Brain penetration of drugs

Kelder et al. [19] have shown that PSA can be used to model oral absorption and brain penetration of drugs that are transported by the transcellular route. A good correlation was found between brain penetration and PSA (n=45, r=0.917). From analyzing a set of 2366 central nervous system (CNS) and non-CNS oral drugs that have reached at least phase 11 clinical trials it was concluded that orally active drugs that are transported passively by the transcellular route should have PSA< 120 Al In addition, different PSA distributions were found for CNS and non-CNS drugs. 

D. M., Delbressine, L. P. C., Ploemen, ).-P. Polar molecular surface as a dominating determinant for oral absorption and brain penetration of drugs. Pharm. Res. 1999, V16, 1514-1519. 

Human CEC cultured on filter inserts can be used to measure brain penetration of drugs to make in vitro-in vivo correlations. They can further be used to study for example brain inflammation that has been implicated in the development of brain edema and secondary brain damage in ischemia and trauma. Zhang et al. (2000) studied leukocyte infiltration across the blood-brain barrier and showed the expression of adhesion molecules and leukocyte chemoattractants under ishemia in vitro conditions. 

General approaches for increasing brain penetration of drugs... 

General Approaches for Increasing Brain Penetration of Drugs... 

Prevent brain penetration of drugs Limit oral absorption... 

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