Preparation of polyethylene oxide with 4-amino-N-(2-pyrimidinyl) benzene sulfonamide and diethylenetriaminepentaacetic acid end groups and its enrichment in tumour tissues

Abstract

Using polyethylene oxide (PEO) with 4-amino-N-(2-pyrimidinyl) benzene sulfonamide (APBS) and hydroxyl end groups (PEOa-h) as parent compounds, PEO with diethylenetriaminepentaacetic acid (DTPA) and APBS end groups (PEOa-d) was prepared by functionization of PEOa-h. After complexation of PEOa-d with isotopes of153Sm and99Tc, and injecting the polymer drug into the Kunming white mouse transplanted with Sarcoma-180, it was confirmed by γ-counter that the PEOa-d could be concentrated selectively in the tumour tissues, the ratio of concentration of the polymer drug in tumour tissue to that in ordinary organs such as liver, heart, spleen, muscle, blood and bone marrow is about 2.3:1 or even 10:1.