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高压乳匀法制备中药固体脂质纳米粒.doc

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高压乳匀法制备中药固体脂质纳米粒.doc

高压乳匀法制备中药固体脂质纳米粒作者厉英超1;董蕾2;贾皑1;苌新明1;薛挥1西安交通大学医学院1第一附属医院消化内科,陕西西安710061;2第二附属医院消化内科,陕西西安710004摘要目的采用高压乳匀法将中药有效成分包载于固体脂质纳米粒SLN,并研究制备的纳米粒的主要性质。方法选择水飞蓟宾SIL和汉防己甲素TET为模型药物,采用高压乳匀法将其分别包载于SLN。在电镜下观察其形态,以粒度分析仪和ZETA电位分析仪测定其粒径和ZETA电位,用葡聚糖凝胶柱层析法和HPLC测定其包封率和载药量,还观察了SLN的稳定性。结果高压乳匀法制备的SILSLN呈球状,形态规则,平均粒径为1578NM,ZETA电位为3536268MV,包封率为9564,载药量为463;TETSLN呈片状存在,不规则,粒径较小,平均粒径为473NM,ZETA电位为3299254MV,包封率为9782,载药量为476。SILSLN和TETSLN有较高稳定性。结论高压乳匀法适于制备包载中药的SLN。关键词水飞蓟宾;汉防己甲素;固体脂质纳米粒;高压乳匀法;中药现代化中图分类号R944文献标识码A文章编号16734254200605054104PREPARATIONOFSOLIDLIPIDNANOPARTICLESLOADEDWITHTRADITIONALCHINESEMEDICINEBYHIGHPRESSUREHOMOGENIZATIONLIYINGCHAO1;DONGLEI2;JIAAI1;CHANGXINMING1;XUEHUI11DEPARTMENTOFGASTROENTEROLOGY,FIRSTAFFILIATEDHOSPITAL,MEDICALCOLLEGEOFXI’ANJIAOTONGUNIVERSITY,XI’AN710061,CHINA;2DEPARTMENTOFGASTROENTEROLOGY,SECONDAFFILIATEDHOSPITAL,MEDICALCOLLEGEOFXI’ANJIAOTONGUNIVERSITY,XI’AN710004,CHINAABSTRACTOBJECTIVETOINVESTIGATETHEPREPARATIONOFSOLIDLIPIDNANOPARTICLESSLNLOADEDWITHTRADITIONALCHINESEMEDICINESBYHIGHPRESSUREHOMOGENIZATION,ANDSTUDYTHEPHYSICOCHEMICALCHARACTERISTICSOFTHEPARTICLESPRODUCEDBYTHISMETHODMETHODSTHEMODELTRADITIONALCHINESEMEDICINES,SILIBININSILANDTETRANDRINETET,WEREINCORPORATEDINTOSLNSEPARATELYBYHIGHPRESSUREHOMOGENIZATIONTRANSMISSIONELECTRONMICROSCOPEWASEMPLOYEDTOSTUDYTHESHAPEOFTHEPARTICLESPARTICLECHARACTERIZATIONSYSTEMANDZETAPOTENTIALANALYZERWEREUSEDTOSTUDYTHEDIAMETERANDZETAPOTENTIALOFSLNINTHESUSPENSIONTHEENTRAPMENTEFFICIENCYANDDRUGLOADINGWEREDETERMINEDWITHTHESEPHADEXGELCHROMATOGRAPHYANDHIGHPERFORMANCELIQUIDCHROMATOGRAPHYTHESTABILITYOFSLNWASALSOSTUDIEDRESULTSTHESILSLNSPREPAREDBYHIGHPRESSUREHOMOGENIZATIONWERESPHERICALANDREGULARTHEMEANDIAMETERANDZETAPOTENTIALOFSILSLNINDISTILLEDWATERWERE1578NMAND3536268MV,RESPECTIVELYTHEENTRAPMENTEFFICIENCYWAS9564,ANDTHEDRUGLOADINGWAS463THETETSLNWASPLATELETSHAPED,IRREGULARANDSMALLERTHEMEANDIAMETERANDZETAPOTENTIALOFTETSLNWERE473NMAND3299254