Evaluation of selenium-75 BISTAES as a potential articular cartilage imaging agent
Abstract
The potential of Se-75 bis ($\beta$-N,N,N-trimethylamino)-ethyl) selenide diiodide (Se-75 BISTAES) as an articular cartilage imaging agent for the early diagnosis of osteoarthritis was evaluated. The compound was synthesized and the identity was established. The radiochemical purity and stability were determined initially and over a two-month period of storage at three temperatures. The biodistribution of Se-75 BISTAES in rabbits and guinea pigs was studied. A high concentration of radioactivity was found in the knee and shoulder cartilage. The radioactivity in the cartilage was the highest at 15 minutes to one hour post-injection. In rabbits, the highest ratio of radioactivity in the cartilage to the surrounding tissues was about 30. A minimal ratio of 10 is required for nuclear medicine imaging. Nuclear medicine imaging conducted on rabbits demonstrated increased radioactivity in the articular cartilage in the knee and shoulder. The impressions from the nuclear medicine images and the findings of the biodistribution study indicated that the route of excretion of Se-75 BISTAES was the urine. The in vitro binding between Se-75 BISTAES and chondroitin sulfate was determined by an equilibrium dialysis technique. The amount of binding was directly proportional to the concentration of the chondroitin sulfate, suggesting that Se-75 BISTAES may be used to demonstrate the destruction of cartilage, the progress of osteoarthritis and the results of treatment. In conclusion, it appears that Se-75 BISTAES or a derivative should have potential as an articular cartilage imaging agent for the early diagnosis of osteoarthritis.
Degree
Ph.D.
Advisors
Shaw, Purdue University.
Subject Area
Pharmaceuticals
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