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RISS 인기검색어
- 검색키워드
- 저자 : Nadeem Ahmed Lodhi (검색결과 2 건)
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Lodhi, Nadeem Ahmed,Park, Ji Yong,Kim, Kyuwan,Kim, Young Joo,Shin, Jae Hwan,Lee, Yun-Sang,Im, Hyung-Jun,Jeong, Jae Min,Khalid, Muhammad,Cheon, Gi Jeong,Lee, Dong Soo,Kang, Keon Wook American Chemical Society 2019 MOLECULAR PHARMACEUTICS Vol.16 No.4
<P>Technetium-99m-labeled human serum albumin (<SUP>99m</SUP>Tc-HSA) has been utilized as a blood pool imaging agent in the clinic for several decades. However, <SUP>99m</SUP>Tc-HSA has a short circulation time, which is a critical shortcoming for a blood pool imaging agent. Herein, we developed a novel <SUP>99m</SUP>Tc-labeled HSA with a long circulation time using click chemistry and a chelator, 2,2′-dipicolylamine (DPA), (<SUP>99m</SUP>Tc-DPA-HSA). Specifically, we examined the feasibility of copper-free strain-promoted alkyne-azide cycloaddition (SPAAC) for the incorporation of HSA to the [<SUP>99m</SUP>Tc (CO)<SUB>3</SUB>(H<SUB>2</SUB>O)<SUB>3</SUB>]<SUP>+</SUP> system by adopting a chelate-then-click approach. In this strategy, a potent chelate system, azide-functionalized DPA, was first complexed with [<SUP>99m</SUP>Tc (CO)<SUB>3</SUB>(H<SUB>2</SUB>O)<SUB>3</SUB>]<SUP>+</SUP>, followed by the SPAAC click reaction with azadibenzocyclooctyne-functionalized HSA (ADIBO-HSA) under biocompatible conditions. Radiolabeling efficiency of azide-functionalized DPA (<SUP>99m</SUP>Tc-DPA) was >98%. Click conjugation efficiency of <SUP>99m</SUP>Tc-DPA with ADIBO-HSA was between 76 and 99% depending on the number of ADIBO moieties attached to HSA. In whole-body in vivo single photon emission computed tomography images, the blood pool uptakes of <SUP>99m</SUP>Tc-DPA-HSA were significantly enhanced compared to those of <SUP>99m</SUP>Tc-HSA at 10 min, 2, and 6 h after the injection (<I>P</I> < 0.001, 0.025, and 0.003, respectively). Furthermore, the blood activities of <SUP>99m</SUP>Tc-DPA-HSA were 8 times higher at 30 min and 10 times higher at 3 h after the injection compared to those of conventional <SUP>99m</SUP>Tc-HSA in ex vivo biodistribution experiment. The results exhibit the potential of <SUP>99m</SUP>Tc-DPA-HSA as a blood pool imaging agent and further illustrate the promise of the pre-labeling SPAAC approach for conjugation of heat-sensitive biological targeting vectors with [<SUP>99m</SUP>Tc (CO)<SUB>3</SUB>(H<SUB>2</SUB>O)<SUB>3</SUB>]<SUP>+</SUP>.</P> [FIG OMISSION]</BR>
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Indigenous Radiosynthesis of [131I]Iodobenzylguanidine ([131I]mIBG) for Neuroblastoma Imaging
Nadeem Ahmed Lodhi,Muhammad Irfan,Muhammad Nasir Saddique,Kahkshan Bashir Mir,Naseer Ahmed,Shazia Fatima,Mumtaz Khan,Muhammad Wasim,Samina Roohi 대한방사성의약품학회 2022 Journal of radiopharmaceuticals and molecular prob Vol.8 No.2
Indigenous diagnostic dose of 131I-labeled meta-iodobenzylguanidine ([131I]mIBG) was prepared via Cu+ catalyzed isotope exchange reaction generated in situ by sodium metabisulfite for imaging of neuroblastoma tumor. [131I]mIBG was produced in overall 85-90% radiochemical yield. The average amount of radioactivity of [131I]mIBG was 2164 MBq (1998-2331MBq) with an average specific activity > 1000 MBq/mg at the end of synthesis. The radiochemical purity was ≥ 99.9% after purification through Dowex-1 × 8 ion exchange resin (100-150 mesh) at the date of preparation. The stability of [131I]mIBG at concentration 480-555 MBq/mL was > 97% at 4 °C after 4 days. The room temperature (25 °C) stability of [131I]mIBG was > 98% after 24 h. Biodistribution of [131I]mIBG in patient showed uptake in salivary glands, liver, spleen and excreted though urinary bladder. Neuroendocrine medicated uptake into tumor lesion and metastatic sites were noted which strongly correlate with the morphological abnormalities of patient.
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