title: Efficacy of albendazole:β-cyclodextrin citrate in the parenteral stage of Trichinella spiralis infection.
abstract: Albendazole-β-cyclodextrin citrate (ABZ:C-β-CD) inclusion complex in vivo antiparasitic activity was evaluated in the parenteral phase of Trichinella spiralis infection in mice. An equimolar complex of ABZ:C-β-CD was prepared by spray-drying and tested in CBi-IGE male mice orally infected with L1 infective larvae. Infected animals were treated with 50 or 30mg/kg albendazole, (ABZ) equivalent amounts of the ABZ:C-β-CD complex and non treated (controls). Mice received a daily dose on days 28, 29 and 30 post-infection. A week later, larval burden and percentage of encysted dead larvae were assessed in the host by counting viable and non-viable larvae in the tongue. Complexation of ABZ with C-β-CD increased the drug dissolution efficiency nearly eightfold. At 37 days p-i, the reduction percentage in muscle larval load was 35% in mice treated with 50mg/kg/day ABZ and 68% in those given the complex. Treatment with the lower dose showed a similar decrease in parasite burden. Treated animals showed a high percentage of nonviable larvae, the proportion being significantly higher in mice receiving the complex than in control animals (72-88% vs. 11%, P=0.0032). These data indicate that ABZ:C-β-CD increases bioavailability and effectiveness of ABZ against encapsulated Trichinella larvae, thus allowing the use of small doses.
authors: Instituto de Genética Experimental, Facultad de Ciencias Médicas, Universidad Nacional de Rosario, Santa Fe 3100, S2000KTR Rosario, Argentina.
authors: Ana V
authors: AV
authors: Codina
authors: IQUIR-CONICET, Suipacha 570, 2000 Rosario, Argentina; Departamento de Farmacia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 570, 2000 Rosario, Argentina.
authors: Agustina
authors: A
authors: García
authors: IQUIR-CONICET, Suipacha 570, 2000 Rosario, Argentina; Departamento de Farmacia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 570, 2000 Rosario, Argentina.
authors: Darío
authors: D
authors: Leonardi
authors: Instituto de Genética Experimental, Facultad de Ciencias Médicas, Universidad Nacional de Rosario, Santa Fe 3100, S2000KTR Rosario, Argentina; Área Parasitología, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 570, 2000 Rosario, Argentina.
authors: María D
authors: MD
authors: Vasconi
authors: Instituto de Genética Experimental, Facultad de Ciencias Médicas, Universidad Nacional de Rosario, Santa Fe 3100, S2000KTR Rosario, Argentina; CIC-UNR, Universidad Nacional de Rosario, Maipú 1065, 2000 Rosario, Argentina.
authors: Ricardo J
authors: RJ
authors: Di Masso
authors: IQUIR-CONICET, Suipacha 570, 2000 Rosario, Argentina; Departamento de Farmacia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 570, 2000 Rosario, Argentina. Electronic address: mlamas@fbioyf.unr.edu.ar.
authors: María C
authors: MC
authors: Lamas
authors: Instituto de Genética Experimental, Facultad de Ciencias Médicas, Universidad Nacional de Rosario, Santa Fe 3100, S2000KTR Rosario, Argentina; CIC-UNR, Universidad Nacional de Rosario, Maipú 1065, 2000 Rosario, Argentina. Electronic address: lhinrich@unr.edu.ar.
authors: Lucila I
authors: LI
authors: Hinrichsen
mesh_terms: D015766:Albendazole / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D000977:Antiparasitic Agents / Q000737:chemistry* / Q000494:pharmacology*; D019343:Citric Acid / Q000737:chemistry*; D008297:Male; D051379:Mice; D017160:Trichinella spiralis / Q000187:drug effects* / Q000502:physiology; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D000977:Antiparasitic Agents; D047392:beta-Cyclodextrins; D019343:Citric Acid; D015766:Albendazole; C031215:betadex
keywords: Albendazole:β-cyclodextrin citrate complex; Antiparasitic activity; T. spiralis parenteral stages