Pharmacokinetics and anthelmintic efficacy of albendazole microcrystalline formulations in CBi-IGE mice differing in susceptibility to Trichinella spiralis infection

PRIOTTI, J.; LAMAS, M. C.; VASCONI, M. D.; HINRICHSEN, L.; CODINA, A. V.; LEONARDI, D.

CABA

Congreso; Drug Discovery for Neglected Diseases International Congress 2018 4th Scientific Meeting of ResNet NPND; 2018

Drug Discovery for Neglected Diseases

Albendazole (ABZ), the drug of choice to treat trichinellosis orally, is characterized by its poor aqueous solubility that conditions an erratic bioavailability. ABZ microcrystals were prepared to improve its solubility (1). After the physicochemical characterization and in vitro analysis of the parasiticide activity, two formulations were selected -hydroxyethyl-cellulose (S4A) and chitosan (S10A) based microcrystals- to determine their therapeutic efficacy in vivo in a murine model of trichinellosis. This work aimed to analyze whether the formulations improved ABZ pharmacokinetic parameters and in vivo efficacy against different morphological forms of T. spiralis, in two mouse lines differing in susceptibility to the parasite (2). CBi/L (resistant) and CBi+ (susceptible) adult mice of both sexes were given an oral dose of ABZ, S4A, or S10A (30 mg ABZ/kg bw) and the plasma concentration-time profile of albendazole sulphoxide, the main ABZ metabolite, was determined by HPLC analysis. The animals given the formulations had higher plasma concentration compared to those that received the pure drug. A significant increase, as well as sex and genotype effects (P