Background: Radionuclide therapy (RNT) has become a very important treatment modality for cancer nowadays. Comparing with other cancer treatment options, sufficient efficacy could be achieved in RNT with lower toxicity. β⁻ emitters are frequently used in RNT due to the long tissue penetration depth of the β⁻ particles. The dysprosium-166/holmium-166 (¹⁶⁶Dy/¹⁶⁶Ho) in vivo generator shows great potential for treating large malignancies due to the long half-life time of the mother nuclide ¹⁶⁶Dy and the emission of high energy β⁻ from the daughter nuclide ¹⁶⁶Ho. However, the internal conversion occurring after β⁻ decay from ¹⁶⁶Dy to ¹⁶⁶Ho could cause the release of about 72% of ¹⁶⁶Ho when ¹⁶⁶Dy is bound to conventional chelators. The aim of this study is to develop a nanoparticle based carrier for ¹⁶⁶Dy/¹⁶⁶Ho in vivo generator such that the loss of the daughter nuclide ¹⁶⁶Ho induced by internal conversion is prevented. To achieve this goal, we radiolabelled platinum-gold bimetallic nanoparticles (PtAuNPs) and core–shell structured gold nanoparticles (AuNPs) with ¹⁶⁶Dy and studied the retention of both ¹⁶⁶Dy and ¹⁶⁶Ho under various conditions. Results: The ¹⁶⁶Dy was co-reduced with gold and platinum precursor to form the ¹⁶⁶DyAu@AuNPs and ¹⁶⁶DyPtAuNPs. The ¹⁶⁶Dy radiolabelling efficiency was determined to be 60% and 70% for the two types of nanoparticles respectively. The retention of ¹⁶⁶Dy and ¹⁶⁶Ho were tested in MiliQ water or 2.5 mM DTPA for a period of 72 h. In both cases, more than 90% of both ¹⁶⁶Dy and ¹⁶⁶Ho was retained. The results show that the incorporation of ¹⁶⁶Dy in AuNPs can prevent the escape of ¹⁶⁶Ho released due to internal conversion. Conclusion: We developed a chelator-free radiolabelling method for ¹⁶⁶Dy with good radiolabelling efficiency and very high stability and retention of the daughter nuclide ¹⁶⁶Ho. The results from this study indicate that to avoid the loss of the daughter radionuclides by internal conversion, carriers composed of electron-rich materials should be used.

In this work, ^177mLu has been produced by irradiation of natural Lu₂O₃ targets at the BR2 reactor (Mol, Belgium) and the obtained data together with literature values have been used to theoretically investigate the production of ^177mLu at different neutron fluxes, irradiation times and enrichment of ¹⁷⁶Lu. The irradiation time (t_max) needed to reach the maximum ^177mLu production has been found to change from 42, 12, 4 days with the increase in the thermal neutron flux from 2*10¹⁴, 8*10¹⁴, 2.5*10¹⁵ n cm⁻² s⁻¹, respectively while keeping the maximum ^177mLu activity unaffected. The results of our calculations suggest that 0.11 TBq ^177mLu with a specific activity of 0.3 TBq g⁻¹ Lu can be produced in a short irradiation time of 4 days using 1g of 84.44% ¹⁷⁶Lu enriched Lu₂O₃ and a thermal neutron flux of 2.5*10¹⁵ n cm⁻² s⁻¹.