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1、冰片-薄荷脑低共熔物对纳米粒鼻腔给药载药入脑的影响[基金项目]国家自然科学基金项目（30772793），浙江省卫生高层次创新人才培养工程柴国宝[作者简介]柴国宝，男，硕士研究生，研究方向：药物新剂型与新技术，Tel：（0571）86613726，夏爱晓，蔡鑫君，魏颖慧，冯健，李范珠*[通讯作者]李范珠，教授，博士生导师，Tel：（0571）86633030Fax：（0571）86613606Email：lifanzhu@zjtcm.net（浙江中医药大学药学院，杭州，310053）摘要目的：考察中药冰
2、片-薄荷脑低共熔物对神经毒素纳米粒鼻腔给药吸收入脑的影响。方法：采用125I同位素标记法，以清醒自由活动大鼠为实验模型，运用脑微透析取样技术，测定脑内神经毒素浓度的变化，并应用药动学软件计算药动学参数。结果：中药冰片-薄荷脑低共熔物纳米粒脑药动学符合二室模型，Tmax、Cmax、AUC、t1/2(β)分别为0.68h、27.32ng/mL、132.68ng·h/mL、3.1076h，其入脑的速度与程度均优于单用薄荷脑或者冰片。结论：神经毒素纳米粒在冰片-薄荷脑低共熔物作用下，可显著增加其鼻腔吸收入脑的
3、药量，且能较快达到峰浓度，消除缓慢。关键词：冰片-薄荷脑低共熔物;纳米粒;鼻腔给药;脑药动学Effectofborneol/mentholumeutecticmixtureonnasal-braindeliveryofneurotoxinloadednanoparticlesCHAIGuo-bao,XIAAi-xiao,CAIXin-jun,WEIYing-hui,FenJian,LIFan-zhu*(CollegeofPharmacy,ZhejiangUniversityofTraditionalC
4、hineseMedicine,Hangzhou,310053)ABSTRACTObjectiveToinvestigatetheabsorptionenhanceneffectofborneol/mentholumeutecticmixture(BO/ME)onnasal-braindeliveryofneurotoxinloadednanoparticles.MethodsUsingmicrodialysissamplingtechniqueinawakefreely-movingrats,thec
5、ounterperminute(cpm)ofdialysatesinrightPAGofNT-loadednanoparticleswiththeBO/ME(BO/ME-NT-NP),radiolabeledwithsodium125I-Iodide,weremeasuredinagamma-counterforradioactivity.AfterconvertingcpmintocorrespondingconcentrationsofNTbyinvivorecoveryofmicrodialys
6、isprobes,thepharmacokineticparameterswerecalculated.ResultsThelocatedintheTomb,DongShenJiabang,deferthenextdayfocusedontheassassination.Linping,Zhejiang,1ofwhichliquorwinemasters(WuzhensaidinformationisCarpenter),whogotAfewbayonets,duetomissedfatal,when
7、nightcame7BO/ME-NT-NPcouldbeabsorbedintothebrain,muchbettertoNT-NPandthenanoparticleswithborneolormentholumonly,andthepharmacokineticsaccordedwiththetwo-compartmentmodel.Theparameterstmax,cmax,AUC,t1/2(β)were0.68h,27.32ng/mL,132.68ng·h/mL,3.1076h.Conclu
8、sionWithaddingBO/MEasabsorptionenhancer,NTcouldbesignificantlyincreasedinthebrainwiththehelpofnanopartilcesascarriers,andthetimetomaximalconcentrationwasshort,theeliminationprocesswasprolonged.KeyWords:bornel/mentholumeutecticmix
