PhD ceremony: Mr. J. de Graan, 14.30 uur, Academiegebouw, Broerstraat 5, Groningen
Dissertation: Synthesis and evaluation of dopaminergic prodrugs designed for transdermal iontophoretic drug delivery. Highly water-soluble amino acid ester prodrugs applicable for the treatment of Parkinson’s disease
Promotor(s): prof. B.H.C. Westerink
Faculty: Mathematics and Natural Sciences
Dopamine agonists are used as pharmacotherapy for patients with Parkinson's disease. In his thesis Jeroen de Graan describes the preparation and evaluation of highly water-soluble derivatives of the dopamine agonist 5-OH-DPAT. These derivatives are chemically coupled compounds of 5-OH-DPAT with other molecules, i.e. amino acids. In pharmacy these compounds are named prodrugs. A prodrug is a non-pharmacologically active compound which will release the active drug after conversion in the body.
De Graan's research has led to several findings. First, highly water-soluble prodrugs were synthesized which showed sufficient stability while in solution in the iontophoretic patch (sufficient sustainability), but released the drug on entry in the bloodstream. Second, by coupling 5-OH-DPAT to dipeptides (two combined amino acids) he obtained even more stable prodrugs. Third, 5-OH-DPAT could be administered in a controlled manner, which would facilitate the development of a feedback system. Finally, he found that the iontophoretic delivery of a highly water-soluble prodrug of 5-OH-DPAT led to a prolongation of the pharmacological effect in comparison to 5-OH-DPAT itself.
These results show that the application of prodrugs can be advantageous for the administration of dopamine agonists and other drugs by transdermal iontophoresis. Further research of this pharmaceutical dosage form could eventually lead to a new pharmacotherapy of patients with Parkinson's disease.
Prof. Marthe Walvoort has received the Athena Award, one of the five science awards of the Dutch Research Council (NWO).
Professor of chemistry Sibrand Stratingh, from Groningen, built the first electric vehicle – the precursor to the electric car – around 1830. He also drove a steam-powered carriage through the streets of Groningen. But his innovative scientific...
The prizes are for the advancement of higher scientific education in the fields of science and engineering.
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