MV,RESPECTIVELY,WITHDRUGLOADINGOF476,ANDUPTO9782OFTETWASINCORPORATEDSILSLNANDTETSLNHADGOODSTABILITYCONCLUSIONHIGHPRESSUREHOMOGENIZATIONISFEASIBLEFORPREPARINGSLNLOADEDWITHTRADITIONALCHINESEMEDICINESKEYWORDSSILIBININ;TETRANDRINE;SOLIDLIPIDNANOPARTICLES;HIGHPRESSUREHOMOGENIZATION;TRADITIONALCHINESEMEDICINESSUPPORTEDBYSCIENCEANDTECHNOLOGYPROJECTOFXI’ANCITYGG04133LIYINGCHAO1974,PHD,ATTENDINGPHYSICIAN,SPECIALIZEDINPHARMACEUTICALRESEARCHOFLIVERFIBROSIS,TEL02985324001,EMAILL_163COMCORRESPONDINGAUTHORDONGLEI,MEDICALPROFESSOR,TEL0298727693629368,EMAILDONGLEI4488SOHUCOMSOLIDLIPIDNANOPARTICLESSLNSAREPARTICLESMADEFROMSOLIDLIPIDSWITHAMEANDIAMETEROFAPPROXIMATELY50TO1000NMTOSERVEASANALTERNATIVECOLLOIDALCARRIERSYSTEMFORCONTROLLEDDRUGDELIVERY1COMPAREDWITHOTHERPARTICULATECARRIERSSLNHASSEVERALADVANTAGESFORDRUGDELIVERYSUCHASITSGOODBIOCOMPATIBILITY2,BIODEGRADABILITY3,HIGHBIOAVAILABILITY4,ANDEFFECTSTARGETINGTHELIVERANDSPLEENINRECENTYEARS,MARKEDLYINCREASINGSTUDIESONSLNHAVEBEENREPORTED,ESPECIALLYWITHTHEMETHODOFHIGHPRESSUREHOMOGENIZATION5NEVERTHELESS,ONLYAFEWINVESTIGATIONSHAVEBEENCONDUCTEDINREGARDWITHTHEINCORPORATIONOFEFFECTIVECOMPONENTSOFTRADITIONALCHINESEMEDICINESINTOSLNSILYMARINISAPURIFIEDEXTRACTFROMTHEMILKTHISTLESILYBUMMARIANUMLGAERTN,WHICHISCOMPOSEDOFAMIXTUREOF4ISOMERICFLAVONOLIGNANS,NAMELYSILIBININORSILYBIN,SIL,ISOSILIBININ,SILIDIANINANDSILYCHRISTINSIL,WHICHCONSTITUTES6070OFTHESILYMARINMIXTURE,HASBEENIDENTIFIEDASTHEMAJORACTIVECOMPONENT6TETRANDRINETETISABISBENZYLISOQUINOLINEALKALOIDEXTRACTEDFROMTHETRADITIONALCHINESEMEDICINALHERBRADIXSTEPHANIATETRANDRAESILANDTETPOSSESSWIDESPECTRUMSOFPHARMACOLOGICALACTIVITIES7891011THESETWOEFFECTIVECOMPONENTSOFTHETRADITIONALCHINESEMEDICINESHAVEHIGHLIPOPHILICITYANDAREEXCELLENTCANDIDATESFORSLNENCAPSULATIONBYUSINGTHISDRUGDELIVERYSYSTEM,AHIGHBIOAVAILABILITYANDANINTRAVENOUSADMINISTRATIONAREPOSSIBLEINTHEPRESENTSTUDY,SILSLNANDTETSLNWEREPREPAREDBYHIGHPRESSUREHOMOGENIZATION,ANDTHEPHYSICOCHEMICALCHARACTERISTICSOFTHEPARTICLESPRODUCEDBYTHISMETHODWEREANALYZEDMATERIALSANDMETHODSDRUGSANDREAGENTSSIL95WASPURCHASEDFROMPANJINGREENBIOLOGICALDEVELOPMENTCOLTD,CHINATET98WASPURCHASEDFROMSHANCHUANBIOLOGICALCOLTD,XIANCHOLESTERINOBTAINEDFROMZHENGXIANGCHEMICALRESEARCHINSTITUTE,SHANGHAIANDSTEARICACIDTIANDACHEMICALINDUSTRYLTD,TIANJINWEREUSEDSEPARATELYASTHELIPIDMATERIALSOFSLNSOYBEANLECITHINWASOBTAINEDFROMAUBOXINGCOLTD,BEIJINGSEPHADEXGEL50WASPURCHASEDFROMTIANJINCHEMICALINDUSTRYLTDMETHANOLHPLCGRADEANDABSOLUTEALCOHOLWASSUPPLIEDBYXIANCHEMICALINDUSTRYLTDGLYCERINAMOYGLYCERININDUSTRYLTDWASUSEDASACOEMULSIFIERINWATERPHASEPREPARATIONOFSILSLNSIL75MG,CHOLESTERIN15GANDSOYBEANLECITHIN10GWEREWEIGHEDPRECISELYWITHELECTRONICBALANCEBP121S,SARTORIUSLTD,GERMANYANDDISSOLVEDIN10MLABSOLUTEALCOHOLINWATERBATHAT70℃ANAQUEOUSPHASEWASPREPAREDBYDISSOLVING45MLGLYCERININ75MLDISTILLEDWATERTHERESULTANTORGANICSOLUTIONWASRAPIDLYINJECTEDINTOTHESTIRREDAQUEOUSPHASE80℃THERESULTINGSUSPENSIONWASSTIRREDCONTINUOUSLYAT80℃FOR2HTHEORIGINALSILSLNSUSPENSIONWASTHENLOADEDINTOAHIGHPRESSUREHOMOGENIZER15M8BA,APV,UK,5CYCLESAT50MPAANDTHESAMPLESWEREKEPTAT4℃PREPARATIONOFTETSLNTET75MG,STEARICACID15GANDSOYBEANLECITHIN10GWEREWEIGHEDPRECISELYANDPREPAREDINTOTETSLNSUSPENSIONACCORDINGTOTHEMETHODDESCRIBEDABOVETRANSMISSIONELECTRONMICROSCOPYTHEMORPHOLOGYOFSILSLNANDTETSLNWASEXAMINEDWITHTRANSMISSIONELECTRONMICROSCOPEH600,HITACHI,JAPANTHESAMPLESWERESTAINEDWITH2M/VPHOSPHOTUNGSTICACIDFOR30SANDPLACEDONCOPPERGRIDSWITHFILMSFORVIEWINGMEANDIAMETERANDZETAPOTENTIALPARTICLECHARACTERIZATIONSYSTEMMASTERSIZER2000,MALVERNINSTRUMENTS,UK,20NM2000ΜMANDZETAPOTENTIALANALYZERZETASIZERNANO,MALVERNINSTRUMENTS,UKWEREUSEDTOSTUDYTHEDIAMETERANDZETAPOTENTIALOFSLNINDISTILLEDWATERTHREESAMPLESOFSILSLN/TETSLNWEREPREPAREDACCORDINGTOTHEPREVIOUSLYDESCRIBEDMETHODANDEACHSAMPLEWASMEASURED3TIMESTOCALCULATETHEMEANDIAMETERANDZETAPOTENTIALENTRAPMENTEFFICIENCYEEANDDRUGLOADINGDLOFSILSLNCHROMATOGRAPHICCONDITIONTHECHROMATOGRAPHICCOLUMNOFPLANETSILC1846MM15CMWASUSEDWITHMOBILEPHASEOFMETHANOL/01MOL/LPHOSPHATEBUFFER35/65,V/V,PH30,FLOWRATEOF10ML/MIN,COLUMNTEMPERATUREOF40℃,ANDDETECTIONWAVELENGTHOF288NMTHECONTROLSOLUTIONS0050,0161,1605,1419,2838,5