Paclitaxel-loaded micelles composed of folate-poly(ethylene glycol) and poly(γ-benzyl l-glutamate) diblock copolymer

Zhuo Du, Shirong Pan, Qiao Yu, Yuanpei Li, Yuting Wen, Wei Zhang, Min Feng, Chuanbin Wu

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

In this study folate-poly(ethylene glycol) and poly(γ-benzyl l-glutamate) diblock copolymer (FEG) was synthesized and the FEG chemical structure was characterized by 1H nuclear magnetic resonance (NMR) and Fourier transformation infrared (FTIR). Paclitaxel (PTX)-loaded FEG micelles were self-assembled and the properties of the FEG micelles were evaluated by fluorescence spectroscopy, scanning electron microscope (SEM), transmission electron microscope (TEM), dynamic light scattering (DLS), and in vitro drug-release experiments. It was found that folate groups of the FEG micelles were exposed on the micellar surface, while hydrophobic PTX was successfully entrapped in the core of the micelles to enhance aqueous solubility. The PTX was sustained-released from the FEG micelles depending on the molecular weight of FEG and the pH value of media. The cytotoxicity of blank FEG micelles was low even at high concentration. Through the analysis of fluorescence microscopy and flow cytometry, it indicated that the FITC-labeled FEG micelles were selectively transported to the folate receptor FR(+) HepG-2 cells, but not the FR(-) A549 cells. The free folate in culture media significantly reduced both the uptake of the FITC-labeled FEG micelles by the FR(+) HepG-2 cells and the cytotoxicity of the PTX-loaded FEG micelles against the FR(+) HepG-2 cells. The results suggest that FEG micelles could be transported into FR(+) HepG-2 cells by a FR-mediated endocytosis. FEG micelles will be a promising carrier for targeted delivery of hydrophobic anticancer drug, such as PTX.

Original languageEnglish (US)
Pages (from-to)140-148
Number of pages9
JournalColloids and Surfaces A: Physicochemical and Engineering Aspects
Volume353
Issue number2-3
DOIs
StatePublished - Jan 15 2010
Externally publishedYes

Fingerprint

glutamates
Micelles
Paclitaxel
Polyethylene glycols
Block copolymers
glycols
Glutamic Acid
micelles
copolymers
ethylene
Folic Acid
cells
Fluorescein-5-isothiocyanate
Cytotoxicity
drugs
poly(ethylene glycol)-folate
Electron microscopes
electron microscopes
fluorescence
culture media

Keywords

  • Folate receptor
  • Folate-PEG-PBLG
  • Micelles
  • Paclitaxel
  • Self-assembly

ASJC Scopus subject areas

  • Colloid and Surface Chemistry

Cite this

Paclitaxel-loaded micelles composed of folate-poly(ethylene glycol) and poly(γ-benzyl l-glutamate) diblock copolymer. / Du, Zhuo; Pan, Shirong; Yu, Qiao; Li, Yuanpei; Wen, Yuting; Zhang, Wei; Feng, Min; Wu, Chuanbin.

In: Colloids and Surfaces A: Physicochemical and Engineering Aspects, Vol. 353, No. 2-3, 15.01.2010, p. 140-148.

Research output: Contribution to journalArticle

Du, Zhuo ; Pan, Shirong ; Yu, Qiao ; Li, Yuanpei ; Wen, Yuting ; Zhang, Wei ; Feng, Min ; Wu, Chuanbin. / Paclitaxel-loaded micelles composed of folate-poly(ethylene glycol) and poly(γ-benzyl l-glutamate) diblock copolymer. In: Colloids and Surfaces A: Physicochemical and Engineering Aspects. 2010 ; Vol. 353, No. 2-3. pp. 140-148.
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AU - Zhang, Wei

AU - Feng, Min

AU - Wu, Chuanbin

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AB - In this study folate-poly(ethylene glycol) and poly(γ-benzyl l-glutamate) diblock copolymer (FEG) was synthesized and the FEG chemical structure was characterized by 1H nuclear magnetic resonance (NMR) and Fourier transformation infrared (FTIR). Paclitaxel (PTX)-loaded FEG micelles were self-assembled and the properties of the FEG micelles were evaluated by fluorescence spectroscopy, scanning electron microscope (SEM), transmission electron microscope (TEM), dynamic light scattering (DLS), and in vitro drug-release experiments. It was found that folate groups of the FEG micelles were exposed on the micellar surface, while hydrophobic PTX was successfully entrapped in the core of the micelles to enhance aqueous solubility. The PTX was sustained-released from the FEG micelles depending on the molecular weight of FEG and the pH value of media. The cytotoxicity of blank FEG micelles was low even at high concentration. Through the analysis of fluorescence microscopy and flow cytometry, it indicated that the FITC-labeled FEG micelles were selectively transported to the folate receptor FR(+) HepG-2 cells, but not the FR(-) A549 cells. The free folate in culture media significantly reduced both the uptake of the FITC-labeled FEG micelles by the FR(+) HepG-2 cells and the cytotoxicity of the PTX-loaded FEG micelles against the FR(+) HepG-2 cells. The results suggest that FEG micelles could be transported into FR(+) HepG-2 cells by a FR-mediated endocytosis. FEG micelles will be a promising carrier for targeted delivery of hydrophobic anticancer drug, such as PTX.

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