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1、华西药学杂志2008,23(3):249~252WCJPS壳聚糖/海藻酸钠自组装微球的制备及释药性能*李华,史国齐,万昌秀(四川大学高分子科学与工程学院,四川成都610065)摘要:目的利用壳聚糖(CS)聚阳离子及海藻酸钠(ALG)聚阴离子电解质的性质,在药物微球表面自组装形成多层包覆结构的壳聚糖载药微球,并研究组装层数、温度及盐离子浓度对自组装微球释药性能的影响。方法采用乳化交联法制备CS载四环素(TC)的药物微球,并在其表面交替自组装ALG及CS。利用IR测试技术及电极电位法进行表征。结果CS交联微球未破坏CS
2、及TC的结构,CS与ALG以静电作用相结合。CS交联微球的载药量为40.2%,自组装六层的微球载药量为32%。组装后,药物释放时间延长,初期暴释现象得到极大改善,释药速率随组装层数的增加而下降,温度较高时组装完整,盐-1离子浓度存在较佳点。结论温度为60、盐离子浓度为0.5molL、组装层数为四层的微球释药性能较佳。关键词:壳聚糖;海藻酸钠;四环素;自组装;释药性能中图分类号:R943文献标识码:A文章编号:1006-0103(2008)03-0249-04PreparationofChitosan/alginate
3、microspheresbylayer-by-layerself-assemblymethodandinvitrodrugrelease*LIHua,SHIGuo-q,iWANChang-xiu(DepartmentofPolymerScienceandEngineering,SichuanUniversity,Chengdu610065,China)Abstract:OBJECTIVEChitosan(CS)andalginate(ALG)werecationandanionpolyelectrolyterespectiv
4、ely.Layer-by-layer(LbL)self-assemblytechniquewasusedtopreparetetracycline(TC)microspherescoatedwithCSandALG.Theeffectsofthelayernumber,depositiontemperatureandNaClconcentrationonthereleasepropertyofmicrosphereswereinvestigated.METHODSCSmicrospheresloadedwithTCwerep
5、reparedbycrosslinking-emulsionmethod.CSandALGwereabsorbedontheCS/TCmicrospheresviaLbLself-assemblytechnique.IRandelectrodemethodswereusedtotoken.ThereleaserateofTCfromthemicrosphereswasmonitoredbyUV.RESULTSTheconfigurationsofCSandTCwerenotdestroyedduringcrosslinki
6、ng,CScombinedwithALGbyelectrostaticinteraction.ThedrugcontentofCS/TCmicrosphereswas40.2%,whilemicrosphereswith6layersofALGandCSwas32%.Thereleasetimeforthemicrospheresprolongedwiththelayernumberandtheinitialburstphenomenonwasrelievedafterassembly.Increasingthedepos
7、itiontemperaturecangetamoreperfectstructure.AddingNaCldoesnotreducethereleaseratesignificantlyunless-1itsconcentrationupto0.5molL.CONCLUSIONTheoptimizedconditionswerefourlayers,assembleat60,withioncon-1centrationof0.5molL.Keywords:Chitosan;Alginate;Tetracycline;
8、Self-assembly;DrugreleaseCLCnumber:R943Documentcode:AArticleID:1006-0103(2008)03-0249-04四环素为广谱杀菌剂,可用于骨髓炎的治形态、载药量和药物在体外释放行为的影响。[1,2]
