The blood-brain barrier (BBB) is a highly selective and protective barrier that separates the circulating blood from the brain tissue. This barrier consists of tightly packed endothelial cells that line the blood vessels in the brain, as well as specialized transport proteins and enzymes that restrict the entry of certain substances into the brain.
While the blood-brain barrier serves as a protective mechanism for the brain to prevent harmful substances from entering, researchers are developing various strategies to enhance drug penetration and improve treatment outcomes for brain-related conditions.
In the paper Development and validation of PAMPA-BBB QSAR model to predict brain penetration potential of novel drug candidates, researchers tested ~2,000 small molecules to explore their permeability across the blood-brain barrier and correlated in vitro PAMPA-BBB data with in vivo brain permeation data in rodents to observe a categorical correlation of 77%, suggesting that models developed using data from PAMPA-BBB can forecast in vivo brain permeability.
The Pion PAMPA (Parallel Artificial Membrane Permeability Assay) for Blood-Brain Barrier (BBB) is a laboratory test that measures the permeability of a compound across an artificial membrane that mimics the properties of the BBB. This assay was used in this study to predict the ability of a drug or compound to penetrate the BBB and reach the brain, which is important for determining the potential efficacy of the compound in treating central nervous system disorders.
The researchers concluded, "By providing valuable insights into blood-brain barrier permeation, our research contributes significantly to advancing drug discovery efforts. Ultimately, the successful implementation of these in silico tools holds the promise of revolutionizing the drug discovery process, leading to considerable time savings and improved efficiency."
Contact us today to learn more about Pion's PAMPA for BBB studies.
