Preparation, characterization and water solubility evaluation of porous starch loaded artemisinin microspheres / 中草药

ABSTRACT

Objective The fat-soluble artemisinin (Art), which is poorly soluble in water, was loaded with porous starch to form Art microspheres, and its physical and chemical properties were better than the original powder, so as to improve the water solubility of Art. Methods The porous starch particles were loaded on Art powder by physical adsorption method. The physical and chemical properties of Art microspheres loaded with porous starch were characterized and analyzed by SEM, BET, FTIR, XRD, DSC, and TG respectively. The saturated solubilities of porous starch loaded Art microspheres in water, artificial gastric juice and artificial intestinal fluid were determined. Results In the characterization test, we found that under the optimal preparation conditions, porous starch had successfully loaded Art to form microspheres with drug loading of (20.37 ± 0.61)% and entrapment efficiency of (81.86 ± 3.06)%. In the process of loading Art with porous starch, only physical changes happened. The original Art powder had been completely loaded by porous starch, showing that it had the same amorphous structure as porous starch, thus improving the water solubility of the original Art powder. The saturated solubility of the porous starch loaded Art microspheres was significantly improved, and the water, artificial gastric juice and artificial intestinal fluid were 3.77, 1.64, and 1.72 times higher than the original Art powder, respectively. Conclusion This paper significantly improved the water solubility of Art powder and provided important research basis for solving the clinical application of insoluble drugs.