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时间:2020-03-27
《赖氨酸在甘草次酸弹性囊泡形成过程中的作用机制.pdf》由会员上传分享,免费在线阅读,更多相关内容在行业资料-天天文库。
1、物理化学学~(WuliHuaxueXuebao)SeptemberActaP.一Chim.Sin.2011,27(9),2167-21722167[Article]www.whxb.pku.edu.CII赖氨酸在甘草次酸弹性囊泡形成过程中的作用机制李爽邱玉琴’张锁慧’高云华(。中国科学院理化技术研究所,光化学转换和功能材料重点实验室,北京100190;中国科学院研究生院,北京100049)摘要:制备和评价含赖氨酸的甘草次酸弹性囊泡,并考察赖氨酸在囊泡形成过程中的作用机制.在水合介质中加入赖氨酸。利用薄膜.高压均质法制备甘草次酸弹性囊泡.并合成了甘草次酸赖氨酸盐及其弹性囊泡作为
2、对比制剂.通过对粒径、zeta电位、包封率、相转变温度、变形性和体外经皮渗透性的测试,考察赖氨酸在甘草次酸弹性囊泡中的存在形式及作用.结果显示加入赖氨酸后,甘草次酸弹性囊泡的粒径略有降低,膜相转变温度降低,包封率和囊泡变形性显著提高,载药量提高近30倍(1.5mg·m),并显著高于其赖氨酸盐所形成囊泡的载药量和弹性.此外,赖氨酸的加入使弹性囊泡的变形能力增加,8h累积透过量和皮肤驻留量分别提高4.3倍和9.2倍.表明赖氨酸与甘草次酸形成离子缔合物,促进甘草次酸参与膜的形成,使膜的流动性增加,赖氨酸与弹性囊泡对提高囊泡载药量起协同作用.关键词:甘草次酸弹性囊泡赖氨酸:载药量机理
3、中图分类号:O641MechanismofLysineontheFormationofGlycyrrheticAcidElasticVesiclesLIShuang’。QIUYu—Qin’ZHANGSuo—Hui’GAOYun—Hua’,(IKeyLaboratoryofPhotochemicalConversionandOptoelectronicMaterials,TechnicalInstituteofPhysicsandChemistryChineseAcademyofSciences,Beijing100190,R.China;GraduateUniversityo
4、fChineseAcademyofSciences,Beijing100049,R.China)Abstract:Elasticvesiclesofglycyrrheticacid(GA)withlysineintheaqueousphasewerepreparedbythef¨m.highpressurehomogenizationmethod.TheinfluenceofIysineontheformationofGAelasticvesicleswasevaluatedinthiswork.ThelysinesaltofGAwassynthesizedandentrap
5、pedinelasticvesiclesasacontroIformulation.Theparticlesize,zeta.potential。entrapmenteficiency,phasetransformationtemperature,deformabilityoftheelasticvesicles,andthepermeationofGAthroughratskinwereinvestigated.Bytheincorporationoflysineintoelasticvesiclestheparticlesizedecreasedslightlyandth
6、ephasetransformationtemperaturedecreasedwhiletheentrapmenteficiencyanddeformabilityoftheelasticvesiclesincreasedobviously.ThedrugIoadingreached1.5mg·mL~,whichwas30timeshigherthanthatofGAelasticvesicleswithoutlysine.ThedrugIoadinganddeformabilityoftheelasticvesicleswasremarkablyhigherthantha
7、tobtainedusingtheIysinesalt.Inaddition.thecumulativeamountofGApermeationthroughratskinwithin8handtheresiduaJamountintheskinwerefoundtobe4.3timesand9.2timeshigherthanthatofthevesicleswithoutIysine.whichwashigherthanthatoftheelasticvesicleswiththelysinesal
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