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| 題名: | Highly bioavailable silibinin nanoparticles inhibit HCV infection. |
| 作者: | 林良宗
Ching-Hsuan Liu, Chun-Ching Lin, Wen-Chan Hsu, Chueh-Yao Chung, Chih-Chan Lin, Alagie Jassey, Shun-Pang Chang, Chen-Jei Tai, Cheng-Jeng Tai, Justin Shields, Christopher D Richardson, Ming-Hong Yen, D Lorne J Tyrrell, Liang-Tzung Lin |
| 貢獻者: | 醫學系微生物免疫學科 |
| 關鍵詞: | Keywords: ANTIVIRAL THERAPY;HCV;HEPATITIS C |
| 日期: | 2017-10 |
| 上傳時間: | 2025-04-02 21:02:54 (UTC+8) |
| 摘要: | Abstract
Objective: Silibinin is a flavonolignan that is well established for its robust antiviral activity against HCV infection and has undergone several clinical trials for the management of hepatitis C. Despite its potency, silibinin suffers from poor solubility and bioavailability, restricting its clinical use. To overcome this limitation, we developed highly bioavailable silibinin nanoparticles (SB-NPs) and evaluated their efficiency against HCV infection.
Design: SB-NPs were prepared using a nanoemulsification technique and were physicochemically characterised. Infectious HCV culture systems were used to evaluate the influence of SB-NP on the virus life cycle and examine their antioxidant activity against HCV-induced oxidative stress. The safety profiles of SB-NP, in vivo pharmacokinetic studies and antiviral activity against infection of primary human hepatocytes were also assessed.
Results: SB-NP consisted of nanoscale spherical particles (<200 nm) encapsulating amorphous silibinin at >97% efficiency and increasing the compound's solubility by >75%. Treatment with SB-NP efficiently restricted HCV cell-to-cell transmission, suggesting that they retained silibinin's robust anti-HCV activity. In addition, SB-NP exerted an antioxidant effect via their free radical scavenging function. Oral administration of SB-NP in rodents produced no apparent in vivo toxicity, and pharmacokinetic studies revealed an enhanced serum level and superior biodistribution to the liver compared with non-modified silibinin. Finally, SB-NP efficiently reduced HCV infection of primary human hepatocytes.
Conclusions: Due to SB-NP's enhanced bioavailability, effective anti-HCV activity and an overall hepatoprotective effect, we suggest that SB-NP may be a cost-effective anti-HCV agent that merits further evaluation for the treatment of hepatitis C. |
| 關聯: | Gut. 2017 Oct; 66(10): 1853-1861 |
| 描述: | 【108-1 升等】臺北醫學大學教師升等專門著作
職別：專任
送審等級：教授
著作送審 |
| 資料類型: | article |
| 顯示於類別: | [教師升等送審著作] 108
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