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20 Pharmaceutical Technology ® Trends in Formulation 2022 eBook PharmTech.com YURI HOYDAS - STOCK.ADOBE.COM V itamin E TPGS, or d-α-tocopheryl poly- ethylene glycol 1000 succinate, was first developed more than 60 years ago as a water-soluble form of naturally occur- ring vitamin E. Originally used to treat vitamin E deficiency in cholestatic patients, TPGS quickly at- tracted attention as a versatile solubilizer due to its amphiphilic nature and surfactant properties. Fur- ther application of this molecule emerged in the 1990s, when TPGS was shown to improve epithelial absorption by modulating cellular efflux. Research- ers have continued to find a variety of new and ex- citing applications of this molecule, and TPGS has become an important tool for drug delivery for- mulators. This report serves to summarize some of recent innovations using TPGS for improved deliv- ery of bioactive materials. History of TPGS Vitamin E is a fat-soluble nutrient with important prop- erties relating to vision, reproduction, and the general health of the skin, brain, and blood (1). Vitamin E oc- curs naturally in plant-based oils, nuts, and fruits, but low solubility in water limits its field of application, and in the case of malabsorbing patients, their ability to obtain adequate doses of this essential nutrient. This limitation led Eastman Kodak to develop TPGS (CAS 9002-96-4), or tocophersolan, in 1950 as a water-soluble form of vitamin E (2). The pharmaceutical field began to take a serious interest in TPGS in the 1990s, after Sokol demonstrated that Vitamin E TPGS overcame vitamin E deficiencies in cholestatic children with se- vere malabsorption (3). These patients were previously unresponsive to oral forms of vitamin E supplementa- tion and were forced to rely on painful intramuscular Emerging Applications of Vitamin E TPGS in Drug Delivery Greg Paddon-Jones, PhD, is director of Product Development at Antares Health Products. The author discusses some new applications of TPGS in the pharmaceutical field that should see this versatile excipient retain its place in the drug formulators toolbox.