Artesunate (AST), the most widely used artemisnin derivative, has poor aqueous solubility and suffers from low oral bioavailability (~40%). Under these conditions, nanoparticles with controlled and sustained released properties can be a suitable
solution for improving its
biopharmaceuticals properties. This work reports the preparation and characterization of auto-assembled
chitosan/
lecithin nanoparticles loaded with AST and AST complexed with β-
cyclodextrin (β-CD) to boost its
antimalarial activity. The nanoparticles prepared by direct injection of
lecithin alcoholic
solution into
chitosan/water
solution have shown the particle size distribution below 300 nm.
Drug entrapment efficiency was found to be maximum (90%) for nanoparticles containing 100 mg of AST. Transmission electron microscopy images show spherical shape with contrasted corona (
chitosan) surrounded by a lipidic core (
lecithin +
isopropyl myristate). Differential scanning calorimeter thermograms demonstrated the presence of
drug in
drug-loaded nanoparticles along with the disappearance of decomposition exotherm suggesting the increased physical stability of
drug in prepared formulations. Negligible changes in the characteristic peaks of
drug in Fourier-transform infrared spectra indicated the absence of any interaction among the various components entrapped in the nanoparticle formulation. In vitro drug release behavior was found to be influenced by pH value. Increased in vivo
antimalarial activity in terms of less mean percent
parasitemia was observed in infected Plasmodium berghei mice after the
oral administration of all the prepared nanoparticle formulations.