Tocofersolan은 α-토코페롤의 폴리에틸렌 글리콜 유도체이자 수용성 비타민 E 유사체이다. Tocofersolan은 항산화 활성을 가지고 경구 생체이용 가능한 비타민 E 공급원으로 작용한다[2]. Tocofersolan은 일부 약물의 용해도와 생체 이용성을 증가시키고 약동학적 특성을 개선한다[3]. Tocofersolan은 일반적으로 약물 전달 시스템 또는 뉴트라슈티컬에 사용된다[4][5].
체외 실험에서 Tocofersolan(3.3µM~16.5mM; 60분)은 Caco-2 세포에서 P-글리코단백질(P-gp) 매개 마약 유출을 억제하였고 IC50은 5.86µM이었다[6].
체내 실험에서 수정 후 5일 된 어린 제브라피시에서 Tocofersolan(1µM) 공동 노출은 벤조[a]피렌(5µM) 노출로 인한 운동 억제를 역전시켰다[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.