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采用薄膜分散法制备的ZS1肽修饰共载紫杉醇(1)和姜黄素(2)的脂质体平均粒径为(92.8±3.5)nm,ζ电位为(13.50±2.55)mV。脂质体对1和2的包封率为84.5%和75.6%。脂质体在含50%胎牛血清的磷酸盐缓冲液(pH 7.4)中孵育24 h,透光率未发生明显变化,提示制品在血清中稳定性较好。体外细胞摄取试验表明,A549肺癌细胞对ZS1肽修饰脂质体的摄取效率是未修饰脂质体的3.3倍;而人脐静脉内皮细胞株(HUVEC)对两种脂质体的摄取效率相当,提示ZS1肽修饰可使脂质体具有潜在的主动靶向于A549肺癌细胞作用。细胞毒性试验结果显示,空白脂质体对A549肺癌细胞无明显细胞毒性,ZS1肽修饰共载脂质体、ZS1肽修饰1脂质体、ZS1肽修饰2脂质体及未修饰的共载药脂质体的细胞存活率分别为11%、36%、51%和61%。
The ZS1 peptide modified by thin film dispersion modified paclitaxel (1) and curcumin (2) had an average diameter of (92.8 ± 3.5) nm and a zeta potential of (13.50 ± 2.55) mV. The entrapment efficiency of liposomes to 1 and 2 was 84.5% and 75.6%. The liposomes incubated in phosphate buffered saline (pH 7.4) containing 50% fetal bovine serum for 24 h showed no obvious change in light transmittance, suggesting that the stability of the product in serum is good. In vitro cellular uptake assays showed that uptake efficiency of ZS1 peptide-modified liposomes by A549 lung cancer cells was 3.3-fold higher than that of unmodified liposomes, while HUVECs uptake efficiency of the two liposomes was comparable, It is suggested that the modification of ZS1 could make liposomes potentially active in A549 lung cancer cells. Cytotoxicity assay showed that the blank liposomes had no cytotoxicity on A549 lung cancer cells. ZS1 peptide modified liposomes, ZS1 peptide modified liposomes, ZS1 peptide modified 2 liposomes and unmodified co-drug The cell viability of liposomes was 11%, 36%, 51% and 61%, respectively.