Anticryptosporidial activity of furan derivative G1 and its inclusion complex with beta-cyclodextrin

J Pharm Sci. 2004 Jan;93(1):197-206. doi: 10.1002/jps.10528.

Abstract

The capacity of beta-cyclodextrin (betaCD) to form a complex with a new furanic derivative, G1, was investigated. Interactions of the drug and betaCD in solution and in the solid state were studied using phase solubility techniques, thermal methods, X-ray, and IR spectroscopy. Preparation of a kneaded mix of G1/betaCD increased both the aqueous solubility and the dissolution rate of the furan derivative. The anticryptosporidial efficacies of the drug and of the inclusion complex were evaluated using a suckling murine model. Oral administration of G1 considerably decreased the intensity of the infection, but betaCD showed similar anticryptosporidial activity to that of the betaCD-G1 complex and higher activity than G1 alone.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cattle
  • Chemistry, Pharmaceutical
  • Cryptosporidiosis / drug therapy*
  • Cryptosporidiosis / parasitology
  • Cryptosporidium parvum / drug effects*
  • Cryptosporidium parvum / parasitology
  • Cyclodextrins / chemistry
  • Cyclodextrins / pharmacology
  • Cyclodextrins / therapeutic use*
  • Female
  • Furans / chemistry
  • Furans / pharmacology
  • Furans / therapeutic use*
  • Mice
  • Nitro Compounds / chemistry
  • Nitro Compounds / pharmacology
  • Nitro Compounds / therapeutic use*
  • Oocysts / drug effects
  • Solubility
  • beta-Cyclodextrins*

Substances

  • Cyclodextrins
  • Furans
  • Nitro Compounds
  • beta-Cyclodextrins
  • betadex
  • furan