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[F]AlF-NOTA-帕米膦酸的制备、优化及体外评估用于骨骼成像 PET。

Preparation, Optimisation, and In Vitro Evaluation of [F]AlF-NOTA-Pamidronic Acid for Bone Imaging PET.

机构信息

Centre for Diagnostic Nuclear Imaging, Universiti Putra Malaysia (UPM), Serdang 43400, Malaysia.

Department of Pharmacy Practice, Faculty of Pharmacy, Universiti Teknologi MARA, Bandar Puncak Alam 42300, Malaysia.

出版信息

Molecules. 2022 Nov 17;27(22):7969. doi: 10.3390/molecules27227969.

DOI:10.3390/molecules27227969
PMID:36432069
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9696850/
Abstract

[F]sodium fluoride ([F]NaF) is recognised to be superior to [mTc]-methyl diphosphate ([Tc]Tc-MDP) and ([F]FDG) in bone imaging. However, there is concern that [F]NaF uptake is not cancer-specific, leading to a higher number of false-positive interpretations. Therefore, in this work, [F]AlF-NOTA-pamidronic acid was prepared, optimised, and tested for its in vitro uptake. NOTA-pamidronic acid was prepared by an Hydroxysuccinimide (NHS) ester strategy and validated by liquid chromatography-mass spectrometry analysis (LC-MS/MS). Radiolabeling of [F]AlF-NOTA-pamidronic acid was optimised, and it was ensured that all quality control analysis requirements for the radiopharmaceuticals were met prior to the in vitro cell uptake studies. NOTA-pamidronic acid was successfully prepared and radiolabeled with F. The radiolabel was prepared in a 1:1 molar ratio of aluminium chloride (AlCl) to NOTA-pamidronic acid and heated at 100 °C for 15 min in the presence of 50% ethanol (/), which proved to be optimal. The preliminary in vitro results of the binding of the hydroxyapatite showed that [F]AlF-NOTA-pamidronic acid was as sensitive as [F]sodium fluoride ([F]NaF). Normal human osteoblast cell lines (hFOB 1.19) and human osteosarcoma cell lines (Saos-2) were used for the in vitro cellular uptake studies. It was found that [F]NaF was higher in both cell lines, but [F]AlF-NOTA-pamidronic acid showed promising cellular uptake in Saos-2. The preliminary results suggest that further preclinical studies of [F]AlF-NOTA-pamidronic acid are needed before it is transferred to clinical research.

摘要

氟[化]钠（[F]NaF）在骨成像方面被认为优于[锝]-甲基二膦酸盐（[Tc]Tc-MDP）和[氟]脱氧葡萄糖（[F]FDG）。然而，人们担心[F]NaF 的摄取不是癌症特异性的，导致更多的假阳性解释。因此，在这项工作中，[F]AlF-NOTA-帕米膦酸被制备、优化，并测试其体外摄取。NOTA-帕米膦酸通过 NHS 酯策略制备，并通过液相色谱-质谱分析（LC-MS/MS）进行验证。[F]AlF-NOTA-帕米膦酸的放射性标记进行了优化，并确保在进行体外细胞摄取研究之前满足放射性药物的所有质量控制分析要求。成功地用 F 对[F]AlF-NOTA-帕米膦酸进行了放射性标记。在存在 50%乙醇（/）的情况下，将氯化铝（AlCl）和 NOTA-帕米膦酸以 1:1 的摩尔比加热至 100°C 15 分钟，证明这是最佳条件。对羟磷灰石结合的初步体外结果表明，[F]AlF-NOTA-帕米膦酸与[F]氟[化]钠（[F]NaF）一样敏感。正常人类成骨细胞系（hFOB 1.19）和人类骨肉瘤细胞系（Saos-2）用于体外细胞摄取研究。结果发现，[F]NaF 在两种细胞系中的摄取均较高，但[F]AlF-NOTA-帕米膦酸在 Saos-2 中显示出有前途的细胞摄取。初步结果表明，在将[F]AlF-NOTA-帕米膦酸转移到临床研究之前，需要进行进一步的临床前研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8516/9696850/ab38fa26deaf/molecules-27-07969-g016.jpg
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