Italia Jagdish L, Bhardwaj Vivekanand, Kumar M N V Ravi
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar 160 062, Punjab, India.
Drug Discov Today. 2006 Sep;11(17-18):846-54. doi: 10.1016/j.drudis.2006.07.015.
Since its discovery in 1971, ciclosporin has revolutionized organ transplantation and the treatment of autoimmune disorders. The wide array of applications resulting from its clinical efficacy warrant unique administration strategies and varying doses, times of exposure and extents of distribution, depending on target tissue. The poor biopharmaceutical characteristics of low solubility and permeability makes this uphill task even more challenging for the drug delivery scientist. Efforts underway have explored various body routes employing approaches like emulsions, microspheres, nanoparticles, liposomes, iontophoresis and penetration enhancers. This review attempts a brief holistic view of the "four Ds" (disease, destination, dose and delivery) surrounding this immunomodulator drug.
自1971年被发现以来，环孢素彻底改变了器官移植和自身免疫性疾病的治疗。因其临床疗效而产生的广泛应用需要独特的给药策略以及不同的剂量、暴露时间和分布范围，这取决于靶组织。低溶解度和低渗透性这种较差的生物药剂学特性，使得药物递送科学家面临的这项艰巨任务更具挑战性。目前正在进行的研究已探索了各种给药途径，采用了诸如乳剂、微球、纳米颗粒、脂质体、离子导入法和渗透促进剂等方法。本综述试图对围绕这种免疫调节药物的“四个D”（疾病、靶点、剂量和递送）进行简要的全面概述。
