Abstract: 【Objective】 The aim of this study was to prepare an efficient polymeric anticancer drug delivery system and to investigate its effect on cell activity. The anticancer drug 6-MP was covalently bonded to the-OH group of poly-HPMA through the carbonyl sulfide vinyl linker of glutathione reaction, and two polymers HPMA-PTA and polymers HPMA-FA-PTA were prepared.【Method】 The structures of the two complexes were characterised by Fourier transform infrared spectroscopy, thermogravimetric analysis,UV analysis and scanning electron microscopy.【Result】 The two complexes were spherical particles with a diameter of about 100～150 nm. The cytotoxicity analysis of the prepared polymers was performed by MTT method and flow cytometry, which confirmed the good anticancer effects of the products.【Conclusion】 Poly（HPMA）-PTA and poly（HPMA）-FA-PTA polymers have obvious targeting and antitumour effects. It shows a good prospect of biological application.