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Preparation and In Vitro Characterization of Artemisinin Freeze-Dried Powders with Various Carriers

Gamal Osman Elhassan, Yuen Kah Hay, Wong Jia Woei, Jiyauddin Khan, Khalid Omer Alfarouq, Javed Akhter, Habibullah Khalilullah, MU Khan, Riyaz Ahmed Khan and Kamal Ahmad Qureshi

The present study was conducted to investigate the enhancing effect of different polymeric carriers on solubility and hence oral bioavailability of artemisinin, a poorly water-soluble drug. Freeze-dried powder preparations of artemisinin and various carriers (polyvinyl pyrrolidone K-25 (PVP K-25), Hydroxypropyl Cellulose (HPC) and dextrin) were obtained by dissolving different carriers (PVP K-25, HPC and dextrin) in water, followed by the addition of artemisinin at a ratio of 1:4. The resultant products were evaluated using solubility and dissolution studies, Differential Scanning Calorimetry (DSC) and Scanning Electron microscopy (SEM). These in vitro studies showed that the aqueous solubility of artemisinin was significantly increased for the preparation containing artemisinindextrin at a ratio of 1:4. Further, the effect of incorporation of different co-carriers (citric acid or mannitol) to artemisinin-dextrin freeze-dried powder at different ratios was evaluated. A significant increase in the solubility and dissolution rate of artemisinin was obtained with the artemisinin-dextrin-citric acid freeze-dried powder at a ratio of 1:3:1.