Amine functionalized graphene sheet conjugated with amphotericin B for the treatment of visceral leishmaniasis

Abstract

The treatment options for visceral leishmaniasis (VL), potentially caused by Leishmania donovani, are limited and unsatisfactory. Conventional AmB exhibits low solubility and instability at gastric pH and is unable to penetrate the brush border membrane of the small intestine and have have serious toxicity. Different nano vectors have been explored for the transportation of these drugs to the target. We evaluated a novel formulation of Amphotericin B (AmB) conjugated to amine-functionalized graphene (f-Gr) for safety and efficacy over conventional AmB. Graphene sheet have been synthesized by thermal exfoliation of chemically prepared graphite oxide by rapid heating at 1050°C in an Ar atmosphere. As synthesized graphene sheet was amine functionalized non-covalently with L-cysteine at room temperature. As functionalized graphene sheet was further used to conjugate AmB. The conjugate (f-Gr-AmB) was characterized by FTIR, SEM and TEM that established successful attachment of AmB to f-Gr. The f-Gr-AmB was found to exhibit lesser cytotoxity as compared to AmB also it showed significantly enhanced efficacy of f-Gr-AmB over AmB. However the results of in vivo and in vitro studies are not described here. © 2014, Advanced Engineering Solutions (AES.COM) Ottawa, Canada.