Separation of nuclear isomers for cancer therapeutic radionuclides based on nuclear decay after-effects

Abstract

177Lu has sprung as a promising radionuclide for targeted therapy. The low soft tissue penetration of its β− emission results in very efficient energy deposition in small-size tumours. Because of this, 177Lu is used in the treatment of neuroendocrine tumours and is also clinically approved for prostate cancer therapy. In this work, we report a separation method that achieves the challenging separation of the physically and chemically identical nuclear isomers, 177mLu and 177Lu. The separation method combines the nuclear after-effects of the nuclear decay, the use of a very stable chemical complex and a chromatographic separation. Based on this separation concept, a new type of radionuclide generator has been devised, in which the parent and the daughter radionuclides are the same elements. The 177mLu/177Lu radionuclide generator provides a new production route for the therapeutic radionuclide 177Lu and can bring significant growth in the research and development of 177Lu based pharmaceuticals.

<p>A Chelate-Free Nano-Platform for Incorporation of Diagnostic and Therapeutic Isotopes</p>

“…For [ 177 Lu] Lu-FH, the average RCY (n = 3) was 91 ± 0.7% with RCP of ≈ 95 ± 0.7% (Table 3 and Figure 3). For [ 64 Cu]Cu-FH, the Figure 3. The highest RCY was achieved by HV-HRR-HIR, ≈ 87.2 ± 1.2%.…”

“…There are two major physical processes that can affect the stability of chelate-based radio-agents: bond rupture and recoil effect. 64 Both of these processes result from nuclear decay of the radiolabeled isotope. Radioisotope decay that involves the production of isomeric daughter nuclides (with excited nucleus) results in internal conversion (following γ emission from nuclear de-excitation) that consequently leads to ejecting an inner electron (from K or M shells).…”

“…Previous HIR related studies used this technique to develop a diagnostic radiolabeled SPION using FH ([ 89 Zr]Zr 4+ , [ 64 Cu]Cu 2+ , [ 111 In]In 3+ ). [26][27][28][29] FH has been radiolabeled with zirconium-89 ([ 89 Zr]Zr-FH) and used to image monocyte infiltration as a way to assess inflammatory diseases since intravenously injected [ 89 Zr]Zr-FH showed enhanced uptake at the site of injury and in the draining lymph nodes.…”

“…29 HIR and surface click chemistry modification of FH also work cooperatively to provide a versatile nanoparticle platform for biomedical applications such as ex vivo cell labeling [27][28][29] and in vivo cell tracking including isolated B cells. 43 An aim of this study was to investigate the HIR reaction for a range of therapeutic metals and to extend the use of the HIR radiolabeling technique for the development of a therapeutic/ diagnostic FH platform (eg, [ 90 Y]Y-FH, [ 177 Lu]Lu-FH and [ 64,67 Cu]Cu-FH). A second aim was to further optimize the HIR technique to achieve higher radiochemical yield (RCY) for relatively short-lived isotopes (eg, copper-64).…”

Исследование Кинетических Параметров Схемы Лазерной Фотоионизации Лютеция

“…Недостатком второго метода является низкое сечение поглощения нейтронов. Использование лазерного фотоионизационного метода предоставляет возможность модифицировать изотопный состав природного лютеция, облученного в реакторе, осуществляя очистку от изомера при выделении 177 Lu и/или выделение изомера 177m Lu для дальнейшего использования в независимом генераторе 177 Lu [1]. Указанные возможности непосредственно вытекают из свойств трехступенчатой схемы фотоионизации лютеция: 5d6s 2 2 D 3/2 − −5d6s6p 4 F • 5/2 −5d6s7s 4 D 3/2 −(53375сm −1 ) • 1/2 , спектроскопия которой для различных изотопов детально исследована в работах [2,3].…”