Abstract
Objective: The aim of the present investigation is to formulate and evaluate amphotericin B-miltefosine combination nanovesicles for application in the treatment of visceral leishmaniasis.
 Methods: Amphotericin B-miltefosine combination (AmB-MTF) nanovesicles were prepared by ethanol injection method. Formulations of nanovesicles were evaluated at varying conditions of lipids composition, drug-lipid proportion, ethanol-water composition and stirring rate, on drug entrapment efficiency and particle size.
 Results: The study showed that entrapment efficiency was significantly affected (p<0.01) by the effects of lipids composition, drug-lipid proportion, ethanol-water composition, and stirring rate. Particle size of nanovesicles was significantly affected (p<0.05) by drug-lipid proportion and stirring rate. An optimized formulation of amphotericin B-miltefosine nanovesicles was prepared at optimal factors composition of: phosphatidylcholine-cholesterol-stearic acid 20:4:1, drug-lipid 1:8, AmB-MTF 1:1; ethanol-water 1:4 ratios, and stirring rate 1000 rpm. The AmB-MTF 1:1 nanovesicles formulation showed particle size of 145.6 nm, poly dispersity index 0.19, zeta potential-27.3 mV and drug entrapment efficiency 87%.
 Conclusion: Evaluation of AmB-MTF 1:1 nanovesicles showed development of a successful formulation with very good compatibility, extended drug release, convenient vesicle size and high drug entrapment efficiency. To conclude, AmB-MTF 1:1 nanovesicles formulation could be a safe and reliable therapeutic option over the conventional combination therapy provided further antileishmanial investigations are investigated in vitro and in vivo.
Highlights
Visceral leishmaniasis is the most severe form of leishmaniasis by which patients nearly always die if untreated
Amphotericin B-miltefosine combination (AmB-MTF) nanovesicles were prepared by ethanol injection method
Nanovesicles were evaluated at different conditions of lipids composition, drug-lipid proportion, ethanol-water composition and stirring rate on drug entrapment efficiency and particle size
Summary
Visceral leishmaniasis is the most severe form of leishmaniasis by which patients nearly always die if untreated. It causes half a million new cases and 50,000 deaths each year. The current treatment for visceral leishmaniasis is with drugs developed 50 y ago. The best strategy that remains as effective solution in crisis associated with the neglected diseases is using combination of the exciting drugs and developing novel drug delivery systems to improve the efficacy, specificity, tolerability, and emergence of resistance of existing antiparasitic agents [3]. Nanocarriers drug delivery to the liver and spleen, the main infection site of visceral leishmaniasis, have been developed [4]. Ambisome monotherapy unresponsiveness and drug resistance cases have been reported in some places such as Bahir, India [5]
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