In the normal human brain (left), SST is highly expressed throughout the brain and in the cerebrospinal fluid. The most abundant SST isoform in the brain is SST-14, which contains 14 amino acids with a disulfide bond between cysteine residues. In the context of various neurological disorders (right), alterations in SST expression in a specific region or throughout the brain are observed. A decrease in SST expression might lead to a shrinkage of the brain and an imbalance in neural networks and function. The following disorders showing such pathologies are discussed in the text: Alzheimer’s disease, Parkinson’s disease, Huntington’s disease, major depressive disorder, and schizophrenia. Three approaches can be used to deliver functional neuropeptide SST to the brain for the treatment of these disorders: chemical modification to enhance BBB penetration, nanoformulations, and gene therapy techniques.