In vivo Testing of a Bone-selective Fullerene: Preliminary Safety and Efficacy Testing

Purpose and Methods: Previous in vitro experiments have demonstrated that the addition of bisphosphonate groups to a fullerene (C60) molecule may lead to a drug delivery system targeted to bone. To determine the safety and the efficacy of the C60 bisphosphonated compound, a rat model of osteoporosis has been employed. Results: Two different doses were studied and the results demonstrated that the C60 compound is safe in the rat model: no significant behavior changes occurred, weight gains were normal, and no significant pathology was noted in the kidney, liver or esophagi of the animals when the test compound was administered orally over the course of eight weeks. The test compound also resulted in positive changes in the bone architecture of the treated ovariectomized animals. Conclusion: This indicates that the compound was delivered to bone and that it was bioactive.