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用于靶向、成像和药物递送目的的含聚乙二醇共聚物合成的化学路线。

Chemistry Routes for Copolymer Synthesis Containing PEG for Targeting, Imaging, and Drug Delivery Purposes.

作者信息

Rahme Kamil, Dagher Nazih

机构信息

Department of Sciences, Faculty of Natural and Applied Sciences, Notre Dame University-Louaize, Zouk Mosbeh, P.O. Box 72, Zouk Mikael, Lebanon.

出版信息

Pharmaceutics. 2019 Jul 11;11(7):327. doi: 10.3390/pharmaceutics11070327.

Abstract

Polyethylene glycol (PEG) is one of the most frequently used polymers for coating nanocarriers to enhance their biocompatibility, hydrophilicity, stability, and biodegradability. PEG is now considered to be among the best biocompatible polymers. It offers sterical hindrance against other nanoparticles and blood components such as opsonin, preventing their macrophage phagocytosis and resulting in a prolonged circulation time in blood stream, consequently a 'stealth character' in vivo. Therefore, PEG has a very promising future for the development of current therapeutics and biomedical applications. Moreover, the vast number of molecules that PEG can conjugate with might enhance its ability to have an optimistic perspective for the future. This review will present an update on the chemistry used in the modern conjugation methods for a variety of PEG conjugates, such methods include, but are not limited to, the synthesis of targeting PEG conjugates (i.e., Peptides, Folate, Biotin, Mannose etc.), imaging PEG conjugates (i.e., Coumarin, Near Infrared dyes etc.) and delivery PEG conjugates (i.e., doxorubicin, paclitaxel, and other hydrophobic low molecular weight drugs). Furthermore, the type of nanoparticles carrying those conjugates, along with their biomedical uses, will be briefly discussed.

摘要

聚乙二醇(PEG)是用于包覆纳米载体以增强其生物相容性、亲水性、稳定性和生物降解性的最常用聚合物之一。PEG现在被认为是最佳生物相容性聚合物之一。它对其他纳米颗粒和血液成分(如调理素)提供空间位阻,防止它们被巨噬细胞吞噬,从而在血流中延长循环时间,因此在体内具有“隐身特性”。因此,PEG在当前治疗方法和生物医学应用的发展方面具有非常广阔的前景。此外,PEG能够与之共轭的大量分子可能会增强其对未来持乐观态度的能力。本综述将介绍用于各种PEG共轭物的现代共轭方法中所使用化学方法的最新进展,这些方法包括但不限于靶向PEG共轭物(即肽、叶酸、生物素、甘露糖等)、成像PEG共轭物(即香豆素、近红外染料等)和递送PEG共轭物(即阿霉素、紫杉醇和其他疏水性低分子量药物)的合成。此外,还将简要讨论携带这些共轭物的纳米颗粒类型及其生物医学用途。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/008c/6680653/a2d384e22c12/pharmaceutics-11-00327-g001.jpg

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