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166钬标记的羟基磷灰石颗粒:一种可能用于肝癌治疗的药物。

166Ho-labeled hydroxyapatite particles: a possible agent for liver cancer therapy.

作者信息

Das Tapas, Chakraborty Sudipta, Sarma Haladhar D, Venkatesh Meera, Banerjee Sharmila

机构信息

Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai, India.

出版信息

Cancer Biother Radiopharm. 2009 Feb;24(1):7-14. doi: 10.1089/cbr.2008.0545.

Abstract

PURPOSE

Intra-arterial administration of particulates labeled with -emitting radionuclides is one of the promising modalities for the treatment of liver cancer. 166Ho [T1/2=26.9 hours, E(max) = 1.85 MeV, Egamma = 81keV (6.4%)] could be envisioned as an attractive radionuclide for use in liver cancer therapy owing to its high energy emission, short half-life, and feasibility of its production with adequately high specific activity and radionuclidic purity. Hydroxyapatite (HA) particles in the size range of 20-60 micros were chosen as the particulate carrier due to their biocompatibility and ease of labeling with lanthanides.

METHODS

166Ho was produced by thermal neutron bombardment on a natural holmium target. HA particles of the desired size range were synthesized, characterized, and radiolabeled with 166Ho. The biologic behavior of166Ho-HA was tested in normal Wistar rats by carrying out biodistribution and imaging studies.

RESULTS

166Ho was produced with a specific activity of 5.55-6.48 TBq/g and radionuclidic purity of approximately 100%. HA particles were labeled with 166Ho with a high radiochemical purity of >99% and good in vitro stability up to 7 days. The biodistribution and imaging studies revealed satisfactory hepatic retention (approximately 89% of injected activity after 2 days) with insignificant uptake in any other major organ/tissue.

CONCLUSIONS

166Ho-HA exhibited promising features as an agent for liver cancer therapy in preliminary studies and warrants further investigation

摘要

目的

动脉内注射发射γ射线的放射性核素标记的微粒是治疗肝癌的一种有前景的方法。166Ho(半衰期T1/2 = 26.9小时,最大能量E(max) = 1.85 MeV,γ射线能量Egamma = 81keV(6.4%))因其高能量发射、短半衰期以及能够以足够高的比活度和放射性核素纯度进行生产,有望成为用于肝癌治疗的一种有吸引力的放射性核素。由于其生物相容性以及易于用镧系元素标记,选择了尺寸范围为20 - 60微米的羟基磷灰石(HA)颗粒作为微粒载体。

方法

通过热中子轰击天然钬靶产生166Ho。合成了所需尺寸范围的HA颗粒,对其进行表征并用166Ho进行放射性标记。通过进行生物分布和成像研究,在正常Wistar大鼠中测试了166Ho - HA的生物学行为。

结果

产生的166Ho比活度为5.55 - 6.48 TBq/g,放射性核素纯度约为100%。HA颗粒用166Ho标记,放射化学纯度>99%,体外稳定性良好,长达7天。生物分布和成像研究显示肝脏摄取良好(2天后约为注射活度的89%),在任何其他主要器官/组织中的摄取不显著。

结论

在初步研究中,166Ho - HA作为一种肝癌治疗药物表现出有前景的特性,值得进一步研究。

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