Haller Stephanie, Ametamey Simon M, Schibli Roger, Müller Cristina
Center for Radiopharmaceutical Sciences ETH-PSI-USZ, Paul Scherrer Institute, Villigen-PSI, Switzerland.
Department of Chemistry and Applied Biosciences, ETH Zurich, Zurich, Switzerland.
Nucl Med Biol. 2015 Mar;42(3):226-33. doi: 10.1016/j.nucmedbio.2014.10.010. Epub 2014 Oct 28.
The chick embryo is an emerging in vivo model in several areas of pre-clinical research including radiopharmaceutical sciences. Herein, it was evaluated as a potential test system for assessing the biodistribution and in vivo stability of radiopharmaceuticals. For this purpose, a number of radiopharmaceuticals labeled with (18)F, (125)I, (99m)Tc, and (177)Lu were investigated in the chick embryo and compared with the data obtained in mice.
Chick embryos were cultivated ex ovo for 17-19 days before application of the radiopharmaceutical directly into the peritoneum or intravenously using a vein of the chorioallantoic membrane (CAM). At a defined time point after application of radioactivity, the embryos were euthanized by shock-freezing using liquid nitrogen. Afterwards they were separated from residual egg components for post mortem imaging purposes using positron emission tomography (PET) or single photon emission computed tomography (SPECT).
SPECT images revealed uptake of [(99m)Tc]pertechnetate and [(125)I]iodide in the thyroid of chick embryos and mice, whereas [(177)Lu]lutetium, [(18)F]fluoride and [(99m)Tc]-methylene diphosphonate ([(99m)Tc]-MDP) were accumulated in the bones. [(99m)Tc]-dimercaptosuccinic acid ((99m)Tc-DMSA) and the somatostatin analog [(177)Lu]-DOTATOC, as well as the folic acid derivative [(177)Lu]-DOTA-folate showed accumulation in the renal tissue whereas [(99m)Tc]-mebrofenin accumulated in the gall bladder and intestine of both species. In vivo dehalogenation of [(18)F]fallypride and of the folic acid derivative [(125)I]iodo-tyrosine-folate was observed in both species. In contrast, the 3'-aza-2'-[(18)F]fluorofolic acid ([(18)F]-AzaFol) was stable in the chick embryo as well as in the mouse.
Our results revealed the same tissue distribution profile and in vivo stability of radiopharmaceuticals in the chick embryo and the mouse. This observation is promising with regard to a potential use of the chick embryo as an inexpensive and simple test model for preclinical screening of novel radiopharmaceuticals.
鸡胚是临床前研究多个领域中新兴的体内模型,包括放射性药物科学。在此,对其作为评估放射性药物生物分布和体内稳定性的潜在测试系统进行了评估。为此,在鸡胚中研究了多种用(18)F、(125)I、(99m)Tc和(177)Lu标记的放射性药物,并与在小鼠中获得的数据进行了比较。
在将放射性药物直接注入腹膜或通过绒毛尿囊膜(CAM)静脉内给药之前,将鸡胚在体外培养17 - 19天。在给予放射性物质后的特定时间点,使用液氮将胚胎速冻处死。之后,将它们与残留的卵成分分离,以便使用正电子发射断层扫描(PET)或单光子发射计算机断层扫描(SPECT)进行死后成像。
SPECT图像显示,鸡胚和小鼠的甲状腺中摄取了高锝酸盐[(99m)Tc]和碘化物[(125)I],而镥[(177)Lu]、氟化物[(18)F]和亚甲基二膦酸盐[(99m)Tc] - MDP[(99m)Tc - MDP]则在骨骼中积累。二巯基丁二酸[(99m)Tc] - DMSA和生长抑素类似物[(177)Lu] - DOTATOC,以及叶酸衍生物[(177)Lu] - DOTA - 叶酸在肾组织中积累,而[(99m)Tc] - 美罗芬宁在两种动物的胆囊和肠道中积累。在两种动物中均观察到了氟哌利多[(18)F]和叶酸衍生物碘酪氨酸 - 叶酸[(125)I]的体内脱卤作用。相比之下,3'-氮杂 - 2'-[(18)F]氟叶酸[(18)F] - AzaFol在鸡胚和小鼠中均稳定。
我们的结果揭示了放射性药物在鸡胚和小鼠中的相同组织分布特征和体内稳定性。这一观察结果对于将鸡胚作为一种廉价且简单的新型放射性药物临床前筛选测试模型的潜在应用具有前景。