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1、冰片-薄荷腦低共熔物對(duì)納米粒鼻腔給藥載藥入腦的影響[基金項(xiàng)目]國家自然科學(xué)基金項(xiàng)目(30772793),浙江省衛(wèi)生高層次創(chuàng)新人才培養(yǎng)工程柴國寶[作者簡(jiǎn)介]柴國寶,男,碩士研究生,研究方向:藥物新劑型與新技術(shù),Tel:(0571)86613726,夏愛曉,蔡鑫君,魏穎慧,馮健,李范珠*[通訊作者]李范珠,教授,博士生導(dǎo)師,Tel:(0571)86633030Fax:(0571)86613606Email:lifanzhu@zjtcm.net(浙江中醫(yī)藥大學(xué)藥學(xué)院,杭州,310053)摘要目的:考察中藥冰片-薄荷腦低共熔物對(duì)神經(jīng)毒素納米粒鼻腔給藥吸收入腦的影響。方法:采用12
2、5I同位素標(biāo)記法,以清醒自由活動(dòng)大鼠為實(shí)驗(yàn)?zāi)P停\(yùn)用腦微透析取樣技術(shù),測(cè)定腦內(nèi)神經(jīng)毒素濃度的變化,并應(yīng)用藥動(dòng)學(xué)軟件計(jì)算藥動(dòng)學(xué)參數(shù)。結(jié)果:中藥冰片-薄荷腦低共熔物納米粒腦藥動(dòng)學(xué)符合二室模型,Tmax、Cmax、AUC、t1/2(β)分別為0.68h、27.32ng/mL、132.68ng·h/mL、3.1076h,其入腦的速度與程度均優(yōu)于單用薄荷腦或者冰片。結(jié)論:神經(jīng)毒素納米粒在冰片-薄荷腦低共熔物作用下,可顯著增加其鼻腔吸收入腦的藥量,且能較快達(dá)到峰濃度,消除緩慢。關(guān)鍵詞:冰片-薄荷腦低共熔物;納米粒;鼻腔給藥;腦藥動(dòng)學(xué)Effectofborneol/mentholume
3、utecticmixtureonnasal-braindeliveryofneurotoxinloadednanoparticlesCHAIGuo-bao,XIAAi-xiao,CAIXin-jun,WEIYing-hui,FenJian,LIFan-zhu*(CollegeofPharmacy,ZhejiangUniversityofTraditionalChineseMedicine,Hangzhou,310053)ABSTRACTObjectiveToinvestigatetheabsorptionenhanceneffectofborneol/mentholume
4、utecticmixture(BO/ME)onnasal-braindeliveryofneurotoxinloadednanoparticles.MethodsUsingmicrodialysissamplingtechniqueinawakefreely-movingrats,thecounterperminute(cpm)ofdialysatesinrightPAGofNT-loadednanoparticleswiththeBO/ME(BO/ME-NT-NP),radiolabeledwithsodium125I-Iodide,weremeasuredinagam
5、ma-counterforradioactivity.AfterconvertingcpmintocorrespondingconcentrationsofNTbyinvivorecoveryofmicrodialysisprobes,thepharmacokineticparameterswerecalculated.ResultsThe8BO/ME-NT-NPcouldbeabsorbedintothebrain,muchbettertoNT-NPandthenanoparticleswithborneolormentholumonly,andthepharmacok
6、ineticsaccordedwiththetwo-compartmentmodel.Theparameterstmax,cmax,AUC,t1/2(β)were0.68h,27.32ng/mL,132.68ng·h/mL,3.1076h.ConclusionWithaddingBO/MEasabsorptionenhancer,NTcouldbesignificantlyincreasedinthebrainwiththehelpofnanopartilcesascarriers,andthetimetomaximalconcentrationwasshort,thee
7、liminationprocesswasprolonged.KeyWords:bornel/mentholumeutecticmixture;nanoparticles;intranasaladminister-ation;brainpharmacokinetic納米藥物載體系統(tǒng)具有靶向、緩釋、保護(hù)藥物等多重作用。前期實(shí)驗(yàn)表明[1-2]:納米粒作為神經(jīng)毒素(Neurotoxin,NT)的載體,既能保持藥物的活性,又能增加藥物的腦內(nèi)含量。臨床上,NT主要的給藥方式為肌內(nèi)注射[3],但起效慢(3~5h),難以滿足臨床要求。鼻腔給藥