POLYMERIC CONJUGATES OF PACLITAXEL AND DOCETAXEL WITH PH-CONTROLLED RELEASING OF THE CANCEROSTATIC AGENT

摘要

The present invention describes a polymeric conjugate consisting of a derivative of a cytostatic agent selected from the group of taxanes, in particular paclitaxel (PTX), docetaxel (DTX) or larotaxel (LTX), and a polymeric carrier prepared on the basis of a linear or biodegradable grafted copolymer consisting of units of the basic copolymer N-(2-hydroxypropyl)methacroylamide (HPMA) and units containing methacryloylated hydrazones of amino acids or oligopeptides. The invention also deals with a method of preparation of the above mentioned polymeric conjugate, in which the polymeric carrier is subjected to polymer-analogous transformation of the carrier by reaction with an ester of the oxo acid and the cytostatic agent. The polymeric conjugate is used for the preparation of a medicament for treatment of tumour diseases.