Preparation, Physicochemical Characterization, and In Vitro Biological Evaluation of Amorphous Solid Dispersions with α,β-Amyrenone.
Obesity; α,β-amyrenone; Solid Dispersions; Lipase Inhibition; Antioxidant.
Obesity is a serious global public health problem, frequently associated with a diet high in fats and carbohydrates, as well as sedentary behavior. In Brazil, it affects approximately 25% of the population, predominantly women. Although conventional treatment, based on lifestyle changes, is recommended, it faces challenges due to the demands of modern life, leading to an increased reliance on medications and surgical interventions as the most sought-after alternatives. However, the medications used to treat obesity present various adverse effects, which has driven the search for natural alternatives. In this context, triterpenes, such as α,β-amyrinone (ABAME), the focus of this study, show significant anti-obesity potential. However, its low water solubility limits its biological activity and compromises its oral efficacy. To overcome this challenge, solid dispersions (SD) were prepared with ABAME using malaxation (MX) and physical mixing (FM) techniques with the polymers PEG and PVP, aiming to improve its solubility and pharmacological properties. The samples were characterized by techniques such as DSC, TG, XRD, FTIR, and SEM, which indicated that the interaction of ABAME with the polymers promoted a transition from the crystalline to the amorphous state, as well as improved thermal stability compared to the isolated compound, particularly in the SD obtained by MX. The quantification of ABAME was performed by HPLC, meeting the criteria set by ANVISA, and demonstrated success in the development of the SD. In vitro biological tests showed that the SD exhibited greater efficacy in inhibiting lipase compared to isolated ABAME, especially the SD prepared by MX, with a reduced IC50. Although the antioxidant tests showed moderate results, with lower performance in the CAT and DPPH assays, the SD demonstrated excellent reducing power. Although preliminary, the data reveal the anti-obesity potential of the SD, highlighting them as a promising strategy compared to conventional treatments, which often present adverse effects.