School of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui 230012, China; Traditional Chinese Hospital of LuAn, Luan, Anhui 237006, China.
School of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui 230012, China.
Nanomedicine. 2024 Nov;62:102786. doi: 10.1016/j.nano.2024.102786. Epub 2024 Sep 27.
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).
葛根素(Pur)的口服生物利用度低,影响其疗效。制备葛根素立方液晶纳米粒(Pur-Cub)可通过提高其生物利用度来增强 Pur 对缺血性脑卒中(IS)的保护作用。Pur-Cub 的平均粒径、PDI 和 Zeta 电位分别为 274.70±16.20nm、0.24±0.05 和-25.30±2.34mV。偏光显微镜(PLM)和小角 X 射线衍射(SAXS)表明 Pur-Cub 为立方相(Pn3m)。Pur-Cub 的体外释放速度先快后慢,符合双相动力学方程。与 Pur 混悬液相比,Pur-Cub 增加了 Pur 在肠道(主要是十二指肠)中的渗透,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)。Pur-Cub 缩小了脑梗死范围,显著降低了大脑中动脉闭塞(MCAO)大鼠模型中 TNF-α、IL-1β 和 IL-6 的水平。