Lapazine loaded Alginate/Chitosan microparticles: Enhancement of anti-mycobacterium activity

Lapazine, a phenazine synthesized from lapachol, presents activity against M. tuberculosis. However, the low solubility of lapazine represents an obstacle for the development of an innovative drug. In order to improve lapazine solubility and subsequent delivery, an encapsulation carrier based on alginate-chitosan microparticles was developed by the method of emulsification, interfacial complexation and solvent evaporation. Alginate and chitosan microparticles synthesized by this route were physical-chemical evaluated showing medium diameter of 1358 nm, zeta potential equal to −24.28 mV and spherical morphology. The activity of the microparticles containing lapazine was tested by Resazurin Microtiter Assay, using resistant and susceptible strains. Our results show that alginate-chitosan microparticles were able to encapsulate lapazine and improve its anti-mycobacterium activity in 30 times than the free lapazine. These results raise a new possibility of treatment for Tuberculosis and multidrug resistant cases.