Davis S S, Hunneyball I M, Illum L, Ratcliffe J H, Smith A, Wilson C G
Pharmacy Department, University of Nottingham, University Park, UK.
Drugs Exp Clin Res. 1985;11(9):633-40.
In recent years the concept of using small colloidal particles for the selective delivery of drugs has been explored experimentally using a variety of different physical systems (for example, phospholipid vesicles (liposomes), triglyceride emulsions, albumin microspheres) and routes of administration. In such studies the aim has been to target a potent pharmacological agent on an organ or tissue site, thereby reducing adverse reactions and side-effects, or to provide a means of controlled release. The design of appropriate delivery systems must take into account the nature of the target and physiological barriers to targeting as well as factors such as drug loading and drug release, stability of the carrier system and its biocompatibility and biodegradation. Targeting with microspheres can be divided into passive methods that rely upon physiological and physicochemical determinants such as entrapment in capillary beds (lungs - particle size) or uptake by phagocytic cells (liver-surface characteristics), an active method whereby the particle is directed to a specific site through the use of surface coatings (surfactants, glycolipids, monoclonal antibodies) or a material sensitive to an external influence. Candidate systems presently under study are described. These include lipid emulsions for intravenous administration and microspheres for intra-articular delivery.
近年来，利用小胶体颗粒进行药物选择性递送的概念已通过各种不同的物理系统（例如磷脂囊泡（脂质体）、甘油三酯乳剂、白蛋白微球）和给药途径进行了实验探索。在此类研究中，目标是将强效药理剂靶向作用于器官或组织部位，从而减少不良反应和副作用，或者提供一种控释手段。合适的递送系统的设计必须考虑靶点的性质、靶向的生理屏障以及诸如药物负载和药物释放、载体系统的稳定性及其生物相容性和生物降解等因素。微球靶向可分为被动方法和主动方法，被动方法依赖于生理和物理化学决定因素，如毛细血管床截留（肺部 - 粒径）或吞噬细胞摄取（肝脏 - 表面特征）；主动方法是通过使用表面涂层（表面活性剂、糖脂、单克隆抗体）或对外部影响敏感的材料将颗粒导向特定部位。本文描述了目前正在研究的候选系统。这些系统包括用于静脉给药的脂质乳剂和用于关节内递送的微球。
