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Blood-Brain Barrier: Drug Transport to the Brain


Admission requirements

Master students of Bio-Pharmaceutical Sciences, Biomedical Sciences, Life Science & Technology, Molecular Science & Technology. Required background knowledge is thorough knowledge of pharmacokinetics (BFW1 TE1 and TE2, or similar).


The development of new drugs with an action on the central nervous system (CNS) is notoriously difficult. For a proper CNS effect, the drug should have the ability to cross the BBB, and then has to find its way to the relevant target site within the CNS. This course will address the role and function of the Blood-Brain Barrier (BBB) and brain tissue distribution in research concerning CNS drug development, CNS drug delivery and CNS diseases. It will provide profound insight in the complex function of the BBB with regard to transport kinetics in health and disease.

It will include the following parts:

  • Basic Aspects of the BBB and Pharmacokinetic Principles.

  • Principles and Methods for Investigating BBB Transport.

  • Integration and Translation of CNS Drug Delivery Principles.

  • Exercises.

This course aims to:

  • Raise students’ interest and enthusiasm for the field of CNS drug research and development.

  • Give an introduction of the most important concepts and computational methods used and their application in CNS research and development.

  • Give the student sufficient background to interpret fundamental approaches, methodologies, and studies in CNS research.

  • Explain the reasons for current CNS research reproducibility and comparability, and CNS drug development problems, and understand the need for integrative approaches (that will be presented and worked with).

Note that these are expert lectures series and that hence the content might change every year.

Course objectives

At the end of this course the student:

  • Is able to distinguish all factors that play a role in distribution of drugs into and within the brain.

  • Is able to understand the importance of distinguishing between total and free drug concentrations.

  • Is able to understand the importance of distinguishing between rate and extent of equilibration in brain distribution.

  • Is able to understand the type of data that can be obtained by and differences between the different in vitro, in situ, and in vivo monitoring methodologies discussed.

  • Is able to understand that the concentration-effect relationships of drugs depend on concentration-target occupancy and target-occupancy effect relationships.

  • Has in-depth insight into the mechanisms governing BBB transport and intra-brain distribution, with special emphasis on drug delivery and active transport mechanisms.

  • Knows about the driving forces that determine whether or not a CNS drug will be at the right place, at the right time and at the right concentration.

  • Is able to compare and choose between different methods for studying parameters that can be used to understand or predict BBB transport and CNS distribution.


This course is scheduled for semester 2, period 3.
A detailed course schedule will be published on Brightspace.

Mode of instruction

Lectures (hoorcolleges).
Tutorial (werkcollege).
Self-tuition (zelfstudie).

Assessment method

The course will be assessed by an exam (open questions).
The final grade should be 6.0 to successfully complete this course.

Reading list

A reading list will be announced during the course.


Application via uSis for both the course and exam is mandatory. Registration for the course closes 14 days before the start of the course or earlier when the maximum number of students is reached. Registration for the exam closes 7 days before the exam date or earlier when the maximum number of students is reached.


Coordinator: Prof dr Elizabeth (Liesbeth) de Lange.
Email:, Tel 071-5276330.


This information is without prejudice. Alterations can be made for next year.