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首页> 外文期刊>Acta biomaterialia >Flt1 peptide-hyaluronate conjugate micelle-like nanoparticles encapsulating genistein for the treatment of ocular neovascularization.
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Flt1 peptide-hyaluronate conjugate micelle-like nanoparticles encapsulating genistein for the treatment of ocular neovascularization.

机译：Flt1肽-透明质酸缀合物胶束状纳米粒，包裹染料木黄酮，用于治疗眼部新生血管。

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摘要

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 24h. 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.
机译：GNQWFI的Flt1肽是血管内皮生长因子受体1（VEGFR1或Flt1）的拮抗肽。在这项工作中，成功合成了Flt1肽-透明质酸（HA）缀合物，并将所得的胶束状纳米颗粒用于封装染料木黄酮（酪氨酸特异性蛋白激酶的抑制剂），用于治疗眼部新生血管。染料木黄酮负载的Flt1肽-HA偶联物胶束的平均直径经测量为172.0±18.7 nm，载药效率为40-50％。从染料木黄酮负载的Flt1肽-HA共轭胶束中进行染料木黄酮的体外释放测试，其控释时间超过24小时。从人脐静脉内皮细胞（HUVEC）的协同抗增殖证实了染料木黄酮/ Flt1肽-HA胶束的体外生物学活性。此外，我们可以从统计上显着抑制SD大鼠硝酸银烧灼的角膜中角膜新生血管的形成来证实染料木黄酮/ Flt1肽-HA胶束的抗血管生成作用。通过在糖尿病性视网膜病模型大鼠中的治疗，视网膜血管的通透性也大大降低。

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