PEGylation as a strategy for improving nanoparticle-based drug and gene delivery.
PEGylation as a strategy for improving nanoparticle-based drug and gene delivery.
复制标题
Pegylation作为改善基于纳米颗粒的药物和基因递送的策略。
DOI：
10.1016/j.addr.2015.09.012
复制
发表时间：
2016-04-01
影响因子：
16.1
通讯作者：
Ensign LM
中科院分区：
文献类型：
--
作者：
Suk JS;Xu Q;Kim N;Hanes J;Ensign LM
用聚乙二醇（PEG）或“PEG化”涂覆纳米颗粒的表面是用于提高药物和基因递送至靶细胞和组织的效率的常用方法。从PEG化蛋白质成功改善全身循环时间和降低免疫原性的基础上，PEG涂层对全身给药的纳米颗粒制剂命运的影响已经并将继续得到广泛研究。纳米颗粒上的PEG涂层保护表面免于聚集、调理作用和吞噬作用，延长体循环时间。在这里，我们简要描述了用于全身给药的聚乙二醇化纳米颗粒制剂的发展历史，包括PEG分子量、PEG表面密度、纳米颗粒核心特性和重复给药等因素如何影响循环时间。一个不太经常讨论的话题，然后我们描述了如何PEG涂层的纳米粒子也被用于克服各种生物学障碍，有效的药物和基因传递与其他模式的管理，从胃肠道到眼睛。最后，我们描述了PEG化纳米颗粒的方法和表征PEG表面密度的方法，PEG表面涂层改善药物和基因递送的有效性的关键因素。
Coating the surface of nanoparticles with polyethylene glycol (PEG), or “PEGylation”, is a commonly used approach for improving the efficiency of drug and gene delivery to target cells and tissues. Building from the success of PEGylating proteins to improve systemic circulation time and decrease immunogenicity, the impact of PEG coatings on the fate of systemically administered nanoparticle formulations has, and continues to be, widely studied. PEG coatings on nanoparticles shield the surface from aggregation, opsonization, and phagocytosis, prolonging systemic circulation time. Here, we briefly describe the history of the development of PEGylated nanoparticle formulations for systemic administration, including how factors such as PEG molecular weight, PEG surface density, nanoparticle core properties, and repeated administration impact circulation time. A less frequently discussed topic, we then describe how PEG coatings on nanoparticles have also been utilized for overcoming various biological barriers to efficient drug and gene delivery associated with other modes of administration, ranging from gastrointestinal to ocular. Finally, we describe both methods for PEGylating nanoparticles and methods for characterizing PEG surface density, a key factor in the effectiveness of the PEG surface coating for improving drug and gene delivery.