Abstract
Background: Artemisinin (ART) is a potent antimalarial drug, practically has a low aqueous solubility thereby exhibits poor and low bioavailability after oral administration. Therefore, the improvement of artemisinin solubility and dissolution from its oral solid dosage forms is an important issue for enhancing its bioavailability and therapeutic efficiency.
Objectives: The present study was carried out to investigate the utilization of Gelucire 44/14 for preparing solid dispersion of artemisinin with aim of increasing its aqueous solubility.
Methods: Solid dispersion, with Gelucire 44/14 at ratios ranging from 1: 10 to 8: 10 was prepared using the melt (fusion) method. Scanning electron microscopy (SEM), solubility determination and diferential scanning calorimetry (DSC) were used to investigate the physicochemical characteristics of the preparations.
Results: The solubility of artemisinin from the solid dispersion preparations increased linearly with increased the ratio of Gelucire 44/14; however the increase in artemisinin solubility was not very significant. The data obtained from SEM and DSC studies revealed that the solid dispersions with Gelucire 44/14 were not capable of increasing the solubility of ART significantly through increasing the ratio of Gelucire 44/14.
Conclusion These preparations did not result in increasing the aqueous solubility of artemisinin significantly, so it can be concluded that the solid dispersion led to reduce the drug crystal as compared to pure artemisinin.