Abstract: Drugs need to be transported across membranes in the body in order to play their roles in cells. As a tool for loading drugs into target cells/tissues, drug carriers can solve such problems as short half-life, poor stability and insolubility in water or lipids during drug transport in living organisms in spite of the disadvantages of low drug encapsulation rate and easy leakage. Self-assembly refers to the spontaneous arrangement of disordered basic structural units into an ordered structure. Self-assembled drug carrier can protect the drug from the immune system in the organism and allow it to function in a controlled, efficient and low side-effect way on target cells under the right conditions. This review summarizes the basic concepts of self-assembly structure-driven drug transmembrane transport and relevant research progress and clinical applications in the biomedical field in recent years, providing researchers with new design strategies for selfassembly structure-driven drug transmembrane transport.