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Biological Implications of Polyethylene Glycol and PEGylation: Therapeutic Approaches Based on Biophysical Studies and Protein Structure-Based Drug Design Tools

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Innovations and Implementations of Computer Aided Drug Discovery Strategies in Rational Drug Design

Abstract

Polyethylene glycol (PEG) is one of the most extensively used biocompatible polymer. PEG-modification improves the original properties of conjugates and thus being exploited in different fields. PEGs demonstrated their ability to bind DNA, dyes and proteins, in solution and in solid phase via amine and thiol groups. Covalent linkage of PEG to drug molecules improves water-solubility, bioavailability, pharmacokinetics, immunogenic properties, and biological activities. Entrapment of drugs into the PEG vesicle offers substantial benefits in the treatment of many diseases including type 2 diabetes over conventional injection-based therapies. Therapeutic enzymes are conjugated with PEG for targeted therapy of diseases in which the native enzyme was inefficient. PEG has been most extensively investigated polymers for gene delivery due to its capability to form stable complexes by electrostatic interactions with nucleic acids. Many PEG-enzymes conjugates have already obtained FDA approval for clinical implications. PEGylated copolymers have least cytotoxicity and cell-compatibility concern, high efficiency, safety and biocompatibility and thus considered as an attractive polymer for gene and drug delivery system. For instance, many tissue engineering applications, PEG and its derivatives are likely to precise control of cell behaviour in growing tissues. For this application numerous bioresponsive and intelligent biomaterials are developed and extensively used in bone and tissue regeneration. PEG-derived hydrogels increase gene expression of bone-specific markers, secretion of bone-related matrix, and mineralization and may have a potential impact on bone-engineering therapies. PEG-coated poly(amidoamine) exhibits low toxicity to human corneal epithelial cells and effectively used as antimicrobial agents.

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Acknowledgements

This work was supported by the grant from the Indian Council of Medical Research (ICMR)BIC/12(16)/2014. The authors are very indebted to Sharda University, FIST Program (SR/FST/LSI-541/2012) and Jamia Millia Islamia (a Central University) for facilitating the research.

Conflict of Interest

The authors declare no conflict of interest.

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Authors and Affiliations

  1. Department of Biotechnology, Sharda University, Greater Noida, Uttar Pradesh, India

    Neha Raina & Amit Kumar Singh

  2. Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia, New Delhi, India

    Asimul Islam

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  1. Neha Raina
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Correspondence to Amit Kumar Singh or Asimul Islam .

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  1. Computer Aided Drug Design and Molecular Modelling Lab, Department of Bioinformatics, Alagappa University, Karaikudi, Tamil Nadu, India

    Sanjeev Kumar Singh

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Raina, N., Singh, A.K., Islam, A. (2021). Biological Implications of Polyethylene Glycol and PEGylation: Therapeutic Approaches Based on Biophysical Studies and Protein Structure-Based Drug Design Tools. In: Singh, S.K. (eds) Innovations and Implementations of Computer Aided Drug Discovery Strategies in Rational Drug Design. Springer, Singapore. https://doi.org/10.1007/978-981-15-8936-2_11

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  • DOI: https://doi.org/10.1007/978-981-15-8936-2_11

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  • Publisher Name: Springer, Singapore

  • Print ISBN: 978-981-15-8935-5

  • Online ISBN: 978-981-15-8936-2

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