Questioning the use of PEGylation for drug delivery

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• 作者：Johan J. F. Verhoef (1)
  Thomas J. Anchordoquy (2)
  
• 关键词：Polyethylene glycol ; PEG ; Transfection ; DNA ; RNA ; Drug delivery ; Immunogenicity ; Stealth
• 刊名：Drug Delivery and Translational Research
• 出版年：2013
• 出版时间：December 2013
• 年：2013
• 卷：3
• 期：6
• 页码：499-503
• 全文大小：
• 作者单位：Johan J. F. Verhoef (1)
  Thomas J. Anchordoquy (2)
  
  1. School of Pharmacy and Pharmaceutical Sciences, University of Utrecht, Utrecht, 3584 CG, The Netherlands
  2. Skaggs School of Pharmacy and Pharmaceutical Sciences, University of Colorado Denver, Aurora, CO, 80045, USA
  
• ISSN：2190-3948

文摘

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.