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1、華西藥學(xué)雜志2008,23(3):249~252WCJPS殼聚糖/海藻酸鈉自組裝微球的制備及釋藥性能*李華,史國(guó)齊,萬(wàn)昌秀(四川大學(xué)高分子科學(xué)與工程學(xué)院,四川成都610065)摘要:目的利用殼聚糖(CS)聚陽(yáng)離子及海藻酸鈉(ALG)聚陰離子電解質(zhì)的性質(zhì),在藥物微球表面自組裝形成多層包覆結(jié)構(gòu)的殼聚糖載藥微球,并研究組裝層數(shù)、溫度及鹽離子濃度對(duì)自組裝微球釋藥性能的影響。方法采用乳化交聯(lián)法制備CS載四環(huán)素(TC)的藥物微球,并在其表面交替自組裝ALG及CS。利用IR測(cè)試技術(shù)及電極電位法進(jìn)行表征。結(jié)果CS交聯(lián)微球未破壞CS
2、及TC的結(jié)構(gòu),CS與ALG以靜電作用相結(jié)合。CS交聯(lián)微球的載藥量為40.2%,自組裝六層的微球載藥量為32%。組裝后,藥物釋放時(shí)間延長(zhǎng),初期暴釋現(xiàn)象得到極大改善,釋藥速率隨組裝層數(shù)的增加而下降,溫度較高時(shí)組裝完整,鹽-1離子濃度存在較佳點(diǎn)。結(jié)論溫度為60、鹽離子濃度為0.5molL、組裝層數(shù)為四層的微球釋藥性能較佳。關(guān)鍵詞:殼聚糖;海藻酸鈉;四環(huán)素;自組裝;釋藥性能中圖分類號(hào):R943文獻(xiàn)標(biāo)識(shí)碼:A文章編號(hào):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)03-0249-04四環(huán)素為廣譜殺菌劑,可用于骨髓炎的治形態(tài)、載藥量和藥物在體外釋放行為的影響。[1,2]