Assessment of Diet-Related Changes on Albendazole Absorption, Systemic Exposure, and Pattern of Urinary Excretion in Treated Human Volunteers

CEBALLOS L; NIEVES E; JUAREZ M; AVELDAÑO R; TRAVACIO M; MARTOS J; CIMINO R; WALSON JL; KROLEWIECKI A; LANUSSE C; ALVAREZ L

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

AMER SOC MICROBIOLOGY

Lugar: Washington; Año: 2021 vol. 65 p. 1 - 12

0066-4804

Soil-transmitted-helminth (STH) infections are a persistent global publichealth problem. Control strategies for STH have been based on the use of massdrug administration (MDA) mainly targeting preschool- and school-aged-children,although there is increasing interest in expanding treatment to include adults andothers through community-wide MDA. Coverage assessment is critical to understandingthe real effectiveness of albendazole (ALB) treatment in those MDA programs.The work described here aims to (i) evaluate the effect of type of diet (a heavy orlight meal) and fasting before ALB treatment on the systemic disposition of ALB andits metabolites in treated human volunteers and (ii) evaluate the potential feasibilityof detecting albendazole metabolites in urine. The data reported here demonstratethat the systemic availability of the active ALB-sulfoxide (ALBSO) metabolite wasenhanced more than 2-fold after food ingestion (a heavy or light meal). ALB dissolutionimprovement related to the ingestion of food may modify the amount of drug/metabolites reaching the parasite, affecting drug efficacy and the overall success ofMDA strategies. The measurement in urine samples of the amino-ALB-sulfone(NHALBSO2) derivative and ALBSO for up to 96 h suggests that it may be feasible todevelop a noninvasive tool to evaluate compliance/adherence to ALB treatment.