GalNAc修饰的HepG2细胞靶向的紫杉醇脂质体研究  

Study on Paclitaxel Liposomes Modified by GalNAc Targeting HepG2 Cells

作　　者：钟娜娜 张娟 聂华[1] 刘小敏 Zhong Nana;Zhang Juan;Nie Hua;Liu Xiaomin(Medical College of Jiaying University,Meizhou 514031,China)

机构地区：[1]嘉应学院医学院,广东梅州514031

出　　处：《广东化工》2021年第12期61-63,55,共4页Guangdong Chemical Industry

基　　金：广东省自然科学基金项目(2017A030307025);广东省医学科研基金项目(A2020372);2019年大学生创新创业训练计划国家级项目(201910582030);梅州市应用型科技专项资金项目(2020B0205003)。

摘　　要：目的:构建一种半乳糖修饰的肝靶向紫杉醇脂质体,并对其制备工艺进行筛选优化。方法:采用生物酶催化法,在反应介质丙酮和脂肪酶催化下,合成肝靶向脂质材料GalNAc-C8-Chol,并利用ESI-MS、NMR表征确证产物结构;以薄膜分散法制备NGal-PTX-LP,对其处方中膜材比、药脂比、DSPG-Na和MCT用量进行单因素优化。结果:经ESI-MS、NMR确证为目标产物,NGal-PTX-LP最佳制备工艺为:胆固醇与氢化大豆磷脂比例为3︰8,DSPG-Na用量为6.25%,MCT用量为2.50%,药脂比为1︰16。结论:酶促法合成GalNAc-C8-Chol,反应条件温和,无毒高效,绿色环保,潜在应用价值大。经工艺优化的NGal-PTX-LP粒径适中、稳定性好,包封率高。Objective:To construct a liver targeted paclitaxel liposome modified and optimize its preparation process.Methods:With the catalysis of acetone and Lipozyme TL IM lipase,liver targeted lipid material was synthesized.The structure of the product was characterized by ESI-MS and NMR.NGal-PTX-LP was prepared by thin film dispersion method,and single factor investigation was carried out to optimize the dosage of film material.Results:ESI-MS and NMR confirmed that GalNAc-C8-Chol was the target product,and the optimal preparation process of NGal-PTX-LP was as follows:the ratio of CHS to hydrogenated soybean phospholipid(HSPC)was 3︰8,the dosage of DSPG-Na was 6.25%,the dosage of MCT was 2.50%,and the ratio of PTX to HSPC was 1︰16.Conclusion:The enzymatic synthesis of GalNAc-C8-Chol is mild,non-toxic and efficient,green and environmentally friendly.The optimized NGal-PTX-LP has moderate particle size,good stability and high encapsulation rate.

关 键 词：生物酶催化法 肝靶向 胆固醇衍生物 紫杉醇脂质体 单因素考察 

分 类 号：TQ[化学工程]