Provided is a method for treatment of liver cancer and inhibition of metastasis with CXCR4-targeted nanoparticle. A CXCR4 antagonist is used as a targeting molecule to modify a lipid carrier for the formation of nanoparticle carrying an anti-angiogenesis drug or an anti-angiogenic nucleotide. Such nanoparticle can enhance the accumulation and uptake of the drug and nucleotide in liver cancer cells as well as sensitize the liver cancer cells to treatment of said drug and nucleotide, providing a synergistic suppression of angiogenesis and tumor progression. Furthermore, the CXCR4-targeted nanoparticle can effectively inhibit metastasis of liver cancer. The pharmaceutical composition is an injectable composition hence, is suitable for clinical application for the treatment of liver cancer.
