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本研究构建了能够靶向肿瘤的新型纳米粒(脂质体-鱼精蛋白-硫酸软骨素纳米粒,LPC-NP)。该纳米粒粒径约90 nm,zata电位约+35 mV。采用后插法对LPC纳米粒进行DSPE-PEG_(2000)或DSPE-PEG_(2000)-T7修饰。T7是与转铁蛋白功能类似的七肽,能够靶向转铁蛋白受体过度表达的乳腺癌细胞MCF-7。PEG修饰可显著降低血清对LPC纳米粒的聚集作用,T7修饰的纳米粒显著提高siRNA的细胞摄取和基因沉默效率。体外细胞毒实验表明抗EGFR siRNA显著抑制MCF-7细胞生长。实验结果表明经T7肽修饰的LPC纳米粒有望成为RNA干扰肿瘤治疗的递送载体。
In this study, a novel nanoparticle targeting liposome (liposome-protamine chondroitin sulfate nanoparticles, LPC-NP) was constructed. The nanoparticles have a diameter of about 90 nm and a zata potential of about +35 mV. The LPC nanoparticles were modified with DSPE-PEG_ (2000) or DSPE-PEG_ (2000) -T7 using post-insert method. T7 is a heptapeptide functionally similar to transferrin and is capable of targeting breast cancer cell MCF-7 overexpressing transferrin receptor. PEG modification can significantly reduce serum aggregation of LPC nanoparticles, T7 modified nanoparticles significantly improve siRNA cell uptake and gene silencing efficiency. In vitro cytotoxicity experiments showed that anti-EGFR siRNA significantly inhibited the growth of MCF-7 cells. The experimental results show that the T7 peptide-modified LPC nanoparticles is expected to become a delivery vector for RNA interference tumor therapy.