Influence of particle size and dissolution conditions on the degradation properties of polylactide-co-glycolide particles.

Abstract

Polymer degradation usually plays a crucial role in drug release from sustained release polyester systems, therefore in order to elucidate the mechanism governing release, it appears essential to analyse the in vitro degradation behaviour of these devices. In this study the influence of processing conditions, particle characteristics and release media temperature on the degradation of PLGA spherical particles were examined. It was found that a linear relationship between the degradation rate and particle size existed, with the larger particles degrading fastest. In smaller particles degradation products formed within the particle can diffuse easily to the surface while in larger particles degradation products have a longer path to the surface of the particle during which autocatalytic degradation of the remaining polymer material can occur. The influence of release media temperature on the degradation of PLGA particles was also examined. At lower incubation temperatures PLGA microparticles showed an induction period after which polymer degradation proceeded. The rate of polymer degradation was found to increase with increasing incubation temperature. The polymer erosion profile was fitted to the Prout-Tompkins equation and the rate constants were used to determine the activation energy of PLGA hydrolysis.