TPGS's amphipathic structure --- a lipophilic tocopherol tail linked to a hydrophilic PEG head group --- gives it dramatically enhanced water solubility (~200 g/L) compared to native alpha-tocopherol (21 mg/L), roughly a 100-fold improvement. With a calculated HLB value of approximately 13.2--16, it functions as an effective oil-in-water emulsifier, solubilizer for poorly water-soluble drugs, and permeation enhancer, notably as a documented P-glycoprotein (P-gp) efflux pump inhibitor, which helps improve oral bioavailability of P-gp substrate drugs. It also retains vitamin E's inherent antioxidant activity, delivering approximately 387 IU/g when used nutritionally.
D-alpha-Tocopheryl Polyethylene Glycol 1000 Succinate (TPGS), also known as Vitamin E TPGS or tocofersolan, is a water-soluble ester derivative of natural vitamin E, formed by esterifying d-alpha-tocopheryl succinate's carboxyl group with polyethylene glycol 1000 (PEG 1000). This amphiphilic conjugation transforms fat-soluble vitamin E into a versatile pharmaceutical surfactant, solubilizer, and absorption enhancer.
| Chemical Name | D-alpha-Tocopheryl Polyethylene Glycol 1000 Succinate (Tocofersolan, Vitamin E TPGS) |
| CAS Number | 9002-96-4 |
| IUPAC Name | Tocofersolan / Vitamin E TPGS |
| Molecular Formula | N/A |
| Molecular Weight | N/A |
Widely used to improve solubility and absorption of poorly water-soluble drugs, notably via P-glycoprotein inhibition (e.g., used in Agenerase/amprenavir formulation).
Key excipient in self-emulsifying formulations, micelles, hot-melt extrusion, and nanoparticle-based (PLGA) drug delivery systems.
Used clinically (as tocofersolan) to treat vitamin E deficiency in pediatric patients with chronic cholestasis and digestive malabsorption.
Applied to extend corneal residence time in eye drops and as a surfactant in nasal spray formulations (e.g., beclometasone dipropionate).
J. Control. Release
J. Pediatr. Gastroenterol. Nutr.
Pharm. Res.
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