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《多烯紫杉醇长循环脂质体的制备工艺优选及体外释放性能考察-论文.pdf》由会员上传分享,免费在线阅读,更多相关内容在行业资料-天天文库。
1、第20卷第12期中国实验方剂学杂志V01.20.No.122014年6月ChineseJournalofExperimentalTraditionalMedicalFormulaeJun.,2014多烯紫杉醇长循环脂质体的制备工艺优选及体外释放性能考察陈宇潮,程怡,仝一丹,陈静(广州中医药大学中药学院,广州510006)[摘要]目的:优选多烯紫杉醇长循环脂质体(DPL)的处方与制备工艺并考察其体外释药性能。方法:以蛋黄卵磷脂(EPC)、胆固醇(CH)和聚乙二醇2000一二硬脂酰磷脂酰乙醇胺(PEG2000一DSPE)为膜材,采用薄膜分散.高压均质法制备DPL。通
2、过单因素试验确定均质压力和均质循环次数,正交试验筛选处方工艺;利用透析法测定脂质体包封率,透射电镜观察脂质体形态,动态光散射粒度分析仪测定脂质体粒径分布与Zeta电位,考察DPL的体外释放规律。结果:最佳处方为药物一类脂(1:5),EPC—CH(4:1),PEG2000-DSPE加入量4%;高压均质条件为50MPa,循环数3次;DPL包封率(97.44±1.33)%,平均粒径(162.17±2.63)nm,平均Zeta电位(一14.54±1.82)mV;DPL在48h内仅释放65%,体外药物释放符合Weibull方程。结论:采用PEG2000一DSPE作为长循环
3、材料可增大脂质体的粒径,DPL具有一定缓释作用。[关键词]多烯紫杉醇;长循环脂质体;包封率;体外释放性能;薄膜分散一高压均质法[中图分类号]R283.6【文献标识码]A[文章编号]1005—9903(2014)12-0006—04[doi】lO.13422/j.cnki.syfjx.2014120006[网络出版地址]http://www.cnki.net/kems/detaiL/11.3495.R.20140409.1447.001.html[网络出版时间]2014-04-0914:47OptimizationofPreparationTechnologyfo
4、rLong-circulatingLiposomesofDocetaxelandInvestigationofItsinvitroReleasePropertiesCHENYu—chao,CHENGYi,TONGYi—dan,CHENJing(SchoolofChineseMateriaMedica,GuangzhouUniversityofChineseMedicine,Guangzhou510006,China)[Abstract]0bjective:Tooptimizepreparationandformulationtechnologyoflong—ci
5、rculatingliposomesofdocetaxel(DPL)andinvestigateitsinvitroreleaseproperties.Method:Usingeggphosphatidylcholine(EPC),cholesterol(CH)andpolyethyleneglycol2000-distearoylph0sphatidylethan0lamine(PEG2000一DSPE)asrawmaterials,DPLwaspreparedbyfilmdispersion—highpressurehomogenizationtechniq
6、ue.Homogenizationpressureandrecurringnumberweredeterminedbysinglefactortests,orthogonaldesignwasusedtoselectformulation.Encapsulationeficiencyofliposomeswasdeterminedbydialysis,transmissionelectronmicroscopywasusedtoobservemorphousanddynamiclightscatteringparticlesizemeterwasusedtode
7、tectparticledistributionandZetapotential,theninvitroreleaseconductsofliposomeswereinvestigated.Result:Optimalpreparationandformulationconditionswereasfollows:drug-lipid(1:5),EPC—CH(4:1),PEG2000.DSPEaddedinanamountof4%.H0mogenizationpressureof50MPafor3times;undertheseconditions,averag
8、eencapsulati
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