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目的制备肺癌细胞特异性ZS1肽修饰脂质体(ZS1-LP),并评价其肺癌靶向性。方法采用薄膜分散法制备ZS1-LP,考察其形态、粒径、电位以及体外稳定性。以A549细胞为阳性细胞,HUVEC细胞为阴性细胞研究细胞对ZS1-LP的摄取。构建肿瘤球模型,研究ZS1-LP的肿瘤球穿透能力。结果 ZS1-LP的平均粒径为98.8±7.5 nm,Zeta电位为13.50±2.41 m V。ZS1-LP在24 h内具有良好的血清稳定性。体外细胞摄取实验表明:A549肺癌细胞对ZS1-LP的摄取效率是普通脂质体的3.2倍。HUVEC细胞对ZS1-LP的摄取效率与对LP的摄取效率相当。定性的细胞摄取实验和肿瘤球穿透实验结果显示:ZS1-LP组的荧光强度显著强于LP组的。结论 ZS1-LP的制备方法简单,能够与肺癌细胞特异性结合,是一种潜在、高效的肺癌靶向给药系统。
Objective To prepare lung cancer cell-specific ZS1 peptide modified liposomes (ZS1-LP) and evaluate its lung cancer targeting. Methods ZS1-LP was prepared by thin-film dispersion method and its morphology, particle size, potential and in vitro stability were investigated. A549 cells as positive cells, HUVEC cells as negative cells to study cell uptake of ZS1-LP. Tumor ball models were constructed to investigate the tumor ball penetration ability of ZS1-LP. Results The average diameter of ZS1-LP was 98.8 ± 7.5 nm and the zeta potential was 13.50 ± 2.41 mV. ZS1-LP has good serum stability within 24 h. In vitro cellular uptake experiments showed that the uptake efficiency of ZS1-LP in A549 lung cancer cells was 3.2 times higher than that of the normal liposomes. The uptake efficiency of ZS1-LP by HUVEC cells is comparable to that of LP. Qualitative cellular uptake experiments and tumor ball penetration experiments showed that the fluorescence intensity of ZS1-LP group was significantly higher than that of LP group. Conclusion The preparation method of ZS1-LP is simple and can bind specifically with lung cancer cells. It is a potential and efficient targeted drug delivery system for lung cancer.