Journal
MATERIALS SCIENCE AND ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS
Volume 74, Issue -, Pages 167-176Publisher
ELSEVIER
DOI: 10.1016/j.msec.2017.02.008
Keywords
Brain cancer; Transferrin receptor; Targeted nanomedicines; Synergistic effect; Chitosan; TPGS
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Funding
- Science and Engineering Research Board (SERB), New Delhi, India [SR/FT/LS-132/2011]
- Commission (UGC) for research fellowship
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Brain cancer, up-regulated with transferrin receptor led to concept of transferrin receptor targeted anticancer therapeutics. Docetaxel loaded D-alpha-tocopherol polyethylene glycol 1000 succinate conjugated chitosan (TPGS-chitosan) nanoparticles were prepared with or without transferrin decoration. In vitro experiments using C6 glioma cells showed that docetaxel loaded chitosan nanoparticles, non-targeted and transferrin receptor targeted TPGS-chitosan nanoparticles have enhanced the cellular uptake and cytdtoxicity. The IC50 values of non targeted and transferrin receptor targeted nanoparticles from cytotoxic assay were found to be 27 and 148 folds, respectively higher than Docel (TM). In vivo pharmacokinetic study showed 3.23 and 4.10 folds enhancement in relative bioavailability of docetaxel for non-targeted and transferrin receptor targeted nanoparticles, respectively than Docel (TM). The results have demonstrated that transferrin receptor targeted nanoparticles could enhance the cellular internalization and cytotoxicity of docetaxel via transferrin receptor with improved pharmacokinetics for clinical applications. (C) 2017 Elsevier B.V. All rights reserved.
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