AN INJECTABLE COMPOSITION COMPRISING POLYMERIC NANOPARTICLES CONTAINING RAPAMYCIN WITH AN IMPROVED WATER SOLUBILITY AND A METHOD FOR PREPARING THE SAME, AND AN ANTICANCER COMPOSITION COMPRISING THE SAME FOR A COMBINATION THERAPY WITH RADIATION

摘要

PURPOSE: A polymeric nanoparticle injection formulation composition containing rapamycin with improved water solubility is provided to ensure biocompatibility and to enhance anticancer efficiency. CONSTITUTION: A rapamycin-containing polymeric nanoparticle injection formulation composition contains A-B type double block copolymer containing hydrophilic polymer and hydrophobic block; an alkali metal salt of polylactic acid or derivative thereof containing at least one carbonxy groups; and rapamycin as an active ingredient. The composition additionally contains bivalent or trivalent metal ion. The bivalent or trivalent metal ion is calcium, magnesium, barium, chrome, manganese, nickel, copper, zinc, or aluminum. A method for preparing the composition comprises: a step of solubilizing the A-B type double block copolymer, alkali metal salt of the polylactic acid or derivative thereof, and rapamycine in an organic solvent; a step of removing organic solvent from the resultant; and a step of adding aqueous medium.