POLYMERIC MICELLE COMPLEXES OF LOW MOLECULAR WEIGHT ANTITUMOR AGENTS AND STYRENE MALEIC ACID COPOLYMERS

摘要

The present invention relates to polymeric antitumor agents in whichpolymeric complex micelle structures are formed by intermolecular binding ormutual interaction between styrene maleic acid copolymer (SMA) and a lowmolecular antitumor agent which is an anthracyclin drug such as pirarubicin,doxorubicin, epirbicin, daunorbicin, aclarubicin, or alkaloid antitumor agentsuchas cis-platinum or taxol.These polymeric micelle antitumor agents may improve selectiveaccumulation of drugs to cancer tissue for improved antitumor effect, whileconcentrating less at normal organs or tissues, so that a lesser adverseeffect maybe accomplished.These polymeric antitumor agents may be prepared by dissolvingSMA and a low molecular antitumor agent in aqueous solution, then in thepresence of aqueous soluble carbodiimide, amino acids, or polyamine, adjustingpH to form micelle complexes, and separating and recovering the polymericmicelle component.