载替诺福韦的甘草次酸修饰阳离子脂质体用于乙型肝炎病毒的靶向治疗。
A Tenofovir-Loaded Glycyrrhetinic Acid-Modified Cationic Liposome for Targeted Therapy of Hepatitis B Virus.
出版信息
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。
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