Cell-Penetrating Peptides-Mediated Therapeutic Agents Delivery into the Central Nervous System

There has been a significant increase in the prevalence of central nervous system (CNS) disorders, resulting in a considerable decrease in the overall well-being for affected individuals. Moreover, the therapeutic effectiveness of CNS diseases is greatly impeded by the inability of the majority of small molecule drugs and almost all large molecule drugs to penetrate the brain barrier. Therefore, it is crucial to develop an efficient drug delivery system to effectively treat CNS disorders by transporting therapeutic agents to the CNS. Cell-penetrating peptides (CPPs), which are well-known for their efficient membrane penetration capabilities and their ability to facilitate the rapid passage of therapeutic drugs across the brain barrier, offer a potential strategy for the transportation of macromolecules across the brain barrier. This study has provided a comprehensive overview of the utilization of CPP-mediated therapeutic agents in the management of CNS diseases and summarized the recent advancements in clinic, aiming to establish a scientific foundation for the application of CPPs in the treatment of CNS diseases.