This review discusses the potential and advantages of using mesenchymal stem cells (MSCs) as carriers for drug delivery across the blood–brain barrier (BBB). MSCs, known for their multilineage differentiation capacity and anti-inflammatory properties, can be used to deliver various substances, including low molecular weight compounds and genetically modified protein expression products, to target sites in the brain. The review highlights the challenges in drug development for neurodegenerative diseases, such as Alzheimer's and Parkinson's, due to the BBB's impermeability. MSC-mediated drug delivery offers a solution by allowing non-invasive administration of drugs directly to the brain. The review also covers the clinical trials and applications of MSCs in regenerative medicine, particularly in treating brain cancers, neurodegenerative diseases, stroke, traumatic brain injury, amyotrophic lateral sclerosis, and multiple sclerosis. Additionally, it explores the use of MSCs as carriers for nanoparticles, which may be more technologically feasible than encapsulating drugs within MSCs. The conclusion emphasizes the potential of MSC therapy in delivering innovative medical care to patients with various neurological disorders.This review discusses the potential and advantages of using mesenchymal stem cells (MSCs) as carriers for drug delivery across the blood–brain barrier (BBB). MSCs, known for their multilineage differentiation capacity and anti-inflammatory properties, can be used to deliver various substances, including low molecular weight compounds and genetically modified protein expression products, to target sites in the brain. The review highlights the challenges in drug development for neurodegenerative diseases, such as Alzheimer's and Parkinson's, due to the BBB's impermeability. MSC-mediated drug delivery offers a solution by allowing non-invasive administration of drugs directly to the brain. The review also covers the clinical trials and applications of MSCs in regenerative medicine, particularly in treating brain cancers, neurodegenerative diseases, stroke, traumatic brain injury, amyotrophic lateral sclerosis, and multiple sclerosis. Additionally, it explores the use of MSCs as carriers for nanoparticles, which may be more technologically feasible than encapsulating drugs within MSCs. The conclusion emphasizes the potential of MSC therapy in delivering innovative medical care to patients with various neurological disorders.