Abstract
Chlorambucil (CLB) is an aromatic nitrogen mustard and an alkylating agent. It has been mainly used in the chemotherapy.A method for radiopharmaceutical preparation of [ 125 I]iodo-Chlorambucila potential cancer therapeutic agent is described. The method is based on direct electrophilic radioiodination of Chlorambucil with [ 125 I] in the presence of chloramine-T (CAT) as oxidizing agent. The reaction conditions were optimized in order to obtain a radiochemical yield higher than 98% of [ 125 I]-iodo chlorambucil.Different chromatographic techniques (electrophoresis, and high pressure liquid chromatography (HPLC)) were used to evaluate the radiochemical yield and purity of the labeled product. Biodistribution studies of 125 I-chlorambucil were carried out in both normal and tumor bearing Albino Swiss mice. The results revealed that this new tracer, 125 I-chlorambucil, has a high affinity to be localized in the tumor site for a long period which indicates the specificity of this tracer to the tumor cells. The results indicate the possibility of using [ 125 I]iodochlorambucilfor imaging and treatment of cancer.
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