Obtaining and characterization of Clofazimine cocrystals, aiming at its application to the treatment of Tuberculosis

Tuberculosis (TB) is an infectious disease caused by Mycobacterium tuberculosis, which causes most deaths worldwide, according to WHO.1 The low success rate for the treatment of multidrug-resistant tuberculosis (MDR-TB) has motivated the exploration of different approaches to drug seeking.1 In this work, it was proposed to obtain cocrystals using clofazimine (CFZ) as a model drug and caffeine (CAF), dapsone (DAP) and saccharin (SAC) as coformer, aiming to improve solubility. Slow solvent evaporation and ball milling methods were used to obtain the cocrystals. Preliminary results showed that it was possible to identify eutectic mixture formation from CFZ/CAF (1:1), amorphous formation from CFZ/SAC (1:1). The CFZ/DAP results obtained by grinding and evaporation showed a possible formation of cocrystal in the presence of chloroform. From these results, it was preliminarily found the potential development of clofazimine cocrystals with, for now, dapsone as the most promising coformer.