Evaluation of Antitumor Activity and Development of Solid Lipid Nanoparticles of Metronidazole Analogue

Author: Lages Eduardo Burgarelli   de Freitas Maria Betânia   Gonçalves Isadora Marques Brum   Alves Ricardo José   Vianna-Soares Cristina Duarte   Ferreira Lucas Antônio Miranda   de Oliveira Mônica Cristina   de Oliveira Renata Barbosa  

Publisher: American Scientific Publishers

ISSN: 1550-7033

Source: Journal of Biomedical Nanotechnology, Vol.9, Iss.11, 2013-09, pp. : 1939-1944

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Abstract

Nitroheterocyclic compounds have received considerable interest as hypoxia-selective cytotoxins (HSC) for cancer treatment. In the present study, we investigated antitumor activity of an iodide analogue of metronidazole, 1-(2-iodoethyl)-2-methyl-5-nitroimidazole (MTZ-I), using Swiss mice bearing solid Ehrlich tumor. MTZ-I showed potent anti-cancer activity at a dose of 40 mg/kg. MTZ-I loaded solid lipid nanoparticles (SLN) were developed as an alternative colloidal carrier system to enhance tumor drug uptake. SLN were characterized for particle size, polydispersity index, zeta potential and entrapment efficiency. In addition, the influence of presence of the cationic lipid stearylamine (STE) on stability of formulation was assessed. The results of DSC study showed that MTZ-I exhibited interaction with STE.

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