Obtenção de um insumo farmacêutico ativo vegetal com atividade ansiolítica obtido a partir de Erytrina velutina Willd (Mulungu)

Abstract

Anxiety is one of the main mental disorders of today, thus configuring itself as a research tool of great interest, especially regarding effective therapeutic alternatives with fewer adverse effects. In Brazilian folk medicine, Erythrina velutina Willd. (Fabaceae), popularly known as "bico-de-papagaio" or "mulungu," is a plant found in tropical and subtropical regions of the country, for which the decoction of the bark is used against some parasitic infections and mainly as a sedative and calming agent. Therefore, this work aims to produce and standardize a plant-based active pharmaceutical ingredient (API) from a medicinal plant originating from the Brazilian semi-arid region, with potential anxiolytic properties. Initially, the hydroalcoholic extract of E. velutina bark was obtained using different extraction methods (ultrasound and turbolysis) and different solvent concentrations, resulting in the APIs. Subsequently, phytochemical screening was carried out to quantify the main metabolites present. Based on this investigation, the most promising extract underwent standardization of the chemical marker using high-performance liquid chromatography (HPLC) and quantification through UV-visible spectroscopy. Subsequently, the in vivo toxic potential was evaluated in a single dose (2000 mg/kg) using Swiss mice. To assess the anxiolytic activity of the dried extract of E. velutina, behavioral tests were conducted, such as the Elevated Plus Maze Test (EPMT), Spontaneous Locomotor Activity Test (SLAT), and Rotarod Test. Next, the extract was combined with binary mixtures of pharmaceutical excipients using techniques such as Differential Thermal Analysis (DTA), Thermogravimetric Analysis (TG), Fourier Transform Infrared Spectroscopy (FTIR), and chemometric techniques (PCA and HCA) to assess the presence or absence of incompatibilities. As a result, the studies revealed that the extraction method that yielded the highest quantity of secondary metabolites from E. velutina extract was turbolysis, in the ratio of water: ethanol 30/70 v/v. Acute toxicity of the extract in mice did not show any toxicity, classifying it as non-toxic. In vivo pharmacological tests revealed that the E. velutina extract at a dose of 250 mg/kg demonstrated greater anxiolytic potential when compared to other administered doses. During the compatibility investigation, some evidence of interaction between the extract and excipients was observed through DTA, TG, PCA, and HCA techniques, but no chemical interactions were observed in the FTIR technique. Thus, excipients that showed promise for composing a future formulation were lactose, hydroxypropylmethylcellulose, and magnesium stearate. Therefore, the study allowed for the production of an API from E. velutina with proven anxiolytic activity, promising in the treatment of anxiety disorders as a therapeutic alternative. Keywords: Anxiety. Erythrina velutina. Anxiolytic potential.