The invention relates to a targeted
drug-bearing ultrasonic microbubble comprising a lipide dimolecular layer outer shell, targeted polypeptide fixed at the outer side of the lipide dimolecular layer outer shell, a biological
inert gas wrapped in the lipide dimolecular layer outer shell and medicament granules dispersed in the lipide dimolecular layer outer shell. The targeted polypeptide is a polypeptide or
protein derivative containing an
amino acid sequence CGNKRTRGC. By connecting the polypeptide or
protein derivative containing a
tumor targeted peptide sequence outside the lipide dimolecular layer outer shell, the obtained targeted
drug-bearing ultrasonic microbubble can target the
lymph vessels and the
tumor cells of a tumor, can detect and diagnose the generation, the development and the
curative effect on the tumor in real time through high-frequency
ultrasonic imaging and can crush the microbubble through low-frequency
ultrasound to release the medicament granules so as to achieve the aim of controllably and targetedly releasing the medicament, thereby having extremely important meanings to the prevention, diagnose and treatment of the tumor. In addition, the invention also relates to a preparation method of the targeted
drug-bearing ultrasonic microbubble.