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Biomedical Sciences - Pharmacology & Toxicology | Drug Delivery to the Brain - Physiological Concepts, Methodologies and Approaches

Drug Delivery to the Brain

Physiological Concepts, Methodologies and Approaches

Hammarlund-Udenaes, Margareta, de Lange, Elizabeth, Thorne, Robert G. (Eds.)

2014, XX, 731 p. 150 illus., 126 illus. in color.

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  • Describes small and large drug delivery to the brain with emphasis on the physiology and concepts for drug delivery across the BBB and brain distribution
  • Contains methods for studying drug delivery, routes, and approaches of drug administration and drug industry perspectives
  • Cutting-edge and at the same time educational, so that the book can be used in high-level training of academic and industry scientists

This book describes the different approaches for drug delivery to the brain with an emphasis on the physiology of the blood-brain barrier (BBB) and the governing principles and concepts for drug delivery across the BBB. It contains cutting-edge methods for studying drug delivery and administering drugs into the brain. The book also explores different approaches for predicting human brain concentrations as well as the influence of disease and drug industry perspectives. In addition to wide-ranging coverage of physiological concepts relevant to central nervous system (CNS) drug delivery, a detailed review of brain structure, function, blood supply and fluids is also provided. In each chapter, descriptions of future challenges and unresolved questions are combined with points for discussion. This unique combination of material makes this book a valuable resource for students and for established academic and industry scientists looking to learn about state-of-the-art drug delivery research. It is also a source for stimulating new ideas among experts already performing CNS drug delivery research or working in related areas.


Margareta Hammarlund-Udenaes (Ph.D.) is a Professor in Pharmacokinetics and Pharmacodynamics (PK/PD) at Uppsala University and the Head of the Translational PK/PD Group. Her research is focused on studying pharmacokinetic aspects of BBB transport of drugs in relation to CNS effects, and it has led to the development of new concepts and methods within the BBB transport area, focusing on unbound drug relationships.


Elizabeth C.M. de Lange (Ph.D.) is Head of the Target Site Equilibration Group at the Division of Pharmacology of the Leiden Academic Center for Drug Research (LACDR).  Her research program focuses on the development of generally applicable predictive PK/PD models on CNS drugs using advanced in vivo animal models and mathematical modeling techniques, with a number of recent successes.


Robert G. Thorne (Ph.D.) is an Assistant Professor in Pharmaceutical Sciences at the University of Wisconsin-Madison School of Pharmacy. He was previously a research scientist and faculty member in the Department of Physiology & Neuroscience at the New York University School of Medicine. His research focuses on diffusive and convective transport within the CNS and the development, refinement and optimization of strategies for delivering biologics into the brain.

Content Level » Research

Keywords » blood-brain barrier - drug delivery blood-brain barrier - transporters

Related subjects » Biomedical Sciences - Pharmacology & Toxicology

Table of contents 


1.      Anatomy and physiology of the blood-brain barriers

N Joan Abbott

2.      Recent Progress in Blood-Brain Barrier and Blood-CSF Barrier Transport Research: Pharmaceutical Relevance for Drug Delivery to the Brain

Masanori Tachikawa, Yasuo Uchida, Sumio Ohtsuki and Tetsuya Terasaki

3.      Blood-Brain Barrier (BBB) Pharmacoproteomics: A New Research Field Opened up by Quantitative Targeted Absolute Proteomics (QTAP)

Yasuo Uchida, Masanori Tachikawa, Sumio Ohtsuki And Tetsuya Terasaki

4.      Drug Metabolism at the Blood-Brain and Blood-CSF Barriers

Xavier Declèves, Nathalie Strazielle, Jean-Michel Scherrmann and Jean-François Ghersi-Egea


5.      Pharmacokinetic Concepts in Brain Drug Delivery

Margareta Hammarlund-Udenaes

6.      In vitro models of blood-brain barriers

N Joan Abbott, Diana EM Dolman, Siti R Yusof and Andreas Reichel

7.      In situ and in vivo animal models

Quentin Smith and Ramakrishna Samala

8.      Principles of PET and its Role in Understanding Drug Delivery to the Brain

Stina Syvänen and Roger N. Gunn

9.      PKPD Aspects of Brain Drug Delivery in a Translational Perspective

Elizabeth C.M. de Lange


10.  Drug Discovery Methods for Studying Brain Drug Delivery and Distribution

Irena Loryan and Margareta Hammarlund-Udenaes

11.  Prediction of Drug Exposure in the Brain from the Chemical Structure

Markus Fridén

12.  Integrated Approach to Optimizing CNS Penetration in Drug Discovery: From the old to the new Paradigm and Assessment of Drug-Transporter Interactions

Andreas Reichel

13.  Pharmacoeconomic Considerations in CNS Drug Development

David Gray


14.  Intranasal Drug Delivery to the Brain

Jeffrey J. Lochhead and Robert G. Thorne

15.  Blood-To-Brain Drug Delivery using Nanocarriers

Pieter J. Gaillard, Corine C. Visser, Marco de Boer, Chantal C.M. Appeldoorn and Jaap Rip

16.  Development of new Protein Vectors for the Physiologic Delivery of Large Therapeutic Compounds to the CNS

Reinhard Gabathuler

17.  CNS Gene Therapy Utilizing Intravenously Administered Viral Vectors

Adam K. Bevan and Brian K. Kaspar

18.  Neurosurgical Approaches: Drug Infusion Directly into the Parenchyma or Cerebrospinal Fluid

Krystof Bankiewicz

19.  Osmotic Opening of the BBB for Drug Treatment of Brain Tumors (Focus on Methodological Issues)

David Fortin

20.  Emerging Engineering Technologies for Opening the BBB

Elisa E. Konofagou


21.  Disease Influence on BBB Transport in Inflammatory Disorders

Geert Schenk, Gijs Kooij, Arie Reijerkerk and Helga de Vries

22.  Disease Influence on BBB Transport in Neurodegenerative Disorders

Elizabeth C.M. de Lange

23.  Drug Delivery in the Context of Stroke and Brain Trauma

Richard F. Keep, Jianming Xiang, Ningna Zhou and Anuska V. Andjelkovic

24.  Which Drug or Drug Delivery Method can change Clinical Practice for Brain Tumor Therapy?

Tali Siegal

Appending – Primer on Central Nervous System Structure / Function and the Vasculature, Ventricular System and Fluids of the Brain.  Robert Thorne

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