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Article

Novel IMB16-4 Compound Loaded into Silica Nanoparticles Exhibits Enhanced Oral Bioavailability and Increased Anti-Liver Fibrosis In Vitro

by
Xia Niu
†,
Xiaomei Wang
†,
Bingyu Niu
,
Guoqing Li
,
Xinyi Yang
,
Yucheng Wang
* and
Guiling Li
*
Institute of Medicinal Biotechnology, Chinese Academy of Medical Science & Peking Union Medical College, Beijing 100050, China
*
Authors to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Molecules 2021, 26(6), 1545; https://doi.org/10.3390/molecules26061545
Submission received: 9 February 2021 / Revised: 7 March 2021 / Accepted: 8 March 2021 / Published: 11 March 2021
(This article belongs to the Special Issue Nanobiotechnology for Drug Discovery and Diagnostics)
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Abstract

Background: Liver fibrosis, as a common and refractory disease, is challenging to treat due to the lack of effective agents worldwide. Recently, we have developed a novel compound, N-(3,4,5-trichlorophenyl)-2(3-nitrobenzenesulfonamide) benzamide (IMB16-4), which is expected to have good potential effects against liver fibrosis. However, IMB16-4 is water-insoluble and has very low bioavailability. Methods: Mesoporous silica nanoparticles (MSNs) were selected as drug carriers for the purpose of increasing the dissolution of IMB16-4, as well as improving its oral bioavailability and inhibiting liver fibrosis. The physical states of IMB16-4 and IMB16-4-MSNs were investigated using nitrogen adsorption, thermogravimetric analysis (TGA), HPLC, UV-Vis, X-ray diffraction (XRD) and differential scanning calorimetry (DSC). Results: The results show that MSNs enhanced the dissolution rate of IMB16-4 significantly. IMB16-4-MSNs reduced cytotoxicity at high concentrations of IMB16-4 on human hepatic stellate cells LX-2 cells and improved oral bioavailability up to 530% compared with raw IMB16-4 on Sprague–Dawley (SD) rats. In addition, IMB16-4-MSNs repressed hepatic fibrogenesis by decreasing the expression of hepatic fibrogenic markers, including α-smooth muscle actin (α-SMA), transforming growth factor-beta (TGF-β1) and matrix metalloproteinase-2 (MMP2) in LX-2 cells. Conclusions: These results provided powerful information on the use of IMB16-4-MSNs for the treatment of liver fibrosis in the future.
Keywords: mesoporous silica nanoparticle; liver fibrosis; oral bioavailability; TGF-β1; dissolution rate mesoporous silica nanoparticle; liver fibrosis; oral bioavailability; TGF-β1; dissolution rate

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MDPI and ACS Style

Niu, X.; Wang, X.; Niu, B.; Li, G.; Yang, X.; Wang, Y.; Li, G. Novel IMB16-4 Compound Loaded into Silica Nanoparticles Exhibits Enhanced Oral Bioavailability and Increased Anti-Liver Fibrosis In Vitro. Molecules 2021, 26, 1545. https://doi.org/10.3390/molecules26061545

AMA Style

Niu X, Wang X, Niu B, Li G, Yang X, Wang Y, Li G. Novel IMB16-4 Compound Loaded into Silica Nanoparticles Exhibits Enhanced Oral Bioavailability and Increased Anti-Liver Fibrosis In Vitro. Molecules. 2021; 26(6):1545. https://doi.org/10.3390/molecules26061545

Chicago/Turabian Style

Niu, Xia, Xiaomei Wang, Bingyu Niu, Guoqing Li, Xinyi Yang, Yucheng Wang, and Guiling Li. 2021. "Novel IMB16-4 Compound Loaded into Silica Nanoparticles Exhibits Enhanced Oral Bioavailability and Increased Anti-Liver Fibrosis In Vitro" Molecules 26, no. 6: 1545. https://doi.org/10.3390/molecules26061545

APA Style

Niu, X., Wang, X., Niu, B., Li, G., Yang, X., Wang, Y., & Li, G. (2021). Novel IMB16-4 Compound Loaded into Silica Nanoparticles Exhibits Enhanced Oral Bioavailability and Increased Anti-Liver Fibrosis In Vitro. Molecules, 26(6), 1545. https://doi.org/10.3390/molecules26061545

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