Background <p>Neurological disorders, including Parkinson’s and Alzheimer’s disease, impose a significant burden on individuals and healthcare systems. Effective treatment is often hindered by the restrictive nature of the blood–brain barrier (BBB), limiting drug access to the central nervous system (CNS).</p> Aim <p>The purpose of this review is to provide an overview of existing methods to deliver therapeutics to the CNS across the BBB with an emphasis on drug delivery systems that utilize nanotechnology.</p> Method/source <p>We performed a thorough review of the published literature on recently emerging trends in pharmacology and nanomedicine that have attempted to deliver drugs to the CNS by addressing the challenge of delivering therapeutics across the BBB.</p> Result/finding <p>Nanoparticles and nanocarriers have shown promise for crossing the blood–brain barrier (BBB), improving drug bioavailability in the brain, and facilitating targeted delivery. Several systems applying nanomaterials, including polymeric nanoparticles, liposomes, solid-lipid nanoparticles, and quantum dots, have successfully advanced through preclinical or early clinical studies. However, demonstrated evidence of the implementation and uptake of nanoparticles in specific antitumor and neurotherapeutic indications have several significant challenges, primarily due to safety, biocompatibility, and scalability.</p> Conclusion <p>The combination of traditional pharmacology and nanotechnology provides valuable opportunities for drug delivery to the CNS. Gains in the design of nanocarrier systems have great potential for addressing the limits of BBBs and for improving therapeutic outcomes in neurological disease, but more research is necessary for the development of translational clinical studies.</p>