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 µM).² It reverses locomotor deficits induced by the polycyclic aromatic hydrocarbon benzo[a]pyrene in zebrafish larvae when used at a concentration of 1 µM.³ Intravenous administration of nanocrystals containing tocofersolan (50 mg/kg) and paclitaxel (Item No. 10461) reduces tumor growth in an NCI/ADR-RES ovarian cancer mouse xenograft model.⁴ Liposomes containing tocofersolan and DOTMA (Item No. 25926) and encapsulating anti-miR-21 accumulate in the liver, lung, and spleen and decrease lung fibrosis in a mouse model of pulmonary fibrosis induced by the glycopeptide antitumor antibiotic bleomycin (Item No. 13877).⁵

WARNING This product is not for human or veterinary use.

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 fluorometry. J. 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 fluidity. Mol. 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 development. Neurotoxicology 86, 78-84 (2021).

4. Liu, Y., Huang, L., and Liu, F. Paclitaxel nanocrystals for overcoming multidrug resistance in cancer. Mol. Pharm. 7(3), 863-869 (2010).

5. Yan, L., Su, Y., Hsia, I., et al. Delivery of anti-microRNA-21 by lung-targeted liposomes for pulmonary fibrosis treatment. Mol. Ther. Nucleic Acids 32, 36-47 (2023).