Pharmacokinetics of trifluralin in blood and heart tissue of mice.

ZAIDEMBERG, ANÍBAL; MARRA, CARLOS ALBERTO; VILLAGRA, SERGIO; RULE, ROBERTO

CHEMOTHERAPY

KARGER

Lugar: Oxford; Año: 2009 vol. 55 p. 327 - 334

0009-3157

Trifluralin (á,á,á-2,6-dinitro-N-N-dipropyl-p-toluidine) displays anti-Trypanosoma cruzi activity and potential therapeutic effect for the treatment of Chagas disease. In this study, we assessed peroral and intramuscular trifluralin pharmacokinetics in blood and heart tissue of mice. Healthy adult male CF1 albino mice (n=108; 25-35 g bw) received a single peroral or intramuscular trifluralin dose (50 mg/kg in peanut oil). Mice blood and tissues samples were obtained at specific time-intervals after trifluralin administration. Trifluralin concentrations were determined by HPLC. After intramuscular and peroral administration, maximum blood concentrations (Cmax) were attained at 30 min and 2.0 h (tmax) (28.2 ± 0.7 and 7.8 ± 0.033 µg/mL; P < 0.05, respectively). Cmax in heart tissue  were attained at 1.0 and 2.0 h (0.6 ± 0.004 and 0.2 ± 0.002 µg/mL; P < 0.05, respectively). Peroral and intramuscular penetration ratios into heart tissue were 6.3 and 4.0%, respectively. Samples of perirenal and subcutaneous fat, liver and cardiac muscle exhibited important concentrations-time 12 h after intramuscular trifluralin administration. We conclude that intramuscular trifluralin could be a new alternative drug for the treatment of Chagas disease that should be included in future pharmacological experimental studies.