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KMID : 0043320030260020168
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Archives of Pharmacal Research
2003 Volume.26 No. 2 p.168 ~ p.172
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DA-7977, 188Rhenium-tin Colloid, as a New Therapeutic Agent of Rheumatoid Arthritis
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Shin CY
Son MW/Ko JI/Jung MY/Lee IK/Kim SH/Kim WB/Jeong JM
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Abstract
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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 avoi dance of surgery. In this study, we investigated the toxicity, stability and biodistribution of a rhenium-188(188Re)-tin colloid to evaluate its suitability as a synovectomy agent. Twenty four hours after injecting the 188Re-tin colloids (74 KBq/0.1 Ml) into the tail vein of ICR mice, most of the 188Re-tin colloidal particles was found in the lungs. In addition, there were no particle size changes at either room temperature or at 37oC after injecting the 188Re-tin colloids in human plasma and synovial fluid. In vitro stability tests showed that the fssRe-tin colloid remained in a colloidal form without a critical size variation over a 2-day period. We investigated the leakage of 188Re-tin colloids from the intraarticular injection site with gamma counting in New Zealand white rabbits. The 188Re-tin colloids (55.5 MBq/0.15 Ml) were injected at the caecum articular and the mean retention percentage of the 188Re-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 Oval-bumin (0VA)-induced arthritic rabbits, the 188Re-tin colloid improved the macroscopic, the his- tological score and reduced the knee joint diameter when compared to the arthritic control. In conclusion, a 188Re-tin-colloid is considered as a strong candidate for radiation synovectomy with a superior efficacy and safety.
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