Nematodicidal activity of flubendazole and its reduced metabolite on a murine model of Trichinella spiralis infection

Chemotherapy. 2012;58(4):295-8. doi: 10.1159/000342924. Epub 2012 Oct 17.

Abstract

Background: Flubendazole (FLBZ) is a broad-spectrum benzimidazole anthelmintic compound. The parent FLBZ is metabolized to its reduced (R-FLBZ) and hydrolyzed (H-FLBZ) metabolites. There are no data on the potential nematodicidal activity of R-FLBZ, the main plasma metabolite found in sheep and mice. The goal of the current work was to assess the efficacy of FLBZ and R-FLBZ against Trichinella spiralis in a mouse model.

Methods: Both compounds were administered to Balb/c mice infected with T. spiralis as either a cyclodextrin aqueous solution or as a carboxymethylcellulose suspension. Treatments were performed orally (5 mg/kg) at 1 day after infection with T. spiralis. The efficacy of the treatments was assessed at day 6 after infection.

Results: While the efficacy obtained for FLBZ and R-FLBZ administered as a solution was 94 and 98%, respectively, the efficacies obtained after the treatment with FLBZ suspensions were 38% (FLBZ) and 64% (R-FLBZ).

Conclusion: Under the current experimental conditions, a high nematodicidal efficacy of both FLBZ and R-FLBZ administered as solution preparations was observed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Anthelmintics / metabolism
  • Anthelmintics / therapeutic use*
  • Carboxymethylcellulose Sodium / chemistry
  • Cyclodextrins / chemistry
  • Disease Models, Animal
  • Mebendazole / analogs & derivatives*
  • Mebendazole / metabolism
  • Mebendazole / therapeutic use
  • Mice
  • Mice, Inbred BALB C
  • Oxidation-Reduction
  • Trichinella spiralis / pathogenicity*
  • Trichinellosis / drug therapy*

Substances

  • Anthelmintics
  • Cyclodextrins
  • Mebendazole
  • Carboxymethylcellulose Sodium
  • flubendazole