Vitamin e TPGS coated liposomes enhanced cellular uptake and cytotoxicity of docetaxel in brain cancer cells

Abstract

The aim of this work was to develop a drug delivery system of liposomes, which are coated with d-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS), a PEGylated vitamin E, with docetaxel as a model drug for enhanced treatment of brain tumour in comparison with the nude liposomes as well as with the so-called stealth liposomes, i.e. those coated with polyethylene glycol (PEG), which have been intensive investigated in the literature. Docetaxel or coumarin-6 loaded liposomes were prepared by the solvent injection method and characterized for their particle size, polydispersity, zeta potential and drug encapsulation efficiency. C6 glioma cells were employed as an in vitro model to access cellular uptake and cytotoxicity of the drug or coumarin-6 loaded liposomes. The particle size of the PEG or TPGS coated liposomes was ranged between 126 and 191 nm. High-resolution field-emission transmission electron microscopy (FETEM) confirmed the coating of TPGS on the liposomes. The IC50 value, which is the drug concentration needed to kill 50% cells in a designated time period, was found to be 37.04 ± 1.05, 31.04 ± 0.75, 7.70 ± 0.22, and 5.93 ± 0.57 μg/ml for the commercial Taxotere ®, the nude, PEG coated and TPGS coated liposomes, respectively after 24 h culture with C6 glioma cells. The TPGS coated liposomes showed great advantages in vitro than the PEG coated liposomes. © 2011 Elsevier B.V. All rights reserved.