Tocofersolan is a polyethylene glycol derivative of α-tocopherol and is a water-soluble vitamin E analog[1]. Tocofersolan has antioxidant activity and serves as an orally bioavailable source of vitamin E[2]. Tocofersolan increases the solubility and bioavailability of some drugs, and improves their pharmacokinetic properties[3]. Tocofersolan is usually used in drug delivery systems or nutraceuticals[4][5].
In vitro, Tocofersolan (3.3µM to 16.5mM; 60min) inhibited P-glycoprotein (P-gp) - mediated drug efflux in Caco-2 cells with an IC50 of 5.86µM[6].
In vivo, Tocofersolan (1µM) co-exposure for 5 days post-fertilization in larval zebrafish reversed the locomotor hypoactivity caused by benzo[a]pyrene (5µM) exposure[7].
References:
[1] Sadoqi M, Lau-Cam CA, Wu SH. 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. 2009;333(2):585-589.
[2] Thebaut A, Nemeth A, Le Mouhaer J, et al. Oral Tocofersolan Corrects or Prevents Vitamin E Deficiency in Children With Chronic Cholestasis. J Pediatr Gastroenterol Nutr. 2016;63(6):610-615.
[3] Wande DP, Cui Q, Chen S, Xu C, Xiong H, Yao J. Rediscovering Tocophersolan: A Renaissance for Nano-Based Drug Delivery and Nanotheranostic Applications. Curr Drug Targets. 2021;22(8):856-869.
[4] Tan S, Zou C, Zhang W, Yin M, Gao X, Tang Q. Recent developments in d-α-tocopheryl polyethylene glycol-succinate-based nanomedicine for cancer therapy. Drug Deliv. 2017;24(1):1831-1842.
[5] Srivastava A, Lall R, Talukder J, DuBourdieu D, Gupta RC. Iron Transport Tocopheryl Polyethylene Glycol Succinate in Animal Health and Diseases. Molecules. 2019;24(23):4289.
[6] Collnot EM, Baldes C, Wempe MF, et al. Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity. Mol Pharm. 2007;4(3):465-474.
[7] Holloway Z, Hawkey A, Asrat H, Boinapally N, Levin ED. The use of tocofersolan as a rescue agent in larval zebrafish exposed to benzo[a]pyrene in early development. Neurotoxicology. 2021;86:78-84.
Tocofersolan是α-生育酚的聚乙二醇衍生物，是一种水溶性的维生素E类似物[1]。Tocofersolan具有抗氧化活性，可作为维生素E的口服生物可利用来源[2]。Tocofersolan能够增加某些药物的溶解度和生物利用度，从而改善药物的药代动力学特性[3]。Tocofersolan常用于药物递送系统或营养保健品中[4][5]。
体外实验中，Tocofersolan（3.3µM-16.5mM；60分钟）在Caco-2 细胞中抑制了 P-糖蛋白（P-gp）介导的药物外排，IC50值为5.86µM[6]。
体内实验中，斑马鱼幼虫受精后5天暴露于Tocofersolan（1µM）可逆转苯并[a]芘（5µM）暴露引起的运动能力低下[7]。