Please use this identifier to cite or link to this item:
|Title:||Formulation of Docetaxel by folic acid-conjugated D-α-tocopheryl polyethylene glycol succinate 2000 (Vitamin E TPGS2k) micelles for targeted and synergistic chemotherapy|
|Source:||Mi, Y., Liu, Y., Feng, S.-S. (2011-06). Formulation of Docetaxel by folic acid-conjugated D-α-tocopheryl polyethylene glycol succinate 2000 (Vitamin E TPGS2k) micelles for targeted and synergistic chemotherapy. Biomaterials 32 (16) : 4058-4066. ScholarBank@NUS Repository. https://doi.org/10.1016/j.biomaterials.2011.02.022|
|Abstract:||Although high efficacy has been showed, Paclitaxel and Docetaxel cause serious side effects due to the adjuvant used in their clinical formulation Taxol® and Taxotere®. We developed a micelle system with a newly synthesized TPGS2k polymer, which shows lower CMC of 0.0219 mg/ml compared with 0.2 mg/ml for traditional micelles with TPGS involved, to achieve sustained and controlled drug delivery with Docetaxel used as a model anti-cancer drug. The TPGS2k micelles were further conjugated to folic acid (FA) for targeted drug delivery. The Docetaxel-loaded TPGS2k micelles with and without FA conjugation were found of desired size and size distribution, high drug encapsulation efficiency and favorable drug release. In vitro studies using MCF-7 cancer cells demonstrated significantly the higher cellular uptake of the formulated drug for TPGS2k micelle formulation than that for Taxotere®. The targeting effects for the FA conjugated TPGS2k micelles are also demonstrated. The IC50 value, which is the drug concentration needed for 50% cell viability in the designated time period, is 103.4, 1.280 and 0.1480 μg/ml for MCF-7 cancer cells after 24, 48, and 72 h treatment respectively, which is greatly decreased to be 0.526, 0.251 and 0.233 μg/ml, i.e. a 99.5%, 80.4% decrease and 57.5% increase for the TPGS2k micelle formulation, and further decreased to be 0.1780, 0.1520 and 0.1140 μg/ml, i.e. a 99.8%, 88.1% and 23.0% decrease for the folic acid conjugated micelles, respectively. A synergistic effect between TPGS2k and Docetaxel is also achieved. The present work represents a new concept in the design of drug delivery systems - the carrier materials of the drug delivery system can also have therapeutic effects, which either modulate the side effects of, or promote a synergistic interaction with the formulated drug. © 2011 Elsevier Ltd.|
|Appears in Collections:||Staff Publications|
Show full item record
Files in This Item:
There are no files associated with this item.
checked on Feb 15, 2018
WEB OF SCIENCETM
checked on Feb 7, 2018
checked on Feb 20, 2018
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.