Preparation and properties of a new artemisinin lipid emulsion for parenteral administration

Abstract

Artemisinin is difficult to formulate for parenteral administration because of its low aqueous solubility and Cremophor EL, the excipient used for its formulation, has been shown to cause serious side effects. This study reports the preparation method and properties of artemisinin lipid emulsion for parenteral administration. High-pressure homogenization was used to prepare artemisinin lipid emulsion. The factors influencing the stability of artemisinin lipid emulsion were monitored, such as drug loading methods and sterilization methods. It has been found that the optimum formulation of artemisinin lipid emulsion were composed of artemisinin 0.4%(w/v), soybeen oil 10%(w/v), egg lecithin 1.2%(w/v), F68 0.4%(w/v), oleate 0.02%(w/v) and glycerol 2.5%(w/v). Artemisinin lipid emulsion was stable enough to withstand rotating steam sterilization at 121°C for 15 min.