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
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.
Last modified: | 13 March 2020 01.02 a.m. |
More news
-
29 April 2024
Tactile sensors
Every two weeks, UG Makers puts the spotlight on a researcher who has created something tangible, ranging from homemade measuring equipment for academic research to small or larger products that can change our daily lives. That is how UG...
-
29 April 2024
Behind the scenes: how UG and Hanze UAS students are jointly developing a Mars rover
This year the students of the Makercie team are participating in the physical edition of the European Rover Challenge in Poland. Read more about the team and the collaboration between the RUG and Hanze UAS here.
-
23 April 2024
Nine MSCA Doctoral Network grants for FSE researchers
Nine researchers of the Faculty of Science and Engineering have received a Horizon Europe Marie Sklodowska Curie Doctoral Network grant.