Efficacy of albendazole:β-cyclodextrin citrate in the parenteral stage of Trichinella spiralis infection

Int J Biol Macromol. 2015:77:203-6. doi: 10.1016/j.ijbiomac.2015.02.049. Epub 2015 Mar 16.

Abstract

Albendazole-β-cyclodextrin citrate (ABZ:C-β-CD) inclusion complex in vivo antiparasitic activity was evaluated in the parenteral phase of Trichinella spiralis infection in mice. An equimolar complex of ABZ:C-β-CD was prepared by spray-drying and tested in CBi-IGE male mice orally infected with L1 infective larvae. Infected animals were treated with 50 or 30mg/kg albendazole, (ABZ) equivalent amounts of the ABZ:C-β-CD complex and non treated (controls). Mice received a daily dose on days 28, 29 and 30 post-infection. A week later, larval burden and percentage of encysted dead larvae were assessed in the host by counting viable and non-viable larvae in the tongue. Complexation of ABZ with C-β-CD increased the drug dissolution efficiency nearly eightfold. At 37 days p-i, the reduction percentage in muscle larval load was 35% in mice treated with 50mg/kg/day ABZ and 68% in those given the complex. Treatment with the lower dose showed a similar decrease in parasite burden. Treated animals showed a high percentage of nonviable larvae, the proportion being significantly higher in mice receiving the complex than in control animals (72-88% vs. 11%, P=0.0032). These data indicate that ABZ:C-β-CD increases bioavailability and effectiveness of ABZ against encapsulated Trichinella larvae, thus allowing the use of small doses.

Keywords: Albendazole:β-cyclodextrin citrate complex; Antiparasitic activity; T. spiralis parenteral stages.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Albendazole / chemistry*
  • Albendazole / pharmacology*
  • Animals
  • Antiparasitic Agents / chemistry*
  • Antiparasitic Agents / pharmacology*
  • Citric Acid / chemistry*
  • Male
  • Mice
  • Trichinella spiralis / drug effects*
  • Trichinella spiralis / physiology
  • beta-Cyclodextrins / chemistry*

Substances

  • Antiparasitic Agents
  • beta-Cyclodextrins
  • Citric Acid
  • Albendazole
  • betadex