Abstract

Abstract Potential drugs for the treatment of most brain diseases are often not able to cross barriers protecting the central nervous system (CNS). As a result, various drug delivery and targeting strategies are currently being developed to enhance the absorption and distribution of drugs into the brain. This article discusses the biology and physiology of the blood–brain barrier (BBB) and the blood–cerebrospinal fluid barrier with respect to drug transport (absorption, distribution), the in vitro and in vivo methods to measure BBB transport, and the possibilities to deliver large molecular drugs, by viral and receptor‐mediated nonviral drug delivery, to the (human) brain.

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