Release of a macromolecular drug from alginate-impregnated microspheres.
Macroporous microspheres were impregnated with calcium alginate to encapsulate fluorescein isothiocyanate-labeled dextran (FITC-dextran) and control its release. The detailed study of the impregnation process lead to its optimization: the quantity of alginate in the impregnated microspheres and the FITC-dextran encapsulation efficiency were increased. FITC-dextran diffused out of the impregnated microspheres in a slow rate in deionised water, while in presence of sodium ions, its release rate was increased as a consequence of the progressive swelling and erosion of calcium alginate. Release studies from different formulations of impregnated microspheres were performed in a continuous flow apparatus. The release profiles were composed of a slow release phase explained by the progressive erosion of calcium alginate and a faster release phase related to eroded impregnated microspheres. Therefore, the delayed release by microspheres induced by impregnation would permit the delivery of their payload at the vascular occlusion site, limit the amount of drug lost in the systemic circulation and improve the therapy.
Chretien
C
C
R&D Galénique, AGEPS, Faculté de Sciences Pharmaceutiques et Biologiques, Université Paris 5, 4 avenue de l'Observatoire, 75270 Paris cedex 06, France.
Chaumeil
J C
JC
D000464:Alginates / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000737:chemistry*; D003911:Dextrans / Q000737:chemistry*; D004339:Drug Compounding; D016650:Fluorescein-5-isothiocyanate / Q000031:analogs & derivatives* / Q000737:chemistry; D007700:Kinetics; D008863:Microspheres; D010316:Particle Size; D012995:Solubility
D000464:Alginates; D003692:Delayed-Action Preparations; D003911:Dextrans; C015219:fluorescein isothiocyanate dextran; D016650:Fluorescein-5-isothiocyanate