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. This evidence concerns the gene MMP2 and glioma.