Tocofersolan

Tocofersolan is a nonionic surfactant and derivative of vitamin E.¹ It has a critical micelle concentration (CMC) of 0.02 mM at room temperature. Tocofersolan inhibits P-glycoprotein (P-gp), also known as multidrug resistance protein 1 (MDR1), substrate-induced ATPase activity in cell-free assays (IC₅₀s = 0.4-3.25 ?M).² It reverses locomotor deficits induced by the polycyclic aromatic hydrocarbon benzo[a]pyrene in zebrafish larvae when used at a concentration of 1 ?M.³ Intravenous administration of nanocrystals containing tocofersolan (50 mg/kg) and paclitaxel reduces tumor growth in an NCI/ADR-RES mouse xenograft model.⁴

1.Sadoqi, M., Lau-Cam, C.A., and Wu, S.H.Investigation of the micellar properties of the tocopheryl polyethylene glycol succinate surfactants TPGS 400 and TPGS 1000 by steady state fluorometryJ. Colloid Interface Sci.333(2)585-589(2009) 2.Collnot, E.-M., Baldes, C., Wempe, M.F., et al.Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: Influence on ATPase activity and membrane fluidityMol. Pharm.4(3)465-474(2007) 3.Holloway, Z., Hawkey, A., Asrat, H., et al.The use of tocofersolan as a rescue agent in larval zebrafish exposed to benzo[α]pyrene in early developmentNeurotoxicology8678-84(2021) 4.Liu, Y., Huang, L., and Liu, F.Paclitaxel nanocrystals for overcoming multidrug resistance in cancerMol. Pharm.7(3)863-869(2010)