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用于治疗利什曼病的黑种草籽油包封聚己内酯纳米颗粒

Nigella sativa oil entrapped polycaprolactone nanoparticles for leishmaniasis treatment.

作者信息

Abamor Emrah Sefik, Tosyali Ozlem Ayse, Bagirova Melahat, Allahverdiyev Adil

机构信息

Bioengineering Department, Yildiz Technical University, Esenler, Istanbul, Turkey.

出版信息

IET Nanobiotechnol. 2018 Dec;12(8):1018-1026. doi: 10.1049/iet-nbt.2018.5115.

Abstract

This study is the first to investigate the antileishmanial activities of Nigella sativa oil (NSO) entrapped poly--caprolactone (PCL) nanoparticles on promastigotes and amastigotes in vitro. NSO molecules with variable initial doses of 50, 100, 150, and 200 mg were successfully encapsulated into PCL nanoparticles identified as formulations NSO1, NSO2, NSO3, and NSO4, respectively. This process was characterised by scanning electron microscope, dynamic light scattering, Fourier transform infrared, encapsulation efficiency measurements, and release profile evaluations. The resulting synthetised nanoparticles had sizes ranging between 200 and 390 nm. PCL nanoparticles encapsulated 98% to 80% of initial doses of NSO and after incubation released approximately 85% of entrapped oil molecules after 288 h. All investigated formulations demonstrated strong antileishmanial effects on promastigotes by inhibiting up to 90% of parasites after 192 h. The tested formulations decreased infection indexes of macrophages in a range between 2.4- and 4.1-fold in contrast to control, thus indicating the strong anti-amastigote activities of NSO encapsulated PCL nanoparticles. Furthermore, NSO-loaded PCL nanoparticles showed immunomodulatory effects by increasing produced nitric oxide amounts within macrophages by 2-3.5-fold in contrast to use of free oil. The obtained data showed significant antileishmanial effects of NSO encapsulated PCL nanoparticles on promastigotes and amastigotes.

摘要

本研究首次调查了包裹于聚己内酯(PCL)纳米颗粒中的黑种草籽油(NSO)对前鞭毛体和无鞭毛体的体外抗利什曼原虫活性。分别将初始剂量为50、100、150和200mg的NSO分子成功封装到PCL纳米颗粒中,这些纳米颗粒分别被鉴定为制剂NSO1、NSO2、NSO3和NSO4。通过扫描电子显微镜、动态光散射、傅里叶变换红外光谱、包封率测量和释放曲线评估对该过程进行了表征。合成得到的纳米颗粒尺寸在200至390nm之间。PCL纳米颗粒包封了80%至98%的NSO初始剂量,孵育后288小时释放了约85%的包封油分子。所有研究的制剂对前鞭毛体均表现出较强的抗利什曼原虫作用,192小时后可抑制高达90%的寄生虫。与对照组相比,测试制剂使巨噬细胞的感染指数降低了2.4至4.1倍,这表明包裹NSO的PCL纳米颗粒具有较强的抗无鞭毛体活性。此外,与使用游离油相比,负载NSO的PCL纳米颗粒通过使巨噬细胞内产生的一氧化氮量增加2至3.5倍而表现出免疫调节作用。所得数据表明,包裹NSO的PCL纳米颗粒对前鞭毛体和无鞭毛体具有显著的抗利什曼原虫作用。

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