Polypeptides as alternatives to PEGylation of therapeutic agents

作者全名："Chen, Huali; Zhang, Qianyu"

作者地址："[Chen, Huali; Zhang, Qianyu] Chongqing Med Univ, Coll Pharm, Chongqing, Peoples R China; [Zhang, Qianyu] Chongqing Med Univ, Coll Pharm, 1 Yixueyuan Rd, Chongqing 400016, Peoples R China"

通信作者："Zhang, QY (通讯作者)，Chongqing Med Univ, Coll Pharm, 1 Yixueyuan Rd, Chongqing 400016, Peoples R China."

来源：EXPERT OPINION ON DRUG DELIVERY

ESI学科分类：PHARMACOLOGY & TOXICOLOGY

WOS号：WOS:001130107800001

JCR分区：Q1

影响因子：6.6

年份：2024

卷号：21

期号：1

开始页：1

结束页：12

文献类型：Review; Early Access

关键词：Polypeptides; protein/peptide drugs; nanomedicine; hydrophilic polymers; long circulating; drug delivery

摘要："IntroductionDue 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 coveredIn 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 opinionPolypeptides 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."

基金机构："National Natural Science Foundation for Young Scientists of China [81903549]; Science and Technology Research Program of Chongqing Municipal Education Commission [KJQN202200451, KJQN202000407]"

基金资助正文：This work was supported by the National Natural Science Foundation for Young Scientists of China [Grant No. 81903549] and Science and Technology Research Program of Chongqing Municipal Education Commission [Grant No. KJQN202200451 and KJQN202000407].