Two novel ternary albendazole-cyclodextrin-polymer systems: dissolution, bioavailability and efficacy against Taenia crassiceps cysts.
The effect of two water-soluble polymers: pectin and polyvinylpyrrolidone in combination with beta-cyclodextrin, on the dissolution, bioavailability and cysticidal efficacy of albendazole was evaluated using a commercial suspension as reference product. The dissolution of the albendazole-beta-cyclodextrin-pectin formulation was slow and incomplete (44.7%). No statistical differences in C(max) and AUC were found between this formulation and the reference. Also its cysticidal efficacy (33%) was similar to the reference (38%). The albendazole-beta-cyclodextrin-polyvinylpyrrolidone formulation exhibited the highest dissolution rate (78.5%) and its bioavailability was also significantly increased (2.3-fold). In addition, the cysticidal activity of this formulation (83%) was greater than a commercial suspension. Our results suggest that the ternary system of albendazole-beta-cyclodextrin-polyvinylpyrrolidone could be a potential alternative for the treatment of systemic helmintic diseases and it is worth to continue its preclinical evaluation.
Palomares-Alonso
Francisca
F
Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía. México DF, 14269, Mexico. ingpalomares@yahoo.com.mx
González
Cesar Rivas
CR
Bernad-Bernad
Ma Josefa
MJ
Montiel
María Dolores Castillo
MD
Hernández
Guadalupe Palencia
GP
González-Hernández
Iliana
I
Castro-Torres
Nelly
N
Estrada
Enrique Pinzón
EP
Jung-Cook
Helgi
H
D015766:Albendazole / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D000923:Anticestodal Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D010368:Pectins / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013621:Taenia / Q000187:drug effects*; D047392:beta-Cyclodextrins / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*
D000923:Anticestodal Agents; D047392:beta-Cyclodextrins; D010368:Pectins; D015766:Albendazole; C031215:betadex