硫酸长春新碱热敏脂质体的制备和质量评价

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1、硫酸长春新碱热敏脂质体的制备和质量评价*李明媛，张慧，杨臻博，李晗，梅乐，梅兴国(军事医学科学院毒物药物研究所，北京100850)摘要:目的制备硫酸长春新碱(vincristine，VCＲ)热敏脂质体，测定其粒径及体外释药热敏特性，建立脂质体含量、包封率及有关物质的测定方法。方法pH梯度主动载药法制备长春新碱热敏脂质体，激光粒度分析仪测定脂质体粒径;以水为释放介质，分别考察脂质体在37和42℃的释放特性;超滤离心法测定脂质体包封率;HPLC测定脂质体中长春新碱的含量及有关物质。结果长春新碱热敏脂质体的平均粒径为(86±6)nm，37℃几乎不释放，42℃30min内释放约90%;3批样品包封

2、率均－1高于95%;含量为1.92mg·mL，有关物质符合药典要求。结论长春新碱长循环热敏脂质体的制备工艺简单稳定，所制备的脂质体粒径均一，具有明显的热敏特性，包封率高，适于－20℃长期储存。脂质体含量、包封率及有关物质测定方法简便、快速、准确。关键词:硫酸长春新碱;热敏脂质体;粒径;热敏特性;包封率;超滤离心;含量;有关物质doi:10.11669/cpj.2014.18.009中图分类号:Ｒ944文献标志码:A文章编号:1001－2494(2014)18－1615－05PreperationandQualityEvaluationofVincristineSulfateThermose

3、nsitiveLiposomes*LIMing-yuan，ZHANGHui，YANGZhen-bo，LIHan，MEILe，MEIXing-guo(InstituteofPharmacologyandToxicology，AcademyofMilitaryMedicalSciences，Beijing100850，China)ABSTＲACT:OBJECTIVETopreparevincristinesulfate(VCＲ)thermosensitiveliposomes，andevaluateitsparticlesizeandre-leasecharacteristicsinvitro

4、andestablishthemethodsfordeterminationofcontent，entrapmentefficiencyandrelatedsubstances.METHODSpHgradientactivedrug-loadingwasusedtoprepareVCＲliposomes;photoncorrelationspectroscopywasusedtodeterminetheparticlesize;theinvitroreleasepropertiesofVCＲliposomesin37and42℃waterwerecompared;theentrapment

5、efficiencyoftheliposomeswasdeterminedbyusingcentrifugalultrafiltration;HPLCwasappliedforthedeterminationofcontentandrelatedsubstances.ＲESULTSTheaverageparticlesizeofVCＲliposomeswas(86±6)nm，andtheliposomeshardlyreleasedat37℃andreleasedabout90%within30minat42℃，showingobviousthermosensitiveproperty;t

6、heentrapmentefficienciesfor3batcheswerehigherthan95%;－1thecontentwas1.92mg·mL，withtherelatedsubstanceinlinewiththepharmacopoeiarequirements.CONCLUSIONTheprepa-rationprocessforVCＲliposomeissimpleandstable.Theliposomeshavenarrowparticlesizedistributionaswellasobviousthermosensi-tiveproperty，anditals

7、ohashighdrugencapsulationefficiencyandisstableat－20℃inlong-termstorage.Thedeterminationmethodsforthecontent，encapsulationefficiencyandrelatedsubstancesofVCＲliposomesaresimple，rapidandaccurate.KEYWOＲDS:vincristine