ABSTRACT
This chapter presents an overview of tumor angiogenesis, strategies for targeting angiogenic vasculature, and developments in angiogenesis-targeted polymeric conjugates for diagnosis and therapy. There is a tremendous interest in targeted drug delivery to tumor vasculature given the genetic stability and accessibility of angiogenesis markers and the importance of angiogenesis in tumor growth and metastasis. A number of ligands targeting angiogenic markers have been identified, but the major focus has been on targeting αvß3 integrins using RGD peptides. Non-invasive imaging of angiogenesis markers should be important, both in therapy planning and in monitoring anti-angiogenic therapy. RGD peptides labeled with therapeutically relevant isotopes such as ß-particle emitters have been investigated as potential angiogenesis targeted radiotherapy. As additional vascular targets are identified by in vitro and in vivo methods, angiogenesis targeting may become a critically important strategy for fighting neoplastic as well as non-neoplastic diseases.
