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用于伤口愈合的局部抗菌肽制剂:当前的发展和未来的前景。

Topical antimicrobial peptide formulations for wound healing: Current developments and future prospects.

机构信息

Section for Pharmaceutics and Social Pharmacy, Department of Pharmacy, University of Oslo, P.O. Box 1068 Blindern, NO-0316 Oslo, Norway.

Department of Chemistry, Biotechnology, and Food Science, Norwegian University of Life Sciences, P.O. Box 5003, NO-1432 Ås, Norway.

出版信息

Acta Biomater. 2020 Feb;103:52-67. doi: 10.1016/j.actbio.2019.12.025. Epub 2019 Dec 23.

Abstract

Antimicrobial peptides (AMPs) are the natural antibiotics recognized for their potent antibacterial and wound healing properties. Bare AMPs have limited activity following topical application attributable to their susceptibility to environment (hydrolysis, oxidation, photolysis), and wound (alkaline pH, proteolysis) related factors as well as minimal residence time. Therefore, the formulation of AMPs is essential to enhance stability, prolong delivery, and optimize effectiveness at the wound site. Different topical formulations of AMPs have been developed so far including nanoparticles, hydrogels, creams, ointments, and wafers to aid in controlling bacterial infection and enhance wound healing process in vivo. Herein, an overview is provided of the AMPs and current understanding of their formulations for topical wound healing applications along with suitable examples. Furthermore, future prospects for the development of effective combination AMP formulations are discussed. STATEMENT OF SIGNIFICANCE: Chronic wound infection and subsequent development of antibiotic resistance are serious clinical problems affecting millions of people worldwide. Antimicrobial peptides (AMPs) possess great potential in effectively killing the bacteria with minimal risk of resistance development. However, AMPs susceptibility to degradation following topical application limits their antimicrobial and wound healing effects. Therefore, development of an optimized topical formulation with high peptide stability and sustained AMP delivery is necessary to maximize the antimicrobial and wound healing effects. The present review provides an overview of the state-of-art in the field of topical AMP formulations for wound healing. Current developments in the field of topical AMP formulations are reviewed and future prospects for the development of effective combination AMP formulations are discussed.

摘要

抗菌肽 (AMPs) 是天然抗生素的代表,因其具有强大的抗菌和伤口愈合特性而备受关注。由于其对环境(水解、氧化、光解)和伤口(碱性 pH 值、蛋白水解)相关因素的敏感性以及极短的停留时间,裸 AMP 在局部应用后的活性有限。因此,AMP 的配方对于增强稳定性、延长输送时间和优化伤口部位的效果至关重要。迄今为止,已经开发出多种 AMP 的局部制剂,包括纳米粒子、水凝胶、乳膏、软膏和薄片,以帮助控制细菌感染并促进体内伤口愈合过程。本文概述了 AMP 及其目前对局部伤口愈合应用的配方理解,同时提供了合适的例子。此外,还讨论了开发有效组合 AMP 配方的未来前景。

意义声明

慢性伤口感染和随后抗生素耐药性的发展是一个严重的临床问题,影响着全球数以百万计的人。抗菌肽 (AMPs) 在有效杀死细菌方面具有巨大的潜力,而且耐药风险极小。然而,AMP 在局部应用后易降解,限制了其抗菌和伤口愈合效果。因此,开发一种具有高肽稳定性和持续 AMP 输送的优化局部制剂对于最大限度地发挥抗菌和伤口愈合效果是必要的。

本综述提供了局部 AMP 制剂在伤口愈合方面的最新研究进展概述。综述了局部 AMP 制剂领域的最新发展,并讨论了开发有效组合 AMP 制剂的未来前景。

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