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Pharmaceutical Applications

Antares Vitamin E TPGS solubilizes, emulsifies and enhances absorption of difficult to absorb lipophilic APIs in a wide range of dosage forms. 

Typical Uses in Pharmaceuticals:

BY FUNCTIONALITY

  • Solubilizer
  • Emulsifier
  • Absorption & Bioavailability Enhancer of difficult to absorb lipophilic compounds
  • Carrier

BY DOSAGE FORM

  • Solid oral – tablets, powders, capsules and softgels
  • Liquid oral – aqueous emulsions, small particle dispersions, oil blends
  • Topical delivery
  • Ocular delivery
  • Mucosal delivery
  • Parenteral delivery
  • Devices

LITERATURE REFERENCES

  • Solubilization and formulation of lipophilic and poorly soluble APIs including cyclosporine, amprenavir and paclitaxel (references 3, 4, 5 and 7 below).
  • Drug delivery and control release of APIs (references 2 and 7 below).
  • Increased absorption and bioavailability of poorly soluble APIs (references 4, 5 and 6 below).
  • Supply of vitamin E in malabsorbing patients (reference 7 below).

 

Formulating Advantages of Antares Vitamin E TPGS:

  • Available in NF grade
  • Versatile, functional excipient with proven utility in oral (solids and liquids), topical, ocular, mucosal and parenteral delivery 
  • Long history (over 50 years) of safe use
  • Solubilizes and/or emulsifies a wide range of water-immiscible, lipid and poorly-soluble APIs (also see reference 1 below).
  • Is water-soluble, has amphiphilic molecular structure, a low critical micelle concentration (CMC) and creates a large surface area of oil it disperses in water – all characteristics of an effective emulsifier. 
  • Forms physically/chemically/thermodynamically stable micelle and other liquid crystalline phase structures in water and oil/water systems and can serve as a carrier or matrix component in drug delivery/controlled release systems (references 2 and 3 below).
  • Enhances absorption and bioavailability of poorly-soluble APIs in malabsorbing patients due to several factors: its emulsifying/solubilizing properties and its ability to form micelles combined with its unique activity in the body (also see references 4 and 5 below).
  • Supplies natural d-α-tocopherol in water-soluble form. (It is universally accepted that the natural form of vitamin E, d-α-tocopherol, is more potent than the synthetic form of vitamin E, dl-α-tocopherol. This body of acceptance extends throughout industry and includes the Food and Drug Administration (FDA) and the National Academy of Sciences (NAS)). For more information on the advantages of the natural d-α- over the synthetic dl-α- tocopherol, please see The Vitamin E Factor by Andreas Papas, PhD.

If you need additional assistance regarding the use of Antares Vitamin E TPGS in your specific application, please Contact Us

 

For basic handling and use guidelines for Antares Vitamin E TPGS, see How To Use TPGS.

 

Download Safety Data Sheet, Product Data Sheet and additional product documentation from our Documentation page. 

 

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.
  7. 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.