Journal of Pharmaceutical Research International

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 [¹²⁵I]-iodo-Chlorambucil a potential cancer therapeutic agent is described. The method is based on direct electrophilic radioiodination of Chlorambucil with [¹²⁵I] 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 [¹²⁵I]-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 ¹²⁵I- chlorambucil were carried out in both normal and tumor bearing Albino Swiss mice. The results revealed that this new tracer, ¹²⁵I-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 [¹²⁵I]-iodo chlorambucil for imaging and treatment of cancer.