The present invention belongs to the field of pharmaceutical technology and clinical pharmacy, relates to a cyclopeptide containing arginine-glycine-aspartic acid (RGD) sequence and its active liposome targeting, its preparation and application. The described cyclopeptide structure meets the requirements as ligand, and is cyclized by amido bond, its spatial conformation is stable, and is not easily degraded, its one end contains active sulphydryl group, and is convenient for modifying artificially-synthetic function peptide, its molecular weight is small, so that it is not easy to result in immune reaction, and can be used as ligand, and can be combined with hepatic stellate cell (HSC) surface integrator acceptor to construct active liposome targeting and implement target therapy for experimental hepatic fibroid cell. Said invention can obtain good therapeutic effect for curing hepatitis fibrosis.