RSC Publishing


Publishing

 

Cover image for Chemical Biology , select for current issue

Chemical Biology

Chemical biology news and research from across RSC Publishing.



Following drugs into the brain


17 December 2008

An international team has developed a potentially safer way to monitor drug delivery to the brain. 

Lomustine and a nitroxyl labelled analogue
Adding a nitroxyl radical to lomustine allows the drug to be mapped in the brain
Mapping drugs in the brain and assessing how well they reach it are both vitally important for testing new pharmaceuticals for brain diseases. But until now, this could be done only by using radioactive chemicals, which are expensive and risk human safety. 

In their search for a lower risk alternative, Rumiana Bakalova of the National Institute of Radiological Sciences in Chiba, Japan, and colleagues in Japan and Bulgaria have developed a non-radioactive way to monitor conventional drugs in the brain. By attaching nitroxyl radicals to the anticancer drug lomustine they found that its movement into the brain could be tracked using magnetic resonance imaging. 

"Mapping the drug localisation in the brain could be useful for planning chemo- and radiotherapy of cancer and other diseases."
- Rumiana Bakalova
Adding the nitroxyl radicals does not affect the drug's movement through the blood-brain barrier, which is a crucial step for the drug, explains Bakalova. 'We observed that the drug was localised in the brain tissue and were able to map the drug localisation in different parts of the brain,' she says. This information could be useful for planning chemo- and radiotherapy of cancer and other diseases, she adds. 

Baklova's team now plans to look into using the labelling for other dugs and also to map drugs in different organs and tissues in the body. 

Sarah Dixon

Enjoy this story? Spread the word using the 'tools' menu on the left or add a comment to the Chemistry World blog.

Link to journal article

Nitroxyl radicals as low toxic spin-labels for non-invasive magnetic resonance imaging of blood–brain barrier permeability for conventional therapeutics
Zhivko Zhelev, Rumiana Bakalova, Ichio Aoki, Ken-ichiro Matsumoto, Veselina Gadjeva, Kazunori Anzai and Iwao Kanno, Chem. Commun., 2009, 53
DOI: 10.1039/b816878d

Also of interest

Beyond the blood-brain barrier

A treatment for Alzheimer's disease or schizophrenia is little use if it can't reach its target in the brain

Chemistry and Medicines

Chemistry and Medicines

Copyright: 2006
James R Hanson

Providing a general introduction to this fascinating subject, this book is aimed at those studying advanced undergraduate and postgraduate courses in medicinal chemistry.


Life Saving Drugs

Life Saving Drugs

Copyright: 2004
John Mann

This book describes the discovery and development of antibacterial, anti-viral and anti-cancer drugs and highlights the colourful characters behind their inventions.