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分别采用二硬脂酰磷脂酰胆碱(DSPC)、氢化大豆磷脂(HSPC)、二棕榈酰磷脂酰胆碱(DPPC)和二肉豆蔻酰磷脂酰胆碱(DMPC)为载体,制备了NGR肽(Asn-Gly-Arg)修饰的主动靶向脂质体,并用其负载香豆素-6。结果表明,4种脂质体的粒径为120~160 nm,粒度分布均匀,?电位接近中性,包封率均在95%以上。差示扫描量热分析(DSC)表明,4种脂质体的相变温度(Tm)值由高至低分别为DSPC脂质体>HSPC脂质体>DPPC脂质体>DMPC脂质体。以CD13高表达的HT1080细胞为模型,采用流式细胞仪、激光共聚焦显微镜观察评价脂质体的入胞效果。结果显示,脂质体的入胞效率与Tm值呈正相关。
NGR peptide was prepared by using DSPC, HSPC, DPPC and DMPC as carriers respectively. (Asn-Gly-Arg) modified active targeting liposomes, and use it to load coumarin-6. The results showed that the four liposomes had a particle size of 120-160 nm, a uniform particle size distribution and a near neutral potential with entrapment efficiencies above 95%. Differential scanning calorimetry (DSC) showed that the phase transition temperature (Tm) values of the four liposomes were DSPC liposomes> HSPC liposomes> DPPC liposomes> DMPC liposomes from high to low, respectively. The high expression of CD13 HT1080 cells as a model, the use of flow cytometry, laser confocal microscopy evaluation of liposomes into the cell effect. The results showed that the efficiency of liposome entry was positively correlated with Tm.