Improving bioavailability and anthelmintic activity of albendazole by preparing albendazole-cyclodextrin complexes.
The bioavailability and anthelmintic activity of albendazole-cyclodextrin complexes (ABZ-CDC) compared to albendazole suspensions in carboxymethylcellulose (ABZ-CMC) was assessed in a mouse model for Trichinella infections. Swiss CD-1 mice experimentally infected with T. spiralis were treated with both formulations against enteral (adult worms) and parenteral (migrating and encysted larvae). Oral bioavailability was assessed in age matched mice treated with 50 mg/kg of both formulations. The anthelmintic effects and plasma concentration of the active metabolite albendazole-sulphoxide (ABZSO) enantiomer (-) were significantly increased following administration of ABZ-CDC in relation to ABZ-CMC.
García-Rodriguez
J J
JJ
Departmento de Parasitología, Facultad de Farmacia, Universidad Complutense, Spain.
Torrado
J
J
Bolás
F
F
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000284:Administration, Oral; D015766:Albendazole / Q000097:blood / Q000493:pharmacokinetics*; D000818:Animals; D000871:Anthelmintics / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D003505:Cyclodextrins; D005079:Excipients; D051379:Mice; D013237:Stereoisomerism; D013997:Time Factors; D017160:Trichinella spiralis; D014235:Trichinellosis / Q000097:blood / Q000188:drug therapy*; D047392:beta-Cyclodextrins
D000871:Anthelmintics; D003505:Cyclodextrins; D005079:Excipients; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D015766:Albendazole