Cyclodextrin-encapsulated new drug with promising anti-Trypanosoma cruzi activity

In the present study, a host–guest complex was obtained between a modified Chalcone (CHC) with anti T. cruzi activity and hydroxypropyl beta-cyclodextrin (HpBCD). This approach was chosen due to the low water solubility of CHC, in a drug delivery approach against Chagas disease. The complexes CHC:HpBCD were obtained by three synthetic routes: lyophilization, grinding method and calcinated method. TG assays point to the formation of an in situ complex of CHC with HpBCD. The 1H NMR assays give an idea of how the inclusion of CHC in HpBCD occurs and give the association constant of these species, that is around 60. UV–vis measurements demonstrate that the stoichiometry of complexation is 1:1. The FTIR and PXRD results show that solid state complex formation was successfully formed. Biological assays were carried out and demonstrate that the obtained complexes have antiparasitic activity against T. cruzi, having the advantage of a better water solubility and requiring a smaller mass amount of CHC to work.