Sythesis of anti-angiogenic drug conjugates against breast canser

Abstract

Angiogenesis, formation of new blood vessel, has a primary role in local growth and distant metastasis in breast cancer. By an anti-angiogenic therapy for breast cancer, this process can be inhibited. Different from conventional chemotherapy agents, selectivity of anti-angiogenic agents toward newly formed and disorganized blood vessels around the tumor is an attractive tool for reduced toxicity. Polymer-drug conjugates are designed to achieve improved drug targeting to the tumor, to reduce drug toxicity and to overcome the mechanisms of drug resistance. By conjugation of a therapeutic agent to a water soluble polymer, its aqueous solubility can be significantly improved. Therapeutically effective concentration of an agent can be achieved when a particular drug delivery profile like rate and duration are designed. Moreover, accumulation of these macromolecules only in the tumor tissue can be accomplished by “enhanced permeability and retention effect”. In this thesis, we disclose the synthesis of novel poly(ethylene glycol) methacrylate based copolymers containing drug units as side chains by free radical polymerization, analytical characterization and examination the effect of the prepared conjugates on human umbilical vein endothelial cells (HUVECs) in vitro.