• Archives of Pharmacal Research
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• v.26 no.2
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• pp.168-172
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• 2003

Radiation synovectomy is one of the most useful methods for treating patients with refractory synovitis because of its convenience, long-term effects, repeatability and the avoidance of surgery. In this study, we investigated the toxicity, stability and biodistribution of a rhenium-188 ($^{188}$Re)-tin colloid to evaluate its suitability as a synovectomy agent. Twenty four hours after injecting the $^{188}$Re-tin colloids (74 KBq/0.1 mL) into the tail vein of ICR mice, most of the $^{188}$Retin colloidal particles was found in the lungs. In addition, there were no particle size changes at either room temperature or at $37^{\circ}C$ after injecting the $^{188}$Re-tin colloids in human plasma and synovial fluid. In vitro stability tests showed that the $^{188}$Re-tin colloid remained in a colloidal form without a critical size variation over a 2-day period. We investigated the leakage of $^{188}$Retin colloids from the intraarticular injection site with gamma counting in New Zealand white rabbits. The $^{188}$Re-tin colloids (55.5 MBq/0.15 mL) were injected at the cavum articular and the mean retention percentage of the $^{188}$Re-tin colloid was 98.7% for 1 day at the injection site, which suggests that there was neither change in the particle size nor leakage at the injection sites. In the biodistribution study with the SD rats, the liver showed the highest radioactivity (0.0427% ID/organ) except for the injected knees (99.49%). In the SD rats, mild toxicities including the skin or a synovium inflammation were observed as a result of a radioactivity of 15 mCi/kg at the intraarticular injection site. However, there was no systemic toxicity. In the Ovalbumin (OVA)-induced arthritic rabbits, the $^{188}$Re-tin colloid improved the macroscopic, the histological score and reduced the knee joint diameter when compared to the arthritic control. In conclusion, a $^{188}$Re-tin-colloid is considered as a strong candidate for radiation synovectomy with a superior efficacy and safety.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.3 no.2
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• pp.80-84
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• 2017

Re-188 is an excellent and practical radioisotope produced by W-188/Re-188-generator for therapy. We prepared Re-188-tin colloid for therapy of various diseases and tried to treat peritoneal effusion in animal model. Sarcoma-180 cells were injected into ICR mice to induce peritoneal effusion and the mice were grown for 3 d. Re-188-tin colloids (0.25, 0.5, and 1 mCi/mL per 30 g body weight) were injected into the mice and the mice were grown for 90 d. Planar gamma scintigraphy showed even distribution of Re-188-tin colloid radioactivity. Bax expression was found to be dose dependent to Re-188-tin colloid. Normal saline treated group showed the shortest survival time. Among the treated groups, 0.5 mCi dose group showed the longest survival time. In conclusion, Re-188-tin colloid was prepared successfully and showed the feasibility to use as a peritoneal effusion treatment in mice.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.1 no.2
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• pp.109-117
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• 2015

Radiation synovectomy has been proposed as a promising palliative therapy for recurrent joint effusions for the last two or three decades. Ionizing radiations emitted by intrarticularly administered radiolabelled colloids. The aim of this study was to assess the effectiveness of radiation synovectomy (RSV) using $^{188}Re$-tin colloid in the treatment of recurrent joint effusions and chronic synovitis of knee joints. Three phase bone scan was acquired for the concerned joint prior to radiosynovectomy. $^{188}Re$-tin colloid was prepared as per the reported protocol. 9 patients, diagnosed with rheumatoid arthritis and suffering from chronic resistant synovitis of the knee, ankle or elbow joints were administered the radiopharmaceuticals, checked for radiochemical purity >95% by intraarticular route. A whole body scan was acquired 2 h post-radiosynovectomy. In all the 9 treatments, no leakage to non-target organs was visible in the whole body scan. Static scans of the joint revealed complete retention of $^{188}Re$-tin colloid in the joints post administration of the agent. Clinically all patients exhibited a complete or partial response. RSV with $^{188}Re$-tin colloid was safe and effective in patients with chronic synovitis of rheumatoid origin.