Preparation and in vitro/in vivo property evaluations of&nbsp; 68 Ga-radiolabeled tetrazine probe&nbsp; 68 Ga-NOTA-Tz

ZHANG Fengsheng; WANG Nian; SONG Shaoli; YANG Hong; WANG Mingwei

doi:10.19732/j.cnki.2096-6210.2023.05.008

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Preparation and in vitro/in vivo property evaluations of ⁶⁸ Ga-radiolabeled tetrazine probe ⁶⁸Ga-NOTA-Tz

更新时间：2025-12-15

- Preparation and in vitro/in vivo property evaluations of ⁶⁸ Ga-radiolabeled tetrazine probe ⁶⁸Ga-NOTA-Tz
- Vol. 32, Issue 5, Pages: 445-452(2023)
- 作者机构：
  
  上海师范大学化学与材料科学学院,上海,200234
- 作者简介：
- 基金信息：
- DOI：10.19732/j.cnki.2096-6210.2023.05.008
  CLC：
- Published Online：01 November 2023，
  
  Published：01 November 2023
- 稿件说明：
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张丰盛,王撵,宋少莉,等. ⁶⁸ Ga标记四嗪探针 ⁶⁸ Ga-NOTA-Tz的制备与体内外性质评价[J]. 肿瘤影像学, 2023, 32(5): 445-452 https://doi.

org/10.19732/j.cnki.2096-6210.2023.05.008
张丰盛,王撵,宋少莉,等. ⁶⁸ Ga标记四嗪探针 ⁶⁸ Ga-NOTA-Tz的制备与体内外性质评价[J]. 肿瘤影像学, 2023, 32(5): 445-452 https://doi. DOI： 10.19732/j.cnki.2096-6210.2023.05.008.

org/10.19732/j.cnki.2096-6210.2023.05.008 DOI：

摘要

目的：

探索一种

Ga标记四嗪探针（

Ga-NOTA-Tz）的优化标记条件，并评价其体内外性质。

方法：

开展

Ga-NOTA-Tz的标记条件优化实验，包括反应体系的pH值、温度、时间和前体用量等4种影响因素。利用放射性快速薄层色谱（Radio-iTLC）和放射性高效液相色谱（Radio-HPLC）测定

Ga-NOTA-Tz的标记率和体外稳定性，并进行脂水分配系数log

、血浆蛋白结合率、BALB/c正常鼠血液半衰期和生物分布、以及在SMMC-7721移植瘤模型MicroPET/CT显像等体内外性质评价。

结果：

根据优化实验结果，

Ga-NOTA-Tz最佳标记条件是反应体系pH=3.8、反应温度45 ℃、反应时间10 min、前体用量5 nmol，在此条件下其标记率大于95%。体外实验显示，

Ga-NOTA-Tz在生理盐水和胎牛血清中的稳定性分别保持在95%和90%以上（4 h内），其脂水分配系数log

为-2.06±0.02，血浆蛋白结合率为20%左右（1.5 h内）。血液半衰期实验表明，

Ga-NOTA-Tz的早期快速分布半衰期为1.1 min、终末缓慢清除半衰期为29.1 min。体内生物分布和肿瘤MicroPET/CT发现，

Ga-NOTA-Tz主要分布于肝、胆、肾脏和膀胱等代谢器官，对应的%ID/g均较高，同时在肿瘤组织均匀分布，0.5、1.0、1.5 h时的%ID/g

mean

分别为1.6±0.11、1.3±0.15和1.3±0.12，与肌肉和心脏的较为接近。

结论：

本研究优化建立了四嗪探针

Ga-NOTA-Tz的制备条件，其标记率高，具有良好的稳定性和亲水性，在体内能快速而均匀地分布至肿瘤组织，有利于其应用于基于体内生物正交点击反应的肿瘤预靶向PET/CT显像。

Abstract

Objective:

To explore the op

timal radiolabeling conditions of

Ga-labeled tetrazine probe (

Ga-NOTA-Tz)

and to evaluate it’s i

n vitro

and

in vivo

properties.

Methods:

The optimization experiments of the radiolabeling conditions of

Ga-NOTA- Tz were carried out

including 4 influencing factors such as pH

temperature

time and precursor amount. The radiolabeling efficiency and

in vitro

stability of

Ga-NOTA-Tz were determined by Radio-iTLC and Radio-HPLC and its lipid-water partition coefficient log

plasma protein binding ratio

blood half-life and biodistribution in normal BALB/c mice

as well as MicroPET/CT imaging in SMMC-7721 xenograft tumor mouse model were evaluated.

Results:

According to the results of optimization experiments

the optimized radiolabeling conditions of

Ga-NOTA-Tz were pH=3.8

temperature at 45℃

reaction time of 10 min

and precursor amount of 5.0 nmol and the radiolabeling efficiency under these conditions was above 95%.

In vitro

assays showed the stability of

Ga-NOTA-Tz in saline and fetal bovine serum remained above 95% and 90% within 4.0 h

respectively

its log

was -2.06±0.02，and the plasma protein binding rate was about 20% within 1.5 h. The blood half-life tests of

Ga-NOTA-Tz found the early rapid distribution half-life was 1.1 min and the terminal slow clearance half-life was 29.1 min.

In vivo

biodistribution and tumor MicroPET/CT imaging revealed that

Ga-NOTA-Tz was mainly distributed in metabolic organs such as liver

gallbladder

kidney and bladder with relatively high %ID/g

and was homogeneously distributed in tumor lesion with %ID/g

mean

of 1.6±0.11

1.3±0.15 and 1.3± 0.12 at 0.5

1.0 and 1.5 h

respectively

which were closer to those of muscle and heart.

Conclusion:

In this study

the radiolabeling conditions of

Ga-NOTA-Tz were optimized with high radiol

abeling efficiency

and it possessed good stability and hydrophilicity

and could rapidly and uniformly distributed into tumor lesion

in vivo

which could benefit for its application into tumor pretargeted PET/CT imaging based on

in vivo

bioorthogonal click reaction.

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Preparation and in vitro/in vivo property evaluations of 68 Ga-radiolabeled tetrazine probe 68 Ga-NOTA-Tz

DOI：10.19732/j.cnki.2096-6210.2023.05.008

摘要

Abstract

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Preparation and in vitro/in vivo property evaluations of ⁶⁸ Ga-radiolabeled tetrazine probe ⁶⁸Ga-NOTA-Tz