Evaluation of antitumor activity and development of solid lipid nanoparticles of metronidazole analogue.
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.
Faculty of Pharmacy, Department of Pharmaceutical Products, Federal University of Minas Gerais (UFMG), Av. Antônio Carlos, 6627, 31270-901 Belo Horizonte, Minas Gerais, Brazil.
Eduardo Burgarelli
EB
Lages
Maria Betânia
MB
de Freitas
Isadora Marques Brum
IM
Gonçalves
Ricardo José
RJ
Alves
Cristina Duarte
CD
Vianna-Soares
Lucas Antônio Miranda
LA
Ferreira
Mônica Cristina
MC
de Oliveira
Renata Barbosa
RB
de Oliveira
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy* / Q000473:pathology*; D045744:Cell Line, Tumor; D004058:Diffusion; D008055:Lipids / Q000737:chemistry*; D008795:Metronidazole / Q000008:administration & dosage* / Q000031:analogs & derivatives*; D051379:Mice; D053769:Nanocapsules / Q000008:administration & dosage* / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D016896:Treatment Outcome
D000970:Antineoplastic Agents; D008055:Lipids; D053769:Nanocapsules; D008795:Metronidazole