Biodegradable microspheres. VIII. Killing of Leishmania donovani in cultured macrophages by microparticle-bound primaquine

Abstract Primaquine covalently bound to polyacryl starch microparticles has been shown to kill Leishmania donovani in cultured mouse peritoneal macrophages. The drug was derivatized with a tetrapeptide spacer and the derivative (Ala-Leu-Ala-Leu-PQ) coupled to the microparticles. This drug-carrier complex did not kill free promastigotes in suspension, but was effective against amastigotes in cultured mouse peritoneal macrophages. These results show that lysosomal processing of the drug-carrier complex is necessary in order to liberate the pharmacologically active drug. Also, the possible role of reactive oxygen intermediates for the anti-leishmanial effect was studied.