文章摘要
键合SN38的磺酸甜菜碱胶束药物载体的合成与表征
Synthesis and Characterization of Micellar Drug Carriers of SN38-Linked Amphiphilic Random Copolymers Containing Sulfobetaines
  
DOI:10.16865/j.cnki.1000-7555.2018.05.001
中文关键词: 胶束  药物载体  pH/还原双敏感性  聚磺酸甜菜碱
英文关键词: micelles  drug carrier  pH/reduction sensitive  polysulfonatebetaine
基金项目:国家自然科学基金资助项目(51473099;51673129)
作者单位
黎 洪1, 蔡媛媛1, 李 帅1, 罗祥林1,2 1. 四川大学 高分子科学与工程学院2. 高分子材料工程国家重点实验室(四川大学)四川 成都 610065 
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中文摘要:
      高分子胶束在肿瘤治疗方面显现出美好的前景。文中通过电子活化再生原子转移自由基聚合(AGET ATRP)以及磺化反应合成了两亲性的无规共聚高分子,并通过二硫代二丙酸将SN38(7-乙基-10-羟基喜树碱)接枝到该高分子上得到了聚[(甲基丙烯酸羟乙酯/甲基丙烯酸羟乙酯ss-SN38)]-co-(甲基丙烯酸N,N-二乙氨基乙基酯/N,N-二乙氨基甲基丙烯酸硫代甜菜碱酯),比较研究了接药和未接药的两亲无规高分子形成胶束的能力及胶束性质。结果表明,这2种两亲无规高分子在水中都能形成很稳定的胶束。同时,研究了胶束包载和释放疏水性药物DOX能力。动态光散射法和体外药物释放显示,这些胶束具有pH和还原敏感性。用Ecs及Hela细胞研究了接药和未接药的载药胶束的细胞毒性,接SN38的载DOX胶束能够较好地杀死肿瘤细胞。
英文摘要:
      Polymeric micelles show good prospects in tumor treatment. In this study, amphiphilic random copolymers poly(2-Hydr-oxyethyl-methacrylate)-co-poly[(N,N-diethylaminoethylmethacrylate)/(N-(3-sulfopropyl)-N-methacryloxyethy-N,N-diethyl-ammoniumbetaine] (PHEMA-co-(PDEA/PS)) were synthesized with activator generated by electron transfer atom transfer radical polymerization(AGET ATRP) and sulfonation reaction. And SN38 (7-ethyl-10-hydroxycamptothecin) was grafted to the copolymers to obtain [PHEMA/(HEMA-SS-SN38)]-co-(PDEA/PS).The micellization and micellar properties of the amphiphilic random copolymers with and without SN38 were compared. Meanwhile, to load and release hydrophobic drug DOX were investigated. Dynamic light scattering (DLS) and in vitro drug release show that micelles were responsive to pH and reduction. Cell-culture studied with Ecs and Hela cells to investigate cytotoxicity of blank and DOX-loaded micelles. The results indicate the DOX-loaded micelles could kill tumor cells effectively.
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