Questioning the Use of PEGylation for Drug Delivery.

Questioning the Use of PEGylation for Drug Delivery.
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DOI:
10.1007/s13346-013-0176-5
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发表时间:
2013-12
影响因子:
5.4
通讯作者:
Anchordoquy, Thomas J.
Anchordoquy, Thomas J.
中科院分区:
医学2区
文献类型:
--
作者:
Verhoef, Johan J. F.;Anchordoquy, Thomas J.

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聚乙二醇(PEG)由于其“隐形”特性和生物相容性而被广泛用于药物递送和纳米技术。通常认为PEG化允许微粒递送系统和生物材料逃避免疫系统,从而延长循环寿命。然而,过去十年的许多研究已经证明,PEG化导致药物递送显著减少,包括血清蛋白结合增强、靶细胞摄取减少以及引发促进体内清除的免疫应答。这份报告回顾了一些广泛的文献记录聚乙二醇化的有害影响,从而质疑在药物开发中采用这种策略背后的智慧。
Polyethylene glycol (PEG) is widely utilized in drug delivery and nanotechnology due to its reported “stealth” properties and biocompatibility. It is generally thought that PEGylation allows particulate delivery systems and biomaterials to evade the immune system and thereby prolong circulation lifetimes. However, numerous studies over the past decade have demonstrated that PEGylation causes significant reductions in drug delivery, including enhanced serum protein binding, reduced uptake by target cells, and the elicitation of an immune response that facilitates clearance in vivo. This report reviews some of the extensive literature documenting the detrimental effects of PEGylation, and thereby questions the wisdom behind employing this strategy in drug development.
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