title: Anticryptosporidial activity of furan derivative G1 and its inclusion complex with beta-cyclodextrin.
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.
authors.affiliation: Department of Microbiology and Parasitology, Faculty of Pharmacy, University of Santiago de Compostela, 15782 Santiago de Compostela, Spain.
authors.forename: J A
authors.initials: JA
authors.lastname: Castro-Hermida
authors.forename: H
authors.initials: H
authors.lastname: Gómez-Couso
authors.forename: M E
authors.initials: ME
authors.lastname: Ares-Mazás
authors.forename: M M
authors.initials: MM
authors.lastname: Gonzalez-Bedia
authors.forename: N
authors.initials: N
authors.lastname: Castañeda-Cancio
authors.forename: F J
authors.initials: FJ
authors.lastname: Otero-Espinar
authors.forename: J
authors.initials: J
authors.lastname: Blanco-Mendez
mesh_terms: D000818:Animals; D002417:Cattle; D002626:Chemistry, Pharmaceutical; D003457:Cryptosporidiosis / Q000188:drug therapy* / Q000469:parasitology; D016785:Cryptosporidium parvum / Q000187:drug effects* / Q000469:parasitology; D003505:Cyclodextrins / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D005260:Female; D005663:Furans / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D051379:Mice; D009574:Nitro Compounds / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D033661:Oocysts / Q000187:drug effects; D012995:Solubility; D047392:beta-Cyclodextrins
chemical_list: D003505:Cyclodextrins; D005663:Furans; D009574:Nitro Compounds; D047392:beta-Cyclodextrins; C031215:betadex; C039281:furan