复乳冻干法制备甲氨蝶呤囊泡-论文.pdf

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1、复乳冻干法制备甲氨蝶呤囊泡丁林，王慧云¨，辛姗姗，周萧云，赵斌(1．济宁医学院药学院，山东日照276826；2．曲阜师范大学，山东曲阜273165)摘要：目的采用复乳冻干法制备非离子表面活性剂囊泡，研究囊泡对水溶性药物甲氨蝶呤的包封作用。方法以非离子表面活性剂Span60、胆固醇、聚乙二醇6000为囊材，采用复乳冻干法制备甲氨蝶呤囊泡，通过正交实验设计优化其制备工艺，并利用光散射技术测定其粒度分布及Zeta电位值，考察了载药囊泡的包封率、稳定性及其体外释放情况。结果采用复乳冻干法制备出的非离子表面活性囊泡粒度分布均匀

2、、具有良好的稳定性及复溶性，对甲氨蝶呤包封率可高迭83．71％。体外释放实验显示，5h时，游离药物释放完全，而囊泡中甲氨蝶呤的累计释放率仅达到50％，囊泡具有明显的缓释性能。结论复乳冻干法是制备非离子表面活性剂囊泡的一种可靠、有效的方法，为囊泡栽药体系的储存、运输及推广应用奠定了基础。关键词：复乳冻干法；囊泡；非离子表面活性剂；包封率；体外释放；甲氨蝶呤doi：10．11669／cpj．2014．15．013中图分类号：R944文献标志码：A文章编号：1001—2494(2014)15—1327—06Preparat

3、ionofMethotrexateNiosomesUsingFreeze—DryingofDoubleEmulsionsMethodDINGLin，WANGHui—yun，XINShan．shan，ZHOUXiao．yun，ZHAOBin(1．JiningMedicalUniversityPharma—ceuticalCollege，Rizhao276826，China；Q咖NormalUniversityQ273165，China)ABSTRACT：OBJECTIVETopreparenonionicsurfact

4、antniosomesbymultipleemulsionfreeze—dryingmethodandstudytheiren—eapsulationeffectsforthewater—solubledrug，methotrexate．METHODSUsingnonionicsurfaetantsSpan60，cholesterol，orPEG6000ascapsulematerial，methotrexateniosomeswerepreparedbythemethodofmultipleemulsionlyop

5、hilization．Thepreparationprocesswanoptimized，andtheniosomesphysicochemicalproperties，entrapmenteficiency，stabilityandinvitroreleasewereinvestigated．RE-SULTSThepreparedniosomeshaduniformparticlesizedistributionandrelativelyhighentrapmenteficiency．andthemaximumch

6、eap-sulationeficiencyofmethotrexatereached83．71％．Thelyophilizedproductofniosomeshadgoodstabilityandsolubility．Theinvitroreleaseexperimentshowedthatthefreedrugreleasedcompletelyafter5h，whilethecumulativereleaserateofmethotrexateintheniosomesreachedonly50％，whichi

7、ndicatedthesustainedreleaseeffectofniosomes．CONCLUSIONMultipleemulsionlyophilizationisaneffectivemethodforthepreparationofnonionicsurfaetantniosomes，whichprovidesanewchoiceforthedevelopmentofanoveldrugdeliverysystem．KEYWORDS：multipleemulsionfreeze—dryingmethod；

8、niosome；nonionicsurfactant；encapsulationeficiency；invitrorelease；meth—otrexate非离子表面活性剂囊泡(nonionicsurfactant水相与溶解囊材的油相(有机相)混合后超声处理，得basedvesicles，niosomes)¨是由非离子表面活性到初乳，再向初乳中