Page 148 - 《精细化工》2022年第7期
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第 39 卷第 7 期                             精   细   化   工                                  Vol.39, No.7
             2022 年 7 月                              FINE CHEMICALS                                  July  2022


              医药与日化原料
                                热响应全氟聚醚丙烯酸酯共聚物


                                            的制备及载药性能



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                      徐德忠      1,2 ,肖旺钏      1,2 ,林伟杰 ,王长园 ,李   翱 ,黄   方
                 (1.  福建农林大学  材料工程学院,福建  福州  350108;2.  三明学院  资源与化工学院,福建  三明
                   365004;3.  福建医科大学附属协和医院  小儿外科,福建  福州  350001)
                 摘要:以甲基丙烯酸羟乙酯(HEMA)和全氟聚醚酰氟(HFPO)反应生成的全氟聚醚酰氟甲基丙烯酸羟乙酯
                 (PFPHM)为疏水内核,N,N-二甲基丙烯酰胺(DMAA)为热响应功能段,聚乙二醇甲基丙烯酸酯(PEGMA 360 )
                 为亲水外壳,通过 3 次原子转移自由基聚合反应制备出热响应聚合物〔P(PFPHM 9 -b-DMAA-b-PEGMA 360 )〕,考
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                 察了其对盐酸阿霉素(DOX/HCl)的载药性能。通过 FNMR、 HNMR、FTIR、DLS、UV-Vis、激光共聚焦显
                 微镜和荧光分光光度计对其化学结构、临界胶束浓度(CMC)、最低临界溶解温度(LCST)、生物毒性、胶束稳
                 定性及载药性能进行了研究。结果表明,P(PFPHM 9 -b-DMAA-b-PEGMA 360 )的 CMC 为 1.0 μg/mL,LCST 为 38.7  ℃,
                 胶束稳定性良好,载药量为 20.6%,包封率为 86.6%,在 42 和 37  ℃下,72 h 的累积释药率分别为 91.9%和 35.4%,
                 表明 P(PFPHM 9 -b-DMAA-b-PEGMA 360 )具有热响应性,作为 DOX/HCl 物载体具有很大潜力。
                 关键词:热响应性;全氟聚醚酰氟;两亲性;药物载体;最低临界溶解温度;医药原料
                 中图分类号:TQ460.1;TQ317      文献标识码:A      文章编号:1003-5214 (2022) 07-1434-09


                      Preparation and drug loading properties of thermally responsive

                                     perfluoropolyether acrylate copolymer

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                  XU Dezhong , XIAO Wangchuan , LIN Weijie , WANG Changyuan , LI Ao , HUANG Fang
                 (1. School of Materials Engineering, Fujian  Agriculture and Forestry University, Fuzhou  350108,  Fujian, China;
                 2. School of Resources and Chemical Engineering, Sanming College, Sanming 365004, Fujian, China; 3. Department of
                 Pediatric Surgery, Fujian Medical University Union Hospital, Fuzhou 350001, Fujian, China)
                 Abstract: Thermally responsive  polymer [P(PFPHM 9-b-DMAA-b-PEGMA 360)]  was prepared by atom
                 transfer  radical polymerization using  perfluoropolyetheryl fluoromethyl acrylate (PFPHM) synthesized
                 from hydroxyethyl  methacrylate (HEMA) and hexafluoropropylene  oxide (HFPO) as hydrophobic  core,
                 N,N-dimethylacrylamide as thermal response function segment, and poly(polyethylene glycol methacrylate 360 ) as
                 hydrophilic shell. Then, its  DOX/HCl  drug loading  properties  was investigated. The chemical structure,
                 critical  micelle concentration  (CMC), lower critical  solution  temperature (LCST), biological  toxicity,
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                 stability of  micelles and  drug loading properties were characterized and analyzed  by  FNMR, HNMR,
                 FTIR, DLS, UV-Vis, laser confocal microscopy and fluorescence spectrophotometer. The results showed
                 that P(PFPHM 9-b-DMAA-b-PEGMA 360) exhibited a CMC of 1.0 μg/mL, LCST of 38.7  ℃ and excellent
                 micelle stability. Moreover, analysis of drug loading indicated that the polymer displayed a drug loading
                 capacity for DOX/HCl of 20.6%, encapsulation rate of 86.6%, and 72 h cumulative drug release rate at
                 42 and 37  ℃  were 91.9% and 35.4%, respectively, which suggested that P(PFPHM 9 -b-DMAA-b-PEGMA 360 )
                 was temperature sensitive and had great potential as a drug carrier for DOX/HCl.


                 收稿日期:2021-11-27;  定用日期:2022-03-28; DOI: 10.13550/j.jxhg.20211211
                 基金项目:国家自然科学基金项目(22078061);福建省科技创新联合资金资助项目(2018Y9003);福建省自然科学基金项目(2018J01305)
                 作者简介:徐德忠(1995—),男,硕士生,E-mail:dezhongxu@fafu.edu.cn。联系人:黄   方(1974—),男,博士,副教授,E-mail:
                 fang.huang@fafu.edu.cn。
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