A Drug Carrier for Sustained Zero-Order Release of Peptide Therapeutics
Abstract Peptides have great potential as therapeutic agents, however, their clinic applications are severely hampered by their instability and short circulation half-life. Zero-order release carriers could not only extend the circulation lifetime of peptides, but also maintain the plasma drug level...
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Nature Portfolio
2017
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oai:doaj.org-article:a9bf00e765dd4c13b15512e8f3dd66312021-12-02T16:07:57ZA Drug Carrier for Sustained Zero-Order Release of Peptide Therapeutics10.1038/s41598-017-05898-62045-2322https://doaj.org/article/a9bf00e765dd4c13b15512e8f3dd66312017-07-01T00:00:00Zhttps://doi.org/10.1038/s41598-017-05898-6https://doaj.org/toc/2045-2322Abstract Peptides have great potential as therapeutic agents, however, their clinic applications are severely hampered by their instability and short circulation half-life. Zero-order release carriers could not only extend the circulation lifetime of peptides, but also maintain the plasma drug level constant, and thus maximize their therapeutic efficacy and minimize their toxic effect. Here using PEGylated salmon calcitonin (PEG-sCT)/tannic acid (TA) film as an example, we demonstrated that hydrogen-bonded layer-by-layer films of a PEGylated peptide and a polyphenol could be a platform for zero-order peptide release. The films were fabricated under mild conditions. The second component, TA, is a natural product and presents potential therapeutic activities itself. Unlike common carriers, the new carrier releases the peptide via gradual disintegration of the film because of its dynamic nature. The release of PEG-sCT follows a perfect zero-order kinetics without initial burst release. In addition the release rate could be tuned via external stimuli, such as pH and temperature. When implanted in rats, the films could remain the plasma level of PEG-sCT constant over an extended period. Accordingly, the serum calcium level was reduced and maintained constant over the same period, suggesting an improved therapeutic efficacy of the released drug.Ya-Nan ZhaoXiaoyu XuNa WenRui SongQingbin MengYing GuanSiqi ChengDanni CaoYansheng DongJiankun QieKeliang LiuYongjun ZhangNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 7, Iss 1, Pp 1-9 (2017) |
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Medicine R Science Q Ya-Nan Zhao Xiaoyu Xu Na Wen Rui Song Qingbin Meng Ying Guan Siqi Cheng Danni Cao Yansheng Dong Jiankun Qie Keliang Liu Yongjun Zhang A Drug Carrier for Sustained Zero-Order Release of Peptide Therapeutics |
description |
Abstract Peptides have great potential as therapeutic agents, however, their clinic applications are severely hampered by their instability and short circulation half-life. Zero-order release carriers could not only extend the circulation lifetime of peptides, but also maintain the plasma drug level constant, and thus maximize their therapeutic efficacy and minimize their toxic effect. Here using PEGylated salmon calcitonin (PEG-sCT)/tannic acid (TA) film as an example, we demonstrated that hydrogen-bonded layer-by-layer films of a PEGylated peptide and a polyphenol could be a platform for zero-order peptide release. The films were fabricated under mild conditions. The second component, TA, is a natural product and presents potential therapeutic activities itself. Unlike common carriers, the new carrier releases the peptide via gradual disintegration of the film because of its dynamic nature. The release of PEG-sCT follows a perfect zero-order kinetics without initial burst release. In addition the release rate could be tuned via external stimuli, such as pH and temperature. When implanted in rats, the films could remain the plasma level of PEG-sCT constant over an extended period. Accordingly, the serum calcium level was reduced and maintained constant over the same period, suggesting an improved therapeutic efficacy of the released drug. |
format |
article |
author |
Ya-Nan Zhao Xiaoyu Xu Na Wen Rui Song Qingbin Meng Ying Guan Siqi Cheng Danni Cao Yansheng Dong Jiankun Qie Keliang Liu Yongjun Zhang |
author_facet |
Ya-Nan Zhao Xiaoyu Xu Na Wen Rui Song Qingbin Meng Ying Guan Siqi Cheng Danni Cao Yansheng Dong Jiankun Qie Keliang Liu Yongjun Zhang |
author_sort |
Ya-Nan Zhao |
title |
A Drug Carrier for Sustained Zero-Order Release of Peptide Therapeutics |
title_short |
A Drug Carrier for Sustained Zero-Order Release of Peptide Therapeutics |
title_full |
A Drug Carrier for Sustained Zero-Order Release of Peptide Therapeutics |
title_fullStr |
A Drug Carrier for Sustained Zero-Order Release of Peptide Therapeutics |
title_full_unstemmed |
A Drug Carrier for Sustained Zero-Order Release of Peptide Therapeutics |
title_sort |
drug carrier for sustained zero-order release of peptide therapeutics |
publisher |
Nature Portfolio |
publishDate |
2017 |
url |
https://doaj.org/article/a9bf00e765dd4c13b15512e8f3dd6631 |
work_keys_str_mv |
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