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1、紫杉醇mPEG2PLGA纳米粒的制备及其抗肿瘤作用研究12333方琴,王季石,许红玮,李芳琼(11贵阳医学院附属医院药剂科,贵阳550004;21贵阳医学院附属医院血液科,贵阳550004;31贵阳医学院药学院,贵阳550004)摘要:目的探讨负载紫杉醇的聚乙二醇单甲醚2聚乳酸2乙醇酸(mPEG2PLGA)亲性嵌段共聚物纳米粒及其对肝癌H22细胞的体内抗肿瘤作用。方法采用界面沉积法制备紫杉醇mPEG2PLGA纳米粒(Ptx2Nps);应用透射电镜表征纳米粒的形态;粒径分析仪测其粒径及Zeta电位;研究mPEG在共聚物中的含量及紫
2、杉醇投药量对纳米粒的影响;考察纳米粒对昆明小鼠肝癌H22的疗效和过敏实验。结果Ptx2Nps成球型,粒径为纳米级(<120nm),均带负电荷(适合于静脉注射),与紫杉醇注射液(Ptx)相比,Ptx2Nps对肝癌H22的抑制作用比Ptx好。结论采用界面沉积法制备的纳米粒在紫杉醇投药量为1%,mPEG含量为4%时包封率最佳,本研究为开发紫杉醇新型静脉注射制剂提供了实验依据,mPEG2PLGA共聚物可成为抗肿瘤药物的理想新型载体。关键词:界面沉积法;聚乙二醇单甲醚2聚乳酸2乙醇酸;紫杉醇;纳米粒;肝癌中图分类号:R943;R944.9
3、文献标识码:A文章编号:1001-2494(2007)19-1483-04StudisonPreparationofPaclitaxel2loadedmPEG2PLGANanoparticlesandItsInhibitionEffectonTumor12333FANGQin,WANGJi2shi,XUHong2wei,LIFang2qiong(11DepartmentofPharmaceutics,AffiliatedHospitalofGuiyangMedicalCollege,Guiyang550004,China;21D
4、epartmentofHematology,AffiliatedHospitalofGuiYangMedicalCollege,Guiyang550004,China;31SchoolofPharmaceutics,GuiyangMedicalCollege,Guiyang550004,China)ABSTRACT:OBJECTIVEToinvestigatethecharacterizationofpaclitaxel2loadedmethoxypoly(ethyleneglyeol)2poly(lactic2co2glyco
5、licacid)copolymernanoparticlesandtheanti2tumoralactivityofthePtx2NpsonmicelivercancerH221METHODSThepacli2taxel(Ptx)poly(ethyleneglyeol2lactic2co2glycolicacid)(mPEG2PLGA)nanoparticleswerepreparedbytheinterfacialdepositionmethod1TheparticlesizeandZetapotentialwereevalu
6、atedbyMalvernZertasizer.ThemorphologyofmPEG2PLGAPtx/Npswaschar2acterizedbytransmissionelectronmicroscopy1Theinfluencesofthepaclitaxel2fedamountanddifferentcontentsofmPEGinthecopoly2meronPtx2Npswerestudied1TherapeuticeffectoftheNpswasstudiedonKunmingmicelivercancerH22
7、andhypersusceptibletestwasalsocarriedout1RESULTSPtx2Npsofpreparationallowedtheformationofsphericalnanometric(<120nm),homogeneousandnegativelychargedparticleswhichweresuitableforintravenousadministration1ThetumorinhibitingeffectofPtx2Npswasmoreeffectivecomparedwithpac
8、litaxelinjection1CONCLUSIONTheincorporationefficiencyofpaclitaxelinnanoparticleswasthebestwhenu2sing1%paclitaxel2fedamountand4%mPEG
