Disorders of the CNS, such as brain tumors, ischemic strokes, Alzheimer’s, and Parkinson’s disease, pose a significant risk to human well-being. The presence of the BBB further complicates the transportation of medications and the development of targeted drug delivery methods. In recent decades, considerable attention has been directed towards biomimetic vehicles derived from cell membranes, driven by the emergence of targeted drug delivery systems and biomimetic nanotechnology. Cell membranes are recognized as inherent multifunctional biomaterials, holding promise for the design and adaptation of targeted delivery strategies. The current conjunction of cell membranes and nanoparticles gives rise to biomimetic vehicles, offering fresh insights into BBB recognition, transportation, and efficient therapy. These vehicles leverage the diverse biological functions and strong biocompatibility of cell membranes, presenting a promising avenue for enhanced treatments. This article offers a summary of the current obstacles in achieving targeted delivery within the CNS and highlights recent progress made in utilizing various types of biomimetic vehicles derived from cell membranes for efficient CNS targeting. The discussion includes an exploration of the mechanisms involved in BBB targeting, in addition to an examination of the challenges and potential for clinical application. Ultimately, novel perspectives for advancement and development are also presented.