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1、紫杉醇脂质体的体内外抗肿瘤作用研究作者：杨爱珍李军徐海军陈惠英【摘要】［目的］研究注射用紫杉醇脂质体的体外细胞毒作用和体内抗瘤作用及药物毒性。［方法］用MTT法检测紫杉醇脂质体对人肺腺癌细胞株SPC-A1的体外杀伤作用；建立小鼠实体型S180肿瘤模型，共50只，随机分为5组：5%葡萄糖溶液组佐白对照组)、紫杉醇注射液10mg/kg组和15mg/kg组，紫杉醇脂质体10mg/kg组和15mg/kg组，观察各组抑瘤作用和小鼠一般状态的变化，并检测肝功能和骨髓像改变。［结果］紫杉醇脂质体对体外培养的人肺腺癌细胞株SPC-A1在浓度为2.5ng/mK5.Ong/ml和10.0ng
2、/m1时，其抑制率分别为39.1%、51.9%和55.8%。体内给予紫杉醇脂质体10mg/(kg・d),15mg/(kg・d)3d,对才、鼠S180实体型的抑瘤率分别为31.12%和45.29%,与同样剂量紫杉醇注射液组比较无显著性差异；给药后动物行为和小鼠体重变化率较紫杉醇注射液组接近对照组；骨髓抑制程度亦低于同剂量紫杉醇注射液组。［结论］相同给药剂量下，紫杉醇脂质体的体内外抗肿瘤活性与紫杉醇注射液相接近，但药物毒副反应明显降低。【关键词】紫杉醇脂质体人肺腺癌细胞株小鼠移植性肿瘤抗肿瘤作用AStudyonAntitumorEffectofLiposomeEncapsul
3、atedPaclitaxelinVivoandinVitroYANGAi-zhenl,LIJun2,XUHai-junl,etal.(l.PLACancerCenter,the81stHospital,Nanjing210002,China;2.LabofFunction,SchoolofBasicMedicalScience,NanjingMedicalUniversity,Nanjing210002,China)Abstract:[Purpose]Tostudythecytotoxiceffectofpaclitaxelliposomeforinjectioninvi
4、tro,aswellastoobservetheantitumoractivityandtoxicityinvivo.[Methods]ThecytotoxiceffectofpaclitaxelliposomeonhumanlungadenocarcinomacelllineSPC-A1invitrowasdetectedbythiazolylblue(MTT)assay・ThemodelofmicesolidS180sarcomawasestablishedand50miceweredividedinto5groups:5%glucosesolutiongroup(c
5、ontrolgroup),lOmg/kgand15mg/kgpaclitaxelinjectiongroups,lOmg/kgand15mg/kgpaclitaxelliposomegroups・Theantitumoractivityofeachgroupandgeneralconditionofmicewereobserved,themyelogramandthehepaticfunctionindexofSI80miceweredetected・[Results]Theinhibitoryrateofpaclitaxelliposomeonhumanlungaden
6、ocarcinomacelllineSPC-A1was39.1%,51.9%and55.8%attheconcentrationsof2.5ng/ml,5.0ng/mland10.0ng/ml,respectively・Underthedosesof10mg/(kg•d),15mg/(kg•d)for3days,theinhibitoryrateofpaclitaxelliposomeagainstxenograftofsolidS180tumorinmicewas31.12%and45.29%,andtherewerenosignificantdifferenceamo
7、ngthoseofthepaclitaxelinjectiongroups・Comparingwiththepaclitaxelinjectiongroups,theanimalbehaviorandmiceweightvariablerateofpaclitaxelliposomegroupsweresimilartothecontrolgroup,andlessmyelosuppression.[Conclusion]Itsuggeststhatpaclitaxelliposomepossessedthesameanti-
