文献:Optimization of tumor-selective targeting by basic fibroblast growth factor-binding peptide grafted PEGylated liposomes

作者：Takeshi Terada, Miki Mizobata, Shigeru Kawakami, Fumiyoshi Yamashita, Mitsuru Hashida

文献链接：https://www.sciencedirect.com/science/article/abs/pii/S0168365907000703

摘要：

KRTGQYKLC (bFGF), is recognized by fibroblast growth factor (FGF) receptor (FGFR) via binding to basic FGF (bFGF), and is capable of being used for drug delivery to tumors highly expressing FGFR and bFGF. However, although the binding and uptake of the liposomes (bFGFp-liposomes) modified by the peptide increased in the presence of bFGF, the modification induced non-specific uptake. To overcome this problem, here, we prepared bFGFp-liposomes including mPEG-DSPE. The 5 and 10% mPEG5000/ and 10% mPEG3000/bFGFp-liposomes reduced most of the interaction with erythrocytes and the uptake by macrophages, suggesting the sustained blood circulation of bFGFp grafted PEGylated liposomes. Furthermore, 10% mPEG3000/bFGFp-liposomes produced a significant increase in uptake in NIH3T3, A549, and B16BL6 cells with the expression of FGFR following pre-incubation with bFGF, but no increase in CHO-K1 cells lacking FGFR expression. Taken together, these results lead us to believe that bFGFp grafted PEGylated liposomes possess the functions of both PEGylated stealth liposomes and the tumor-targeting liposomes. 

肽KRTGQYKLC（bFGF）通过与碱性FGF（bFGF）结合被成纤维细胞生长因子（FGF）受体（FGFR）识别，并且能够用于向高表达FGFR和bFGF的肿瘤递送药物。

然而，尽管在bFGF存在下，肽修饰的脂质体（bFGFp脂质体）的结合和摄取增加，但这种修饰诱导了非特异性摄取。为了克服这个问题，我们在这里制备了含有mPEG-DSPE的bFGFp脂质体。

5%mPEG5000/和10%mPEG3000/bFGFp脂质体减少了与红细胞的大部分相互作用和巨噬细胞的摄取，表明bFGFp接枝PEG化脂质体的持续血液循环。

此外，10%mPEG3000/bFGFp脂质体在与bFGF预孵育后，在表达FGFR的NIH3T3、A549和B16BL6细胞中显著增加了摄取，但在缺乏FGFR表达的CHO-K1细胞中没有增加。

综上所述，这些结果使我们相信bFGFp接枝的PEG化脂质体具有PEG化隐形脂质体和肿瘤靶向脂质体的功能。

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DSPE-PEG-NTA-NI

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DSPE-PEG-PEI

DSPE-PEG-PLA

DSPE-PEG-PLGA

DSPE-PEG-Progestrone

DSPE-PEG-RGD

DSPE-PEG-SC

DSPE-PEG-SCM

DSPE-PEG-SG

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