cis-Diaminedichloroplatinum(II) complexes reversibly bound to water-soluble polyaspartamide carriers for chemotherapeutic applications. II: Platinum coordination to ethylenediamine ligands attached to poly(ethylene oxide)-grafted carrier polymers

In continuation of previous investigations aiming at the development of macromolecular metal complexes for biomedical use, this communication describes poly(alkylene oxide)-grafted polymeric platinum complexes. The platinum-containing macromolecules are obtained from presynthesized polyaspartamide carriers bearing poly(ethylene/propylene oxide) side chains and hydroxyethyl side groups as hydrosolubilizing units in addition to ethylenediamine side group terminals for metal coordination. Platination is brought about by treatment of the carriers with tetrachloroplatinate(II) ion in aqueous solution at 25–60°C. pH 4–6. The polymeric products, purified by dialysis in aqueous solution, are isolated by freeze-drying in yields of 60–80%. Platinum contents are in the range of 4–15%. The metal is bound to the carrier through chelation with the ethylenediamine ligands, forming square-planarcis-dichloroethylenediamine-platinum(II) complex species as side-chain terminals. Initially, the product polymers dissolve smoothly in water. Although on room-temperature storage in the solid state they gradually turn insoluble as a consequence of intermolecular solid-state interaction, solubility is retained on low-temperature storage and in frozen aqueous solutions.