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Flt1 peptide–hyaluronate conjugate micelle-like nanoparticles encapsulating genistein for the treatment of ocular neovascularization

Paper ID Volume ID Publish Year Pages File Format Full-Text
370 40 2012 9 PDF Available
Title
Flt1 peptide–hyaluronate conjugate micelle-like nanoparticles encapsulating genistein for the treatment of ocular neovascularization
Abstract

Flt1 peptide of GNQWFI is an antagonistic peptide for vascular endothelial growth factor receptor 1 (VEGFR1 or Flt1). In this work, Flt1 peptide–hyaluronate (HA) conjugates were successfully synthesized and the resulting micelle-like nanoparticles were exploited to encapsulate genistein, an inhibitor of tyrosine-specific protein kinases, for the treatment of ocular neovascularization. The mean diameter of genistein-loaded Flt1 peptide–HA conjugate micelles was measured to be 172.0 ± 18.7 nm, with a drug-loading efficiency of 40–50%. In vitro release tests of genistein from the genistein-loaded Flt1 peptide–HA conjugate micelles exhibited the controlled release for longer than 24 h. In vitro biological activity of genistein/Flt1 peptide–HA micelles was corroborated from the synergistic anti-proliferation of human umbilical vein endothelial cells (HUVECs). Furthermore, we could confirm the anti-angiogenic effect of genistein/Flt1 peptide–HA micelles from the statistically significant suppression of corneal neovascularization in silver nitrate cauterized corneas of SD rats. The retinal vascular hyperpermeability was also drastically reduced by the treatment in diabetic retinopathy model rats.

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Keywords
Flt1 peptide; Genistein; Hyaluronate; Corneal neovascularization; Diabetic retinopathy
First Page Preview
Flt1 peptide–hyaluronate conjugate micelle-like nanoparticles encapsulating genistein for the treatment of ocular neovascularization
Publisher
Database: Elsevier - ScienceDirect
Journal: Acta Biomaterialia - Volume 8, Issue 11, November 2012, Pages 3932–3940
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering