Effect of Sulodexide on Plasma Transforming Growth Factor-β1 in Healthy Volunteers

It is unknown whether the glycosaminoglycan drug sulodexide interferes with transforming growth factorβ1—a member of heparin-binding family and a potent regulator of human biology and diseases. Hence, a 2-week pilot study was performed in 11 healthy men. Sulodexide was initially administered intravenously in a single dose, then—orally for 12 days and—again intravenously on study completion. Initial injection had no effect on activated form of the growth factor measured in plasma after 10 and 120 min; no change was also observed after 120 min from drug ingestion on day 7. On final intravenous administration, the growth factor levels increased by almost 60% after 10 min and remained elevated; the 120-min levels directly correlated with sulodexide dosage. Baseline cytokine levels decreased during the 2-week trial by more than 50%. In conclusion, transforming growth factor-β1 release and likely downregulation of its expression may constitute novel pharmacological effects of sulodexide.