Preparation and in vitro and in vivo evaluations of 10-hydroxycamptothecin liposomes modified with stearyl glycyrrhetinate
Preparation and in vitro and in vivo evaluations of 10-hydroxycamptothecin liposomes modified with stearyl glycyrrhetinate
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DOI：
10.1080/10717544.2019.1636422
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发表时间：
2019-01
期刊：
影响因子：
6
通讯作者：
Ting Zhou;Xin Tang;Wei Zhang;Jianfang Feng;Wei Wu
中科院分区：
文献类型：
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作者：
Ting Zhou;Xin Tang;Wei Zhang;Jianfang Feng;Wei Wu
摘要采用薄膜分散法制备了羟基喜树碱（HCPT）脂质体，并对其表面进行了修饰。对脂质体进行了体外释药、药代动力学和组织分布等表征。采用高效液相色谱法（HPLC）测定血浆和组织中的HCPT。与常规羟基喜树碱脂质体和市售羟基喜树碱注射液（HCPT Inject）相比，SG-HCPT脂质体具有更好的生物利用度。关于组织分布，SG修饰脂质体负载的HCPT在肝脏中的浓度高于其他组织，对肾脏的风险低于HCPT-脂质体和HCPT注射液。这些结果支持SG修饰的HCPT-脂质体通过大黄酸（GA）受体显示增强的肝靶向性的假设，这可能有助于改善未来肝脏疾病的治疗方法。
Abstract 10-Hydroxycamptothecin (HCPT) liposomes surface modified with stearyl glycyrrhetinate (SG) were prepared by the film dispersion method. Characterization of the liposomes, including drug release in vitro, pharmacokinetics and tissue distribution, was done. HCPT in plasma and tissues was determined by high-performance liquid chromatography (HPLC). Compared with the conventional HCPT-liposomes and commercially available hydroxycamptothecin injection (HCPT Inject), pharmacokinetic parameters indicated that SG-HCPT-liposomes had better bioavailability. Regarding tissue distribution, the concentration of HCPT loaded by SG modified liposomes in the liver was higher than other tissues and the risk to the kidney was lower than HCPT-liposomes and HCPT Inject. These results support the hypothesis that the HCPT-liposomes modified with SG show enhanced liver-targeting through the glycyrrhetinic acid (GA) receptor to be an efficient drug carrier, which may help to improve therapeutic methods for hepatic diseases in the future.