Biomedicines. 2022 Apr 14
Weiming Xu, Yijun Niu, Xin Ai, Chengjie Xia, Ping Geng, Haiyan Zhu, Wei Zhou, Hai Huang, and Xunlong Shi
Products used in the paper Details Operation
AAVDJ vectors The HepG2 cells were transfected with AAVDJ vectors (PackGene Biotech, Guangzhou, China) carrying the HBV genome (genotype B) and called the AAVDJ- transfected HepG2 cells. Request Quote

Research Field: liver

Keywords: baicalin, liposomes, HBV, bioavailability, liver-targeted drug delivery, apolipoprotein A1

AAV Serotype: AAVDJ vectors


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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