Biodegradable microsphere-loaded tacrolimus enhanced the effect on mice islet allograft and reduced the adverse effect on insulin secretion.

摘要: The adverse effects of tacrolimus have limited the use this potent immunosuppressive drug in clinical transplantation. To improve therapeutic effects, we developed a new type with biodegradable microsphere technology and examined on allogeneic islet transplantation side-effects insulin secretion vivo. With single subcutaneous injection, mouse blood concentrations (M-FK) carried microspheres remained flat for 2 weeks (only 10 h conventional tacrolimus). A administration 20 mg/kg M-FK significantly prolonged survival allografts (MST = 28 days) compared control group days). Series at 7-day intervals markedly grafts, resulted 60% allograft acceptance. In mice syngeneic transplantations, 30 inhibited secretion, whereas an equal dosage did not. results suggested that enhanced rejection more effectively reduced secretion.