%0 Journal Article
%T Preparation of 99mTc-Clomiphene Citrate as a Novel Agent for Breast Cancer Imaging
%A Ismail Taha Ibrahim
%A Mohamed Taha Elkolally
%A Ibrahim Yousof Abd Elgany
%A Ahmed Abd Albary
%A Mohamed Hodhod Elsayed
%J ISRN Oncology
%D 2012
%R 10.5402/2012/581281
%X The aim of this work was to develop a novel 99mTc-labelled derivative based on triphenylethylene for breast cancer imaging. 99mTc-Clomiphene was obtained with a radiochemical yield of 94.4% by adding 99mTc to 1.5£¿mg Clomiphene citrate in the presence of 10£¿¦Ìg SnCl2 at pH 7. The optimization of the labeling yield of Clomiphene citrate, with 99mTc, is described. The reaction parameters that affect the labeling yield were studied to optimize the labeling conditions. Radiochemical purity of the final product has been verified by means of paper chromatography and paper electrophoresis. Ehrlich Ascites Carcinoma (EAC) as a model of breast cancer cells was injected intraperitoneally (IP) to produce ascites and intramuscularly (IM) to produce solid tumor. Biodistribution study was carried out by the injecting solution of 99mTc-Clomiphene in normal and tumor bearing mice. The uptake in ascites was over 12.5 % injected dose per gram tissue body weight, at 1hr after injection and above 12% in solid tumor. The T/NT value for 99mTc-Clomiphene complex was found to be which was higher than that of the commercially available 99mTc-MIBI. This data revealed the localization of tracer in tumor tissue with high percent sufficient to use 99mTc-Clomiphene as a promising tool for the diagnosis of breast cancer. 1. Introduction The diagnosis of breast cancer is based on physical examination supported by mammography and fine-needle aspiration cytology or core biopsy. The increasing use of MRI and especially ultrasonography has improved diagnostic accuracy but there is still a need for additional diagnostic methods. One of the diagnostic tools to confirm or exclude breast cancer is scintimammography. Various radiopharmaceuticals were used in detecting that breast cancer 99mTc-sestamibi (MIBI) is the most popular agent [1, 2]. But 99mTc-MIBI blood clearance is known to be very rapid, with a half-life of only a few minutes [3]. Clinical in vivo studies also have established significant correlations between 99mTc-sestamibi efflux from tumors and P-glycoprotein (P-gp) expression in cancer patients [4, 5]. High levels of P-gp in tumor may indeed cause rapid washout of MIBI, decreasing the net cellular uptake of the tracer [6]. Tumor models have shown low tumor-to-muscle ratios (1£¿:£¿1) for all studied cations, including 99mTc-MIBI [7]. Therefore, there is an urgent need for a radio pharmaceutical product which can be prepared in house with a simple and rapid procedure. In addition should accumulate in cancer cells at a high concentration to give high target-to-nontarget ratios to give
%U http://www.hindawi.com/journals/isrn.oncology/2012/581281/