Imatinib-Loaded Micelles of Hyaluronic Acid Derivatives for Potential Treatment of Neovascular Ocular Diseases,Molecular Pharmaceutics

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Imatinib-Loaded Micelles of Hyaluronic Acid Derivatives for Potential Treatment of Neovascular Ocular Diseases
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2018-09-24 00:00:00 , DOI: 10.1021/acs.molpharmaceut.8b00620
Flavia Bongiovì ₁ , Calogero Fiorica ₁ , Fabio S. Palumbo ₁ , Giulia Di Prima ₁ , Gaetano Giammona _{1,

2} , Giovanna Pitarresi ₁

Affiliation

In this work, new micellar systems able to cross corneal barrier and to improve the permeation of imatinib free base were prepared and characterized. HA-EDA-C₁₆, HA-EDA-C₁₆–PEG, and HA-EDA-C₁₆–CRN micelles were synthesized starting from hyaluronic acid (HA), ethylenediamine (EDA), hexadecyl chains (C₁₆), polyethylene glycol (PEG), or l-carnitine (CRN). These nanocarriers showed optimal particle size and mucoadhesive properties. Imatinib-loaded micelles were able to interact with corneal barrier and to promote imatinib transcorneal permeation and penetration. In addition, a study was conducted to understand the in vitro imatinib inhibitory effect on a choroidal neovascularization process. Imatinib released from polymeric micelles was able to inhibit endothelial cell sprouting and to promote cell tube disruption.

中文翻译：

伊马替尼负载的透明质酸衍生物胶束用于潜在治疗新生血管性眼病

在这项工作中，制备并表征了能够穿越角膜屏障并改善伊马替尼游离碱渗透性的新胶束系统。从透明质酸（HA），乙二胺（EDA），十六烷基链（C ₁₆），聚乙二醇开始合成HA-EDA-C ₁₆，HA-EDA-C ₁₆ -PEG和HA-EDA-C ₁₆ -CRN胶束（PEG）或1-肉碱（CRN）。这些纳米载体表现出最佳的粒度和粘膜粘附性能。载有伊马替尼的胶束能够与角膜屏障相互作用，并促进伊马替尼经角膜的渗透和渗透。另外，进行了一项研究以了解体外伊马替尼对脉络膜新生血管形成过程有抑制作用。从聚合胶束释放的伊马替尼能够抑制内皮细胞发芽并促进细胞管破裂。

更新日期：2018-09-24

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