Biodistribution of calcitonin encapsulated in liposomes in mice with particular reference to the central nervous system.

The biodistribution of [125I]porcine calcitonin (pCT) encapsulated in reverse-phase evaporation vesicles (REVs) in mice upon the intravenous administration was examined. It was found that sulfatide significantly improved the stability of REVs in vivo, and altered the relative distribution of [125I]pCT encapsulated in liposomes in mice. These sulfatide-containing REVs were able to target [125I]pCT into the liver and central nervous system (CNS) reasonably well, with the maximal effect of about 40% and 2% of the injected doses occurring at 30 min and 90 min, respectively, after injection. Neither free [125I]pCT, nor sulfatide-free liposome-encapsulated [125I]pCT, nor a mixture of free [125I]pCT and empty sulfatide liposomes was effective. [125I]pCT was widely distributed in the CNS, with predominance in hypothalamus, brainstem, striatum and spinal cord. The results indicate that pCT encapsulated in sulfatide-containing liposomes is able to pass through the blood-brain barrier (BBB), and calcitonin, thus encapsulated, may be applicable to studies on its functions in the CNS.