Vitamin E TPGS D-α-Tocopherol Polyethylene Glycol 1000 Succinate

TPGS (Tocopheryl Polyethylene Glycol Succinate) is a water-soluble derivative of vitamin E. It is formed by the reaction of the carboxyl group of vitamin E succinate with the hydroxyl group of polyethylene glycol. Its structure includes both the lipophilic ester group from vitamin E and the hydrophilic long chain from polyethylene glycol, which gives it excellent surfactant properties and water solubility. This allows it to significantly enhance the absorption and bioavailability of poorly soluble drugs in the gastrointestinal tract.

TPGS is widely used in formulation research abroad, where it serves as a solubilizer, absorption enhancer, emulsifier, plasticizer, and carrier for water-insoluble or lipid-soluble drug delivery systems, such as solid dispersions, ocular drug delivery carriers, and nasal drug delivery carriers, among others.

Recent studies have shown that TPGS can not only serve as a pharmaceutical excipient but also possesses various unique properties, such as functioning as an absorption enhancer and a multidrug resistance (MDR) reversal agent. TPGS can also be used in prodrug formulations, micelles, liposomes, and TPGS-copolymer carriers to improve the solubility, permeability, and stability of formulations, achieving controlled release, sustained release, and targeted effects, thereby promoting the absorption of drugs.

TPGS is a versatile pharmaceutical excipient primarily used to enhance the solubility, bioavailability, and stability of drugs. It works in drug delivery systems through the following mechanisms:

● Increase drug solubility: TPGS has excellent water solubility and can form complexes with hydrophobic drugs, thereby improving the solubility of drugs in water and promoting drug absorption and bioavailability.

● Protect drugs from enzymatic degradation: TPGS can form a protective film on the surface of the drug, preventing enzymatic degradation in the body, extending the enterohepatic circulation of the drug, and enhancing its therapeutic effect.

● Regulate drug release rate: By adjusting the amount of TPGS, controlled release or rapid release of the drug can be achieved.

● Improve drug stability: TPGS has antioxidant properties, which protect drugs from oxidative damage and inhibit interactions with other substances, reducing degradation.

● Improve pharmacokinetic properties: TPGS improves oral drug absorption and reduces fluctuations in plasma concentration, thereby optimizing pharmacokinetic characteristics.

Nutritional and Therapeutic Value of Vitamin E TPGS

TPGS is a potent source of natural vitamin E and can be used for treatment and nutritional supplementation. Unlike lipid-soluble vitamin E, TPGS, as water-soluble vitamin E, is absorbed through a unique mechanism: while lipid-soluble vitamin E depends on bile acids for absorption in the intestine, TPGS can transport vitamin E directly into intestinal cells without requiring bile acids.