Certain properties of blood vessels in the brain limit their permeability to blood-borne ions, molecules, and cells. This blood–brain barrier (BBB) is essential for neurons to function properly and avoid brain damage, but it is also a major obstacle to drug delivery.

The blood-brain barrier is sometimes considered a static, impenetrable barrier. In fact, it has physical, transport, immune and other dynamic properties, which together tightly regulate the molecular movement between blood vessels and the brain, thereby regulating the molecular environment of the brain.

A major factor affecting the success of central drug development is the blood-brain barrier (BBB), which blocks almost 100% of macromolecular drugs and more than 98% of small molecule drugs. Therefore, in addition to the properties of better activity, metabolism and lower toxicity, CNS drugs also need to overcome the blood-brain barrier and achieve sufficient exposure in the CNS, which is the key to the success of CNS drug development. premise.

Drugs that target the central nervous system need to be able to effectively penetrate the blood-brain barrier, and blood-brain barrier permeability evaluation experiments can help understand the distribution ratio of compounds in plasma and brain tissue.

Blood-brain Barrier Permeability Study Protocol

SpeciesMouse, rat,
Dosing routeP.O., I.V., I.M.; I. P. etc
Groupsmultiple groups, one group per time point
Dosing frequencySingle dose
Number of animals3 per group
Time pointsTBD
Analysis methodLC-MS/MS
Data analysisWinnonlin

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