Preparation of Pellets Containing a Standardized Artemisia Annua L. Extract by Extrusion-Spheronization

Artemisinin, the major substance with antimalarial activity of Artemisia annua L., is a poorly water-soluble drug. The development of pellets containing a standardized hydroethanolic extract of A. annua may overcome these drawbacks while offer an intermediate product with good technological properties for subsequent tablet manufacture. This work aimed to obtain and characterize A. annua pellets using the extrusion-spheronization technique. The extract was prepared by percolation and artemisinin content was determined using a validated HPLC method. The standardized extract was then used as a liquid binder in the preparation of pellets with different liquid: solid ratio. The formulation PF5 containing microcrystalline cellulose: A. annua extract (40:58) resulted in pellets with 1.49 ± 0.02 % (w/w) artemisinin, average size of approximately 500 µm and sphericity of 0.82 ± 0.08. These pellets were encapsulated in hard gelatin capsules and the percentage released was higher than 80% in 10 min using 0.1N HCl and phosphate buffer media. These data allow to suggest that the pelletizing strategy used made it possible to achieve the desired artemisinin dissolution and generates perspectives for the potential further use of the A. annua pellets as a solid dosage form for malaria treatment.