Background and Aims: Niclosamide (Nic), an old FDA-approved anti-helminthic drug, has
recently been shown to inhibit the growth of various cancer cells. However, this drug shows low
aqueous solubility restricting its systemic use. The present study was aimed to prepare and characterize
niclosamide nanoliposomes and to evaluate their in vivo anti-tumor effects.
Methods: Nanoliposomes composed of hydrogenated soya phosphatidylcholine (HSPC) and 1,2-
distearoyl-sn-glycero-3-phosphoethanolamine-N- [methoxy (polyethylene glycol)-2000] (DSPE) were
prepared using lipid-film hydration method and Nic was encapsulated with remote loading method. The
prepared nanoliposomes were characterized by visualizing morphology,and measuring particle size and
Zeta potential. HPLC analysis was used to quantify encapsulated Nic. The in vitro cytotoxicity of the
nanoliposomal Nic on CT26 colon carcinoma cells was evaluated. The inhibition of tumor growth was
investigated in BALB/c mice bearing CT26 colon carcinoma cells.
Results: Analytical results revealed that the nanoliposomal system was a homogeneous and stable colloidal
dispersion of Nic particles. The atomic force microscopy images and particle size analysis indicated
that all Nic particles had a spherical shape with a diameter of approximately 108 nm. According
to in vitro and in vivo studies, nanoliposomal Nic showed a higher growth inhibitory activity against
CT26 colon carcinoma cells compared with free Nic.
Conclusion: The encapsulation of Nic in liposome nanoparticles elevated its aqueous solubility, which
was accompanied by enhanced anti-tumor properties in vivo.