To study different formulations of Budesonide-containing microparticles for a colon-specific delivery of the drug to treat Crohn’s disease. Microparticles were prepared by solvent evaporation technique. The organic phase (10%) was composed by 5% (w/v) of polymer in methilene chloride and Budesonide 0.05% (w/v), while the dispersing phase was a solution of PVA 0.1% (w/w). Size and morphology of the obtained microparticles were analyzed by optical and scanning electron microscopies. The loading efficiency of Budesonide within microparticles was determined by HPLC and DSC analyses. The “in vitro” release was performed using receiving solutions able to simulate gastric (FaSSGF) and intestinal (FaSSIF) conditions. The amount of Budesonide released was quantified by HPLC. Microparticles of Eudragit RS100 or of Eudragit RS100/Eudragit RL100 70:30 (w/w) were prepared. The production yields were about 92% both in Eudragit RS100 microparticles and Eudragit RS100/RL100 particles. The mean diameters of microparticles preparations were superimposable being 24.86 µm ± 5.97 in the first case and 22.86 µm ± 6.24 in the second one. The DSC analysis confirms an interaction between the drug and the polymers. The loading efficiency of Budesonide was about 12% in the two preparations with only few variations. The “in vitro” studies, performed both in FaSSGF and in FaSSIF solutions, showed that after 3 hours the drug release from Eudragit RS100/RL100 microparticles was about six-fold higher than that obtained with monopolymer formulation (3.56% vs 22.92%). The intestinal simulating release after 6 hours was similar in both preparations (24.45% vs 23.87%). Microparticles produced with Eudragit RS100 showed a better protection of the drug from gastric acidity than Eudragit RS100/RL100 microparticles and an hypothetical system of colon specific controlled delivery
Preparation and characterization of microparticles containing budesonide
RAVANI, Laura;ESPOSITO, Elisabetta;MENEGATTI, Enea;CORTESI, Rita
2009
Abstract
To study different formulations of Budesonide-containing microparticles for a colon-specific delivery of the drug to treat Crohn’s disease. Microparticles were prepared by solvent evaporation technique. The organic phase (10%) was composed by 5% (w/v) of polymer in methilene chloride and Budesonide 0.05% (w/v), while the dispersing phase was a solution of PVA 0.1% (w/w). Size and morphology of the obtained microparticles were analyzed by optical and scanning electron microscopies. The loading efficiency of Budesonide within microparticles was determined by HPLC and DSC analyses. The “in vitro” release was performed using receiving solutions able to simulate gastric (FaSSGF) and intestinal (FaSSIF) conditions. The amount of Budesonide released was quantified by HPLC. Microparticles of Eudragit RS100 or of Eudragit RS100/Eudragit RL100 70:30 (w/w) were prepared. The production yields were about 92% both in Eudragit RS100 microparticles and Eudragit RS100/RL100 particles. The mean diameters of microparticles preparations were superimposable being 24.86 µm ± 5.97 in the first case and 22.86 µm ± 6.24 in the second one. The DSC analysis confirms an interaction between the drug and the polymers. The loading efficiency of Budesonide was about 12% in the two preparations with only few variations. The “in vitro” studies, performed both in FaSSGF and in FaSSIF solutions, showed that after 3 hours the drug release from Eudragit RS100/RL100 microparticles was about six-fold higher than that obtained with monopolymer formulation (3.56% vs 22.92%). The intestinal simulating release after 6 hours was similar in both preparations (24.45% vs 23.87%). Microparticles produced with Eudragit RS100 showed a better protection of the drug from gastric acidity than Eudragit RS100/RL100 microparticles and an hypothetical system of colon specific controlled deliveryI documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
