The aim of this study was to prepare a nano-structured lipid carrier (NLC) containing Meglumine Antimoniate (MA) for treatment of leishmaniasis. Haftyzer-Van Krevelen mathematical modeling was applied to select the best components for preparing nanoparticles with smaller particle size, higher drug encapsulation efficiency, and more stability over time. Mathematical results were approved by the experimental study. Then, ex-vivo and in-vivo antileishmanial performance of the NLC formulation was investigated on the healthy and leishmania major BALB/C female mice, respectively. Characterization results showed that the optimal NLC formulation had a mean particle size of 93 ± 0.1 nm with uniform particle size distribution and proper zeta potential about 30 ± 0.25 mV. Drug entrapment efficiency was 74 ± 0.37%. In-vitro drug release studies at pH = 7.4 showed a controlled drug release from NLC formulation in comparison to commercial ampule. Ex-vivo analysis results approved the highest reduction of the promastigotes number and proper penetration of drug from the skin layers of the healthy BALB/C female mice for NLC sample. In-vivo results showed that new NLC formulation created a significant reduction in leishmaniasis wound size with reducing the number of parasites in comparison to the commercial ampule. Furthermore, lower inflammation, redness, depth and stiffness was observed for NLC formulation group. Hematological analysis results confirmed that unlike the commercial formulation, the new formulation signifi-cantly reduced systemic drug absorption and drug side effects, including variance of liver enzymes and blood factors. In conclusion, NLC formulation was proposed as a safe alternative for delivering glucantime in injection administration route compared with commercial ampule

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