Division of Pharmacotherapy and Experimental Therapeutics, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, USA.
J Liposome Res. 2012 Sep;22(3):177-92. doi: 10.3109/08982104.2012.655285. Epub 2012 Feb 15.
Various attempts to increase the therapeutic index of the drug while minimizing side effects have been made in drug delivery systems. Among several promising strategies, liposomes represent an advanced technology to target active molecules to the site of action. Rapid clearance of circulating liposomal drugs administered intravenously has been a critical issue because circulation time in the blood affects drug exposure at the target site. The clinical use of liposomal drugs is complicated by large intra- and interindividual variability in their pharmacokinetics (PK) and pharmacodynamics (PD). Thus, it is important to understand the factors affecting the PK/PD of the liposomal formulation of drugs and to elucidate the mechanisms underlying the variability in the PK/PD of liposomal drugs. In this review article, we describe the characteristics of liposome formulations and discuss the effects of various factors, including liposome-associated factors, host-associated factors, and treatment on the PK/PD of liposomal agents.
在药物传递系统中，人们尝试了各种方法来提高药物的治疗指数，同时将副作用降至最低。在几种有前途的策略中，脂质体是一种将活性分子靶向作用部位的先进技术。静脉内给予的循环脂质体药物的快速清除一直是一个关键问题，因为血液循环时间会影响药物在靶部位的暴露。脂质体药物的临床应用受到其药代动力学（PK）和药效学（PD）个体内和个体间变异性大的影响。因此，了解影响脂质体药物制剂 PK/PD 的因素，并阐明脂质体药物 PK/PD 变异性的机制非常重要。在这篇综述文章中，我们描述了脂质体制剂的特点，并讨论了各种因素对脂质体药物 PK/PD 的影响，包括与脂质体相关的因素、宿主相关的因素和治疗方法。
