Torchilin V P
Department of Pharmaceutical Sciences, Northeastern University, Mugar Building, Room 312, 360 Huntington Avenue, Boston, Massachusetts 02115, USA.
Cell Mol Life Sci. 2004 Oct;61(19-20):2549-59. doi: 10.1007/s00018-004-4153-5.
Polymeric micelles (micelles formed by amphiphilic block copolymers) demonstrate a series of attractive properties as drug carriers, such as high stability both in vitro and in vivo and good biocompatibility, and can be successfully used for the solubilization of various poorly soluble pharmaceuticals. These micelles can also be used as targeted drug delivery systems. The targeting can be achieved via the enhanced permeability and retention effect (into the areas with the compromised vasculature), by making micelles of stimuli-responsive amphiphilic block copolymers, or by attaching specific targeting ligand molecules to the micelle surface. Immunomicelles prepared by coupling monoclonal antibody molecules to p-nitrophenylcarbonyl groups on the water-exposed termini of the micelle corona-forming blocks demonstrate high binding specificity and targetability. Immunomicelles prepared with cancer-specific monoclonal antibody 2C5 specifically bind to different cancer cells in vitro and demonstrate increased therapeutic activity in vivo. This new family of pharmaceutical carriers can be used for the solubilization and targeted delivery of poorly soluble drugs to various pathological sites in the body.
聚合物胶束（由两亲性嵌段共聚物形成的胶束）作为药物载体展现出一系列吸引人的特性，比如在体外和体内都具有高稳定性以及良好的生物相容性，并且能够成功用于增溶各种难溶性药物。这些胶束还可以用作靶向给药系统。靶向作用可以通过增强的渗透和滞留效应（进入血管系统受损的区域）来实现，通过制备刺激响应性两亲性嵌段共聚物的胶束，或者通过将特定的靶向配体分子连接到胶束表面。通过将单克隆抗体分子偶联到胶束冠层形成嵌段的水暴露末端上的对硝基苯基羰基基团而制备的免疫胶束表现出高结合特异性和靶向性。用癌症特异性单克隆抗体2C5制备的免疫胶束在体外能特异性结合不同的癌细胞，并在体内表现出增强的治疗活性。这类新型药物载体可用于增溶难溶性药物并将其靶向递送至体内的各种病理部位。
