AUTHOR=Yang Siqi , Lan Jinshuai , Li Zhe , Li Ming , Wu Ya , Sun Liyan , Zhang Tong , Ding Yue 

TITLE=Bufonis venenum extract loaded novel cholesterol-free liposome for the treatment of hepatocellular carcinoma

JOURNAL=Frontiers in Pharmacology

VOLUME=15

YEAR=2024

URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2024.1486742

DOI=10.3389/fphar.2024.1486742

ISSN=1663-9812

ABSTRACT=<sec><title>Background</title><p>This study aims to improve the solubility and the toxicity of Bufonis venenum, and finally enhance the therapeutic outcomes of hepatocellular carcinoma (HCC).</p></sec><sec><title>Methods</title><p>The cholesterol-free liposomes simultaneously encapsulate bufadienolides and indolealkylamines (Non-Cholesterol-Bufonis Venenum Extract-Liposome, Non-Chol-BVE-LP) was prepared by the thin-film evaporation technique. <italic>In vitro</italic>, the cytotoxicity, cell apoptosis study, cellular uptake and hemolysis studies were evaluated in HepG2 cells. <italic>In vivo</italic>, the biodistribution and anti-tumor activity studies were conducted in BALB/C mice with HepG2 cells.</p></sec><sec><title>Results</title><p>The liposomes showed good size distribution, encapsulation efficiency drug loading capacity and slower drug release. Non-Chol-BVE-LP had higher cytotoxicity on HepG2 cells and induced more apoptosis on HepG2 Cells compared with BVE. In addition, the liposomes could accumulate in tumor by passive targeting, thus facilitating the anti-tumor effects. <italic>In vivo</italic>, Non-Chol-BVE-LP showed equivalent anti-tumor efficacy to the first-line anti-HCC drug sorafenib.</p></sec><sec><title>Conclusion</title><p>The study provided new ideas for the development and clinical application of Bufonis venenum related formulation and offered new drug for the treatment of HCC.</p></sec>