In vivo, tLyp1-hNPs mainly accumulated in the tumor areas via the enhanced permeability and retention (EPR) effect with decreased accumulation in the spleen and liver, owing to the suitable particle size, surface modification with DSPE-PEG and the NRP-1 targeted peptide, resulting in the significant reduction of the tumor volume and prolong of the survival of mice in the B16/BL6 tumor model. This evidence concerns the gene NRP1 and neoplasm.