Lyophilized solid dispersions of artemisinin to improve saturation solubility and dissolution.

Artemisinin is an oral antimalarial agent which effectively reduces malaria parasites in blood by radical damage to parasite lipids and proteins. However, poor water solubility, which also results in low oral bioavailability of the drug, creates obstacles in drug delivery formulations. The purpose of this study was to develop solid dispersions of artemisinin by lyophilization method and evaluate the effect of a solid dispersion on solubility and in vitro dissolution of artemisinin. The solid dispersion was prepared using natural gum and maltodextrin biopolymers as a carrier. The morphology of artemisinin crystal and artemisinin solid dispersions was determined using a scanning electron microscope (SEM). SEM images of freeze-dried and solid dispersion artemisinin confirmed the embedding, size reduction, and glassy form. The entrapment efficiency, saturation solubility, and dissolution were investigated. The results confirmed that the entrapment efficiencies of solid dispersions were 79.8% - 96.3%. Solid dispersion of artemisinin improved the saturation solubility of artemisinin in water up to 60.04 µg/mL in the ratio of maltodextrin and natural gum 1:2. A solid dispersion system additionally improved the dissolution rate of artemisinin in comparison to the artemisinin crystal. After 180 minutes, the solid dispersion system released 89.6% of artemisinin. The study suggests that high-energy solid forms of artemisinin could enable the delivery of artemisinin. [ABSTRACT FROM AUTHOR]