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建立脂质体包被的 IMB16-4 聚合物纳米颗粒（LNPs）以增加细胞摄取并在体外发挥抗纤维化作用。

Established Liposome-Coated IMB16-4 Polymeric Nanoparticles (LNPs) for Increasing Cellular Uptake and Anti-Fibrotic Effects In Vitro.

机构信息

Institute of Medicinal Biotechnology, Chinese Academy of Medical Science & Peking Union Medical College, Beijing 100050, China.

出版信息

Molecules. 2022 Jun 10;27(12):3738. doi: 10.3390/molecules27123738.

DOI:10.3390/molecules27123738
PMID:35744862
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9230879/
Abstract

As a global health problem, liver fibrosis still does not have approved treatment. It was proved that -(3,4,5-trichlorophenyl)-2(3-nitrobenzenesulfonamide) benzamide (IMB16-4) has anti-hepatic fibrosis activity. However, IMB16-4 displays poor water solubility and poor bioavailability. We are devoted to developing biodegraded liposome-coated polymeric nanoparticles (LNPs) as IMB16-4 delivery systems for improving aqueous solubility, cellular uptake, and anti-fibrotic effects. The physical states of IMB16-4-LNPs were analyzed using a transmission electron microscope (TEM), high-performance liquid chromatography (HPLC), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD) and differential scanning calorimeter (DSC). The results show that IMB16-4-LNPs increased the drug loading compared to liposomes and enhanced cellular uptake behavior compared with IMB16-4-NPs. In addition, IMB16-4-LNPs could repress the expression of hepatic fibrogenesis-associated proteins, indicating that IMB16-4-LNPs exhibited evident anti-fibrotic effects.

摘要

作为一个全球性的健康问题，肝纤维化仍然没有被批准的治疗方法。研究证明，（3,4,5-三氯苯基）-2（3-硝基苯磺酰胺）苯甲酰胺（IMB16-4）具有抗肝纤维化活性。然而，IMB16-4 的水溶性差，生物利用度低。我们致力于开发可生物降解的脂质体包覆的聚合物纳米粒（LNPs）作为 IMB16-4 递药系统，以提高其水溶解度、细胞摄取率和抗纤维化效果。使用透射电子显微镜（TEM）、高效液相色谱（HPLC）、傅里叶变换红外光谱（FTIR）、X 射线衍射（XRD）和差示扫描量热法（DSC）分析了 IMB16-4-LNPs 的物理状态。结果表明，与脂质体相比，IMB16-4-LNPs 增加了药物载药量，与 IMB16-4-NPs 相比，增强了细胞摄取行为。此外，IMB16-4-LNPs 可以抑制肝纤维化相关蛋白的表达，表明 IMB16-4-LNPs 具有明显的抗纤维化作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de3f/9230879/eeed8ca08d8e/molecules-27-03738-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de3f/9230879/92361c1f1e90/molecules-27-03738-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de3f/9230879/1b662bc94bef/molecules-27-03738-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de3f/9230879/544c1ac722ef/molecules-27-03738-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de3f/9230879/f018a0ba8b9d/molecules-27-03738-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de3f/9230879/3b90828ea358/molecules-27-03738-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de3f/9230879/eeed8ca08d8e/molecules-27-03738-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de3f/9230879/92361c1f1e90/molecules-27-03738-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de3f/9230879/1b662bc94bef/molecules-27-03738-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de3f/9230879/544c1ac722ef/molecules-27-03738-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de3f/9230879/f018a0ba8b9d/molecules-27-03738-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de3f/9230879/3b90828ea358/molecules-27-03738-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de3f/9230879/eeed8ca08d8e/molecules-27-03738-g006.jpg

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2
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3
Molecular and cellular mechanisms of liver fibrosis and its regression.
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Regression of liver fibrosis: evidence and challenges.肝纤维化的逆转：证据与挑战。
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