Obtenção, caracterização físico-química e avaliação biológica in vitro de dispersões sólidas amorfas com a,B-amirenona

Abstract

Obesity is a global public health issue, associated with diets high in fats and carbohydrates, as well as sedentary lifestyles, affecting approximately 25% of the Brazilian population, especially women. Lifestyle changes are the conventional treatment but face adherence challenges, leading to an increased search for medications and surgeries, which come with adverse effects. Triterpenes, such as α,βamirenone (ABAME), have shown antiobesity potential, but their poor water solubility limits their oral effectiveness. To overcome this limitation, solid dispersions (SD) of ABAME were prepared with the polymers PEG and PVP using malaxation (MX) and physical mixing (MF) techniques, aiming to improve solubility and pharmacological properties. The samples were characterized by techniques such as Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TG), X-ray Diffraction (XRD), Fourier Transform Infrared Spectroscopy (FTIR), and Scanning Electron Microscopy (SEM), indicating that the interaction between ABAME and the polymers promoted a transition from the crystalline to the amorphous state, as well as greater thermal stability compared to the isolated compound, particularly in the SDs obtained by MX. The quantification of ABAME was performed by High-Performance Liquid Chromatography (HPLC), meeting ANVISA standards and demonstrating success in SD development. In in vitro biological tests, the SDs showed greater efficacy in lipase inhibition compared to isolated ABAME, especially those prepared by MX, with a reduced IC50. Although antioxidant tests showed moderate results, with lower performance in total antioxidant capacity (TAC) and DPPH radical scavenging assessments, the SDs demonstrated excellent reducing power. The data, though preliminary, highlight the antiobesity potential of the SDs, marking them as a promising strategy compared to conventional treatments, which often present adverse effects.