肺癌细胞特异性ZS1肽修饰脂质体的构建及其体外评价
Preparation and evaluation of liposome decorated with ZS1 peptide in vitro
作者:陈娜;张祎捷;韩纪昌;马超楠;
Author:
收稿日期: 年卷(期)页码:2015,30(04):-400-402
期刊名称:华西药学杂志
Journal Name:WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字:ZS1肽;ZS1肽修饰脂质体;肺癌;脂质体;肿瘤靶向;薄膜分散法;细胞摄取;肿瘤球穿透能力
Key words:
基金项目:
中文摘要
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。
参考文献
[1]冯俭,谢萍,秦银花,等.丹参联合5-Fu对小鼠Lewis肺癌中HIF-1α、VEGF和MVD表达的影响[J].华西药学杂志,2014,29(1):42-44.
[2]Luo JQ.Pharmacokinetic study of ZS-1,a targeted peptide to NCI-H1299,in rats following intravenous administration[J].Chromatographia,2011,73(1-2):177-181.
[3]Qin Y,Chen H,Yuan W,et al.Liposome formulated with TATmodified cholesterol for enhancing the brain delivery[J].Int J Pharm,2011,419(1-2):85-95.
[4]Chertok B,David AE,Moffat BA,et al.Substantiating in vivo magnetic brain tumor targeting of cationic iron oxide nanocarriers via adsorptive surface masking[J].Biomaterials,2009,30(35):6780-6787.
[5]Torchilin V.Tumor delivery of macromolecular drugs based on the EPR effect[J].Adv Drug Deliv Rev,2011,63(3):131-135.
[6]Kuai R,Yuan W,Qin Y,et al.Efficient delivery of payload into tumor cells in a controlled manner by TAT and Thiolytic cleavable PEG co-modified liposomes[J].Mol Pharm,2010,7(5):1816-1826.
[7]Huile G,Shuaiqi P,Zhi Y,et al.A cascade targeting strategy for brain neuroglial cells employing nanoparticles modified with angiopep-2 peptide and EGFP-EGF1 protein[J].Biomaterials,2011,32(33):8669-8675.
[8]Li J,Feng L,Fan L,et al.Targeting the brain with PEGPLGA nanoparticles modified with phage-displayed peptides[J].Biomaterials,2011,32(21):4943-4950.
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