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树状高分子药代动力学:大小、结构和表面特性对 ADME 性质的影响。

Dendrimer pharmacokinetics: the effect of size, structure and surface characteristics on ADME properties.

机构信息

Drug Delivery Disposition & Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University. 381 Royal Parade, Parkville, VIC, 3052, Australia.

出版信息

Nanomedicine (Lond). 2011 Aug;6(6):1063-84. doi: 10.2217/nnm.11.67.

DOI:10.2217/nnm.11.67
PMID:21955077
Abstract

Dendrimers show increasing promise as drug-delivery vectors and can be generated with a wide range of scaffold structures, sizes and surface functionalities. To this point, the majority of studies of dendrimer-based drug-delivery systems have detailed pharmacodynamic outcomes, or have followed the pharmacokinetics of a solubilized or conjugated drug. By contrast, detailed commentary on the in vivo fate of the dendrimer carrier is less evident, even though the pharmacokinetics of the carrier will likely dictate both pharmacodynamic and toxicokinetic outcomes. In the current article, the influence of size, structure and surface functionality on the absorption, distribution, metabolism and elimination (ADME) properties of dendrimers have been examined and the implications of these findings for delivery system design are discussed.

摘要

树状高分子作为药物传递载体的前景越来越广阔,并且可以用各种支架结构、大小和表面官能团来生成。到目前为止,大多数基于树状高分子的药物传递系统的研究都详细描述了药效学结果,或者跟踪了溶解或共轭药物的药代动力学。相比之下,对树状高分子载体体内命运的详细评论就不那么明显了,尽管载体的药代动力学很可能决定药效学和毒代动力学结果。在本文中,研究了大小、结构和表面官能团对树状高分子的吸收、分布、代谢和消除(ADME)性质的影响,并讨论了这些发现对传递系统设计的意义。

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