Enhanced Anticancer Therapeutic Delivery to Tumor Microenvironment via Simultaneous Angiogenesis and Tumor Targeting

Abstract Angiogenesis is an event commonly occurring during tumorigenesis and the following development and progression provide an ideal target for anticancer drug‐targeted delivery. Nanoparticles with tumor‐cell binding ability are usually used for tumor therapy and proved to be able to accumulate in tumor tissues. The nanoparticles with dual angiogenesis and tumor‐cell targeting capacity are expected to deliver therapeutics to the lesions of tumors more efficiently and should achieve a better tumor therapeutical effect. In the present study, we employed melanoma xenograft as a tumor model, with VGB peptide and FA as angiogenesis and tumor cell guiding moieties, and with micelles as a model nanoparticle to examine our hypothesis. As a result, we proved that the dual strategy enhanced the delivery of bufalin, an anticancer agent, and achieved a better therapeutical outcome for melanoma, compared to the conventional single‐targeting methods. Since angiogenesis is common in tumor development, the simultaneous targeting strategy can be flexibly adapted to a wide range of tumors.