Nanotechnology has advanced greatly in recent years and antiangiogenic therapy is becoming a promising approach for cancer treatment. Therefore, a combination of nanotechnology with antiangiogenic therapy should significantly enhance our ability to treat this deadly disease. alpha(v)beta(3)-integrin has often been used to target 'angiogenically active' tumor endothelium and many nanoparticles have been developed by combining this molecule with other agents for imaging and/or therapy. Development of improved and multifunctional nanoparticles is in progress for the enhancement of imaging, targeting, delivery and other processes. Modification for clinical use has been challenging. Concerns remain regarding safety, stability and tissue targeting of the particles, yet significant progress has been made. In this review, studies targeting 'angiogenically active' tumor endothelium using nanoparticles are discussed. The number of studies using multifunctional nanotechnology in tumor angiogenesis is still limited; however, significant advancement in this area is expected to come in the near future.