The present invention relates to a neuropilin-1 ligand polypeptide-polyethylene glycol-phospholipid composite, its active targeting liposome vector system and a preparation method thereof. The liposome vector system comprises the following components: a: phospholipid, b: cholesterol, c: methoxy polyethylene glycol-phospholipid composite (with the molecular weight of methoxy polyethylene glycol ranging from 400 to 6000), and d: a RPAKPAR sequence-containing polypeptide-polyethylene glycol-phospholipid composite (with the molecular weight of polyethylene glycol ranging from 400 to 8000). And for the components, a and b are in a molar ratio of 5:1-1:5, a and c are in a molar ratio of 1000:1-1000:100, and a and d are in a ratio of 1000:0.1-1000:100. The system can make a liposome passively drained into a lymphatic system through subcutaneous interstitial injection or intramuscular injection, and can make the liposome targeted to a lymphatic metastasis lesion through the mediation effect of RPAKPAR. The system can also make the liposome targeted to a primary tumor and a hematogenous metastasis lesion directly through intravenous injection administration, through a tumor EPR (electron paramagnetic resonance) effect and the mediation effect of RPAKPAR. The liposome vector system of the invention can be used for targeted drug delivery in diagnosis or treatment of prostate cancer primary tumors and metastatic tumors.