Liver-Targeted Nanoparticles Facilitate the Bioavailability and Anti-HBV Efficacy of Baicalin In Vitro and In Vivo

Autor: Weiming Xu, Yijun Niu, Xin Ai, Chengjie Xia, Ping Geng, Haiyan Zhu, Wei Zhou, Hai Huang, Xunlong Shi
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Biomedicines, Vol 10, Iss 4, p 900 (2022)
Druh dokumentu: article
ISSN: 10040900
2227-9059
DOI: 10.3390/biomedicines10040900
Popis: The anti-hepatitis B virus (HBV) efficacy of baicalin (BA) is mediated by HBV-related hepatocyte nuclear factors (HNFs). However, this efficacy is severely limited by the low bioavailability of BA. Therefore, a novel liver-targeted BA liposome was constructed to promote the bioavailability and antiviral ability of BA. The results showed that apolipoprotein A1 (ApoA1)–modified liposomes (BAA1) significantly enhanced BA’s cellular uptake and specific distribution in the liver. Furthermore, the substantial inhibitory effects of BAA1 on HBsAg, HBeAg, HBV RNA, and HBV DNA were assessed in HB-infected cells and mice. Western blotting, co-immunoprecipitation, and transcriptomics analysis further revealed that the enhanced anti-HBV efficacy of BAA1 was attributed to the interaction between hepatocyte nuclear factors (HNFs) and estrogen receptors (ERs). Based on the findings, we propose that the ApoA1-modified liposomes aid BA in inhibiting HBV transcription and replication by augmenting its bioavailability and the HNFs–ERs axis.
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