There have been great advancements in targeted nanodrug delivery systems for tumor therapy. Liposomes, polymeric nanoparticles, and inorganic nanoparticles are commonly employed as nanocarriers for drug delivery, and it has been found that arginine glycine aspartic acid (RGD) peptides and their derivatives can be used as ligands of integrin receptors to enhance the direct targeting ability. In this paper, we review the recent applications of RGD-modified liposomes, polymeric nanoparticles, and inorganic nanocarriers in cancer diagnosis and treatment, discuss the current challenges and prospects, and examine the progress made by the latest research on RGD peptide–modified nano delivery systems in cancer therapy. In recent years, RGD peptide–modified nanodrug delivery systems have been proven to have great potential in tumor therapy. Finally, we provide an overview of the current limitations and future directions of RGD peptide–modified nano-drug delivery systems for cancer therapy. This review aims to elucidate the contribution of RGD peptide–modified nanodrug delivery systems in the field of tumor therapy.

Malignant tumors are life-threatening, and chemotherapy is one of the common treatment methods. However, there are often many factors that contribute to the failure of chemotherapy. The multidrug resistance of cancer cells during chemotherapy has been reported, since tumor cells’ sensitivity decreases over time. To overcome these problems, extensive studies have been conducted to reverse drug resistance in tumor cells. Elemene, an extract of the natural drug Curcuma wenyujin, has been found to reverse drug resistance and sensitize cancer cells to chemotherapy. Mechanisms by which elemene reverses tumor resistance include inhibiting the efflux of ATP binding cassette subfamily B member 1(ABCB1) transporter, reducing the transmission of exosomes, inducing apoptosis and autophagy, regulating the expression of key genes and proteins in various signaling pathways, blocking the cell cycle, inhibiting stemness, epithelial–mesenchymal transition, and so on. In this paper, the mechanisms of elemene’s reversal of drug resistance are comprehensively reviewed.