ABSTRACT

By conjugating water soluble polymers, the drawbacks of pharmacologically active protein drugs or enzymes can be greatly improved. Antigenicity can be drastically reduced; a 10- to several 100-fold prolongation of plasma half-life can be accomplished; biocompatible macromolecules have enhanced targeting to the sites of lesions such as cancer and inflammation; enhanced stability of polymer conjugates in vivo and in vitro makes them easy to handle, and by manipulating the lipophilicity of the conjugates one can make an oily formulation of protein drugs. Basic pathophysiological differences between tumorous/lesion and normal tissue are discussed, which make macromolecular drugs so unique and advantageous in vivo.