紫杉醇聚氰基丙烯酸正丁酯纳米粒制备研究-南方医科大学学报.PDF

2010;30(4) 南方医科大学学报(JSouthMedUniv) 窑763 窑 紫杉醇聚氰基丙烯酸正丁酯纳米粒制备研究 陈如大袁任 非袁李国锋袁刘思佳渊南方医科大学南方医院药学部袁广东 广州 510515冤 摘要院目的评价紫杉醇聚氰基丙烯酸正丁酯纳米粒渊PTX-PBCA-NP 冤的不同制备工艺对紫杉醇的包封率和载药量的 影响袁优选PTX-PBCA-NP 的制备工艺遥 方法以包封率和载药量为主要评价指标袁分别采用界面缩聚法和乳化聚合 法制备PTX-PBCA-NP 袁进行对比研究遥 用正交设计优选处方遥 结果界面缩聚法尧乳化聚合法制备的PTX-PBCA-NP 的包封率范围均在94.39%~99.23%渊n=3冤之间袁界面缩聚法制备的PTX-PBCA-NP 的载药量可达渊1.07依0.03冤%渊n=3冤袁 而乳化聚合法制备的PTX-PBCA-NP 的载药量可达 渊0.86依0.01冤%渊n=3冤遥 用正交试验优选出最佳工艺条件袁PTX- PBCA-NP 载药量为0.80%袁包封率为95.71%袁粒径为235.6nm遥 结论两种制备方法制备出来的PTX-PBCA-NP 的 包封率符合药典要求遥 经比较研究袁界面缩聚法可能是提高PTX-PBCA-NP 载药量较好的一种制备方法渊P0.05冤遥 关键词院紫杉醇曰聚氰基丙烯酸正丁酯曰纳米粒曰界面缩聚曰乳化聚合 中图分类号院R944 文献标识码院A 文章编号院1673-4254(2010)04-0763-04 Preparationofpaclitaxel-loadedpolybutylcyanoacrylatenanoparticles CHENRu-da,RENFei,LIGuo-feng,LIUSi-jia DepartmentofPharmacy,NanfangHospital,SouthernMedicalUniversity,Guangzhou510515,China Abstract: ObjectiveToevaluatetheeffectofdifferentpreparationmethodsontheencapsulationefficiency (EE) anddrug loading(DL) ofpaclitaxel-loadedpolybutylcyanoacrylatenanoparticles(PTX-PBCA-NPs) and optimizethepreparation of PTX-PBCA-NPs. Methods With DL and EE a sthe major indexes, the qualitie sof PTX-PBCA-NP sproduced by the interfacialpolymerizationandemulsionpolymerizationmethodwerecompared. Theoptimizedprescriptionwasobtainedby orthogonaldesign. ResultsTherangesofEEofPTX-PBCA-NPswiththetwomethodswereboth94.39%-99.23%. The highestDLwithinterfacialpolymerizationwas(1.07依0.03)%, ascomparedto(0.86依0.01)%withemulsionpolymerization. TheoptimizedpreparationconditionsresutedinthemeansizeofPTX-PBCA-NPsof235.6nm, DLof0.80%, andEEof 95.71%. ConclusionsTheEEofPTX-PBCA-NPspreparedbytheabovetwomethodsisconsistentwiththerequirementof thePharmacopoeiaofChina,andPTX-PBCA-NPscontaininghigherDLcanbeobtianedviainterfacialpolymerization. Keywords:paclitaxel;polybutylcyanoacrylate;nanoparticles;interfacialpoly