Two novel ternary albendazole-cyclodextrin-polymer systems: dissolution, bioavailability and efficacy against Taenia crassiceps cysts

Acta Trop. 2010 Jan;113(1):56-60. doi: 10.1016/j.actatropica.2009.09.006. Epub 2009 Sep 19.

Abstract

The effect of two water-soluble polymers: pectin and polyvinylpyrrolidone in combination with beta-cyclodextrin, on the dissolution, bioavailability and cysticidal efficacy of albendazole was evaluated using a commercial suspension as reference product. The dissolution of the albendazole-beta-cyclodextrin-pectin formulation was slow and incomplete (44.7%). No statistical differences in C(max) and AUC were found between this formulation and the reference. Also its cysticidal efficacy (33%) was similar to the reference (38%). The albendazole-beta-cyclodextrin-polyvinylpyrrolidone formulation exhibited the highest dissolution rate (78.5%) and its bioavailability was also significantly increased (2.3-fold). In addition, the cysticidal activity of this formulation (83%) was greater than a commercial suspension. Our results suggest that the ternary system of albendazole-beta-cyclodextrin-polyvinylpyrrolidone could be a potential alternative for the treatment of systemic helmintic diseases and it is worth to continue its preclinical evaluation.

MeSH terms

  • Albendazole / chemistry
  • Albendazole / pharmacokinetics
  • Albendazole / pharmacology*
  • Animals
  • Anticestodal Agents / chemistry
  • Anticestodal Agents / pharmacokinetics
  • Anticestodal Agents / pharmacology*
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Pectins / chemistry
  • Pectins / pharmacokinetics
  • Pectins / pharmacology*
  • Rats
  • Rats, Wistar
  • Taenia / drug effects*
  • beta-Cyclodextrins / chemistry
  • beta-Cyclodextrins / pharmacokinetics
  • beta-Cyclodextrins / pharmacology*

Substances

  • Anticestodal Agents
  • beta-Cyclodextrins
  • Pectins
  • Albendazole
  • betadex