Integrin αvβ3 is restrictedly expressed on angiogenic blood vessels and tumour cells. It plays a key role in angiogenesis for tumour growth and metastasis. RGD peptide can specifically recognise the integrin αvβ3, which serves as targeted molecular for anti-angiogenesis strategies. Therefore, the targeted delivery of therapeutics by RGD peptide-based non-viral vectors to tumour vasculature and tumour cells is recognised as a promising approach for treating cancer. In this review, we illustrate the interaction between RGD peptide and integrin αvβ3 from different perspectives. Meanwhile, four types of RGD peptide-based non-viral gene delivery vectors for cancer therapy, including RGD-based cationic polymers, lipids, peptides and hybrid systems, are summarised. The aim is to particularly highlight the enhanced therapeutic effects and specific targeting ability exhibited by these vectors for cancer gene therapy both in vitro and in vivo.
Keywords: RGD; cancer therapy; integrin αvβ3; non-viral vector; targeted gene delivery.