Polypeptides as alternatives to PEGylation of therapeutic agents.

Expert opinion on drug delivery Pub Date : 2023-12-20 DOI:10.1080/17425247.2023.2297937

Huali Chen, Qianyu Zhang

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Abstract

Introduction: Due to the concerns raised by the extensive application of PEGylation, polypeptides have stood out as excellent candidates with adequate biocompatibility and biodegradability with tunable hydrophilicity.

Areas covered: In this review, polypeptides with the potential to replace PEGylation have been summarized and their application has been reviewed, including XTEN, PASylation, polysarcosine, zwitterion polypeptides, ELPylation, etc. Besides their strengths, the remaining challenges have also been discussed and the future perspectives have been provided.

Expert opinion: Polypeptides have been applied in the designing of peptide/protein drugs as well as nanomedicines, and some of the pharmaceutics have made it into the clinical trials and got approved. These polypeptides showed similar hydrophilic properties to PEGylation, which increased the hydrodynamic volumes of protein drugs, reduced kidney elimination, decreased protein-polymer interaction and potentially improved the drug delivery efficiency due to the extended circulation time in the system. Moreover, they demonstrated superior biodegradability and biocompatibility, compensating for the deficiencies for polymers such as PEG.

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多肽作为治疗剂 PEG 化的替代品。

简介：由于 PEG 化的广泛应用引起了人们的关注，多肽作为具有充分生物相容性和生物降解性以及可调亲水性的优秀候选物质脱颖而出：本综述概述了有可能取代 PEG 化的多肽及其应用，包括 XTEN、PAS 化、聚肌氨酸、齐聚多肽、ELP 化等。除了它们的优势之外，还讨论了仍然存在的挑战，并提供了未来的展望：多肽已被用于设计肽/蛋白质药物以及纳米药物，其中一些药物已进入临床试验并获得批准。这些多肽表现出与 PEG 化相似的亲水性，增加了蛋白质药物的流体力学体积，减少了肾脏的排泄，降低了蛋白质与聚合物之间的相互作用，并由于延长了药物在系统中的循环时间而提高了给药效率。此外，它们还表现出优异的生物降解性和生物相容性，弥补了 PEG 等聚合物的不足。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Expert opinion on drug delivery

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