Supramolecular drug-delivery systems based on polymeric core-shell architectures
Supramolecular drug-delivery systems based on polymeric core-shell architectures
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DOI：
10.1002/anie.200301694
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发表时间：
2004-01-01
影响因子：
16.6
通讯作者：
Haag, R
中科院分区：
文献类型：
--
作者：
Haag, R
新药的理化性质是决定其在体内是否成功的重要因素。基于成功和不成功的药物的许多结构-活性特征，已经根据经验假设了许多标准，用于通过扩散穿过细胞膜有效地细胞摄取这些小药物分子。[1]然而，许多有效的候选药物由于有限的溶解度、稳定性和毒性而在临床前研究中失败。因此，已经开发了许多药物递送系统来克服这些运输问题。[2-4]这些包括两亲分子的物理聚集体，例如聚合物胶束[3-5]以及稳定的单分子胶束[6]，其在聚合物治疗的黎明时代被认为是强大的纳米载体。[7]这一亮点集中在聚合物核壳结构（即嵌段共聚物和单分子胶束）的一些最新发展以及这种超分子药物递送系统的细胞摄取途径。与小表面活性剂分子的胶束相比，聚合物胶束（方案1）通常更稳定，并且可以将负载的药物保留更长的时间。[3]街区-
The physicochemical properties of new drugs are important factors regarding whether they will be successful in vivo. A number of criteria have been empirically postulated based on numerous structure–activity profiles of successful and nonsuccessful drugs for the efficient cellular uptake of these small drug molecules by diffusion through the cell membrane.[1] However, many potent drug candidates fail in preclinical studies because of limited solubility, stability, and toxicity. Thus, a number of drugdelivery systems have been developed to overcome these transport problems.[2–4] These include physical aggregates of amphiphilic molecules, such as polymeric micelles [3–5] as well as stable unimolecular micelles,[6] which have been considered as powerful nanocarriers in the dawning era of polymer therapeutics.[7]This highlight focuses on some recent developments of polymeric core–shell architectures (namely block-copolymer and unimolecular micelles) and the pathway of cellular uptake of such supramolecular drug-delivery systems. In contrast to micelles of small surfactant molecules, polymeric micelles (Scheme1) are generally more stable and can retain the loaded drug for a longer period of time.[3] The block-