Deshayes Caroline, Arafath Md Nasir, Apaire-Marchais Véronique, Roger Emilie
University of Angers, INRAE, SIFCIR, SFR QUASAV, Angers, France.
University of Angers, INSERM, CNRS, MINT, SFR ICAT, Angers, France.
Front Med Technol. 2022 Jan 25;3:778645. doi: 10.3389/fmedt.2021.778645. eCollection 2021.
Antimicrobial peptides (AMPs) have a great potential to face the global expansion of antimicrobial resistance (AMR) associated to the development of multidrug-resistant (MDR) pathogens. AMPs are usually composed of 10-50 amino acids with a broad structural diversity and present a range of antimicrobial activities. Unfortunately, even if the oral route is the most convenient one, currently approved therapeutic AMPs are mostly administrated by the intravenous route. Thus, the development of novel drug delivery systems (DDSs) represents a promising opportunity to protect AMPs from chemical and enzymatic degradation through the gastrointestinal tract and to increase intestinal permeability leading to high bioavailability. In this review, the classification and properties as well as mechanisms of the AMPs used in infectiology are first described. Then, the different pharmaceutical forms existing in the market for oral administration are presented. Finally, the formulation technologies, including microparticle- and nanoparticle-based DDSs, used to improve the oral bioavailability of AMPs are reviewed.
抗菌肽(AMPs)在应对与多重耐药(MDR)病原体发展相关的全球抗菌药物耐药性(AMR)扩展方面具有巨大潜力。抗菌肽通常由10至50个氨基酸组成,结构多样性广泛,并呈现出一系列抗菌活性。不幸的是,即使口服途径是最便捷的途径,但目前获批的治疗性抗菌肽大多通过静脉途径给药。因此,开发新型药物递送系统(DDSs)是一个很有前景的机会,可保护抗菌肽在胃肠道中免受化学和酶促降解,并提高肠道通透性以实现高生物利用度。在本综述中,首先描述了感染病学中使用的抗菌肽的分类、特性及其作用机制。然后,介绍了市场上现有的不同口服给药剂型。最后,综述了用于提高抗菌肽口服生物利用度的制剂技术,包括基于微粒和纳米颗粒的药物递送系统。