675,11350ΜG/MLWASPREPAREDBYDISSOLVINGPRECISELYWEIGHEDSILINTHEMOBILEPHASETHEAMOUNTOFSILENTERINGTHERECEPTORCOMPARTMENTWASDETERMINEDWITHHIGHPERFORMANCELIQUIDCHROMATOGRAMHPLC,LC2010,SHIMADZU,JAPANTHEINTEGRALCALCULUSOFTHECHROMATOGRAPHICPEAKAREAAWASRECORDEDASTHEYAXIS,ANDTHECONCENTRATIONOFSILCASTHEXAXISDRUGRECOVERYWASCALCULATEDFROMTHEFOLLOWINGEQUATIONDRUGRECOVERYMEASUREDDRUGWEIGHTINSLN100/THEORETICALDRUGWEIGHTLOADEDINTHESYSTEMTHESILSLNSUSPENSIONWASSEPARATEDBYSEPHADEXGEL50COLUMNCHROMATOGRAPHYTHECONCENTRATIONSOFSILINTHESUSPENSIONN1ANDFREEDRUGN2WEREASSAYEDBYHPLCAFTERDILUTIONWITHMETHANOLEEANDDLCOULDBECALCULATEDACCORDINGTOTHEFOLLOWINGEQUATIONSEEN1N2/N1100,DLWDRUGLOADEDINSYSTEM/WLIPIDMATRIX100EEANDDLOFTETSLNCHROMATOGRAPHICCONDITIONTHECHROMATOGRAPHICCOLUMNOFSPHERISORBODSC18250MM46MM,5ΜMWASUSEDWITHMOBILEPHASEOFMETHANOL/ETHER/ETHYLAMINEVOLUMEPROPORTIONOF1001005ANDFLOWRATEOF10ML/MINATROOMTEMPERATUREANDDETECTIONWAVELENGTHOF282NMTHEREGRESSIONEQUATION,PERCENTAGERECOVERIESOFTET,EEANDDLOFTETSLNWEREDETERMINEDANDCALCULATEDACCORDINGTOTHEMETHODSANDEQUATIONSDESCRIBEDPREVIOUSLYEVALUATIONOFSTABILITYSILSLNANDTETSLNWERESTOREDAT37℃ANDTHEPARTICLESIZESWEREDETERMINEDAFTER7,45AND90DAYS,RESPECTIVELY,TOEVALUATETHEIRSTABILITYSTATISTICALANALYSISTHERESULTSWEREPRESENTEDASMEANSDSTATISTICALANALYSISWASPERFORMEDUSINGSTUDENTSTTESTWITHP005INDICATINGSIGNIFICANTDIFFERENCERESULTSTRANSMISSIONELECTRONMICROSCOPYTHEELECTRONMICROSCOPYMICROGRAPHSOFSLNLOADEDWITHTRADITIONALCHINESEMEDICINESPREPAREDBYHIGHPRESSUREHOMOGENIZATIONWERESHOWNINFIG1THESILSLNWASSPHERICALANDREGULARA,ANDTHETETSLNAPPEAREDPLATELETSHAPED,IRREGULARANDSMALLERBMEANDIAMETERANDZETAPOTENTIALTHEMEANDIAMETEROFSILSLNWAS1578NM,ANDTHEZETAPOTENTIALWAS3536268MVINDISTILLEDWATERTHEMEANDIAMETEROFTETSLNWAS473NM,ANDTHEZETAPOTENTIAL3299254MVFIG1ELECTRONMICROGRAPHSOFTHEPREPAREDSLNLOADEDWITHTRADITIONALCHINESEMEDICINESORIGINALMAGNIFICATION40000ASILSLN;BTETSLNEEANDDLOFSILSLNTHEREGRESSIONEQUATIONOFSILWASA33071C99102THEASSAYWASLINEARR09999INTHECONCENTRATIONRANGEOF005011350ΜG/MLTHEPERCENTAGERECOVERIESATHIGHANDLOWCONCENTRATIONSWERE9899AND9849,RESPECTIVELY,WITHAMEANOF9896THEEEOFSILSLNWAS9564133ANDTHEDLWAS463021EEANDDLOFTETSLNTHELINEARCALIBRATIONCURVEOFTETWASOBTAINEDINTHERANGEOF12525ΜG/MLR09999THEREGRESSIONEQUATIONOFTETWASA18526C83422THEPERCENTAGERECOVERIESRANGEDFROM9872TO10180MEAN9946UPTO9782145OFTETWASINCORPORATEDINSLN,ANDTHEDLWAS476026STABILITYTAB1SHOWSTHEDATAOFPARTICLESIZESOFSILSLNANDTETSLNAFTER7,45AND90DAYSOFSTORAGEAT37℃THESETWOSLNSUSPENSIONSSHOWEDSUFFICIENTLONGTERMSTABILITYWITHONLYSLIGHTPARTICLEGROWTHP005AFTERSTORAGEAT37℃FOR90DAYSDISCUSSIONSLNSAREACOLLOIDALCARRIERSYSTEMFORCONTROLLEDDRUGDELIVERY,ANDITISCLAIMEDTHATSLNCOMBINESTHEADVANTAGESANDAVOIDSTHEDISADVANTAGESOFOTHERCOLLOIDALCARRIERSITSADVANTAGESINCLUDETHEPOSSIBILITYOFCONTROLLEDDRUGRELEASEANDDRUGTARGETING,INCREASEDDRUGSTABILITY,ABSENCEOFCARRIERBIOTOXICITY,ANDLARGESCALEPRODUCTIONANDSTERILIZATION12HIGHPRESSUREHOMOGENIZATIONHASEMERGEDASARELIABLEANDPOWERFULTECHNIQUEFORSLNPREPARATION12INTHEPRESENTSTUDY,THISMETHODPROVEDTOBEFEASIBLEFORPREPARINGSILSLNANDTETSLN,WHICHARESMALL,STEADYANDHIGHLYINCORPORATEDTHISSUCCESSINDICATESTHEPOSSIBILITYOFINCORPORATINGVARIOUSLIPOPHILICEFFECTIVECOMPONENTSEXTRACTEDFROMTHETRADITIONALCHINESEMEDICINESINSLNBYTHISMETHOD,WHICHMAKEPOSSIBLEHIGHBIOAVAILABILITY,CONTROLLEDDRUGRELEASE,DRUGTARGETING,DECREASEDDRUGTOXICITIESANDMINIMIZEDSIDEEFFECTS,ANDREPRESENTSASUCCESSFULATTEMPTOFNOVELAPPROACHTOTHEMODERNIZATIONOFTRADITIONALCHINESEMEDICINESVARIOUSFACTORSMAYINFLUENCETHEPARTICLESIZEINHIGHPRESSUREHOMOGENIZATION,INCLUDING,FORINSTANCE,HOMOGENIZATIONPRESSURE,NUMBEROFCYCLES,LIPIDSANDEMULSIFIERS/COEMULSIFIERSUSED,ANDOPERATINGTEMPERATUREINTHEPRESENTSTUDY,THETWOKINDSOFSLNWEREPREPAREDUNDERIDENTICALCONDITIONSWITHALMOSTTHESAMEMATERIALSEXCEPTTHEDRUGSINCORPORATEDINSLNANDTHELIPIDMATERIALTHEDIFFERENCEOFTHELIPIDSCHOLESTERINANDSTEARICACIDANDTHEINTERACTIONSBETWEENTHEDRUGSANDTHELIPIDSMIGHTENORMOUSLYCONTRIBUTETOTHEDIFFERENCESOFPARTICLESIZESHOWEVER,THEDETAILEDMECHANISMSREMAINTOBEFURTHERINVESTIGATEDTHESHAPEOFSLNMAYSIGNIFICANTLYDIFFERF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