title: Cancer Targeting Potential of99mTc-Finasteride in Experimental Model of Prostate Carcinogenesis.
abstract: This study aimed to radiolabel finasteride, a novel 5α-reductase inhibitor, to evaluate its cancer targeting potential in experimental model of prostate carcinogenesis. Finasteride was effectively radiolabeled with99mTc and showed >90% labeling efficiency. The radiopharmaceutical was found to be stable up to 6 hours in rat serum at 37°C. The blood kinetics of the99mTc-finasteride followed a biphasic release pattern, whereby fast-release phase was observed at 15 seconds and a slow-release phase was observed after 30 minutes of administration. The plasma protein binding of the radio complex observed was 83.89%. For biodistribution studies, the rats were divided into two groups. Group I served as normal controls, while group II was subjected to carcinogen N-methyl-N-nitrosourea (MNU) and hormone testosterone propionate (T) for induction of prostate carcinogenesis, which was confirmed histopathologically. The biodistribution studies on control and carcinogen-treated rats revealed a significant percent-specific uptake in prostate, which was found to be increased significantly as a function of time. The most significant finding of the study was an increase in the percent-specific uptake in prostate of carcinogen-treated animals when compared to the percent-specific uptake in prostate of normal rats after 2 and 4 hours postinjection. The study concludes that99mTc-finasteride possesses selectively toward prostate cancer tissue and can be explored further for its role in detection of prostate cancer.
authors.affiliation: 1 Center for Nuclear Medicine (UIEAST), Panjab University , Chandigarh, India .
authors.forename: Gowsia
authors.initials: G
authors.lastname: Jan
authors.affiliation: 2 University Institute of Pharmaceutical Sciences, Panjab University , Chandigarh, India .
authors.forename: Neelima D
authors.initials: ND
authors.lastname: Passi
authors.affiliation: 3 Department of Biophysics, Panjab University , Chandigarh, India .
authors.forename: Devinder Kumar
authors.initials: DK
authors.lastname: Dhawan
authors.affiliation: 1 Center for Nuclear Medicine (UIEAST), Panjab University , Chandigarh, India .
authors.forename: Vijayta Dani
authors.initials: VD
authors.lastname: Chadha
mesh_terms: D000135:Acid Phosphatase / Q000097:blood; D000818:Animals; D063646:Carcinogenesis; D002273:Carcinogens; D004195:Disease Models, Animal; D004586:Electrophoresis; D018120:Finasteride / Q000008:administration & dosage* / Q000493:pharmacokinetics; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D008297:Male; D008770:Methylnitrosourea / Q000737:chemistry; D011467:Prostate / Q000000981:diagnostic imaging; D011471:Prostatic Neoplasms / Q000000981:diagnostic imaging*; D019275:Radiopharmaceuticals / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D013667:Technetium / Q000737:chemistry*; D013997:Time Factors; D014018:Tissue Distribution
chemical_list: D002273:Carcinogens; D019275:Radiopharmaceuticals; D018120:Finasteride; D008770:Methylnitrosourea; D013667:Technetium; D000135:Acid Phosphatase; C428439:prostatic acid phosphatase
keywords: animal model; imaging; prostate cancer; radionuclide; radiopharmaceuticals