Development and quality control studies of radiolabelled nanostructured lipid formulations with Ga-68

IF 2.1 3区工程技术 Q3 CHEMISTRY, INORGANIC & NUCLEAR

Applied Radiation and Isotopes Pub Date : 2026-04-01 Epub Date: 2026-01-20 DOI:10.1016/j.apradiso.2026.112453

Emine Selin Demi̇r, Evren Atlıhan Gündoğdu, Emre Özgenç

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引用次数: 0

Abstract

Objective

This study aims to radiolabel a nanoparticle formulation containing donepezil with Ga-68 radionuclide with high efficiency for diagnosing Alzheimer's disease. In order to develop lipid carrier systems with biocompatible contents in nanoparticle structures, extensive formulation studies were conducted. These systems were subsequently radiolabeled with Ga-68 radionuclide to evaluate their radiolabeling efficiencies. The results are highly encouraging, suggesting that effective radiolabeling is indeed possible. These findings are particularly significant as they open up a range of applications for targeted drug delivery, medical imaging, and diagnostics. Overall, this study represents a valuable contribution to the expanding body of knowledge on lipid carrier systems in healthcare.

Material and method

Nanocarrier formulations were prepared. The radiolabeling parameters of the prepared formulations were studied comparatively. A Ga-68 radionuclide with a half-life of 68 min was used for this. Incubation time, amount of radioactivity, and pH parameters were studied.

Results and discussion

The radiolabeling incubation time, pH of the experimental medium, and amount of radioactivity were tested, and the optimal parameters were identified. According to the results of the radiolabeling studies, optimal radiolabeling with Ga-68 radionuclide was obtained in an acid medium (pH: 5), with a 60 min incubation time, and using 5 mCi of activity in the DOTA-functionalized nanolipid formulations, achieving 89.17 % efficiency. Furthermore, quantitative in vivo PET/CT imaging in nude mice (n = 3/group) demonstrated that the optimized Ga-68-DNP-NLC formulation achieved statistically significant and higher brain uptake compared to the free Ga-68 control, confirming its ability to cross the blood-brain barrier.

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Ga-68放射性标记纳米结构脂质制剂的研制与质量控制研究。

目的：利用Ga-68核素对多奈哌齐纳米颗粒制剂进行放射性标记，对阿尔茨海默病进行高效诊断。为了开发在纳米颗粒结构中具有生物相容性的脂质载体系统，进行了广泛的配方研究。随后用Ga-68放射性核素对这些系统进行放射性标记，以评估其放射性标记效率。结果非常令人鼓舞，表明有效的放射性标签确实是可能的。这些发现尤其重要，因为它们为靶向药物输送、医学成像和诊断开辟了一系列应用。总的来说，这项研究代表了一个有价值的贡献，以扩大知识体脂质载体系统在医疗保健。材料与方法：制备纳米载体。比较研究了各制剂的放射性标记参数。使用了半衰期为68分钟的Ga-68放射性核素。对孵育时间、放射线量和pH参数进行了研究。结果与讨论：测试了放射性标记的孵育时间、实验介质的pH、放射性的量，并确定了最佳参数。根据放射性标记研究的结果，Ga-68放射性核素在酸性介质（pH: 5）中获得最佳放射性标记，孵育时间为60 min，在dota功能化纳米脂制剂中使用5 mCi的活性，效率为89.17%。此外，裸鼠体内定量PET/CT成像（n = 3/组）表明，优化后的Ga-68- dnp - nlc配方与游离Ga-68对照相比，具有统计学意义和更高的脑摄取，证实了其穿越血脑屏障的能力。

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.