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1、丹参酮IIA纳米结构脂质载体的处方优化及其体外透皮研究郑娟1,2,3，沈成英3，庞建云1,3，徐方楚3，廖卫波3，胡春晓1,3，徐平华2，韩晋2，袁海龙3*1.成都中医药大学药学院，成都6111372.中国人民解放军第三〇二医院，北京1000393.中国人民解放军空军总医院，北京100142[摘要]为研制丹参酮IIA纳米结构脂质载体（TanIIA-NLC），并进行体外透皮研究。本文采用高压均质技术制备TanIIA-NLC，运用Box-Behnken设计-效应面法优化处方，并对其进行表征。采用Fr
2、anze扩散池法评价TanIIA-NLC体外透皮性能。结果显示，以最优处方：脂药比为88、固液脂质比为2、稳定剂用量为1%,制得的TanIIA-NLC粒径为182±14nm，多分散指数(PDI)为0.1906±0.0245，Zeta电位-27.8±5.4mV,包封率(EE)为86.44±9.26%，载药量(DL)为0.98±0.18%；体外透皮吸收实验结果显示TanIIA-NLC的24h药物累积透皮量低于溶液，但其在表皮中的滞留量是溶液的3.18倍。TanIIA-NLC可有效提高TanIIA在表
3、皮层的滞留量，具有广阔的应用前景。[关键词]：丹参酮IIA；纳米结构脂质载体；Box-Behnken设计；体外透皮；皮肤滞留量PreparationofTanIIAloadednanostructuredlipidcarrieranditsinvitrotransdermaldiffusioncharacteristicsZHENGjuan1,2,3,SHENcheng-ying3,PANGjian-yun1,3,XUfangchu3,LIAOwei-bo3,HUchun-xiao1,3，XUp
4、ing-hua2，HANjin2,YUANHai-long3*1.CollegeofPharmacy,ChengduUniversityofTraditionalChineseMedicine,Chengdu611137,China2.302MilitaryHospitalofChina,Beijing100039,China3.TheGeneralHospitalofAirForce,Beijing100142,China[Abstract]ToprepareTanIIAloadednanos
5、tructuredlipidcarrier(TanIIA-NLC),andtostudyitsinvitroskindistribution.TheTanIIA-NLCwaspreparedbyhighpressurehomogenizationtechnologyandoptimizedbyBox-Behnkendesign-responsesurfacemethod,anditwascharacterizedintermsofmorphology,particlesize,zetapoten
6、tion,etc.ThetransdermalabsorptionofTanIIA-NLCwasevaluatedusingFranzdiffusioncells.Theresultsshowedthat,theaverageparticlesize,PDI,zetapotential,EEandDLofTanIIA-NLCpreparedbyoptimalformulation(thedrug/lipidmaterialsratiowas88,GMS/MCTratiowas2,andemuls
7、ifierconcentrationwas1%)was:182±14nm,0.1906±0.0245,-27.8±5.4mV,86.44±9.26%,and0.98±0.18%,respectively.ComparedwithTanIIAsolution,TanIIAloadedNLChadloweramountsofTanIIApenetratingthroughtheskinafterapplyingdrugfor24h,buthada3.18foldhigherretentioninth
8、eepidermis.TheseresultsindicatethatthepreparedTanIIA-NLChastheabilitytoincreasedrugconcentrationintheepidermis,andhasabroadapplicationprospects.[Keywords]:TanIIA;nanostructuredlipidcarrier;Box-Behnkendesign;invitrotransdermalabsorption;skinretention丹
