Arshady R
Department of Chemistry, Imperial College of Science, Technology and Medicine, University of London, UK.
J Mol Recognit. 1996 Sep-Dec;9(5-6):536-42. doi: 10.1002/(sici)1099-1352(199634/12)9:5/6<536::aid-jmr297>3.0.co;2-s.
One of the major obstacles to the targeted delivery of colloidal carriers (nanocapsules) is the body's own defence mechanism in capturing foreign particles by the reticuloendothelial system (RES). This means that following intravenous administration, practically all nanometer size particles are captured by the RES (mainly the liver). This paper draws attention to a recent initiative on the design of 'macromolecular homing devices' which seem to disguise nanoparticles from the RES, and hence are of potential interest for the targeted delivery of nanocapsular carriers. The idea is based on a graft copolymer model embodying a link site for attachment (binding) to the carrier, a floating pad for maintaining the particles afloat in the blood stream, an affinity ligand for site-specific delivery and a structural tune for balancing the overall structure of the homing device. A general synthetic scheme for the preparation of such graft copolymers is given, and preliminary biological evaluations relating to the floating pad concept are discussed.
胶体载体（纳米胶囊）靶向递送的主要障碍之一是机体自身的防御机制，即网状内皮系统（RES）捕获外来颗粒。这意味着静脉给药后，几乎所有纳米尺寸的颗粒都会被RES（主要是肝脏）捕获。本文关注了一项关于“大分子归巢装置”设计的最新举措，该装置似乎能使纳米颗粒不被RES识别，因此对纳米胶囊载体的靶向递送具有潜在意义。这个想法基于一种接枝共聚物模型，该模型包含一个用于与载体连接（结合）的连接位点、一个使颗粒在血流中保持漂浮的漂浮垫、一个用于位点特异性递送的亲和配体以及一个用于平衡归巢装置整体结构的结构调节部分。给出了制备此类接枝共聚物的一般合成方案，并讨论了与漂浮垫概念相关的初步生物学评估。
