Scientists have long been trying to find accurate methods to measure drug permeability across the blood-brain barrier, a crucial layer of cells that protects the brain from harmful substances. The challenges they faced included factors like blood flow and plasma protein binding, which influenced permeability in various ways.
In a groundbreaking study published in December 2024 in the journal “Fluids and Barriers of the CNS,” Dr. Quentin R. Smith from the Texas Tech University Health Sciences Center developed a method to measure blood-brain barrier permeability accurately. This method aimed to address discrepancies in the field and provide precise measurements across a wide range of compounds, from poorly crossing polar compounds to rapidly crossing CNS drugs.
Dr. Smith, who has been studying the blood-brain barrier since 1981, highlighted the confusion in the field regarding drug permeability and the need for a robust model to determine permeability accurately. The team evaluated 120 compounds and found that many approved CNS drugs permeate the barrier and reach the brain in less than 10 minutes.
The study also emphasized the role of plasma proteins in brain delivery, especially for lipophilic agents. These proteins can help maintain the concentration of free drug in plasma, allowing for rapid uptake into the brain. The findings challenged previous literature and provided new insights into drug permeability and brain uptake mechanisms.
One important application of this research is in the treatment of repetitive epileptic seizures, where rapid brain permeability is crucial for effective treatment. The study showed that most agents used in this condition had high brain permeability values, indicating their ability to reach therapeutic levels quickly.
Dr. Smith’s team included researchers from various institutions, all working together to advance our understanding of blood-brain barrier permeability. The results of this study have important implications for drug development, especially in conditions with low brain blood flow like ischemic stroke or brain bleeds.
Looking ahead, Dr. Smith is optimistic about the future of blood-brain barrier research and expects significant advancements in the field in the coming years. This study represents a significant step forward in our understanding of drug permeability across the blood-brain barrier and opens up new possibilities for developing more effective treatments for CNS disorders.
For more information on this groundbreaking research, you can access the full article in “Fluids and Barriers of the CNS” with the DOI: 10.1186/s12987-024-00584-y. This study was made possible by the collaborative efforts of researchers from Texas Tech University and other institutions, paving the way for future breakthroughs in brain drug delivery.
