Novel drug delivery systems for hirudin-based product development and clinical applications.

Hirudin, a natural biological polypeptide macromolecule secreted by the salivary glands of medicinal leech, is a specific thrombin inhibitor with multiple favourable bioactivities, including anti-coagulation, anti-fibrotic, and anti-tumour. Despite several anticoagulants have been widely applied in clinic, hirudin shows advantages in reducing the incidence of bleeding side effects by virtue of its high specificity in binding to thrombin. As a result, hirudin has been tested in clinical practice to prevent and treat several complex diseases. However, the application of this polypeptide macromolecule is compromised by its low bioavailability and bioactivity due to poor serum stability and susceptibility to protease degradation in vivo. To overcome these drawbacks, several studies have proposed novel drug delivery systems (NDDSs) to prevent the degradation and increase the targeting efficiency of hirudin. This systematic review summarises the clinical research on hirudin, including its classification and bioactivities, and highlights the opportunities and challenges in the clinical use of hirudin. The NDDSs designed to enhance the bioavailability and bioactivity of hirudin are discussed to explore its application in the treatment of related diseases. This review may considerably contribute to the advancement of delivery science and technology, particularly in the context of polypeptide-based therapeutics. Copyright © 2024 Elsevier B.V. All rights reserved.

Citation

Liqing Mo, Can Yang, Yingxuan Dai, Wei Liu, Yuhong Gong, Yujie Guo, Yuxi Zhu, Yan Cao, Xuecheng Xiao, Shi Du, Shan Lu, Jianhua He. Novel drug delivery systems for hirudin-based product development and clinical applications. International journal of biological macromolecules. 2025 Jan;287:138533

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PMID: 39657884

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