Tumor vasculature-targeting nanomedicines.

Uncontrolled tumor growth and subsequent distant metastasis are highly dependent on an adequate nutrient supply from tumor blood vessels, which have relatively different pathophysiological characteristics from those of normal vasculature. Obviously, strategies targeting tumor vasculature, such as anti-angiogenic drugs and vascular disrupting agents, are attractive methods for cancer therapy. However, the off-target effects and high dose administration of these drug regimens critically restrict their clinical applications. In recent years, nanomedicines focused on tumor vasculature have been shown to be superior to traditional therapeutic methods and do not induce side effects. This review will first highlight the recent development of tumor vasculature-targeting nanomedicines from the following four aspects: 1) angiogenesis-inhibiting nanomedicines (AINs); 2) vasculature-disrupting nanomedicines (VDNs); 3) vasculature infarction nanomedicines (VINs); and 4) vasculature-regulating nanomedicines (VRNs). Furthermore, the design principles, limitations, and future directions are also discussed. STATEMENT OF SIGNIFICANCE: Based on the essential roles of tumor blood vessels, the therapeutic strategies targeting tumor vasculature have exhibited good clinical therapeutic outcomes. However, poor patient adherence to free drug administration limits their clinical usage. Nanomedicines have great potential to overcome the abovementioned obstacle. This review summarizes the tumor-vasculature targeting nanomedicines from four aspects: 1) angiogenesis-inhibiting nanomedicines (AINs); 2) vasculature-disrupting nanomedicines (VDNs); 3) vasculature infarction nanomedicines (VINs); and 4) vasculature regulating nanomedicines (VRNs). In addition, this review provides perspectives on this research field.