Transferrin, also known as TRF or Tf, is a major glycoprotein in the plasma of vertebrates that plays a critical role in the transport and metabolism of iron ions. It is synthesized mainly in the liver and is responsible for carrying iron absorbed from the digestive tract and iron released from the degradation of red blood cells. Transferrin enters the bone marrow in the form of TRF-Fe3+ complex, supplying iron for the production of mature red blood cells. This protein can carry two trivalent iron ions (Fe3+) per molecule and interacts with Fe3+ depending on pH; it binds Fe3+ efficiently at pH 7.4 and releases it under acidic conditions. Transferrin also has several physiological and biochemical functions, including antimicrobial activity, involvement in immune system cell protection, and regulation of cell proliferation. Moreover, it serves as a novel active targeting carrier in the field of tumor targeting, showing promise for future applications.