Abstract: OBJECTIVE To study the pharmaceutical properties and anti-tumor activity of 9-nitrocamptothecin(9-NC) stealth liposome between NGR polypeptides modification and unmodified group. METHODS Liposome was prepared using film-ultrasonic method, and its pharmaceutical properties, such as entrapment efficiency, release in vitro, lactone stability, were compared between modified and unmodified group. Based on HT1080 cells model, MTT method was used to investigate the effect on the growth of cells between NGR modified and unmodified group. Flow cytometry experiments were conducted to compare entry effect between two groups. RESULTS No significant differences were observed between liposome modified by NGR polypeptide and unmodified group in terms of pharmaceutical properties, release degree in vitro, and lactone stability. However, the experimental results showed that inhibition rate of HT1080 cells in the modified 9-NC stealth liposome increased significantly than that in unmodified group(P<0.05). Further, HT1080 uptake rate of NGR-modified liposome was significantly higher than unmodified liposomes. CONCLUSION While from the point of pharmaceutical properties, NGR polypeptides modified liposome show no significant difference, their antitumor effect and uptake efficiency are higher than unmodified group.