Design and Challenges of Radiopharmaceuticals
Section snippets
Radiopharmaceutical: General Concept
As the name suggests, a radiopharmaceutical is both a pharmaceutical and radioactive. The radioactive label is used either diagnostically as an emitter of electromagnetic radiation (gamma or X-rays), of which detection allows to quantify the concentration of the radiopharmaceutical. Alternatively, the radiolabel can be used for therapeutic applications where the ionizing radiation emitted upon decay of the radionuclide is used to destroy cells. The in vivo distribution of the radionuclide in
Basic Requirements
When a tracer is administered, the general pharmacokinetic principles of distribution, metabolism, and excretion apply.87 Most radiopharmaceuticals are administered intravenously and thus absorption can be neglected.
The radiopharmaceutical will be distributed over the body with the bloodstream and accumulate in the target tissue as a result of the specific interaction of the vector with its target. At the same time the radiopharmaceutical will be cleared from plasma so that the
Production
The production of a radiopharmaceutical consists of (a) production of the radionuclide (b) incorporation of the radionuclide in the radiopharmaceutical and (c) purification and reformulation (Fig. 7). For diagnostic radiopharmaceuticals, the production time should be as short as possible to avoid loss of activity due to decay during the production process.
Radionuclides are generally obtained from a nuclear reactor (generally β− emitters for radionuclide therapy), a cyclotron (generally β+
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