Abstract Targeted drug delivery system can reduce the side effects of high drug concentration by improving drug pharmacokinetics at lower doses. Citrate-gold nanoparticles (AuNPs) as a drug delivery system were synthesized via green nanotechnology technique to be used as a new imaging platform for tumor targeting. Citrate-AuNPs were synthesized with core size of 10 nm. Citrate-AuNPs were labeled with technetium-99m (99mTc) with radiochemical yield of 95.20 ± 2.70% with good in-vitro stability in both saline and human serum and well in-vivo studied in both normal and solid tumor bearing mice. The in-vivo biodistribution study of [99mTc]Tc-citrate-AuNPs in solid tumor bearing mice (as preliminary study) showed a high accumulation in tumor site with tumor/muscle of 4.35 ± 0.22 after 30 min post injection. The direct intratumoral (I.T) injection of [99mTc]Tc-citrate-AuNPs showed that this complex was retained in the tumor up to 77.86 ± 1.90 % at 5 min and still around 50.00 ± 1.42 % after 30 min post injection (p.i.). The newly presented nano-platform could be presented as a new potential radiopharmaceutical tumor imaging probe.

中文翻译：

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99mTc-柠檬酸金纳米粒子作为肿瘤示踪剂：合成、表征、放射性标记和体内研究

摘要 靶向给药系统可以通过在较低剂量下改善药物的药代动力学来减少高药物浓度的副作用。柠檬酸-金纳米粒子 (AuNPs) 作为药物递送系统通过绿色纳米技术技术合成，用作肿瘤靶向的新成像平台。柠檬酸盐-AuNPs 合成的核心尺寸为 10 nm。柠檬酸盐-AuNPs 用锝-99m (99mTc) 标记，放射化学产率为 95.20 ± 2.70%，在盐水和人血清中具有良好的体外稳定性，并且在正常和携带实体瘤的小鼠中进行了良好的体内研究。[99mTc]Tc-柠檬酸-AuNPs 在携带实体瘤的小鼠中的体内生物分布研究（作为初步研究）显示，在注射后 30 分钟后，肿瘤部位的肿瘤/肌肉的高积累为 4.35 ± 0.22。直接瘤内（I. T) [99mTc]Tc-柠檬酸盐-AuNPs 的注射表明，该复合物在 5 分钟时保留在肿瘤中高达 77.86 ± 1.90 %，并且在注射后 (pi) 30 分钟后仍保留在 50.00 ± 1.42 % 左右。新推出的纳米平台可以作为一种新的潜在放射性药物肿瘤成像探针。