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载有迷迭香酸的电纺纳米纤维:体外释放动力学研究及生物活性评估。

Rosmarinic acid-loaded electrospun nanofibers: In vitro release kinetic study and bioactivity assessment.

作者信息

Vatankhah Elham

机构信息

Department of Bio-systems Faculty of New Technologies Engineering Shahid Beheshti University Tehran Iran.

出版信息

Eng Life Sci. 2018 Sep 25;18(10):732-742. doi: 10.1002/elsc.201800046. eCollection 2018 Oct.

Abstract

This study seeks to develop a nanofibrous matrix containing rosmarinic acid (RosA), an herbal non-steroidal anti-inflammatory and antioxidant drug with low water solubility, for drug delivery applications. Neat and two types of RosA-loaded cellulose acetate (CA) mats varying in the initial content of RosA were electrospun. Microstructure of nanofibers, chemistry and physical state of RosA in nanofibers, RosA loading efficiency and RosA release in acetate buffer were investigated. To evaluate bioactivity of RosA-loaded nanofibers, their ability to inhibit protein denaturation was assayed as an indicator of anti-inflammatory properties and their antioxidant activity was determined by radical scavenging assay. The indirect cytotoxicity assay was used to find if there is a cytotoxic response to nanofibers. The homogeneous distribution of the drug within nanofibers through electrospinning led to high loading efficiency, low burst release and prolonged release of a large percentage of RosA over a period of 64h following Fickian diffusion mechanism. Nanofibers with higher RosA content exhibited anti-inflammatory activity comparable to ibuprofen, and higher antioxidant activity compared to nanofibers with lower RosA content. Additionally, extracts from nanofibers did not give any major harmful effect on cells. Sustained release of RosA, and bioactivity of RosA-loaded nanofibers confirmed the potential of the produced matrix as a drug delivery system.

摘要

本研究旨在开发一种含有迷迭香酸(RosA)的纳米纤维基质,用于药物递送应用。迷迭香酸是一种水溶性低的草本非甾体抗炎和抗氧化药物。制备了纯的以及两种初始迷迭香酸含量不同的负载迷迭香酸的醋酸纤维素(CA)垫,并进行了静电纺丝。研究了纳米纤维的微观结构、纳米纤维中迷迭香酸的化学和物理状态、迷迭香酸的负载效率以及在醋酸盐缓冲液中的释放情况。为了评估负载迷迭香酸的纳米纤维的生物活性,测定了它们抑制蛋白质变性的能力作为抗炎特性的指标,并通过自由基清除试验测定了它们的抗氧化活性。采用间接细胞毒性试验来确定纳米纤维是否存在细胞毒性反应。通过静电纺丝使药物在纳米纤维中均匀分布,导致高负载效率、低突释,并在64小时内按照菲克扩散机制实现了大部分迷迭香酸的缓释。迷迭香酸含量较高的纳米纤维表现出与布洛芬相当的抗炎活性,并且与迷迭香酸含量较低的纳米纤维相比具有更高的抗氧化活性。此外,纳米纤维提取物对细胞没有产生任何重大有害影响。迷迭香酸的持续释放以及负载迷迭香酸的纳米纤维的生物活性证实了所制备的基质作为药物递送系统的潜力。

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