Topical delivery of amphotericin B utilising transferosomes for the treatment of cutaneous leishmaniasis

Amphotericin B (AmB) is a high-molecular weight poorly soluble drug with a high efficacy in the treatment of infectious caused by Leishmania spp. parasites, which possesses a very low topical bioavailability. Transferosomes (TFs) are ultradeformable vesicles that consist of drugs lipids, an edge activator, and a low amount of ethanol (<10%). They have been engineered and optimized to enhance the permeation of AmB across the skin and, thus, its antiparasitic activity. Drug loading of the formulation resulted in 0.086%, while a good physicochemical stability for 6 months under desiccated conditions was observed. AmB-TFs illustrated a flux of 4.91 ± 0.41 µg/cm2/h across mouse skin. In vivo studies demonstrated a good permeation of the drug after topical application on healthy mouse skin, which was increased using microneedles at early exposure times, while in vivo efficacy studies demonstrated that the parasite load was decreased in a 98.24 ± 1.54%.