期刊
COLLOIDS AND SURFACES B-BIOINTERFACES
卷 152, 期 -, 页码 277-288出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.colsurfb.2017.01.021
关键词
Brain cancer; Targeted nanomedicines; Synergistic effect; Chitosan; TPGS; Bioadhesive study
资金
- Science & Engineering Research Board (SERB), New Delhi, India [SR/FT/LS-132/2011]
- University Grants Commission (UGC)
The aim of this work was to prepare targeted bioadhesive D-alpha-tocopheryl glycol succinate 1000 (TPGS) micelles containing docetaxel (DTX) for brain targeted cancer therapy. Considering the unique bioadhesive feature of chitosan, herein, we have developed a synergistic transferrin receptor targeted bioadhesive micelles using TPGS conjugated chitosan (TPGS-chitosan), which target the overexpressed transferrin receptors of glioma cells for brain cancer therapy. The micelles were prepared by the solvent casting method and characterized for their particle size, polydispersity, zeta-potential, surface morphology, drug encapsulation efficiency, and in-vitro release. The IC50 values demonstrated transferrin receptor targeted TPGS-chitosan micelles could be 248 folds more effective than Docel (TM) after 24 h treatment with the C6 glioma cells. Further, time dependent bioadhesive cellular uptake study indicated that a synergistic effect was achieved with the chitosan and transferrin in targeted TPGS-chitosan micelles through the biodhesive property of chitosan as well as transferrin receptor mediated endocytosis. The in-vivo pharmacokinetic results demonstrated that relative bioavailability of non-targeted and targeted micelles were 2.89 and 4.08 times more effective than Docel (TM) after 48 h of treatments, respectively. (C) 2017 Elsevier B.V. All rights reserved.
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