Yu Bo, Tai Heng Chiat, Xue Weiming, Lee L James, Lee Robert J
Department of Chemical and Biomolecular Engineering, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, USA.
Mol Membr Biol. 2010 Oct;27(7):286-98. doi: 10.3109/09687688.2010.521200.
Efficient and site-specific delivery of therapeutic drugs is a critical challenge in clinical treatment of cancer. Nano-sized carriers such as liposomes, micelles, and polymeric nanoparticles have been investigated for improving bioavailability and pharmacokinetic properties of therapeutics via various mechanisms, for example, the enhanced permeability and retention (EPR) effect. Further improvement can potentially be achieved by conjugation of targeting ligands onto nanocarriers to achieve selective delivery to the tumour cell or the tumour vasculature. Indeed, receptor-targeted nanocarrier delivery has been shown to improve therapeutic responses both in vitro and in vivo. A variety of ligands have been investigated including folate, transferrin, antibodies, peptides and aptamers. Multiple functionalities can be incorporated into the design of nanoparticles, e.g., to enable imaging and triggered intracellular drug release. In this review, we mainly focus on recent advances on the development of targeted nanocarriers and will introduce novel concepts such as multi-targeting and multi-functional nanoparticles.
治疗药物的高效且位点特异性递送是癌症临床治疗中的一项关键挑战。诸如脂质体、胶束和聚合物纳米颗粒等纳米级载体已被研究，以通过各种机制改善治疗药物的生物利用度和药代动力学特性，例如增强的渗透与滞留（EPR）效应。通过将靶向配体缀合到纳米载体上以实现对肿瘤细胞或肿瘤脉管系统的选择性递送，有可能实现进一步的改进。事实上，受体靶向纳米载体递送已在体外和体内均显示出能改善治疗反应。已研究了多种配体，包括叶酸、转铁蛋白、抗体、肽和适体。多种功能可以整合到纳米颗粒的设计中，例如实现成像和触发细胞内药物释放。在本综述中，我们主要关注靶向纳米载体开发的最新进展，并将介绍诸如多靶向和多功能纳米颗粒等新概念。
