Absorption and Bioavailability Enhancer
Antares Vitamin E TPGS is widely used in drug delivery systems where it has been shown to improve the efficiency of delivery as well as the therapeutic effect of the active ingredient. This is accomplished via several different mechanisms:
Emulsification of hydrophobic compounds to increase water solubility
Improvement of drug permeation across a variety of membranes
TPGS inhibits ATP dependent permeability glycoprotein (P-gp), also known as the efflux pump. This inhibition is responsible for increased absorption in the gut.
TPGS improves drug accumulation in multidrug-resistant (MDR) cells and often mediates the development of resistance to anticancer drug.
The efficacy of TPGS as an absorption and bioavailability enhancer has been demonstrated in cell culture, animal and major human clinical studies.
Paclitaxel Oral Delivery
Varma, Manthena & Panchagnula, Ramesh. (2005). Enhanced oral paclitaxel absorption with vitamin E-TPGS: Effect on solubility and permeability in vitro, in situ and in vivo. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 25. 445-53. 10.1016/j.ejps.2005.04.003.
Amprenavir Oral Delivery
Yu, Lawrence & Bridgers, Avis & Vickers, Ann & Long, Stacey & Roy, Arup & Winnike, Richard & Coffin, Mark. (2000). Vitamin E-TPGS Increases Absorption Flux of an HIV Protease Inhibitor by Enhancing Its Solubility and Permeability1. Pharmaceutical research. 16. 1812-7. 10.1023/A:1018939006780.
Darunavir Oral Delivery
Rehman, Saleha & Nabi, Bushra & Fazil, Mohammad & Khan, Saba & Kalim Bari, Naimat & Singh, Romi & Ahmad, Shavej & Kumar, Varinder & Baboota, Sanjula & Ali, Javed. (2017). Role of P-Glycoprotein Inhibitors in the Bioavailability Enhancement of Solid Dispersion of Darunavir. BioMed Research International. 2017. 1-17. 10.1155/2017/8274927.
Pulmonary delivery:
Ishak, Rania. (2016). HP-β-Cyclodextrin/TPGS Composite Complexes for Enhanced Resveratrol Solubility, In- Vitro Pulmonary Deposition and Cytotoxicity. International Journal of Pharmacy and Pharmaceutical Research. 7. 199-221.
Ishak, Rania & Osman, Rihab. (2015). Lecithin/TPGS-based spray-dried self-microemulsifying drug delivery systems: In vitro pulmonary deposition and cytotoxicity. International journal of pharmaceutics. 485. 10.1016/j.ijpharm.2015.03.019. Enhanced oral paclitaxel absorption with vitamin E-TPGS: Effect on solubility and permeability in vitro, in situ and in vivo. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.