| Nanoemulsion, also called microemulsion, is a transparent and thermo- dynamically stable and isotropic colloid dispersive system, and as a novel drug delivery system with following advantages: good physical stability, could be sterilized and preserved conveniently, encapsulate drugs had different solubility, increase stability, solubility and availability for drugs in vivo, could promote absorption for water-soluble drug had large molecule structure, and also had sustained-release and targeting effect. Recently, research on nanoemulsion is attracting more attention all over the world.The research screened the drug delivery system of blank nanoemulsion, and prepared artesunate nanoemulsion, established analytical method of drug contents, evaluated stability and safety for quality of artesunate nanoemulsion.Pseudo-ternary phase diagrams were used to screen prescriptions and observe the influence factors of blank nanoemulsion, according to formation principle of microemulsion. The influence factors inspection results of drug delivery system showed that in a certain range, the higher HLB of surfactant, the bigger area of nanoemulsion is. The shorter chain of cosurfactant, the bigger area of nanoemulsion is. The HLB of the oil phase and the mixed surfactant more matches, the bigger area of nanoemulsion. The ratio (Km) of surfactant to cosurfactant be more appropriate, the bigger area of nanoemulsion. Within limits, the area of nanoemulsion has not been changed notablely while the different concentrations medicine and dielectrics were added.Based on the established nanoemulsion drug delivery system, artesunate nanoemulsion was prepared and its quality was evaluated. Results showed that three prescriptions of artesunate nanoemulsion were all transparent spherical liquid droplet. Average diameter of blank nanoemulsion is 50nm, and artesunate nanoemulsion is 57.79nm. The physical and chemistry characters, samples keeping at room temperature, acceleration indicated that the quality of artesunate nanoemulsion was stable. The analytical method of HPLC for content determining of artesunate nanoemulsion has been established. The results showed that the calibration curve was linear in the range of 10～100μg/ml. The mean recovery is 99.77 %. RSD of the recovery is 0.89%. The accuracies with-day and between-day were less than 1.8 %, the analysis method established in this study had high recovery, accuracy and repetition, and can be used in quality control.To evaluate preliminarily the safety of artesunate nanoemulsion by acute toxicity test of artesunate nanoemulsion in mouse by oral administration and peritoneal injection, eye irritation by single and several, intramuscular irritation and haemolyticus test. The results of acute toxicity by oral administration showed that LD50 of the first prescription (AS1) is 7.76g/kg·BW, AS2 is 7.56g/kg·BW. LD0 of AS3 is 15g/kg·BW. The results of acute toxicity by peritoneal injection showed that LD0 of AS3 is 15g/kg·BW. The three prescriptions belonged to practically non-toxic. The results of irritant test showed that AS1 belonged to serious stimulation, AS2 mild stimulation and AS3 had no stimulation. The results of haemolyticus test showed that AS1 and AS2 occurred partly haemolysis and AS3 had no non-haemolysis. AS3 had better safety than the other, and was appropriate to further study.In the research, artesunate nanoemulsions injections which were safe and had a good stability were prepared successfully. The defects in traditional dosage form of artesunate which was not stable to preserve, eliminated quickly and so on were overcomed effectually; its quality safety were evaluated. In conclusion, it did the groundwork for developing new dosage form of artesunate in the future.
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