离子液体中ATRP合成MCC-g-P4VP分子及其药物控释应用  

Atom Transfer Radical Polymerization of MCC-g-P4VP in Ionic Liquids and its Application in Controlled Drug Release

作　　者：杜煌[1] 薛腾[1] 唐二军[1] 袁淼[1] 刘少杰[1] 赵地顺[1] DU Huang;XUE Teng;TANG Er-jun;YUAN Miao;LIU Shao-jie;ZHAO Di-shun(Chemical and Pharmaceutical Engineering,Hebei University of Science and Technology,Hebei Research center of Pharmaceutical and Chemical Engineering, Shijiazhuang 050018, China)

机构地区：[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

出　　处：《高校化学工程学报》2017年第2期352-360,共9页Journal of Chemical Engineering of Chinese Universities

基　　金：河北省自然科学基金(B2013208183)

摘　　要：在离子液体氯化-1-烯丙基-3-甲基咪唑中,利用原子转移自由基聚合(ATRP)法在微晶纤维素(MCC)上接枝了pH敏感性的聚4-乙烯基吡啶(P4VP),合成了具有pH敏感性的药物载体材料MCC-g-P4VP。通过对亲水性模型药物罗丹明B和疏水性模型药物阿司匹林的包载及体外释放,研究了胶束对亲水性药物和疏水性药物的释放机制。利用FT-IR、NMR、GPC、TEM、XRD和UV-Vis等分析手段对聚合物的结构、胶束形貌、胶束对药物的载药性能及释药性能进行了表征分析。结果表明:MCC-g-P4VP聚合物胶束对两种药物的包载效果较好,载药胶束具有球状的核壳结构,载药胶束在药物释放过程中表现出了良好的pH敏感性且在酸性条件下的药物释放符合一级动力学模型,疏水性药物从胶束中释放的过程具有更加明显的pH敏感性。pH-sensitive poly4-vinyl pyridine was grafted onto microcrystalline cellulose to prepare pH-sensitive drug carrier MCC-g-P4VP by atom transfer radical polymerization(ATRP)in ionic liquid1-allyl-3-methyl-imidazole chloride.A soluble model drug rhodamine B and an insoluble model drug aspirin were encapsulated in MCC-g-P4VP micelles,and the release mechanism was investigated in vitro.Polymer structure,micellar morphology,drug loading and release were characterized by FT-IR,NMR,GPC,TEM,XRD and UV-Vis.The results show that MCC-g-P4VP micelles can well encapsulate the two drugs.The drug loaded micelles have spherical morphology with core-shell structure,and it shows excellent drug controlled release properties with pH.Drug release is conformed as first-order kinetics model in acidic environment,and theinsoluble drug shows more obvious pH-sensitivity.

关 键 词：原子转移自由基聚合 纤维素聚合物 载药胶束 PH敏感性 动力学模型 

分 类 号：TQ469[化学工程—制药化工]