Preparation and evaluation of Dihydroartemisinin nanosuspension

Abstract

Dihydroartemisinin (DHA) is an effective antimalarial drug especially against tolerant species Palsmodium falciparum. However, poor solubility in water makes it difficult to formulate in an effective dosage form. Particle size reduction to micro-or nanometer range is a promising technology to overcome solubility and bioavailability problems of poorly water soluble drugs by increasing of solution vecocity and saturatin solubility. Co-grinding technique using hydrophobic drugs with hydrophilic polymer(s) and/or combination with co-polymer(s) was interesting method that can produce fine particles with narrow particle size distribution. This technique is attractive due to organic solvent free and simple step operation. In this research, DHA particles were prepared by co-grinding method, the formation of DHA particle as nanosuspension from ternary ground mixtures of DNA, polyvinylpyrrolidone and sodium deoxycholate was studies. Physical characterization of the co-ground mixtures and suspension and in vitro antimalarial activity against P. falciparum of the obtained suspension was determines. In conclusion, the nanosuspensions with high percentage of DHA nanoparticles were obtained by reconstitution of the coground mixture in distilled water with particle size of 80-200 nm. The nanosuspension was effective antimalarial activity against P. falciparum K1 strain. The PXRD patterns indicating that the co-grinding technique decreased crystallinity of DHA in the coground mixtures to amorphous state whereas DHA existed as crystalline solid in physical mixtures.