van Gent Miriam E, Ali Muhanad, Nibbering Peter H, Kłodzińska Sylvia N
Department of Infectious Diseases, Leiden University Medical Center, 2300 RC Leiden, The Netherlands.
Center for Biopharmaceuticals and Biobarriers in Drug Delivery, Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Pharmaceutics. 2021 Nov 2;13(11):1840. doi: 10.3390/pharmaceutics13111840.
Bacterial infections constitute a threat to public health as antibiotics are becoming less effective due to the emergence of antimicrobial resistant strains and biofilm and persister formation. Antimicrobial peptides (AMPs) are considered excellent alternatives to antibiotics; however, they suffer from limitations related to their peptidic nature and possible toxicity. The present review critically evaluates the chemical characteristics and antibacterial effects of lipid and polymeric AMP delivery systems and coatings that offer the promise of enhancing the efficacy of AMPs, reducing their limitations and prolonging their half-life. Unfortunately, the antibacterial activities of these systems and coatings have mainly been evaluated in vitro against planktonic bacteria in less biologically relevant conditions, with only some studies focusing on the antibiofilm activities of the formulated AMPs and on the antibacterial effects in animal models. Further improvements of lipid and polymeric AMP delivery systems and coatings may involve the functionalization of these systems to better target the infections and an analysis of the antibacterial activities in biologically relevant environments. Based on the available data we proposed which polymeric AMP delivery system or coatings could be profitable for the treatment of the different hard-to-treat infections, such as bloodstream infections and catheter- or implant-related infections.
由于抗菌耐药菌株的出现以及生物膜和持留菌的形成，抗生素的效力越来越低，细菌感染对公共卫生构成了威胁。抗菌肽（AMPs）被认为是抗生素的极佳替代品；然而，它们因其肽的性质和可能的毒性而存在局限性。本综述批判性地评估了脂质和聚合物AMPs递送系统及涂层的化学特性和抗菌效果，这些系统和涂层有望提高AMPs的疗效，减少其局限性并延长其半衰期。不幸的是，这些系统和涂层的抗菌活性主要是在体外针对浮游细菌，在生物学相关性较低的条件下进行评估的，只有一些研究关注配方AMPs的抗生物膜活性以及在动物模型中的抗菌效果。脂质和聚合物AMPs递送系统及涂层的进一步改进可能涉及这些系统的功能化，以更好地靶向感染，并分析在生物学相关环境中的抗菌活性。基于现有数据，我们提出了哪种聚合物AMPs递送系统或涂层可能有利于治疗不同的难治性感染，如血流感染以及与导管或植入物相关的感染。
