甘草次酸衍生物18-GA-Gly介导肝主动靶向脂质体的制备及体内相关研究

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基于国内外对甘草次酸配体介导主动肝靶向脂质体的研究情况,该文主要对以甘草次酸为母核的肝靶向配体18-GA-Gly修饰的脂质体的肝靶向效果进行研究。采用薄膜分散-高压乳匀法制备18-GA-Gly配体介导的丹参酚酸B-丹参酮ⅡA脂质体及未修饰配体的脂质体,考察2种脂质体的制剂学性质,考察粒径、电位、包封率和配体结合率;尾静脉给药后不同时间点获取血浆样本以及小鼠心、肝、脾、肺、肾组织样本,UPLC测定各样本中丹参酚酸B(Sal B)和丹参酮IIA(TSN)含量,评价18-GA-Gly配体的肝靶向效果。结果显示脂质体Gly-TS-Lip和TS-Lip的粒径、电位、包封率、配体结合率基本符合要求;体内靶向性考察结果显示Gly-TS-Lip组脂质体与TS-Lip组脂质体血浆数据无显著性差别;甘草次酸衍生物配体18-GA-Gly介导脂质体可以增加Sal B和TSN在肝组织的峰浓度,但并未显示明显的肝靶向效果。 Based on the domestic and foreign research on glycyrrhetic acid-mediated active liver-targeted liposomes, this paper mainly focused on glycosaminoglycan-based liver targeting ligand 18-GA-Gly modified liposome Liver targeting effects were studied. Liposomes of 18-GA-Gly ligand-mediated liposomes and unmodified ligands of salvianolic acid B-tanshinoneⅡA were prepared by thin-film dispersion-high pressure homogenization. The preparation and characterization of the two liposomes were investigated. The particle size, potential, entrapment efficiency and ligand binding rate were investigated. The plasma samples and the heart, liver, spleen, lung and kidney samples were obtained at different time points after tail vein administration. The concentrations of salvianolic acid B (Sal B) and tanshinone IIA (TSN) content, the liver targeting effect of 18-GA-Gly ligand was evaluated. The results showed that the particle size, potential, entrapment efficiency and ligand binding rate of Gly-TS-Lip and TS-Lip of liposomes basically met the requirements. In vivo targeting assay showed that the interaction between Gly-TS-Lip liposome and TS Lipid plasma lipids did not show any significant difference between liposomes and liposomes. Liposomes with 18-GA-Gly, a ligand of glycyrrhetic acid derivative, could increase the peak concentrations of Sal B and TSN in liver tissue but did not show obvious liver Targeted effects.
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