Tumor-Targeting Peptide for Redox-Responsive Pt Prodrug and Gene Codelivery and Synergistic Cancer Chemotherapy

A new codelivery system combining prodrug strategy, siRNA/BAplatin @CRGDK NPs, to overcome cisplatin (CDDP) resistance in human breast cancer was designed and researched. Negatively charged siRNA was deposited onto the surface of tumor-targeting peptide-functionalized BAplatin@ CRGDK NPs. SiRNA/BAplatin@CRGDK NPs could facilitate cellular uptake of BAplatin and increase the cell proliferation suppression effect of Pt against MDA-MB-231/DDP cells. The tumor-to-kidney uptake ratio of the siRNA/BAplatin@ CRGDK NPs in MB-231/DDP tumors is 2.4-fold higher than that of cisplatin in MB-231/DDP tumors, thus giving rise to more significant antitumor efficacy. It demonstrated that the siRNA/BAplatin@CRGDK NPs is a potential, safe, and efficient therapeutic agent for cancer therapy.