Physico-chemical characterisation and biological evaluation of 188-Rhenium colloids for radiosynovectomy.

Ma Ures, Eduardo Savio, Antonio Malanga, Marcelo Fernández, Andrea Paolino, Javier Gaudiano
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引用次数: 13

Abstract

BACKGROUND: Radiosynovectomy is a type of radiotherapy used to relieve pain and inflammation from rheumatoid arthritis. In this study, 188-Rhenium (188Re) colloids were characterized by physical and biological methodologies. This was used to assess which parameters of the kit formulation would be the basis in the development of a more effective radiopharmaceutical for synovectomy. Intraarticular injection in knees of rabbits assessed cavity leakage of activity. METHODS: The physical characteristics of tin (Sn) and sulphur (S) colloids were determined to assess the formulation with suitable properties. Particles were grouped in three ranges for analyzing their distribution according to their number, volume and surface. The ideal particle size range was considered to be from 2 to 10 microns. Membrane filtration and laser diffraction characterization methodologies were used. RESULTS: While membrane filtration could give misleading data, laser diffraction proportions more reliable results. The Sn colloid showed a better distribution of particle volume and surface than S colloid, in the 2 to 10 microns range. The 188Re-Sn colloid was obtained with a radiochemical purity higher than 95% after 30 minutes of autoclaving. While Sn colloid kit stability was verified for 60 days, the 188Re-Sn preparation was stable in the first 24 hrs. No significant intrabatch variability (n = 3) was detected. Biodistribution and scintigraphic studies in rabbits after intraarticular injection showed relevant activity only in knee, being 90% at 48 hours. CONCLUSION: The 188Re-Sn colloid is easy to prepare, is stable for 24 hours and shows minimal cavity leakage after intraarticular injection into rabbit knees, suggesting this radiotherapeutical agent has suitable physical properties for evaluation for joint treatment in humans.

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放射性滑膜切除术中188-铼胶体的物理化学特征和生物学评价。
背景:放射滑膜切除术是一种用于缓解风湿性关节炎疼痛和炎症的放射疗法。本研究采用物理和生物方法对188-铼(188Re)胶体进行表征。这被用来评估试剂盒配方的哪些参数将是开发更有效的滑膜切除术放射性药物的基础。兔膝关节关节内注射评估腔漏活动。方法:测定锡(Sn)和硫(S)胶体的物理特性,以确定合适的配方。根据颗粒的数量、体积和表面积将颗粒分为三个范围,分析颗粒的分布。理想的粒径范围被认为是从2到10微米。采用膜过滤和激光衍射表征方法。结果:膜过滤所得的数据有误导性,而激光衍射比法所得的结果更可靠。在2 ~ 10 μ m范围内,Sn胶体的颗粒体积和表面分布优于S胶体。经过30分钟的高压灭菌,获得了放射性化学纯度大于95%的188Re-Sn胶体。而锡胶体试剂盒的稳定性验证了60天,188Re-Sn制剂在前24小时是稳定的。未发现显著的批内变异(n = 3)。兔关节内注射后的生物分布和显像研究显示,相关活性仅在膝关节,48小时时为90%。结论:188Re-Sn胶体制备简单,24小时稳定,经兔膝关节内注射后腔漏最小,具有适合人体关节治疗评价的物理性能。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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