Desenvolvimento de micropartículas poliméricas carregadas com Liraglutida para uso oral

Abstract

Liraglutide is a peptide similar to the hormone GLP-1 that clinically promotes significant reductions both in glycated hemoglobin (HbA1c) and in weight loss, has been used in the treatment of one of the main causes of morbidity and mortality in the world, Diabetes Mellitus type 2 (DM2). The present study refers to the development of polymeric microparticles loaded with Liraglutide, for oral use, with the aim of promoting the controlled release of the peptide, providing protection from gastrointestinal effects and increasing patient compliance with treatment. The formulations were developed using the double emulsification method followed by solvent extraction, using the polymer Eudragit® S100 and the drug Victoza® (Liraglutide 6mg/mL). The formulations were evaluated according to yield and encapsulation efficiency, morphological analysis (SEM), particle size distribution, thermogravimetric analysis and in vitro release profile. After characterization, the formulations showed a yield of approximately 55%, with 91.4% encapsulation efficiency and spherical shape. In the size distribution analysis, the microparticles inserted in pH 4,5 medium showed sufficient concentration to carry out the readiness in the device up to 40 minutes, proving the solubilization in this pH range. With the in vitro release analysis, it can be said that the polymer helped to protect the petid in a simulated acid medium and that the microparticles were solubilized in a simulated basic medium, presenting a pseudo first order kinetics with 75% of the peptide release in 4.5 hours. However, the results of this work support the continuity of the study for the development of the formulation of Liraglutide for oral use.