Furthermore, the inhibition rate of SynB3‐PVGLIG‐PTX was significantly higher than those of TMZ and PTX; and 4) the combined use of an MMP‐2‐sensitive peptide can be performed, and CPPs (SynB3) in a dual‐functional peptide enhanced BBB permeation and the glioma targeting effect of SynB3‐PVGLIG‐PTX, leading to high antitumor activity with low adverse effects during treatment. The gene discussed is MMP2; the disease is central nervous system cancer.