Radiochemical and radiopharmacological properties of pirocarbotrat and other labeled charcoal dispersions: comparative studies in rats with NMU-induced mammary tumors.
The purpose of this work is to study the physicochemical properties of Pirocarbotrat to explain its radiopharmacological behavior. We also studied a mixture of charcoal plus chromic [32P]phosphate and charcoal plus sodium [32P]orthophosphate only for comparative purposes. The results show that the mean diameter of the Pirocarbotrat particles was 2.5 microm with an homogeneous distribution, while the other products show an heterogeneous distribution of the particle sizes, with a mean size diameter between 0.5 and 0.9 microm. Hydrolysis studies with a solution of 0.1 N HCl and with sulfochromic mixture revealed that in Pirocarbotrat the 32P is strongly bound to the charcoal particles. Bioelimination studies of Pirocarbotrat show that the total eliminated activity was 12.70 +/- 3.90%, with a higher amount in urine (8.30 +/- 1.80%) than in feces (4.40 +/- 3.50%). When biodistribution studies of Pirocarbotrat were carried out, we found that the 84.50 +/- 2.60% of the activity remained in the tumor with almost null irradiation of the other organs under study. When therapeutic action was evaluated, we observed that the percentage of tumor regression was 78.3% for the tumors injected with Pirocarbotrat. The other dispersions under study showed different behaviors with high activity percentages distributed throughout the organism. These studies demonstrate that Pirocarbotrat has the best radiopharmacological properties to ensure irradiation of the tumor with the least concomitant irradiation of surroundings or other organs or tissues.
Zubillaga
M B
MB
Radioisotope Laboratory, Facultad de Farmacia y Bioquímica, University of Buenos Aires, Argentina. postmaster@radioqui.ffyb.uba.ar
Boccio
J R
JR
Nicolini
J O
JO
Ughetti
R
R
Lanari
E
E
Caro
R A
RA
D000230:Adenocarcinoma / Q000139:chemically induced / Q000378:metabolism* / Q000532:radiotherapy; D000818:Animals; D002606:Charcoal / Q000737:chemistry* / Q000493:pharmacokinetics; D005260:Female; D008325:Mammary Neoplasms, Experimental / Q000139:chemically induced / Q000378:metabolism* / Q000532:radiotherapy; D008657:Metabolic Clearance Rate; D008770:Methylnitrosourea; D010710:Phosphates / Q000493:pharmacokinetics* / Q000627:therapeutic use; D010761:Phosphorus Radioisotopes / Q000493:pharmacokinetics* / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution
D010710:Phosphates; D010761:Phosphorus Radioisotopes; D002606:Charcoal; D008770:Methylnitrosourea