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Hydroxyapatite (HA) microparticles labeled with P-32 - A promising option in the radiation synovectomy for inflamed joints

机译:标记为P-32的羟基磷灰石(HA)微粒-放射性关节滑膜切除术治疗发炎关节的一种有前途的选择

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In the present article we describe a systematic approach pursued for the synthesis of P-32-labeled hydroxyapatite (HA) microparticles (1-10 mu m size range) using no carrier added (NCA) P-32 produced in a nuclear reactor and animal evaluation of its utility as an expected viable radiopharmaceutical for the treatment of pain intensive arthrosis. NCA P-32 was produced via the S-32(n,p)P-32 route in nuclear reactor with high radionuclidic purity (99.95 +/- 0.01%, n=5). Phosphorus-32-labeled hydroxyapatite micro particles (1-10 mu m size range) were synthesized with high radiochemical purity (99.0 +/- 0.3% n=12) under optimized conditions and the, formulation showed excellent in vitro stability in saline as well as in rat serum. Intra-articular administration of the radiolabeled particles in the knee joints of normal Wistar rats showed near-complete retention of activity within the synovial cavity upto 1 month post-administration. The radiochemical formulation thus demonstrated promising features as a radiopharmaceutical for treatment of arthritis with excellent logistic advantage for shipment to sites distant from the production facility thanks to the suitable nuclear decay properties of P-32. (C) 2016 Elsevier Ltd. All rights reserved.
机译:在本文中,我们描述了一种不使用在核反应堆和动物体内产生的未添加载体(NCA)P-32的P-32标记的羟基磷灰石(HA)微粒(1-10微米尺寸范围)合成的系统方法评估其作为治疗疼痛密集型关节病的预期可行放射性药物的效用。 NCA P-32是通过S-32(n,p)P-32途径在核反应堆中以高放射性核素纯度(99.95 +/- 0.01%,n = 5)生产的。在优化的条件下以高放射化学纯度(99.0 +/- 0.3%n = 12)合成了磷32标记的羟基磷灰石微粒(尺寸范围为1-10微米),该制剂在盐水中也显示出优异的体外稳定性如在大鼠血清中。在正常Wistar大鼠的膝关节内进行放射性标记颗粒的关节内给药显示,直至给药后1个月,滑膜腔内的活性几乎完全保留。因此,由于P-32具有适当的核衰变特性,该放射化学制剂具有治疗关节炎的良好作用,并具有出色的后勤优势,可运至远离生产设施的地点,具有良好的后勤优势。 (C)2016 Elsevier Ltd.保留所有权利。

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