Das Tapas, Chakraborty Sudipta, Sarma Haladhar D, Venkatesh Meera, Banerjee Sharmila
Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai, India.
Cancer Biother Radiopharm. 2009 Feb;24(1):7-14. doi: 10.1089/cbr.2008.0545.
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.
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.
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.
166Ho-HA exhibited promising features as an agent for liver cancer therapy in preliminary studies and warrants further investigation
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。
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。
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。
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。