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Comparison of essential oil from Mentha haplocalyx and menthol used as penetration enhancers

薄荷油与薄荷醇促进中药成分经皮吸收的对比研究



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ComparisonofessentialoilfromMenthahaplocalyxand
mentholusedaspenetrationenhancers
LANYi1,2,WANGJingyan1,TAOYe3,RUQingguo1,WANGYifei1,YUJingxin1,LIUYan1,WUQing1
(1.SchoolofChineseMateriaMedica,BeijingUniversityofChineseMedicine,Beijing100102,China;
2.OvationHealthScienceandTechnologyCo.,Ltd.,ENNGroup,Langfang065001,China;
3.QingdaoEyeHospital,ShandongEyeInstitute,ShandongAcademyofMedicalSciences,Shandong266071,China)
[Abstract] Theaimofthispaperwastoinvestigateandcomparethepenetrationenhancingcharacteristicsofmentholandessential
oilfromMenthahaplocalyx(Mhaplocalyxoil)onthetransdermalabsorptionofthecomplextraditionalChinesemedicine(TCM)com
ponentsAseriesofTCMcomponentswereselectedasmodeldrugsbasedontheirlipophilicity(logPvalue),namelyosthole(OT,
logP=385),tetramethylpyrazine(TMP,logP=234),ferulicacid(FA,logP=126),puerarin(PR,logP=-035)andgenipo
side(GP,logP=-101),inordertosimplyandcharacterizetheTCMcomplexcomponentssystemTransdermalexperimentinvitro
wasemployedtoinvestigateandcomparethepenetrationenhancingcharacteristicsofmentholandMhaplocalyxoilonthetransdermal
absorptionofthesemodeldrugsMeanwhile,Fouriertransforminfraredspectroscopy(FTIR)wasusedtofurthercomparetheefectof
mentholandMhaplocalyxoilonthemolecularstructureofstratumcorneum(SC)Theresultsshowedthatbothofmentholand
MhaplocalyxoilatproperconcentrationcouldpromotethetransdermalabsorptionoftheselectedmodeldrugsAfterapplicationof
menthol,thedruglogPvaluesgradualytendedtohavenegativelinearrelationshipwiththelogarithmofpenetrationenhancementratio
(ER);whileafterapplicationofMhaplocalyxoil,thelogPvaluestendedtohaveparabolicrelationshipwiththelogarithmofER
However,bothmentholandMhaplocalyxoilexhibitedhighereficiencyforthedrugswithrelativelowlgPvalue(iehydrophilic
drugs),withsimilarpenetrationenhancingcharacteristicsbetweenthesetwoInfraredspectroscopyresultsshowedthatmentholand
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Mhaplocalyxoilcouldafecttheskinbarierfunctionsmainlyviastratumcorneumlipids,withsimilarefectintensity,andthiswas
consistentwiththeresultsoftransdermalexperimentinvitroThus,Mentholhadsimilarpenetrationenhancingcharacteristicswith
Mhaplocalyxoil,andhadsameefectontheSCmolecularstructureTherefore,astransdermalpenetrationenhancer,thementhol
withsinglecompositioncouldbeconsideredtoreplaceMhaplocalyxoilwithcomplexcompositions
[Keywords] essentialoilfromMenthahaplocalyx;menthol;transdermalpenetrationenhancer;transdermalabsorption;FTIR
doi:10.4268/cjcmm20160825
  
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Fig1 Thepercutaneouskineticprofilesofmodeldrugsacrosstheratskininvitroaftertreatedwithdiferentconcentrationsofmenthol
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Table2 PercutaneouspermeationparametersofOT,TMP,FA,PR,GPthroughexcisedratskin
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/μg·cm-2·h-1 Tlag/h Q24/μg·cm2 ER/lgER
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1%
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189±020 359±055 4211±308 113(005)
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[5] OlivelaMS,LhezL,PappanoNB,etalEfectsofdimethyl
formamideandLmentholpermeationenhancersontransdermal
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[6] PotsRO,GuyRHPredictingskinpermeability[J]Pharm
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[7] MossG,DeardenJ,PatelH,etalQuantitativestructureper
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[8] WangJY,LanY,LiH,etalPercutaneouspenetrationen
hancementefectofessentialoilofMint(Menthahaplocalyx
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[18] LanY,WuQ,MaoYQ,etalCytotoxicityandenhancement
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[19] LanY,LiH,ChenYY,etalEssentialoilfromZanthoxylum
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