Despite the efforts in controlling the parasite and infection, and the significant progress achieved in recent years in its treatment, malaria is still prevalent in many regions and out of control in others. The repertoire of alternatives to fight malaria is being expanded, not only by designing new drugs but also by developing improved drug delivery systems able to enhance the antimalarial efficiency of conventional and new drugs. Among the new drugs that have been investigated, several publications report the use of porphyrin derivatives as antimalarials but their efficiency is contradictory. The low activity of porphyrins seems to be associated with low dispersibility and bioavailability. In this respect, Nanotechnology can provide efficient solutions to enhance bioavailability and delivery of conventional and new antimalarials, in order to assure high enough efficiency levels to inactivate the parasite. Thus, in this review we highlight the use of drug delivery systems for conventional and new antimalarials and we propose the encapsulation of porphyrins as a promising alternative for development of anti-malarial formulations.