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用于阿魏酸眼部递送的交联透明质酸电纺纳米纤维。

Crosslinked Hyaluronan Electrospun Nanofibers for Ferulic Acid Ocular Delivery.

作者信息

Grimaudo Maria Aurora, Concheiro Angel, Alvarez-Lorenzo Carmen

机构信息

Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, I+D Farma (GI-1645), Facultad de Farmacia and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, 15782-Santiago de Compostela, Spain.

出版信息

Pharmaceutics. 2020 Mar 17;12(3):274. doi: 10.3390/pharmaceutics12030274.

Abstract

Electrospun nanofibers are gaining interest as ocular drug delivery platforms that may adapt to the eye surface and provide sustained release. The aim of this work was to design an innovative ophthalmic insert composed of hyaluronan (HA) nanofibers for the dual delivery of an antioxidant (ferulic acid, FA) and an antimicrobial peptide (ε-polylysine, ε-PL). Polyvinylpyrrolidone (PVP) was added to facilitate the electrospinning process. Fibers with diameters of approx. 100 nm were obtained with PVP 5%-HA 0.8% and PVP 10%-HA 0.5% mixtures in ethanol:water 4:6 . An increase in PVP concentration to 20% in both presence and absence of HA rendered fibers of approx. 1 µm. PVP 5%-HA 0.8% fibers were loaded with 83.3 ± 14.0 µg FA per mg. After nanofibers crosslinking with ε-PL, blank and FA-loaded inserts showed a mean thickness of 270 ± 21 µm and 273 ± 41 µm, respectively. Blank and FA-loaded inserts completely released ε-PL within 30 min under sink conditions, whereas FA-loaded inserts released the antioxidant within 20 min. Both blank and FA-loaded inserts were challenged against and , demonstrating their efficacy against relevant microbial species.

摘要

电纺纳米纤维作为一种可适应眼表并能实现持续释放的眼部药物递送平台,正日益受到关注。本研究的目的是设计一种由透明质酸(HA)纳米纤维组成的创新型眼科插入物,用于抗氧化剂(阿魏酸,FA)和抗菌肽(ε-聚赖氨酸,ε-PL)的双重递送。添加聚乙烯吡咯烷酮(PVP)以促进静电纺丝过程。在乙醇与水比例为4:6的体系中,使用PVP 5%-HA 0.8%和PVP 10%-HA 0.5%的混合物可获得直径约为100 nm的纤维。在有或没有HA存在的情况下,将PVP浓度提高到20%会得到直径约为1 µm的纤维。PVP 5%-HA 0.8%的纤维每毫克负载83.3±14.0 µg FA。纳米纤维与ε-PL交联后,空白插入物和负载FA的插入物的平均厚度分别为270±21 µm和273±41 µm。在漏槽条件下,空白插入物和负载FA的插入物在30分钟内完全释放出ε-PL,而负载FA的插入物在20分钟内释放出抗氧化剂。空白插入物和负载FA的插入物均对[具体菌种1]和[具体菌种2]进行了测试,证明了它们对相关微生物物种的有效性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4c26/7151120/be4fab1ee4fb/pharmaceutics-12-00274-g001.jpg

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