Effect of cyclodextrins on artemisinin stability and in vitro dissolution

Abstract

Artemisinin is extracted from the Asian plant Artemisia annua L. It has been proven to be, with its derivatives, the molecules that have shown so far the most powerful activity on malaria, even in its complicated forms and resistance cases. To resolve the problem of low aqueous solubility of this molecule, the use of cyclodextrins (CDs) was envisaged and gave good results in this topic. However, the impact on its stability and in vitro dissolution, important parameters for drug formulation and evaluation, was not evaluated. In this study, stability in accelerated degradation conditions and in vitro dissolution analysis of artemisinin were performed in comparison with complexes of artemisinin and cyclodextrins. The findings of this work allowed us to suggest that CDs improve the stability of artemisinin, especially when it’s in aqueous solution. We also demonstrated the beneficial impact of cyclodextrins on the in vitro dissolution of artemisinin from capsules prepared with rough extracts of A. annua.

Keywords: Artemisia annua capsules, malaria, lyoequivalence, dissolution apparatus, storage conditions