Caracciolo Giulio
Department of Molecular Medicine, "Sapienza" University of Rome, Rome, Italy.
Nanomedicine. 2015 Apr;11(3):543-57. doi: 10.1016/j.nano.2014.11.003. Epub 2014 Dec 30.
Active targeting that exploits the (over)expression of surface receptors in target cells by ligand incorporation is a central concept in nanomedicine research. Despite unprecedented efforts, no targeted liposome-based therapeutics is commercially available for clinical practice. What is inhibiting the efficient translation of targeted liposome technology from bench to bedside? After introduction in the bloodstream, the lipid surface is immediately modified by the adsorption of a "protein corona" and preserving the surface functionality appears to be challenging. On the other hand, a long-standing corona with receptor-binding sites could associate with the target cell long enough to activate the cell's uptake machinery, triggering liposome endocytosis and intracellular cargo delivery. This opens the intriguing possibility to manipulate the corona composition by liposome design. This review will focus on the emerging field of liposome-protein corona research from basic, descriptive research to readily applicable knowledge and technologies for implementation in drug improvement and development. From the clinical editor: This review is addressing the liposome protein corona research concerning the potential gains in drug improvement and for drug development.
通过配体结合利用靶细胞表面受体（过）表达的主动靶向是纳米医学研究的核心概念。尽管付出了前所未有的努力，但目前尚无基于靶向脂质体的疗法可用于临床实践。是什么阻碍了靶向脂质体技术从实验室到临床的有效转化？脂质体进入血液后，其脂质表面会立即被“蛋白冠”的吸附所修饰，而保持表面功能似乎具有挑战性。另一方面，带有受体结合位点的持久蛋白冠可能与靶细胞结合足够长的时间，以激活细胞的摄取机制，触发脂质体的内吞作用和细胞内货物递送。这为通过脂质体设计来操纵蛋白冠组成提供了有趣的可能性。本综述将聚焦于脂质体-蛋白冠研究这一新兴领域，从基础的描述性研究到可直接应用于药物改进和开发的知识与技术。临床编辑点评：本综述探讨了脂质体蛋白冠研究在药物改进和药物开发方面的潜在益处。
