Aliabadi Hamidreza Montazeri, Shahin Mostafa, Brocks Dion R, Lavasanifar Afsaneh
Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta, Canada.
Clin Pharmacokinet. 2008;47(10):619-34. doi: 10.2165/00003088-200847100-00001.
Since their discovery in the early 1980s, polymeric micelles have been the subject of several studies as delivery systems that can potentially improve the therapeutic performance and modify the toxicity profile of encapsulated drugs by changing their pharmacokinetic characteristics. The efforts in this area have led in recent years to the advancement of several polymeric micellar formulations to clinical trials, some of which have shown promise in changing the biodistribution of the incorporated drug after intravenous administration as a means of tumour-targeted drug delivery. Recently, the possible benefit of polymeric micellar delivery in enhancing the absorption and bioavailability of incorporated drugs from alternative routes of drug administration has attracted interest. This article provides an overview of the effect of polymeric micellar delivery on absorption, distribution, metabolism and excretion of incorporated therapeutic agents. It also aims to assess the current information on the performance of polymeric micellar delivery systems in modifying the pharmacokinetics/pharmacodynamics of the incorporated drugs in clinical trials, and to re-examine the important structural factors required for successful design of polymeric micellar delivery systems capable of inducing favourable changes in the pharmacokinetics of the encapsulated drug.
自20世纪80年代初被发现以来，聚合物胶束一直是多项研究的主题，作为一种给药系统，它有可能通过改变药物的药代动力学特性来提高治疗效果并改变被包裹药物的毒性特征。近年来，该领域的努力促使几种聚合物胶束制剂进入临床试验阶段，其中一些制剂在静脉给药后改变所载入药物的生物分布方面显示出有望成为肿瘤靶向给药的手段。最近，聚合物胶束给药在提高所载入药物从其他给药途径的吸收和生物利用度方面的潜在益处引起了人们的兴趣。本文概述了聚合物胶束给药对所载入治疗剂的吸收、分布、代谢和排泄的影响。它还旨在评估目前关于聚合物胶束给药系统在临床试验中改变所载入药物的药代动力学/药效学方面性能的信息，并重新审视成功设计能够诱导被包裹药物药代动力学产生有利变化的聚合物胶束给药系统所需的重要结构因素。
