Direct radiolabeling of Folate with Tc-99m using QbD approach: A step closer to folate based diagnostic agent

IF 1.6 3区工程技术 Q3 CHEMISTRY, INORGANIC & NUCLEAR

Applied Radiation and Isotopes Pub Date : 2024-08-27 DOI:10.1016/j.apradiso.2024.111484

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引用次数: 0

Abstract

The aim of the presented work was to develop folate based radiolabeled compound intended to be used as diagnostic aid for the various folate-receptor overexpressing cancers eg. breast cancer, brain tumors, lung cancer etc. Folate was directly radiolabeled with Tc-99m using Quality-by-Design and encapsulated in micellar nanocarriers. The authors are of the view that the stable radiolabeled folate could be of potential diagnostic value in cancers overexpressing folate receptors thereby opening novel possibilities to diagnostic applications of radiolabeled folate.

Summary for technical notes

Folic acid was directly radiolabeled with Tc-99m utilizing a quality by design approach. The experimental trials were designed using the Box-Behenken design with the concentration of drug, concentration of reducing agent and the incubation time as dependent variable and percent radiolabeling as the response for the same. The applied design in the method section was validated with a series of experiments and the percent labeling of the FA with Tc-99m was found to be around 94%. The radiolabeled compound was imperilled to stability evaluation by incubating the same with serum and physiological pH and the same was found to be stable at the end of 4h. On subjecting to DTPA challenge test, the compound displayed no change in the radiolabeling percentage thereby indicating the robustness of the formed Tc-99m-FA complex, The radiolabeled Tc-99m-FA was further encapsulated into micellar nanocarriers and the same were also found to be robust and stable.

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利用 QbD 方法用锝-99m 直接放射性标记叶酸：向叶酸诊断试剂迈进了一步

这项研究的目的是开发叶酸放射性标记化合物，用于诊断各种叶酸受体过度表达的癌症，如乳腺癌、脑瘤、肺癌等。叶酸通过质量控制设计（Quality-by-Design）直接用锝-99m进行放射性标记，并封装在胶束纳米载体中。作者认为，稳定的放射性标记叶酸对过度表达叶酸受体的癌症具有潜在的诊断价值，从而为放射性标记叶酸的诊断应用提供了新的可能性。实验设计采用 Box-Behenken 设计，以药物浓度、还原剂浓度和培养时间为因变量，以放射性标记百分比为响应变量。通过一系列实验验证了方法部分所采用的设计，发现锝-99m 对 FA 的标记率约为 94%。通过将放射性标记的化合物与血清和生理 pH 培养，对其稳定性进行了评估，结果发现该化合物在 4 小时后保持稳定。放射性标记的 Tc-99m-FA 复合物被进一步封装到胶束纳米载体中，结果发现其同样坚固稳定。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Applied Radiation and Isotopes 工程技术-核科学技术

CiteScore

3.00

自引率

12.50%

发文量

406

审稿时长

13.5 months

期刊介绍： Applied Radiation and Isotopes provides a high quality medium for the publication of substantial, original and scientific and technological papers on the development and peaceful application of nuclear, radiation and radionuclide techniques in chemistry, physics, biochemistry, biology, medicine, security, engineering and in the earth, planetary and environmental sciences, all including dosimetry. Nuclear techniques are defined in the broadest sense and both experimental and theoretical papers are welcome. They include the development and use of α- and β-particles, X-rays and γ-rays, neutrons and other nuclear particles and radiations from all sources, including radionuclides, synchrotron sources, cyclotrons and reactors and from the natural environment. The journal aims to publish papers with significance to an international audience, containing substantial novelty and scientific impact. The Editors reserve the rights to reject, with or without external review, papers that do not meet these criteria. Papers dealing with radiation processing, i.e., where radiation is used to bring about a biological, chemical or physical change in a material, should be directed to our sister journal Radiation Physics and Chemistry.