葛根素立方液晶纳米颗粒的制备及其对缺血性中风的保护作用

IF 4.6 2区医学 Q2 MEDICINE, RESEARCH & EXPERIMENTAL

Nanomedicine : nanotechnology, biology, and medicine Pub Date : 2024-09-27 DOI:10.1016/j.nano.2024.102786

Jingbao Chen MD , Yuhang Xu MD , Yue Liu MD , Yun Meng MD , Long Wu MD , Wenxuan Cao MD , Dayuan Jiang MD , Xiaoqin Chu PhD

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引用次数: 0

摘要

葛根素（Pur）的口服生物利用度较低，影响了其药效。制备葛根素立方液晶纳米颗粒（Pur-Cub）可提高葛根素的生物利用度，从而增强其对缺血性中风（IS）的保护作用。Pur-Cub 的平均粒径、PDI 和 zeta 电位分别为 274.70 ± 16.20 nm、0.24 ± 0.05 和 -25.30 ± 2.34 mV。偏光显微镜（PLM）和小角 X 射线衍射（SAXS）确定 Pur-Cub 为立方相（Pn3m）。Pur-Cub 的体外释放先快后慢，符合双相动力学方程。与 Pur 悬浮液相比，Pur-Cub 增加了 Pur 在肠道（主要是十二指肠）中的渗透性，并显著提高了 Pur 在血液中的生物利用度（304.16%）及其在大脑中的分布（1.69 倍）。在大脑中动脉闭塞（MCAO）大鼠模型中，Pur-Cub缩小了脑梗塞的范围，并显著降低了TNF-α、IL-1β和IL-6的水平。

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Preparation of cubic liquid crystal nanoparticles of puerarin and its protective effect on ischemic stroke

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Preparation of cubic liquid crystal nanoparticles of puerarin and its protective effect on ischemic stroke

The low oral bioavailability of puerarin (Pur) affects its efficacy. Preparation of puerarin cubic liquid crystal nanoparticles (Pur-Cub) enhances the protective effect of Pur against ischemic stroke (IS) by increasing its bioavailability. The average particle size, PDI, and zeta potential of Pur-Cub were 274.70 ± 16.20 nm, 0.24 ± 0.05 and −25.30 ± 2.34 mV, respectively. Polarized light microscopy (PLM) and Small angle X-ray diffraction (SAXS) identified Pur-Cub as a cubic phase (Pn3m). The in vitro release of Pur-Cub was fast and then slow, in accordance with the biphasic kinetic equation. Pur-Cub increased the penetration of Pur in the intestine (mainly the duodenum) and significantly improved the bioavailability of Pur in the blood (304.16 %) and its distribution in the brain (1.69-fold) compared to Pur suspension. Pur-Cub narrowed down cerebral infarcts and significantly reduced levels of TNF-α, IL-1β, and IL-6 in a rat model of middle cerebral artery occlusion (MCAO).

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来源期刊

Nanomedicine : nanotechnology, biology, and medicine 工程技术-纳米科技

CiteScore

11.10

自引率

0.00%

发文量

133

审稿时长

42 days

期刊介绍： The mission of Nanomedicine: Nanotechnology, Biology, and Medicine (Nanomedicine: NBM) is to promote the emerging interdisciplinary field of nanomedicine. Nanomedicine: NBM is an international, peer-reviewed journal presenting novel, significant, and interdisciplinary theoretical and experimental results related to nanoscience and nanotechnology in the life and health sciences. Content includes basic, translational, and clinical research addressing diagnosis, treatment, monitoring, prediction, and prevention of diseases.