RESUMO
Type 2 diabetes is a fast-growing worldwide epidemic. Despite the multiple therapies available to treat type 2 diabetes, the disease is not correctly managed in over half of patients, mainly due to non-compliance with prescribed treatment regimes. The development of analogues to the glucagon-like peptide 1 (GLP-1) has resulted in the extension of its half-life and associated benefits. Further benefits in the use of peptide-based GLP-1 receptor agonists have been achieved by the use of controlled-release systems based on polymeric microparticles. In this review, we focus on commercially available formulations and others that remain in development, discussing the preparation methods and the relationship between in vitro and in vivo kinetic release behaviours.
Assuntos
Peptídeo 1 Semelhante ao Glucagon/análogos & derivados , Receptor do Peptídeo Semelhante ao Glucagon 1/agonistas , Polímeros/química , Diabetes Mellitus Tipo 2/tratamento farmacológico , Composição de Medicamentos , Peptídeo 1 Semelhante ao Glucagon/uso terapêutico , Humanos , Hipoglicemiantes/uso terapêutico , Tamanho da PartículaRESUMO
The GLP1-receptor agonists exert regulatory key roles in diabetes, obesity and related complications. Here we aimed to develop polymeric microparticles loaded with homologous human GLP1 (7-37) or the analogue liraglutide. Peptide-loaded microparticles were prepared by a double emulsion and solvent evaporation process with a set of eight polymers based on lactide (PLA) or lactide-glycolide (PLGA), and evaluated for particle-size distribution, morphology, in vitro release and pharmacologic activity in mice. The resulting microparticles showed size distribution of about 30-50 µm. The in vitro kinetic release assays showed a sustained release of the peptides extending up to 30-40 days. In vivo evaluation in Swiss male mice revealed a similar extension of glycemic and body weight gain modulation for up to 25 days after a single subcutaneous administration of either hGLP1-microparticles or liraglutide-microparticles. Microparticles-loaded hGLP1 shows equivalent in vivo pharmacologic activity to the microparticles-loaded liraglutide.
Assuntos
Peptídeo 1 Semelhante ao Glucagon/administração & dosagem , Peptídeo 1 Semelhante ao Glucagon/farmacologia , Liraglutida/administração & dosagem , Liraglutida/farmacologia , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/química , Animais , Preparações de Ação Retardada , Peptídeo 1 Semelhante ao Glucagon/farmacocinética , Humanos , Masculino , Camundongos , Tamanho da PartículaRESUMO
This work presents the synthesis and characterization of extrinsically magnetic poly(butylene succinate) (PBS). PBS is obtained from succinic acid (SA), which can be efficiently produced from renewable biomass by fermentation. Thus, the use of SA helps to remove CO2 from the atmosphere, constituting a good way to accumulate carbon credits. The magnetic PBS here presented was prepared by fusion using different amounts of maghemite. Obtained materials were characterized using Fourier transform infrared spectroscopy (FTIR), Thermogravimetric analysis (TGA), Differential scanning calorimetry (DSC), X-ray diffraction (XRD), Small angle X-ray scattering and magnetic force tests. Besides, the oil removal capability (OR) of the samples was also studied. All the magnetic composites were able to remove petroleum from the water. Among them, the one filled with the highest amount of magnetic particles was able to remove 11â¯g of oil per gram of composite. Also, XRD and SAXS results showed that PBS is a long size oriented material, which allows it to work as a thermoset, avoiding its dissolution in organic contaminant medium. As PBS can also be considered as a platform, these are promising results for the oil spill cleanup applications.