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暴露神经降压素肿瘤特异性驱动因素的纳米颗粒。

Nanoparticles exposing neurotensin tumor-specific drivers.

机构信息

Department of Medical Biotechnology, University of Siena, Siena, Italy.

出版信息

J Pept Sci. 2013 Apr;19(4):198-204. doi: 10.1002/psc.2493. Epub 2013 Feb 25.

Abstract

Nanoparticles have attracted much attention for their potential application as in vivo carriers of drugs. Labeling of nanoparticles with bioactive markers that are able to direct them toward specific biological target receptors has led to a new generation of drug delivery systems. In particular, low molecular weight peptides that remain stable in vivo could be promising tools to selectively drive nanoparticles loaded with active components to tumor cells. We reported, recently, that tetrabranched neurotensin peptides (NT4) may be used to selectively target tumor cells with liposomes. Liposomes functionalized with tetrabranched neurotensin peptide, NT4, and loaded with doxorubicin showed clear advantages in cell binding, anthracyclin internalization, and cytotoxicity in respect of not functionalized liposomes. In this study, we compare branched (NT4) versus linear (NT) peptides in the ability to drive liposomes to target cells and deliver their toxic cargo. We showed here that the more densely decorated liposomes had a better activity profile in terms of drug delivery. Presentation of peptides to the cell membranes in the grouped shape provided by branched structure facilitates liposome cell binding and fusion.

摘要

纳米粒子因其作为药物体内载体的潜在应用而引起了广泛关注。将生物活性标记物标记到纳米粒子上,使其能够靶向特定的生物靶受体,从而产生了新一代的药物输送系统。特别是,体内稳定的低分子量肽可能是将负载有活性成分的纳米粒子选择性地导向肿瘤细胞的有前途的工具。我们最近报道称,四分支神经降压素肽(NT4)可用于通过脂质体选择性靶向肿瘤细胞。用四分支神经降压素肽(NT4)功能化并负载多柔比星的脂质体在细胞结合、蒽环类药物内化和细胞毒性方面明显优于未功能化的脂质体。在这项研究中,我们比较了支化(NT4)和线性(NT)肽在驱动脂质体靶向细胞和传递其毒性货物的能力。我们在这里表明,用支化结构提供的聚集形状呈现给细胞膜的肽更有利于脂质体与细胞的结合和融合。

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