Synthesis and Biological Evaluation of Amphotericin B Formulations Based on Organic Salts and Ionic Liquids against Leishmania infantum

• Type: Article in International Scientific Journal
• Date: 2022

Authors

Ferraz, R (Author) Other; Santarem, N (Author) Other; Santos, AFM (Author) Other; Jacinto, ML (Author) Other; Anabela Cordeiro da Silva (Author) FFUP; Prudencio, C (Author) Other; Noronha, JP (Author) Other; Branco, LC (Author) Other; Petrovski, Z (Author) Other

Journal

Title: Antibiotics

Vol. 11

Final page: 1841

Publisher: MDPI

Indexing

ISI Web of Knowledge - 0 Citations

Other information

Authenticus ID: P-00X-TFC

DOI: 10.3390/antibiotics11121841

Abstract (EN): Nowadays, organic salts and ionic liquids (OSILs) containing active pharmaceutical ingredients (APIs) are being explored as drug delivery systems in modern therapies (OSILs-API). In that sense, this work is focused on the development of novel OSILs-API based on amphotericin B through an innovative procedure and the evaluation of the respective biological activity against Leishmania infantum. Several ammonium, methylimidazolium, pyridinium and phosphonium organic cations combined with amphotericin B as anion were synthesized in moderate to high yields and high purities by the water-reduced buffer neutralization method. All prepared compounds were characterized to confirm the desired chemical structure and the specific optical rotation ([alpha](D)(25)) was also determined. The biological assays performed on L. infantum promastigotes showed increased activity against this parasitic disease when compared with the starting chloride forms and amphotericin B alone, highlighting [P-6,P-6,P-6,P-14][AmB] as the most promising formulation. Possible synergism in the antiprotozoal activity was also evaluated for [P-6,P-6,P-6,P-14][AmB], since it was proven to be the compound with the highest toxicity. This work reported a simple synthetic method, which can be applied to prepare other organic salts based on molecules containing fragile chemical groups, demonstrating the potential of these OSILs-AmB as possible agents against leishmaniasis.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 12