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EGFR targeted thermosensitive liposomes: A novel multifunctional platform for simultaneous tumor targeted and stimulus responsive drug delivery

The epidermal growth factor receptor (EGFR) is a promising target for anti-cancer therapy. The aim of this study was to design thermosensitive liposomes (TSL), functionalized with anti-EGFR ligands for targeted delivery and localized triggered release of chemotherapy. For targeting, EGFR specific pe... Full description

Journal Title: Colloids and Surfaces B: Biointerfaces 01 October 2016, Vol.146, pp.657-669
Main Author: Haeri, Azadeh
Other Authors: Zalba, Sara , Ten Hagen, Timo L.M , Dadashzadeh, Simin , Koning, Gerben A
Format: Electronic Article Electronic Article
Language: English
Subjects:
ID: ISSN: 0927-7765 ; E-ISSN: 1873-4367 ; DOI: 10.1016/j.colsurfb.2016.06.012
Link: https://www.sciencedirect.com/science/article/pii/S0927776516304428
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recordid: elsevier_sdoi_10_1016_j_colsurfb_2016_06_012
title: EGFR targeted thermosensitive liposomes: A novel multifunctional platform for simultaneous tumor targeted and stimulus responsive drug delivery
format: Article
creator:
  • Haeri, Azadeh
  • Zalba, Sara
  • Ten Hagen, Timo L.M
  • Dadashzadeh, Simin
  • Koning, Gerben A
subjects:
  • Thermosensitive Liposomes
  • Epidermal Growth Factor Receptor (Egfr)
  • Hyperthermia
  • Cetuximab
  • Ge11 Peptide
  • Targeting
  • Engineering
  • Chemistry
  • Anatomy & Physiology
ispartof: Colloids and Surfaces B: Biointerfaces, 01 October 2016, Vol.146, pp.657-669
description: The epidermal growth factor receptor (EGFR) is a promising target for anti-cancer therapy. The aim of this study was to design thermosensitive liposomes (TSL), functionalized with anti-EGFR ligands for targeted delivery and localized triggered release of chemotherapy. For targeting, EGFR specific peptide (GE11) and Fab⿲ fragments of cetuximab were used and the effect of ligand density on tumor targeting was investigated. Ligand conjugation did not significantly change the physicochemical characteristics of liposomes. Fab⿲-decorated TSL (Fab⿲-TSL) can specifically and more efficiently bind to the EGFR overexpressed cancer cells as compared to GE11 modified TSL. Calcein labeled Fab⿲-TSL showed adequate stability at 37 °C in serum (
language: eng
source:
identifier: ISSN: 0927-7765 ; E-ISSN: 1873-4367 ; DOI: 10.1016/j.colsurfb.2016.06.012
fulltext: fulltext
issn:
  • 0927-7765
  • 09277765
  • 1873-4367
  • 18734367
url: Link


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titleEGFR targeted thermosensitive liposomes: A novel multifunctional platform for simultaneous tumor targeted and stimulus responsive drug delivery
creatorHaeri, Azadeh ; Zalba, Sara ; Ten Hagen, Timo L.M ; Dadashzadeh, Simin ; Koning, Gerben A
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subjectThermosensitive Liposomes ; Epidermal Growth Factor Receptor (Egfr) ; Hyperthermia ; Cetuximab ; Ge11 Peptide ; Targeting ; Engineering ; Chemistry ; Anatomy & Physiology
descriptionThe epidermal growth factor receptor (EGFR) is a promising target for anti-cancer therapy. The aim of this study was to design thermosensitive liposomes (TSL), functionalized with anti-EGFR ligands for targeted delivery and localized triggered release of chemotherapy. For targeting, EGFR specific peptide (GE11) and Fab⿲ fragments of cetuximab were used and the effect of ligand density on tumor targeting was investigated. Ligand conjugation did not significantly change the physicochemical characteristics of liposomes. Fab⿲-decorated TSL (Fab⿲-TSL) can specifically and more efficiently bind to the EGFR overexpressed cancer cells as compared to GE11 modified TSL. Calcein labeled Fab⿲-TSL showed adequate stability at 37 °C in serum (<4% calcein released after 1 h) and a temperature dependent release at above 40 °C. FACS analysis and live cell imaging showed efficient and EGFR mediated cellular association as well as dramatic intracellular cargo release upon hyperthermia. Fab⿲-conjugation and hyperthermia induced enhanced tumor cell cytotoxicity of doxorubicin loaded TSL. The relative cytotoxicity of Fab⿲-TSL was also correlated to EGFR density on the tumor cells. These results suggest that Fab⿲-TSL showed great potential for combinational targeted and triggered release drug delivery.
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