Progress in the study of D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) reversing multidrug resistance
Currently, multidrug resistance (MDR) is one of the major reasons for failure in clinical cancer chemotherapy. Overexpression of the ATP binding cassette (ABC) transporter P-glycoprotein (P-gp), which significantly increases the efflux of anticancer drugs from tumor cells, enhances MDR.
Various mechanisms causing multidrug resistance (MDR) are illustrated.
TPGS downregulates the expression of P-glycoprotein and reverses MDR.
TPGS-based nanopreparations elevate the chemotherapy effect to overcome MDR.
TPGS-based nanodelivery systems reversing MDR are summarized.
In the past few decades, four generations of P-gp inhibitors have appeared. However, they are limited in clinical application due to their severe toxic side effects. As a P-gp inhibitor and carrier for loading chemotherapy agents, TPGS has received increasing attention due to its advantages and unique properties of reversing MDR. TPGS is an amphipathic agent that increases the solubility of most chemotherapy drugs and decreases severe side effects.
In addition, TPGS is an excellent carrier with P-gp-inhibiting ability. In this review, we summarize the latest articles on TPGS-based nanodelivery systems to prevent MDR.
Article information: Huixian Yan, Xiyou Du, Rujuan Wang, Guangxi Zhai. Progress in the study of D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) reversing multidrug resistance,
Colloids and Surfaces B: Biointerfaces, Volume 205, 2021. https://doi.org/10.1016/j.colsurfb.2021.111914.