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韩露,葛小玲,宋坤,杨祚辉,周倩,袁泽轩,眭维恕,袁华兵,易晓芳.两种连接臂的mPEG-羟基喜树碱纳米粒的性能研究[J].湖南中医药大学学报英文版,2022,42(1):37-43.[Click to copy
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| 两种连接臂的mPEG-羟基喜树碱纳米粒的性能研究 |
| 韩露,葛小玲,宋坤,杨祚辉,周倩,袁泽轩,眭维恕,袁华兵,易晓芳 |
| (天门市第一人民医院药剂科, 湖北 天门 431700;湖南师范大学医学院, 湖南 长沙 410013;湖南师大附中博才实验 中学, 湖南 长沙 410006;天门市第一人民医院药剂科, 湖北 天门 431700;武汉科技大学职业危害识别与控制湖北省重点实验室, 湖北 武汉 430081;长沙市望城区 人民医院妇产科, 湖南 长沙 410200) |
| 摘要: |
| 目的 设计两种连接臂的聚合物纳米粒，研究其自组装性能及酸度调控下的缓释性，为肿瘤组织外酸度调控下的药物定位释放提供研究基础。方法 使用丁二酸酐（succinic anhydride，SA）、乌头酸酐（cis-aconitic anhydride，CA）作为连接臂，将10-羟基喜树碱（10-hydroxycamptothecin，10-HCPT）与聚乙二醇单甲醚（methoxypolyethylene glycols，mPEG）连接，形成mPEG-SA-HCPT（PSH）、mPEG-CA-HCPT（PCH）聚合物。透析法制备纳米粒，核磁共振氢谱、动态光散射、透射电镜、紫外光谱对纳米材料进行性能研究及其体外释放性能测定。结果 核磁共振氢谱结果表明，聚合物成功合成。动态光散射测定PCH纳米粒径约为84.27 nm，负载HCPT后约为90.67 nm，PSH纳米粒径约为94.42 nm，负载HCPT后粒径约为110.8 nm，透射电镜显示纳米粒形态为均匀的圆形。紫外光谱测定载药的PSH纳米粒载药量约为22.1%，载药的PCH纳米粒的载药量约为25.8%。载药后的PSH纳米粒具有明显缓释性，48 h药物释放量达53.26%，pH值为6.8的释放介质下，药物释放明显加快，48 h药物释放量达到85.53%。而载药的酸敏感性的纳米粒子在48 h药物释放率为46.73%，在pH为6.8的条件下48 h释放率为95.77%。结论 两亲性聚合物可以自组装形成圆形纳米粒，通过化学连接和物理包埋两种手段可以得到高负载药物量的纳米粒。聚合纳米材料中的酸敏感连接臂能调控聚合物纳米粒的缓释性。 |
| 关键词: 10-羟基喜树碱 动态光散射 乌头酸酐 核磁共振氢谱 透射电镜 |
| DOI：10.3969/j.issn.1674-070X.2022.01.008 |
| Received:March 17, 2021 |
| 基金项目:湖南省自然科学基金项目（2016JJ2088）；国家级大学生研究性学习和创新性实验计划项目（202010542019，202012652002）；湖北省卫生健康委员会联合基金项目（WJ2019H169）；湖南师范大学大学生创新创业训练计划项目（2020135）；湖南师范大学课程思政建设项目（校行发教务字〔2020〕3号）。 |
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| Study on the properties of two kinds of mPEG-hydroxycamptothecin nanoparticles with connected arms |
| HAN Lu,GE Xiaoling,SONG Kun,YANG Zuohui,ZHOU Qian,YUAN Zexuan,SUI Weishu,YUAN Huabing,YI Xiaofang |
| (Department of Pharmacy, First People's Hospital of Tianmen City, Tianmen, Hubei 431700, China;Medical College of Hunan Normal University, Changsha, Hunan 410013, China;Bocai Experimental Middle School Affiliated to Hunan Normal University, Changsha, Hunan 410006, China;Department of Pharmacy, First People's Hospital of Tianmen City, Tianmen, Hubei 431700, China;Hubei Province Key Laboratory of Occupational Hazard Identification and Control, Wuhan University of Science and Technology, Wuhan, Hubei 430081, China;Department of Obstetrics and Gynecology, People's Hospital of Wangcheng District, Changsha, Hunan 410200, China) |
| Abstract: |
| Objective To study the self-assembly properties and the slow and controlled-release properties under the control of acidity by designing two kinds of polymer nanoparticles with connecting arms, in order to provide a research basis for drug localization and release under the regulation of acidity outside tumor tissue. Methods Succinic anhydride (SA) and aconitic anhydride (CA) was used as connecting arms, 10-hydroxycamptothecin (10-HCPT) was linked with methoxypolyethylene glycols (mPEG) to form mPEG-SA-HCPT (PSH) and mPEG-CA-HCPT (PCH) polymers. The nanoparticles were prepared by dialysis and the properties of nanomaterials were studied by nuclear magnetic resonance (NMR), dynamic light scattering (DLS), transmission electron microscopy (TEM), ultraviolet (UV) spectroscopy and the property of the in vitro release was studied. Results NMR spectroscopy results showed that the polymer was synthesized successfully. The size of PCH nanoparticles was about 84.27 nm, 90.67 nm after loading HCPT, and the size of PSH nanoparticles was about 94.42 nm, 110.8 nm after loading HCPT. TEM showed that the shape of the nanoparticles was uniform and spherical. UV spectroscopy showed the drug loading capacity of PSH nanoparticles and PCH nanoparticles were about 22.1% and 25.8%, respectively. PSH nanoparticles after drug loading showed obvious sustained release, and the drug release reached 53.26% at 48 h. In the release medium of pH 6.8, the drug release was significantly accelerated, and the drug release reached 85.53% at 48 h. The drug release rate of acid sensitive nanoparticles was 46.73% at 48 h and 95.77% at pH 6.8. Conclusion Amphiphilic polymers can self assemble into spherical nanoparticles, and high drug loading nanoparticles can be obtained by chemical bonding and physical embedding. The acid sensitive arm in polymeric nanomaterials can control the slow release property of polymer nanoparticles. |
| Key words: 10-hydroxycamptothecin dynamic light scattering aconitic anhydride nuclear magnetic resonance spectroscopy transmission electron microscopy |
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