title: Characterization of albendazole-randomly methylated-β-cyclodextrin inclusion complex and in vivo evaluation of its antihelmitic activity in a murine model of Trichinellosis.
abstract: Albendazole is a benzimidazole carbamate extensively used in oral chemotherapy against intestinal parasites, due to its broad spectrum activity, good tolerance and low cost. However, the drug has the disadvantage of poor bioavailability due to its very low solubility in water; as a consequence, a very active area of research focuses on the development of new pharmaceutical formulations to increase its solubility, dissolution rate, and bioavailability. The primary objective of this study was to prepare randomly methylated β-cyclodextrins inclusion complexes to increase albendazole dissolution rate, in order to enhance its antiparasitic activity. This formulation therapeutic efficacy was contrasted with that of the pure drug by treating Trichinella spiralis infected mice during the intestinal phase of the parasite cycle, on days five and six post-infection. This protocol significantly decreased muscle larval burden measured in the parenteral stage on day 30 post-infection, when compared with the untreated control. Thus, it could be demonstrated that the inclusion complexes improve the in vivo therapeutic activity of albendazole.
authors.affiliation: Departamento de Farmacia, Universidad Nacional de Rosario, Rosario, Santa Fe, Argentina; IQUIR-CONICET, Universidad Nacional de Rosario, Rosario, Santa Fe, Argentina.
authors.forename: Agustina
authors.initials: A
authors.lastname: García
authors.affiliation: Departamento de Farmacia, Universidad Nacional de Rosario, Rosario, Santa Fe, Argentina; IQUIR-CONICET, Universidad Nacional de Rosario, Rosario, Santa Fe, Argentina.
authors.forename: Darío
authors.initials: D
authors.lastname: Leonardi
authors.affiliation: Área Parasitología, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Rosario, Santa Fe, Argentina; Instituto de Genética Experimental, Universidad Nacional de Rosario, Rosario, Santa Fe, Argentina.
authors.forename: María D
authors.initials: MD
authors.lastname: Vasconi
authors.affiliation: Instituto de Genética Experimental, Universidad Nacional de Rosario, Rosario, Santa Fe, Argentina; CIC-UNR, Facultad de Ciencias Médicas, Universidad Nacional de Rosario, Rosario, Santa Fe, Argentina.
authors.forename: Lucila I
authors.initials: LI
authors.lastname: Hinrichsen
authors.affiliation: Departamento de Farmacia, Universidad Nacional de Rosario, Rosario, Santa Fe, Argentina; IQUIR-CONICET, Universidad Nacional de Rosario, Rosario, Santa Fe, Argentina.
authors.forename: María C
authors.initials: MC
authors.lastname: Lamas
mesh_terms: D015766:Albendazole / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000977:Antiparasitic Agents / Q000494:pharmacology*; D002152:Calorimetry, Differential Scanning; D004195:Disease Models, Animal; D046911:Macromolecular Substances / Q000737:chemistry / Q000494:pharmacology*; D013058:Mass Spectrometry; D008745:Methylation; D051379:Mice; D018482:Muscle, Skeletal / Q000469:parasitology; D012995:Solubility; D014235:Trichinellosis / Q000188:drug therapy*; D014961:X-Ray Diffraction; D047392:beta-Cyclodextrins / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000977:Antiparasitic Agents; D046911:Macromolecular Substances; D047392:beta-Cyclodextrins; D015766:Albendazole; C031215:betadex