Pharmacokinetics of trifluralin in blood and heart tissue of mice.
BACKGROUND
Trifluralin displays anti-Trypanosoma cruzi activity and a potential therapeutic effect for the treatment of Chagas disease. We assessed peroral and intramuscular trifluralin pharmacokinetics in mouse blood and heart tissue.


METHODS
A parallel experimental design was used. 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). Blood and heart tissue samples were taken at set times after intramuscular and peroral trifluralin administration. Feces and tissue samples were taken 12 h after intramuscular trifluralin administration. Trifluralin concentrations in whole blood, feces and tissues were determined by HPLC.


RESULTS
After intramuscular and peroral administration, maximum whole blood concentration (C(max)) was attained at 30 min and 2.0 h (t(max)) (28.2 +/- 0.7 and 7.8 +/- 0.033 microg/ml; p < 0.05). C(max) in heart tissue was attained at 1.0 and 2.0 h (0.6 +/- 0.004 and 0.2 +/- 0.002 microg/g; p < 0.05). Liver, perirenal and subcutaneous fat concentrations were 55.1, 66.3 and 59.7 ng/mg tissue protein. Peroral and intramuscular penetration ratios determined by comparing heart tissue areas under the curve were 6.3 and 4.0%, respectively.


CONCLUSIONS
Intramuscular trifluralin could be a new alternative for the treatment of Chagas disease.
Zaidenberg
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A
Institute of Paediatric Research and Development Dr Fernando Viteri, La Plata Children's Hospital, La Plata, Argentina.
Marra
C
C
Villagra
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S
Rule
R
R
D000273:Adipose Tissue / Q000378:metabolism; D000818:Animals; D002598:Chagas Cardiomyopathy / Q000188:drug therapy; D014355:Chagas Disease / Q000188:drug therapy; D005243:Feces / Q000737:chemistry; D006801:Humans; D008099:Liver / Q000378:metabolism; D008297:Male; D051379:Mice; D009206:Myocardium / Q000378:metabolism*; D014274:Trifluralin / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D014344:Trypanocidal Agents / Q000097:blood / Q000493:pharmacokinetics*
D014344:Trypanocidal Agents; D014274:Trifluralin