RGD修饰的多柔比星脂质体的制备及体外抗肿瘤活性.pdf

·892· Jo啪alofPhannaceuticals 中国医药工业杂志Chinese 2013，44(9) RGD修饰的多柔比星脂质体的制备及体外抗肿瘤活性 魏霖1，周有霞2，程丽芳1，程亮1，陈大为1’24 (1．苏州大学药学院，江苏苏州215123；2．沈阳药科大学药学院，辽宁沈阳110016) 摘要：合成了胆固醇一聚乙二醇一RGD(CHOL—PEG2000．RGD)，并经1H NMR确证结构。采用pH梯度法制备多柔比星 的空白脂质体并无明显的细胞抑制作用。 关键词：RGD；多柔比星；脂质体；合成；体外抗肿瘤活性 中图分类号：R944．9文献标志码：A 文章编号：100l一8255(2013)09一0892—05 and扔1，f办切Anti—tumorof Preparation ActiVity DoxombicinDecoratedwithRGD Liposomes Peptide WEI Daweil，24 Linl，ZHOUYbuxia2，CHENGLifan91，CHENGLian91，CHEN sctence．S00chow 215123： 01．C0llege可PhnrmnceuticnlUnive凇it))．Suzhou PhnrlHdceHticni llool6) 2．schoot西Phnmncy．shenydngUniversi哆．she，lydng ABSTRACT：The 2000一RGD)was cholesterol—polyemyleneglycol-RGD(CHOL—PEGsuccessfully anditss仃ucturewascon丘n11ed1HNMR．Thedoxolllbicin methodweremodified by liposomespreparedbypH—gradient with 2000一RGDasme method．Themean and CHOL-PEG particle ligandbypost—insertion size，potential ofthe obsenrationof e伍ciencyproductwere(122．5土2．8)nm，(一18．35土0．78)mV 饥msmissionelec仃on showedthatthe wasnanometer-sized resultsof砌1，f办．o microscope product sphericalparticles．The B16cellsshowedthe Valuesofthebulk andRGDmodified cytotoxicitystudya