Strategy for tumor targeting by macromolecule-drug conjugates

Abstract

The disposition and tumor localization of model macromolecules with the same molecular weight but different electric charge were studied in sarcoma 180 bearing mice. Dextran (T-70) with molecular weight of 70,000, cationic DEAE-dextran (T-70), anionic CM-dextran (T-70), bovine serum albumin(BSA), and cationized BSA (cBSA) were injected intravenously and their tissue distribution was determined by radioactivity counting. The cationic macromolecules were rapidly cleared from plasma and accumulated in the liver, and spleen or excreted into urine, while tumor levels remained low. On the contrary, anionic macromolecules were retained in the plasma for a long time and slowly accumulated to the tumor. The present study revealed that macromolecules having an anionic charge are advantageous for tumor targeting. © 1988, THE JAPAN SOCIETY OF DRUG DELIVERY SYSTEM. All rights reserved.