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General Information


The course addresses the latest insights on the mechanisms of Blood-Brain Barrier (BBB) transport and intra-brain distribution for (CNS) drug development. It provides in-depth insight in the complex function of the BBB with regard to transport kinetics in health and disease. Also, it addresses CNS drug delivery, CNS diseases, and preclinical- clinical translation and predictions. It integrates lectures with several extensive hands-on exercises in order to deepen the knowledge conveyed.


There is still a high unmet medical need in the treatment of CNS diseases and this problem is getting worse as the number of people suffering from CNS diseases is growing. This implies that there is a huge market for new CNS drugs. However, the development of new CNS drugs is notoriously difficult. For a proper CNS effect, the drug should have the ability to cross the BBB and then to reach the relevant target site within the CNS by adequate intra-brain distribution. In addition, drugs that are aimed to have a peripheral action but may bear risks for CNS side effects can be better optimized with more knowledge on BBB transport and CNS side effect site distribution.

Thus, knowledge on the physiological and pharmacokinetic aspects of drug delivery to the brain and distribution within the brain compartments is of utmost importance for all drug delivery scientists.

Who should attend?

This course will be of benefit to researchers from Academia, Big and Small Pharma Industries, Regulatory Agencies and Contract Research Organizations with a need for better understanding of the BBB and factors that determine CNS target site distribution of drugs. Also, medicinal chemists who need further knowledge on pharmacokinetic principles of CNS distribution can be guided in finding more optimal molecules for CNS action or for the avoidance of CNS side effects. A general understanding of physiology and minimal knowledge of differential equations is expected (some information can be provided upon request).

Learning Objectives

After having taken this course, the participants will

  • have in-depth insight into the mechanisms governing BBB transport and intra-brain distribution, with special emphasis on drug delivery and active transport mechanisms
  • have knowledge about the driving forces that determine whether or not a CNS drug will be at the right placeat the right time and at the right concentration
  • be able to compare and choose between different methods for studying parameters that can be used to understand or predict BBB transport and CNS distribution
  • understand the basis of preclinical-clinical translation and what tools to be used to that end