A Tenofovir-Loaded Glycyrrhetinic Acid-Modified Cationic Liposome for Targeted Therapy of Hepatitis B Virus.

Dongping Yao, Dongtao Liu, Ruijie Luo, Siyan He, Lang Bai, Yang Yang, Jialin Ma, Xi He, Mingxing Hu, Haozhong Luo, Bin Chen, Feng Liu, Tinghong Ye, Xiangrong Song, Zhongwei Zhang, Yongmei Xie

Journal of biomedical nanotechnology 2020 Oct 01

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Tenofovir (TFV), an acyclic nucleoside analog, exhibits potent anti-HBV activity. However, poor bioavailability, nephrotoxicity and bone toxicity limit its further clinical application. In this work, a novel tenofovir-loaded glycyrrhetinic acidmodified cationic liposome (TGCL) was prepared for targeted therapy of HBV. The TGCL had an average particle size of 107.39 ± 1.21 nm and an entrapment efficiency of 89.83 ± 2.70% with a positive zeta potential of 37.63 ± 1.22 mV. The results of in vitro indicated that the inhibitory effects on HBsAg, HBeAg and HBV cccDNA of TGCL in HepG2.2.15 cells were significantly better than that of free TFV and non-targeted cationic liposome. In the DHBV-infected duck model, TGCL showed remarkably suppression on DHBV DNA than that of free TFV. Overall, TGCL is a promising formulation of TFV for targeted therapy of HBV.

Citation

Dongping Yao, Dongtao Liu, Ruijie Luo, Siyan He, Lang Bai, Yang Yang, Jialin Ma, Xi He, Mingxing Hu, Haozhong Luo, Bin Chen, Feng Liu, Tinghong Ye, Xiangrong Song, Zhongwei Zhang, Yongmei Xie. A Tenofovir-Loaded Glycyrrhetinic Acid-Modified Cationic Liposome for Targeted Therapy of Hepatitis B Virus. Journal of biomedical nanotechnology. 2020 Oct 01;16(10):1504-1517