Dermal absorption of niclosamide in rats and minipigs.
The dermal absorption of niclosamide, a drug shown to prevent Schistosomiasis by blocking the dermal penetration of cercariae, has been examined in Sinclair minipigs and rats. Radioactivity in the urine and feces collected daily for 7 days after application of 14C-niclosamide accounted for less than 2 per cent and 10 per cent of the labelled compound applied to pig and rat skin, respectively. Approximately 20 per cent of the radioactivity from the dose solution was recovered on the skin excised from the area of application in both minipigs and rats. No radioactivity was detected in organs removed from the pig 7 days after application of radiolabelled drug while less than 6 per cent of the dose could be accounted for in the rat organs/carcass. Radioactivity in swine blood, removed 0.5, 1, 2, 4 and at 24 h intervals after dosing, was at or below three times background in all of the samples. Total recovery of the applied radioactivity was 78 per cent in pigs and 57 per cent in rats. These studies indicate that niclosamide is very poorly absorbed after dermal application. The results are consistent with earlier comparative studies showing that dermal penetration of xenobiotics in rats is generally higher than in swine.
Department of Pharmacology and Toxicology, School of Veterinary Medicine, University of California, Davis 95616.
P
P
Brennan
D
D
Johnson
S
S
Rider
N
N
Cone
M
M
Goldman
A
A
Buckpitt
H
H
Chung
D000279:Administration, Cutaneous; D000818:Animals; D002250:Carbon Radioisotopes; D008297:Male; D009534:Niclosamide / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000652:urine; D051381:Rats; D011919:Rats, Inbred Strains; D012869:Skin Absorption; D013552:Swine; D013556:Swine, Miniature; D014018:Tissue Distribution
D002250:Carbon Radioisotopes; D009534:Niclosamide