Abstract
Chagas is a neglected tropical disease caused by Trypanosoma cruzi, and affects about 25 million people worldwide. N, N’-Squaramide 17 (S) is a trypanocidal compound with relevant in vivo effectiveness. Here, we produced, characterized, and evaluated cytotoxic and trypanocidal effects of macrophage-mimetic liposomes from lipids extracted of RAW 264.7 cells to release S. As results, the average hydrodynamic diameter and Zeta potential of mimetic lipid membranes containing S (MLS) was 196.5 ± 11 nm and −61.43 ± 2.3 mV, respectively. Drug entrapment efficiency was 73.35% ± 2.05%. After a 72 h treatment, MLS was observed to be active against epimastigotes in vitro (IC50 = 15.85 ± 4.82 μM) and intracellular amastigotes (IC50 = 24.92 ± 4.80 μM). Also, it induced low cytotoxicity with CC50 of 1199.50 ± 1.22 μM towards VERO cells and of 1973.97 ± 5.98 μM in RAW 264.7. MLS also induced fissures in parasite membrane with a diameter of approximately 200 nm in epimastigotes. MLS showed low cytotoxicity in mammalian cells and high trypanocidal activity revealing this nanostructure a promising candidate for the development of Chagas disease treatment.
Highlights
Chagas disease or American Trypanosomiasis is a neglected tropical disease considered endemic in twenty-one Latin American countries
T. cruzi epimastigote form was maintained at 27 ◦ C in axenic culture RPMI-1640 containing 10 U/mL penicillin, 25 μg/mL streptomycin, 25 mM HEPES buffer, 0.03 M Hemin, and 200 mM glutamine supplemented with 10% inactivated fetal bovine serum (FBS) [15]
Hydrodynamic diameter of the formed nanostructures was determined by dynamic light scattering (DLS) in a ZetaSizer Nano ZS (Malvern Instruments Ltd., Malvern, UK) using He-Ne laser (4 mW) at
Summary
Chagas disease or American Trypanosomiasis is a neglected tropical disease considered endemic in twenty-one Latin American countries. It has been increasingly detected in the United States of America, Canada, and many European countries This is due, mainly, to population mobility between Latin America and the rest of the world and has caused more than 7000 deaths per year and over 25 million people at risk of infection [1]. Chemotherapeutics are based on nitro heterocyclic compounds, such as nitrofuran (nifurtimox) and nitroimidazole (benznidazole) These therapeutic options are unsatisfactory, given their limited effectiveness in preventing the chronic stage of the disease [3]. Liposomes are nanosystems with potential applications as active vectors of drug delivery due to their ability to improve drug’s pharmacological action by their greater solubility, stability, biodistribution, and their mode of release [8]. Toxicity on mammalian cells and their trypanocidal activity (CL-Brener) were evaluated, as well as the damage effects on the parasites using scanning electron microscopy (SEM)
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