Anticryptosporidial activity of furan derivative G1 and its inclusion complex with beta-cyclodextrin.
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.
Castro-Hermida
J A
JA
Department of Microbiology and Parasitology, Faculty of Pharmacy, University of Santiago de Compostela, 15782 Santiago de Compostela, Spain.
Gómez-Couso
H
H
Ares-Mazás
M E
ME
Gonzalez-Bedia
M M
MM
Castañeda-Cancio
N
N
Otero-Espinar
F J
FJ
Blanco-Mendez
J
J
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
D003505:Cyclodextrins; D005663:Furans; D009574:Nitro Compounds; D047392:beta-Cyclodextrins; C031215:betadex; C039281:furan