Feasibility study for production and quality control of Yb-175 as a byproduct of no carrier added Lu-177 preparation for radiolabeling of DOTMP

Australas Phys Eng Sci Med. 2018 Mar;41(1):69-79. doi: 10.1007/s13246-017-0611-x. Epub 2017 Dec 19.

Abstract

Skeletal uptake of β- emitters of DOTMP complexes is used for the bone pain palliation. In this study, two moderate energy β- emitters, 177Lu (T1/2 = 6.7 days, Eβmax = 497 keV) and 175Yb (T1/2 = 4.2 days, Eβmax = 480 keV), are considered as potential agents for the development of the bone-seeking radiopharmaceuticals. Since the specific activity of the radiolabelled carrier molecules should be high, the non-carrier-added (NCA) radionuclides have an effective role in nuclear medicine. Many researchers have presented the synthesis of NCA 177Lu. Among these separation techniques, extraction chromatography has been considered more capable than other methods. In this study, a new approach, in addition to production of NCA 177Lu by EXC procedure is using pure 175Yb that was usually considered as a waste material in this method but because of high radionuclidic purity of 175Yb produced by this method we used it for radiolabeling as well as NCA 177Lu. To obtain optimum conditions, some effective factors on separation of Lu/Yb by EXC were investigated. The NCA 177Lu and pure 175Yb were produced with radionuclidic purity of 99.99 and 99.97% respectively by irradiation of enriched 176Yb target in thermal neutron flux of 5 × 1013 n/cm2 s for 14 days. 177Lu-DOTMP and 175Yb-DOTMP were obtained with high radiochemical purities (> 95%) under optimized reaction conditions. Two radiolabeled complexes exhibited excellent stability at room temperature. Biodistribution studies in rats showed favorable selective skeletal uptake with rapid clearance from blood along with insignificant accumulation of activity in other non-target organs for two radiolabelled complexes.

Keywords: 177Lu; DOTMP; Extraction chromatography; No carrier added.

MeSH terms

  • Animals
  • Chromatography
  • Feasibility Studies
  • Ligands
  • Molecular Weight
  • Organometallic Compounds / chemistry*
  • Quality Control
  • Radioisotopes / chemistry*
  • Radiopharmaceuticals / chemistry*
  • Rats, Wistar
  • Rheology
  • Temperature
  • Tissue Distribution
  • Ytterbium / chemistry*

Substances

  • 177Lu-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrakis(methylenephosphonic acid)
  • Ligands
  • Organometallic Compounds
  • Radioisotopes
  • Radiopharmaceuticals
  • Ytterbium-175
  • Ytterbium