The blood-brain barrier (BBB) isolates the brain from the general circulation of the body and thus protects it from harmful xenobiotics. This isolation, however, renders the pharmacological treatment of the brain most difficult, as most drugs cannot enter the brain owing to the existence of the BBB. BBB research addresses multiple clinical questions (Table 26.1), which together utilize powerful techniques for the evaluation of BBB functions in patients (Table 26.2). Answering these questions will have practical clinical benefits that justify these efforts (Table 26.3).

Numerous diseases have been reported to involve perturbations in BBB integrity (Table 26.4). Based on this information, it appears that both carriers of mutations that induce BBB disruption and individuals exposed to BBB-disrupting insults may be at risk for malfunctions of the BBB (Table 26.5).

Table 26.2 Methods for evaluation of BBB function in humans

(1) Computerized tomography14

(2) Avoidance of undesired brain penetrance by a drug

(3) Single photon emission CT16

(4) Cerebrospinal fluid analyses17

Table 26.3 Potential applications of BBB control


Rationalized drug delivery to the brain


Avoidance of brain penetrance by a drug when

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