Studies on Preparation of Artesunate-Loaded mPEG-PLGA-Nanoparticles and Its Inhibition on K562 cells

Abstract 4712

The aim of the present work was to investigate the characterization of Artesunate-loaded methoxy poly (ethylene glyeol) -poly (lactic-co- glycolic acid) copolymer (mPEG-PLGA) nanoparticles and the anti-tumoral activity of the Art-Nps on human leukemia cells K562. The Artesunate (Art) poly (ethylene glyeol-lactic-co-glycolic acid) nanoparticles (Art-Nps) were prepared by modified-Spontaneous emulsion solvent diffusion method. The shape of the nanoparticles was observed by SEM. The mean diameter and the size distribution of nanoparticles were determined by laser light scattering. The drug loading efficiency, encapsulation rate and releasing behavior of Art -NPs in vitro were examined by HPLC. The effects of Art-Nps on the proliferation of K562 cells were studied by MTT assay and Hoechst staining. Artesunate loaded mPEG-PLGA nanoparticles were spheric with the mean size of (156.7±1.01)nm, zeta potential was -(26.23±1.86) mV, and the average drug loading and encapsulation efficiency were (14.5±0.2)% and (86.5±0.5)%, respectively. In vitro release behavior could be described by the Higuchi equation: Q=4.11t1/2+27.05, r=0.983. MTT assay showed different concentrations. different times of Art-Nps could inhibit the proliferation of K562 cells (P<0.01), and both have a synergistic effect (P=0.002), it showed that concentration was dependented with time, and the inhibition rate after 72h was exceeded to the the control group (P<0.05), it was showed the Art-Nps had sustained-release effect. Art-NPs of the cells (treated by 12.5μ g/m. 25μ g/ml. 50μ g/ml) resulted in significantly higher apoptosis than blank groups. The Art-NP obtained were characted with a small size and high drug loading and entrapment efficiency, in vitro release showed a good sustained-release nature, and it can inhibit the proliferation of human leukemia K562 cells in vitro, extending the time on leukemia cells. This study was provide an experimental basis for develop a new intravenous artesunate formulations.