Since the concept of aggregation-induced emission (AIE) was first coined by Tang and co-workers, AIE-active luminogens (AIEgens) have drawn widespread attention among chemists and biologists due to their unique advantages such as high fluorescence efficiency, large Stokes shift, good photostability, low background noise, and high biological visualization capabilities in the aggregated state, surpassing conventional fluorophores. A growing number of AIEgens have been engineered to possess multifunctional properties, including near-infrared emission, two-photon absorption, reactive oxygen species (ROS) generation and photothermal conversion, making them suitable for deep-tissue imaging and phototherapy. AIEgens show great potential in biomedical applications in vitro and in vivo. However, despite the favorable photophysical stability and ROS/heat generation capability in the aggregated state, limitations including uncontrolled size, low targeting efficiency, and unexpected dispersion in physiological environments have hindered their biomedical applications. The combination of AIEgens with lipids offers a simple, promising, and widely adopted solution to these challenges. This review article provides an overview of the synthesis methods of AIEgen-lipid nanostructures and their applications in the biomedical engineering field, aiming to serve as a guideline for developing these AIEgens-lipid nanostructures with promising biological applications.