Desarrollo y evaluación de microesferas biodegradables para la liberación prolongada de pramipexol

Fuentes, Constanza; von Plessing, Carlos; Fernández, Marcos

Keywords: Pramipexole, microspheres, PLGA, Parkinson's disease


Pramipexole (PMX) is a non-ergot dopamine agonist used to treat Parkinson's disease (PD). The development of an extended release formulation of PMX could be an effective therapeutic strategy to prevent or delay dyskinesias in PD. It would also be fundamental improvement in the treatment of these patients to improve their quality of life and reduce the number of administrations. The aim of this work was to develop and characterize a new formulation for the treatment of PD, consisting in PMX-loaded biodegradable microspheres. The microspheres were prepared using the copolymer of poly (lactic-co-glycolic acid) (PLGA 50:50, Resomer ® RG502) by the technique of emulsion / solvent evaporation from an O / W (A method A) and from a W / O / W (method B) emulsion. The microspheres were characterized by scanning electron microscopy, laser diffraction, differential scanning calorimetry and X-ray. Further, the encapsulation efficiency (EE) was determined and in vitro release studies were performed. The developed microspheres have characteristics of composition and size make it feasible parenteral administration. The EE was significantly higher for microspheres prepared by method B (60.9 ± 8.9%) than for those prepared by method (45.0 ± 5.2%). Best PMX release profile is achieved with the formulation obtained by Method A, with a constant release of the drug for two weeks (K0 = 23.3 ug/día/30mg). The microsphere formulation obtained by method A, is an attractive alternative as sustained release system for parenteral administration for PMX in the treatment of PD.

Más información

Título de la Revista: Revista de Farmacología de Chile
Volumen: 7
Número: 2
Editorial: Sociedad de Farmacologia de Chile
Fecha de publicación: 2014
Página de inicio: 25
Página final: 32
Idioma: Spanish
Notas: Latindex