Department of Pharmaceutical Technology, Faculty of Pharmacy and Biochemistry, University of Zagreb, Zagreb, Croatia.
Eur J Pharm Sci. 2013 Sep 27;50(1):42-55. doi: 10.1016/j.ejps.2013.04.012. Epub 2013 Apr 22.
Non-parenteral delivery of drugs using nanotechnology-based delivery systems is a promising non-invasive way to achieve effective local or systemic drug delivery. The efficacy of drugs administered non-parenterally is limited by their ability to cross biological barriers, and epithelial tissues particularly present challenges. Polymeric micelles can achieve transepithelial drug delivery because of their ability to be internalized into cells and/or cross epithelial barriers, thereby delivering drugs either locally or systematically following non-parenteral administration. This review discusses the particular characteristics of various epithelial barriers and assesses their potential as non-parenteral routes of delivery. The material characteristics of polymeric micelles (e.g., size, surface charge, and surface decoration) and of unimers dissociated from polymeric micelles determine their interactions (non-specific and/or specific) with mucus and epithelial cells as well as their intracellular fate. This paper outlines the mechanisms governing the major modes of internalization of polymeric micelles into epithelial cells, with an emphasis on specific recent examples of the transport of drug-loaded polymeric micelles across epithelial barriers.
利用基于纳米技术的递药系统进行非肠道给药是一种很有前途的非侵入性方法，可实现有效的局部或全身药物递送。非肠道给予的药物的疗效受到其穿过生物屏障的能力的限制，而上皮组织尤其带来了挑战。聚合物胶束由于能够被内化到细胞中和/或穿过上皮屏障，因此可以在非肠道给药后局部或系统地递药，从而实现跨上皮药物递送。本综述讨论了各种上皮屏障的特殊特征，并评估了它们作为非肠道给药途径的潜力。聚合物胶束的材料特性（例如，大小、表面电荷和表面修饰）和从聚合物胶束解离的单体决定了它们与黏液和上皮细胞的相互作用（非特异性和/或特异性）及其细胞内命运。本文概述了控制聚合物胶束进入上皮细胞的主要内化模式的机制，重点介绍了载药聚合物胶束穿过上皮屏障的特定最新实例。
