Ceramide forms stable, fluid bilayers with cholesteryl phosphocholine, and this formulation has been shown to be more potent than solvent-delivered (DMSO) formulations of C6 Ceramide in inhibiting proliferation, inducing apoptosis, and disturbing calcium homeostasis. It is thought that DMSO formulations of C6 Cer are likely to precipitate into the cell culture medium, where the bioavailability of “crystalline” ceramide is limited. However, the formation of fluid bilayers, which are enriched in C6 Cer, prevent crystallization and allow for the transfer of monomeric ceramide to cell membranes with enhanced bioavailability.
Note: This delivery system works primarily with short-chain ceramides. Delivery of long-chain ceramides, e.g., C16 Cer, was generally low or absent during similar incubation times.