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Pharmaceuticals
Volume 14
Issue 10
10.3390/ph14100951
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Article

Costunolide Loaded in pH-Responsive Mesoporous Silica Nanoparticles for Increased Stability and an Enhanced Anti-Fibrotic Effect

by
Xia Niu
†,
Xiaomei Wang
†,
Bingyu Niu
,
Yanan Meng
,
Hongwei He
,
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.
Pharmaceuticals 2021, 14(10), 951; https://doi.org/10.3390/ph14100951
Submission received: 26 August 2021 / Revised: 18 September 2021 / Accepted: 20 September 2021 / Published: 23 September 2021
(This article belongs to the Section Pharmaceutical Technology)
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Abstract

Liver fibrosis remains a significant public health problem. However, few drugs have yet been validated. Costunolide (COS), as a monomeric component of the traditional Chinese medicinal herb Saussurea Lappa, has shown excellent anti-fibrotic efficacy. However, COS displays very poor aqueous solubility and poor stability in gastric juice, which greatly limits its application via an oral administration. To increase the stability, improve the dissolution rate and enhance the anti-liver fibrosis of COS, pH-responsive mesoporous silica nanoparticles (MSNs) were selected as a drug carrier. Methacrylic acid copolymer (MAC) as a pH-sensitive material was used to coat the surface of MSNs. The drug release behavior and anti-liver fibrosis effects of MSNs-COS-MAC were evaluated. The results showed that MSNs-COS-MAC prevented a release in the gastric fluid and enhanced the dissolution rate of COS in the intestinal juice. At half the dose of COS, MSNs-COS-MAC still effectively ameliorated parenchymal necrosis, bile duct proliferation and excessive collagen. MSNs-COS-MAC significantly repressed hepatic fibrogenesis by decreasing the expression of hepatic fibrogenic markers in LX-2 cells and liver tissue. These results suggest that MSNs-COS-MAC shows great promise for anti-liver fibrosis treatment.
Keywords: pH-responsive mesoporous silica nanoparticles; costunolide; stability; dissolution rate; anti-liver fibrosis pH-responsive mesoporous silica nanoparticles; costunolide; stability; dissolution rate; anti-liver fibrosis
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MDPI and ACS Style

Niu, X.; Wang, X.; Niu, B.; Meng, Y.; He, H.; Wang, Y.; Li, G. Costunolide Loaded in pH-Responsive Mesoporous Silica Nanoparticles for Increased Stability and an Enhanced Anti-Fibrotic Effect. Pharmaceuticals 2021, 14, 951. https://doi.org/10.3390/ph14100951

AMA Style

Niu X, Wang X, Niu B, Meng Y, He H, Wang Y, Li G. Costunolide Loaded in pH-Responsive Mesoporous Silica Nanoparticles for Increased Stability and an Enhanced Anti-Fibrotic Effect. Pharmaceuticals. 2021; 14(10):951. https://doi.org/10.3390/ph14100951

Chicago/Turabian Style

Niu, Xia, Xiaomei Wang, Bingyu Niu, Yanan Meng, Hongwei He, Yucheng Wang, and Guiling Li. 2021. "Costunolide Loaded in pH-Responsive Mesoporous Silica Nanoparticles for Increased Stability and an Enhanced Anti-Fibrotic Effect" Pharmaceuticals 14, no. 10: 951. https://doi.org/10.3390/ph14100951

APA Style

Niu, X., Wang, X., Niu, B., Meng, Y., He, H., Wang, Y., & Li, G. (2021). Costunolide Loaded in pH-Responsive Mesoporous Silica Nanoparticles for Increased Stability and an Enhanced Anti-Fibrotic Effect. Pharmaceuticals, 14(10), 951. https://doi.org/10.3390/ph14100951

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