SUBMICRON NANOPARTICLE OF POORLY WATER SOLUBLE CAMPTOTHECIN DERIVATIVES AND PROCESS FOR PREPARATION THEREOF

摘要

A nanoparticle composition comprising a poorly water soluble camptothecin derivative is provided to show effective anti-cancer activity by stabilizing a lactone form of the camptothecin derivative in body fluid. A nanoparticle composition of a camptothecin derivative comprises the camptothecin derivative such as camptothecin and 7-ethyl-10-hydroxycamptothecin and an anti-associative agent selected from the group consisting of a solid phase polyethyleneglycol, a solid phase amphiphilic block copolymer and a solid phase surfactant such as polyethylene glycol tocopherol succinic acid ester. A method for preparing the nanoparticle composition comprises the steps of: (a) melting the camptothecin derivative in the solid phase polyethylene glycol at a temperature of 60-180 deg.C; (b) cooling the molten solution to form a solid dispersion; and (c) dissolving the solid dispersion in an aqueous solution of the solid phase amphiphilic block copolymer or the solid phase surfactant.