Merck, 57668-25G, D-α-Tocopherol polyethylene glycol 1000 succinate

Tocofersolan, also known as Vitamin E-TPGS, is a nonionic surfactant and a synthetic polyethylene glycol derivative of α-tocopherol, commonly known as vitamin E. This water-soluble amphipathic formulation consists of d-alpha-tocopherol succinate coupled to polyethylene glycol (PEG) 1000 through a succinate linker. Its amphipathic nature enables the formation of micelles, facilitating uptake into enterocytes, even in the absence of bile salts. Upon hydrolysis, fat-soluble d-alpha-tocopherol is released. Tocofersolan significantly improves the absorption of d-alpha-tocopherol compared to free administration. Moreover, Tocofersolan acts as an inhibitor of P-glycoprotein (P-gp or MDR1) substrate-induced ATPase activity in cell-free assays. It has demonstrated efficacy against resistant K562 cells by binding to urokinase-type plasminogen activator, a crucial enzyme for cancer cell migration and invasion. Additionally, Tocofersolan inhibits tyrosine kinase, a key player in cancer cell development, offering potential applications in metabolomics and biochemical research. Its ability to enhance the absorption of water-insoluble agents and other fat-soluble vitamins positions it as a promising compound for formulation and drug delivery research.