Cholesterol improves stability of amphotericin B nanoemulsion: promising use in the treatment of cutaneous leishmaniasis

• Published in: Nanomedicine (London, England) Vol. 17; no. 18; pp. 1237 - 1251
• Main Authors: Mansur-Alves, Izabela, Lima, Brenda Lorrayne Furtado, Santos, Thais Tunes, Araújo, Naialy F, Frézard, Frédéric, Islam, Arshad, de Barros, André Lb, Dos Santos, Délia Cm, Fernandes, Christian, Ferreira, Lucas Am, Aguiar, Marta Mg
• Format: Journal Article
• Language: English
• Published: England Future Medicine Ltd 01.08.2022
• Subjects: amphotericin B; Amphotericin B - pharmacology; Amphotericin B - therapeutic use; Animals; antileishmanial efficacy; Antiprotozoal Agents - pharmacology; Antiprotozoal Agents - therapeutic use; Cholesterol; Leishmania major; Leishmaniasis, Cutaneous - drug therapy; nanoemulsion; stability; cholesterol; antileishmanial efficacy; amphotericin B; nanoemulsion; stability
• ISSN: 1743-5889; 1748-6963
• DOI: 10.2217/nnm-2021-0489

Amphotericin B (AmB) is an antileishmanial drug with high toxicity; however, this drawback might overcome by decreasing the AmB self-aggregation state. This work aimed at evaluating the influence of cholesterol on the aggregation state of AmB loaded in a nanoemulsion (NE-AmB) for the treatment of cutaneous leishmaniasis. NE-AmB (1, 4 and 8 mg/kg/day) was administered intravenously to animals infected by every 2 days for a total of five injections. Ultraviolet-visible spectroscopy and circular dichroism studies demonstrated that cholesterol reduced AmB aggregation state in NE. NE-AmB was stable after 180 days, and its hemolytic toxicity was lower than that observed for the conventional AmB. NE-AmB administered intravenously into animals infected by at 8 mg/kg was capable of stabilizing the lesion size and reducing the parasitic load. These findings support the NE potential as a stable nanocarrier for AmB in the treatment of cutaneous leishmaniasis.