Drug Delivery to the Central Nervous System (CNS)

The main objective of the course is to introduce the basic concepts and methods in CNS drug delivery and provide an overview of the different approaches used by academia and industry in the field. The course consists of lectures, discussion classes with student presentations and a final exam. At the end of the course, the students are expected to be able to:

At the end of the course the students are expected to be able to:

Knowledge

• describe how physicochemical properties of a compound relates to its likelihood to become a CNS drug compound
• describe the methods available for estimating brain efflux properties
• describe the molecular properties of the blood-brain barrier
• define the rate limiting steps in brain drug delivery
• demonstrate knowledge on how brain pathologies may alter brain drug disposition
• explain how CNS drug candidates are tested in vitro and in vivo
• identify the pharmacokinetics of drug compound disposition to the brain
• reflect on the concept and importance of free-versus bound drug compound concentrations in brain and blood.

Skills

• deduct if a drug compound is suited for CNS delivery according to its physicochemical properties.
• use Michaelis-Menten kinetics to estimate transporter activity and inhibition
• interpret data from in-vitro test models for CNS barrier permeability and efflux, using permeability estimates and efflux ratio's
• Read, understand and extract general conceptual knowledge from original research articles

Competencies

• integrate knowledge from organic chemistry, formulation, physical chemistry, pharmacokinetics, tissue barrier biology and pharmacology to design formulations for brain drug delivery.
• apply simple mathematical models for predicting and describing brain drug uptake and efflux from both in vivo and in vitro studies.