The blood–brain barrier (BBB) functions as an inherent protective barrier that prevents the infiltration of toxins and pathogens from breaching the central nervous system (CNS). While this barrier is integral for neuroprotection, this barrier complicates the management of CNS conditions by impeding the delivery of most medicinal compounds to the brain. While this obstacle plays a crucial role in safeguarding the nervous system, it also presents difficulties in managing CNS conditions by obstructing the passage of the majority of medicinal compounds to the brain. This limitation in administering the drug across the BBB results in diminished rehabilitation potency and heightened side effects, as drugs tend to accumulate in nontarget organs and tissues. Recent studies have introduced diverse and sophisticated materials characterized by customizable structures and properties. Concurrently, extensive study of the brain and BBB has contributed to the evolution of strategies for exclusive drug administration to the brain specifically designed to enhance BBB permeability. Among these strategies, receptor-mediated drug delivery emerges as a distinctive approach that exploits variations in receptor expression levels among brain cells and other bodily tissues. While reducing the side effects, it permits the active delivery of a diverse range of therapeutics—such as gene therapy, small compounds, and antibodies to the CNS. This study aims to provide a comprehensive summary of the diverse receptors manipulated for BBB penetration and drug delivery, elucidating the recent advancements in this field.