The application of microparticulate systems in the develop-ment and improvement of drugs: in vivo and vitro studies
Triperpenes, α-amirenone, β-amirenone, antioxidant, microparticles.
Microparticles have, among other characteristics, sizes between 1 and 1000 μm, which, in the context of the development of pharmaceutical formulations, can form modified delivery systems, modulating drug characteristics, such as solubility, pharmacokinetics and bioavailability. They are classified as microcapsules or microspheres and can have different types of shapes. There has been a growing number of studies over the years that use this technology to improve existing drugs or to enable the placement of new drug candidates, proving the effectiveness of its use in in vitro and in vivo assays. This study presents a review that describes several works with microparticles, showing how the insertion of substances in these systems improved undesirable characteristics of these substances in several aspects, such as pharmacodynamics, pharmacokinetics and physicochemical. In addition, it brings perspectives for the development of microparticles with the insertion of α, β-amyrenone, a pentacyclic triterpene that consists of an isomeric mixture of compounds with an Ursane and Oleonane skeleton, extracted from native plants in the Amazon region with widespread use in folk medicine. Potential hypoglycemic, lipid-lowering and antioxidant pharmacological activities have been described and show activity and selectivity against key components related to α-glucosidase and pancreatic lipase enzymes, involved in the process of carbohydrate and lipid metabolization and which are targets of studies related to the treatment of Diabetes, dyslipidemia and related illnesses such as metabolic syndrome. These enzymatic activities will be tested, as well as the physicochemical characterization of the system will be carried out in order to obtain better bioavailability profiles compared to the free compound.