TPGS Applications

Pharmaceuticals

Dietary Supplements

Food and Beverage

Personal Care and Cosmetics

Animal Nutrition


PHARMACEUTICAL APPLICATIONS OF TPGS

TPGS has a proven record in solubilizing active pharmaceutical ingredients (APIs) and greatly enhancing their absorption, bioavailability and efficacy.

Major advantages include.

  1. TPGS is water soluble, has a molecular structure similar to an amphiphile, exhibits low critical micellar concentration (CMC) and large surface area. These characteristics make it a good emulsifier. TPGS can emulsify or help solubilize a wide range of water-oil immiscible and other poorly soluble APIs trial (reference 1 below).
  2. The characteristics above coupled with its ability to form various liquid crystalline phases and stability in water solutions enable TPGS to serve in drug delivery/controlled release systems (references 2 and 3 below).
  3. Enhances absorption of and bioavailability especially of poorly soluble APIs and in malabsorbing patients due to its emulsifying/solubilizing properties and its ability to form micelle like particles and affect the absorption mechanisms (references 4 and 5 below).
  4. Supplies in water-soluble form the natural d-α-tocopherol which is universally accepted, including the Food and Drug Administration (FDA), the United States Pharmacopeia (USP) and the National Academy of Sciences (NAS) and industry, as more potent than the synthetic form dl-α-tocopherol. For more information on the advantages of the natural d-α- over the synthetic dl-α- tocopherol, please see the chapter of the Vitamin E Factor by Andreas Papas, PhD.

The major applications of vitamin E TPGS in pharmaceutical formulations include:

TPGS

For a summary of the TPGS vitamin E activity and other nutrient data which are useful in meeting the labeling requirements of the Food and Drug Administration (FDA) and other regulatory agencies in the United States and internationally please see the Nutrient Data Sheet.


Selected 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 May 15;333(2):585-9.
  2. Zhang Z, Lee SH, Gan CW, Feng SS. In vitro and in vivo investigation on PLA-TPGS nanoparticles for controlled and sustained small molecule chemotherapy. Pharm Res. 2008 Aug;25(8):1925-35
  3. Mu L, Feng SS. A novel controlled release formulation for the anticancer drug paclitaxel (Taxol): PLGA nanoparticles containing vitamin E TPGS. J Control Release. 2003 Jan 9;86(1):33-48.
  4. Sokol RJ, Johnson KE, Karrer FM, Narkewicz MR, Smith D, Kam I. Improvement of cyclosporin absorption in children after liver transplantation by means of water-soluble vitamin E. Lancet. 1991 Jul 27;338(8761):212-4.
  5. Chang T, Benet LZ, Hebert MF. The effect of water-soluble vitamin E on cyclosporine pharmacokinetics in healthy volunteers. Clin Pharmacol Ther. 1996 Mar;59(3):297-303.
  6. Brouwers J, Tack J, Lammert F, Augustijns P. Intraluminal drug and formulation behavior and integration in in vitro permeability estimation: a case study with amprenavir. J Pharm Sci. 2006 Feb;95(2):372-83.
    Sokol RJ, Butler-Simon N, Conner C, Heubi JE, Sinatra FR, Suchy FJ, Heyman MB, Perrault J, Rothbaum RJ, Levy J, et al. Multicenter trial of d-alpha-tocopheryl polyethylene glycol 1000 succinate for treatment of vitamin E deficiency in children with chronic cholestasis. Gastroenterology. 1993 Jun;104(6):1727-35.


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