Recent progress on formulations of hirudin

Abstract

Hirudin is an effective active ingredient derived from the salivary glands of leech. It is a small peptide molecule consisting of 65-66 amino acids and demonstrates a strong inhibitory effect on thrombin, providing beneficial anticoagulant and antithrombotic properties. However, as a biopharmaceutical peptide, it has some drawbacks such as easy degradation, short half-life, low bioavailability, and high risk of hemorrhage in clinical use. To overcome these challenges, various formulations were developed. In this work, a comprehensive review of research progress was provided in both traditional and novel hirudin formulations, spanning from lyophilized powders to biotechnology-based pharmaceuticals, covering various dosage forms to offer comprehensive references for field research. Firstly the advantages and limitations of conventional preparations were assessed such as freeze-dried powders, capsules, and injections. Then a detailed exploration of frontier strategies including nanotechnology-based delivery systems, transdermal formulations, and biotechnology-driven prodrug designs were conducted. This article aims to comprehensively analyze cutting-edge advancements in hirudin preparation research, providing updated information for relevant researchers by integrating traditional dosage optimization with breakthrough emerging technologies.

Keywords

Hirudin formulations / Anticoagulant activity / Release-controlled formulations / Dermal delivery formulations / Molecular design and structural modifications

CRediT authorship contribution statement

Zheng Bao: Writing - review & editing, Writing - original draft, Conceptualization. Xingyu Qi: Writing - review & editing, Writing original draft, Conceptualization. Suling Zhu: Writing - original draft, Conceptualization. Mao Zhang: Writing - original draft, Conceptualization. Xinyue Liu: Writing - original draft, Conceptualization. Peidong Chen: Writing - review & editing, Funding acquisition. Li Zhang: Writing - review & editing, Funding acquisition. Ting Geng: Writing review & editing, Supervision, Conceptualization. Fang-Fang Cheng: Writing - review & editing, Supervision, Funding acquisition, Conceptualization.

Data avaliability

Not applicable.

Ethics approval

Not applicable.

Declaration of generative AI in scientific writing

Deepseek was used to correct grammatical errors.

Funding

The authors are thankful to the National Natural Science Foundation of China (82374037, 82374039), the Natural Science Foundation of Jiangsu Province (BK20231258), and Project funded by Jiangsu Administration of traditional Chinese Medicine (MS2021005) for the generous financial supports. This work is also supported by the College Students’ Innovation and Entrepreneurship Training Program (202310315058Z, 202410315Y087).

Declaration of competing interest

The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Acknowledgement

Fig. 1 was created with Adobe Illustrator Software.

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