Due to the importance of in vitro release tests in establishing batch-to-batch reproducibility and in vitro/in vivo correlation, this study investigated the influence of the agitation regimen on the in vitro release behavior of leuprolide from PLGA microparticles. Leuprolide loaded microspheres were prepared using Resomer® RG502H and RG503H as polymers. Leuprolide in vitro release was performed in phosphate buffer solution under continuous or once-a-week agitation. At predetermined intervals, leuprolide release, polymer mass loss (ML), and degree of hydration (DH) were investigated. Leuprolide release and ML were higher under continuous agitation with respect to that under intermittent agitation. Using a modified version of Koizumi equation, it was possible to fit leuprolide release profiles. f2 comparison showed a high level of similarity between experimental and modeled data in the case of once-a-week agitation regimen. This work highlights the importance of the in vitro release conditions on peptide release behavior from polyester microparticles.
Effect of agitation regimen on the in vitro release of leuprolide from PLGA microparticles
SCHOUBBEN, Aurelie Marie Madeleine;BLASI, PAOLO;
2012
Abstract
Due to the importance of in vitro release tests in establishing batch-to-batch reproducibility and in vitro/in vivo correlation, this study investigated the influence of the agitation regimen on the in vitro release behavior of leuprolide from PLGA microparticles. Leuprolide loaded microspheres were prepared using Resomer® RG502H and RG503H as polymers. Leuprolide in vitro release was performed in phosphate buffer solution under continuous or once-a-week agitation. At predetermined intervals, leuprolide release, polymer mass loss (ML), and degree of hydration (DH) were investigated. Leuprolide release and ML were higher under continuous agitation with respect to that under intermittent agitation. Using a modified version of Koizumi equation, it was possible to fit leuprolide release profiles. f2 comparison showed a high level of similarity between experimental and modeled data in the case of once-a-week agitation regimen. This work highlights the importance of the in vitro release conditions on peptide release behavior from polyester microparticles.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
