Cathepsin B degradable star-shaped peptidic macromolecules for delivery of 2-methoxyestradiol.

2-Methoxyestradiol (2ME), a natural metabolite of estradiol, has antiproliferative and antiangiogenic activity. However, its clinical success is limited due to poor water solubility and poor pharmacokinetic parameters suggesting the need for a delivery vehicle. In this study we evaluated cathepsin B degradable star-shaped peptidic macromolecules (SPMs) that can potentially be used to create higher generation and high molecular weight peptidic polymer as delivery vehicle of 2ME.