POLYMERIC CONJUGATES OF DOXORUBICIN WITH PH-REGULATED RELEASE OF THE DRUG AND A METHOD OF PREPARING

摘要

A polymeric drug in the form of a conjugate of a copolymer of N-(2-hydroxypropyl)- methacrylamide (HPMA) with doxorubicin bound to the polymer via spacers containing hydrolytically cleavable hydrazone bonds, of formula (I), wherein SP₁ represents an aminoacyl spacer, x = 40 to 335, y = 1 to 25, consisting of from 90 to 99.5 mol. % of units of HPMA and 10 to 0.5 mol. % of doxorubicin-containing comonomeric units. The conjugate is prepared via direct copolymerization of the doxorubicin-containing monomer of formula (II) with HPMA.