| Abstract: | ![]()
Following a brief discussion of the concept of polymer–drug conjugation and the use of platinum drugs in cancer therapy, the paper presents recent results in the synthesis of water-soluble polymeric carriers designed for the binding of antineoplastic coordination compounds of the cisplatin type. The target polymers, specifically, are linear aliphatic polyamides comprising the ethylenediamine ligand system in the main chain as the potential metal binding site. With solubility in aqueous media a key requirement for intravenously injectable conjugates, the polymers also contain hydrosolubilizing oligo(ethylene oxide) units in the chain, which serve the additional purpose of imparting resistance to serum protein binding and capture by the reticuloendothelial system. The synthesis methods include interfacial polymerization, high-temperature solution polycondensation in polyphosphoric acid and Michael addition polymerization, with 1,2-bis(2-aminoethylamino)ethane and 1,2-bis(3-aminopropylamino)ethane used as the amine comonomers providing the ethylenediamine ligand segment. The target polymers, crudely fractionated by dialysis in 25,000 molecular-mass cult-off tubing, are isolated by freeze-drying as water-soluble solids possessing inherent viscosities of 10–20 ml/g. A selected carrier polymer is converted to the corresponding water-soluble cis-diaminedichloroplatinum(II) conjugate by treatment with tetrachloroplatinate(II) anion in aqueous solution. |
