This review aims to provide a systemic analysis of the in vivo, as well as subcellular, fate of polymeric micelles (PMs), starting from the entry of PMs into the body. Few PMs are able to cross the biological barriers intact and reach the circulation. In the blood, PMs demonstrate fairly good stability mainly owing to formation of protein corona despite controversial results reported by different groups. Although the exterior hydrophilic shells render PMs “long-circulating”, the biodistribution of PMs into the mononuclear phagocyte systems (MPS) is dominant as compared with non-MPS organs and tissues. Evidence emerges to support that the copolymer poly(ethylene glycol)-poly(lactic acid) (PEG-PLA) is first broken down into pieces of PEG and PLA and then remnants to be eliminated from the body finally. At the cellular level, PMs tend to be internalized via endocytosis due to their particulate nature and disassembled and degraded within the cell. Recent findings on the effect of particle size, surface characteristics and shape are also reviewed. It is envisaged that unraveling the in vivo and subcellular fate sheds light on the performing mechanisms and gears up the clinical translation of PMs.

这篇综述旨在提供一个系统的体内分析以及亚细胞聚合物胶束 (PM) 的命运，从 PM 进入体内开始。很少有 PM 能够完整地穿过生物屏障并进入循环系统。在血液中，PM 表现出相当好的稳定性，这主要是由于蛋白质冠的形成，尽管不同小组报告的结果存在争议。尽管外部亲水壳使 PM 成为“长循环”，但与非 MPS 器官和组织相比，PM 在单核吞噬细胞系统 (MPS) 中的生物分布占主导地位。出现的证据支持聚乙二醇-聚乳酸 (PEG-PLA) 共聚物首先分解成 PEG 和 PLA 碎片，然后残余物最终从体内排出。在细胞水平上，PM 倾向于通过由于它们的颗粒性质而被内吞作用并在细胞内分解和降解。还回顾了最近关于粒径、表面特征和形状的影响的发现。设想解开体内和亚细胞命运阐明执行机制并加速 PM 的临床转化。