Page 148 - 《精细化工》2022年第7期
P. 148
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。