In conclusion, these assays strongly suggest that the prepared siTGF-β1@ILP based on cetuximab-functionalization was an excellent system to deliver TGF-β1 siRNA to A549 cells, which could enhance the gene silencing effect of siRNA by promoting tumor-targeting effects, so as to achieve the purpose of treating NSCLC. This evidence concerns the gene TGFB1 and non-small cell lung carcinoma.