Pharmacokinetic parameters and therapeutic efficacy of albendazole (ABZ) microcrystal formulations in susceptible mice of the CBi-IGE murine model of trichinellosis

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

Mar del Plata

Congreso; SAIC 2019; 2019

SAIC

ABZ is commonly used in oral chemotherapy against trichinellosis, its main disadvantage being poor bioavailability due to low solubility in water. Microcrystalline ABZ formulations were developed using a bottom-up methodology to optimize oral absorption. After physicochemical characterization and in vitro anthelmintic assays, hydroxyethyl cellulose (S4A) and chitosan (S10A) based formulations were selected to analyze whether ABZ pharmacokinetic parameters and in vivo efficacy against the encysted T. spiralis larvae improved, in mice susceptible to the parasite. CBi+ mice of both sexes were given a single oral dose of ABZ, S4A, or S10A (30 mg ABZ/kg BW) and afterward, blood samples were collected at different times to quantify plasma concentration of albendazole sulphoxide, the main ABZ metabolite, by HPLC analysis. Mice given S4A and S10A showed an increased Cmax (peak plasma concentration) compared to those receiving pure ABZ (♂ P=0.01, ♀ P=0.009); also, AUC (area under the concentration-time curve) increased significantly (P