assay by UV-VIS spectrophotometer and high-performance liquid chromatography (HPLC) was performed. The NE developed was composed of 10.8% oil phase (isopropyl myristate), 25.87% surfactants (polyethylene glycol (15)-hydroxystearate/sorbitan monooleate 80) and 63.33% water. The ME has 34.5% oil phase, 34.5% surfactants and 31% water. Through isotropy, DSC and MET it was possible to prove that the nanoemulsion is O/A and the ME is a bicontinuous system. The analytical methods were validated, both linear, selective, accurate and robust. The present study was relevant for the area of pharmaceutical technology. We sought to develop novel systems with relevant therapeutic potential, since the proposed systems are unprecedented and the drug has the potential to treat antimicrobial diseases.