AMPHOTERICIN B CONJUGATED STABILIZED GOLD NANOPARTICLES AND USES THEREOF

摘要

The present invention relates to conjugates of amphotericin B and gold nanoparticles stabilized with thiohexoses or thiopentoses, and a method to produce said nanoparticles. As the conjugates of amphotericin B to the stabilized gold nanoparticles show several advantages over amphotericin B alone, the present invention is also directed to pharmaceutical compositions comprising said nanoparticles, and to their use for treat fungal and leishmanial infection. These amphotericin B stabilized gold nanoparticles are dispersible in water and are not toxic for mammalian cells differently from free amphotericin B and other currently used amphotericin B preparations. Importantly, the conjugates of amphotericin B and stabilized gold nanoparticles are more efficacious in treating all forms of Cryptococcal infections (planktonic, intracellular and biofilms) than amphotericin B. Additionally, the conjugates are more effective against extracellular and intracellular forms of Leishmania mexicana and Leishmania major. Therefore, amphotericin B conjugated to thiohexose or thiopentose stabilized gold nanoparticles offer safer and better treatment option than free amphotericin B, and in particular for Cryptococcal and Leishmanial infections.