Abstract: Five crystal modifications of water insoluble
artesunate were generated by recrystallizing it from various solvents
with improved physicochemical properties. These generated crystal
forms were characterized to select the most potent and soluble form.
SEM of all the forms showed changes in external shape leading them
to be different morphologically. DSC thermograms of Form III and
Form V showed broad endotherm peaks at 83.04oC and 76.96oC prior
to melting fusion of drug respectively. Calculated weight loss in TGA
revealed that Form III and Form V are methanol and acetone solvates
respectively. However, few additional peaks were appeared in XRPD
pattern in these two solvate forms. All forms exhibit exothermic
behavior in buffer and two solvates display maximum ease of
molecular release from the lattice. Methanol and acetone solvates
were found to be most soluble forms and exhibited higher
antimalarial efficacy showing higher survival rate (83.3%) after 30
days.