Macrophage Targeting: Comparative Cytotoxicity Activity of Imipramine-loaded Polymeric Nanoparticles and Niosomes

Abstract

The aim of the present study was to prepare niosomal and nanoparticle formulations for drug therapy of
leishmaniasis. Imipramine, an antidepressant, is reported to have anti-leishmaniasis activity in the dose of 5–10 mg/kg.
Materials and Methods: In this study, we tried an approach with imipramine and polymer chitosan to target mannose
receptors on macrophages using nanoparticles as drug carrier and with span 40 as surfactant in niosomes. Formulation
of niosomes encapsulated with imipramine was optimized by changing the proportions of span 40, cetrimide, and
cholesterol. The imipramine encapsulated niosomal formulations based on span 40, cetrimide, and cholesterol was
prepared by hand shaking method and characterized using atomic force microscopy. The nanoparticles were prepared by
modified ionic gelation method, where chitosan was conjugated with mannose for facilitation of uptake by macrophages.
Results: The Atomic Force Microscopy results showed that the particles were spherical in shape and had a size between
200 and 900 nm. The prepared nanoparticles were evaluated for particle size, encapsulation efficiency and in vitro drug
release. The in vitro release of nanoparticles shows 76 ± 1% release in 6 h. Conclusion: Niosomes and nanoparticles
cell uptake studies were evaluated using RAW 264.7 cell lines. The % viability values for niosomes and nanoparticles
were 42.53% and 70.17% at the highest concentration of 100 μg/mL after the incubation period of 24 h, respectively.