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芍药苷纳米颗粒在大鼠模型中的评价及肠道吸收特性研究

evaluation and intestinal absorption characterisation of paeoniflorin nanoparticles in a rat model.

作者信息

Xiao Yifei, Wei Qidong, Du Lixin, Guo Zhihua, Li Ya

机构信息

School of Pharmacy, Hunan University of Chinese Medicine Changsha 410208 China

School of Chinese Medicine, Hunan University of Chinese Medicine Changsha 410208 China.

出版信息

RSC Adv. 2024 Jul 12;14(31):22113-22122. doi: 10.1039/d4ra03419h.

Abstract

: the aim of this study was to improve the stability and bioavailability of paeoniflorin (PF) by using nanoparticle encapsulation technology. : paeoniflorin nanoparticles (PF NPs) were prepared with PLGA as the carrier using the compound emulsion method. The nanoparticles were characterised by using a Malvern laser particle sizer, transmission electron microscope (TEM), X-ray diffraction (XRD) analyser, and Fourier-transform infrared (FT-IR) spectrometry. The PF NPs were subjected to a series of stability investigations (such as for 4 °C storage stability, pH stability, and thermal stability), lyophilisation protection technology investigations, and release studies. Finally, the intestinal absorption properties of PF and PF NPs were studied by the single-pass intestinal perfusion (SPIP) rat model, using the effective permeability coefficient ( ) and the absorption rate constant ( ) as relevant indexes. : the prepared nanoparticles had a particle size of 105.0 nm with blue opalescent, rounded morphology, uniform size, good stability and slow release. We found that 4% alginate was the best lyoprotectant for the PF NPs. In the intestinal absorption experiments, was higher for the PF NPs group compared with the original PF material drug group in all intestinal segments ( < 0.05), and the absorption rate constant increased with the increase in the drug concentration. : the nanoparticles produced by this method have good stability and a slow-release effect; they can thus improve the absorption of PF in rat intestines, helping improve the stability and bioavailability of PF and enhancing its pharmacological effects.

摘要

本研究的目的是通过使用纳米颗粒包封技术提高芍药苷(PF)的稳定性和生物利用度。采用复合乳液法,以聚乳酸-羟基乙酸共聚物(PLGA)为载体制备芍药苷纳米颗粒(PF NPs)。通过马尔文激光粒度仪、透射电子显微镜(TEM)、X射线衍射(XRD)分析仪和傅里叶变换红外(FT-IR)光谱对纳米颗粒进行表征。对PF NPs进行了一系列稳定性研究(如4℃储存稳定性、pH稳定性和热稳定性)、冻干保护技术研究及释放研究。最后,采用单通道肠道灌注(SPIP)大鼠模型,以有效渗透系数( )和吸收速率常数( )为相关指标,研究PF和PF NPs的肠道吸收特性。制备的纳米颗粒粒径为105.0 nm,呈蓝色乳光,形态圆润,尺寸均匀,稳定性好,释放缓慢。我们发现4%的海藻酸盐是PF NPs最好的冻干保护剂。在肠道吸收实验中,PF NPs组在所有肠段的 均高于原PF原料药组( <0.05),且吸收速率常数 随药物浓度的增加而增大。通过该方法制备的纳米颗粒具有良好的稳定性和缓释效果;因此,它们可以提高PF在大鼠肠道中的吸收,有助于提高PF的稳定性和生物利用度,并增强其药理作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bd5/11240214/db64ad363959/d4ra03419h-f1.jpg

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