J Biomed Nanotechnol. 2020 Oct 1;16(10):1504-1517. doi: 10.1166/jbn.2020.2986.
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 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.
替诺福韦（TFV），一种无环核苷类似物，具有很强的抗 HBV 活性。但是，生物利用度差、肾毒性和骨毒性限制了它的进一步临床应用。在这项工作中，我们制备了一种新型的载替诺福韦的甘草次酸修饰的阳离子脂质体（TGCL），用于 HBV 的靶向治疗。TGCL 的平均粒径为 107.39±1.21nm，包封率为 89.83±2.70%，zeta 电位为 37.63±1.22mV。结果表明，TGCL 在 HepG2.2.15 细胞中对 HBsAg、HBeAg 和 HBV cccDNA 的抑制作用明显优于游离 TFV 和非靶向阳离子脂质体。在 DHBV 感染鸭模型中，TGCL 对 DHBV DNA 的抑制作用明显优于游离 TFV。总之，TGCL 是一种有前途的 TFV 制剂，可用于 HBV 的靶向治疗。
