Fanta Gashe

Contact Info

Drug Quality and Registration (DruQuaR) group
Ottergemsesteenweg 460, 9000 Ghent (Belgium)

PhD Research

Title: Development of artemisinin-derived medicines to improve stability and pharmacokinetic properties

Summary:

Artemisinin derived 1,2,4-trioxane compounds are currently crucial drugs in the treatment of malaria. Moreover, these compounds have recently been shown to be of therapeutic value in various other diseases such as microbial infections and cancers. However, the currently available trioxane medicines show a low intrinsic stability and high reactivity with pharmaceutical excipients. They also exhibit short and variable pharmacokinetic characteristics, requiring multiple administrations and efficacy-safety uncertainty, which is detrimental to the therapeutic outcome.

The goal of this project is to develop new formulations of existing trioxane-compounds with increased stability and modified biopharmaceutical profile. To reach this goal, several objectives are defined. First, validated analytical methods will be developed not only to identify and quantify possible degradation products in existing and new formulations, but also to assess the pharmacokinetic profiles and metabolization pathways of these trioxane compounds in biological samples. Secondly, new formulations will be developed and evaluated in vitro for their improved stability and dissolution profile. Finally, the in vivo pharmacokinetics of selected formulations will be investigated in a rat model using the validated bio-analytical methods.

Keywords: Artemisinin-derived medicines; stability; pharmacokinetics