化工学报 ›› 2016, Vol. 67 ›› Issue (S2): 164-170.DOI: 10.11949/j.issn.0438-1157.20161122

• 催化、动力学与反应器 • 上一篇    下一篇

离子液体中ATRP合成MCC-g-PMAA及其分子对阿司匹林控释的应用

杜煌, 常达, 唐二军, 袁淼, 刘少杰   

  1. 河北科技大学化学与制药工程学院, 河北省药物化工工程技术中心, 河北 石家庄 050018
  • 收稿日期:2016-08-08 修回日期:2016-10-10 出版日期:2016-12-30 发布日期:2016-12-30
  • 通讯作者: 唐二军
  • 基金资助:

    河北省自然科学基金项目(B2013208183);河北省教育厅重点项目(ZD2014086)。

Synthesis of MCC-g-PMAA by ATRP in ILs and its application in controlled release to Aspirin

DU Huang, CHANG Da, TANG Erjun, YUAN Miao, LIU Shaojie   

  1. Hebei Research Center of Pharmaceutical and Chemical Engineering, Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang 050018, Hebei, China
  • Received:2016-08-08 Revised:2016-10-10 Online:2016-12-30 Published:2016-12-30
  • Supported by:

    supported by the Natural Science Foundation of Hebei Province (B2013208183)and the State Key Program from Ministry of Education of Hebei Province (ZD2014086).

摘要:

以离子液体氯化1-烯丙基-3-甲基咪唑([Amim]Cl)为反应介质,利用原子转移自由基聚合(atom transfer radical polymerization,ATRP)法合成了微晶纤维素接枝有聚甲基丙烯酸(MCC-g-PMAA)的pH敏感性聚合物。用透析法将模型药物阿司匹林包覆在聚合物胶束内,并对载药胶束的体外药物释放机制进行研究。通过红外、核磁、透射电镜、X射线衍射和紫外分光光度计等分析手段对聚合物的结构、胶束形貌、胶束对阿司匹林的载药性能及释药性能进行了表征分析。结果表明:聚合物胶束能够在水溶液中自组装成球状胶束,对阿司匹林具有良好的包载效果,阿司匹林在碱性条件下的累积释放量大于酸性条件,载药胶束表现出了良好的pH敏感性和药物缓释性能。

关键词: 离子液体, ATRP, 透析, 载药胶束, 水溶液, pH敏感性

Abstract:

Ionic liquid 1-allyl-3-methyl-imidazole chloride ([Amim]Cl) as reaction medium,the microcrystalline cellulose graft poly methylacrylic acid (MCC-g-P4VP) polymer with pH-sensitivity were synthesized by atom transfer radical polymerization (ATRP).The model drug Aspirin was entrapped in polymeric micelles by dialysis method.The release mechanism of drug loaded micelle in vitro was analyzed.The polymer structure,micellar morphology,performance of aspirin loading and drug releasing were characterized by means of FT-IR,1H NMR,TEM,XRD and UV-Vis.The results showed that the micelle could form spherical morphology micelles by self-assembly in aqueous solution, it presented a perfect encapsulation about Aspirin.It was found that the cumulant release of Aspirin in basic environment was higher than that in acidic environment.The drug loaded micelle showed excellent properties of pH-sensitivity and drug sustained-release.

Key words: ionic liquid, ATRP, dialysis, drug loaded micelle, aqueous solution, pH-sensitivity

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