Faculty of Pharmacy, Department of Toxicology, Gazi University, Ankara, Turkey.
Faculty of Medicine, Department of General Surgery, Gazi University, Ankara, Turkey.
Curr Drug Metab. 2019;20(9):720-741. doi: 10.2174/1389200220666190806142835.
The main drawbacks for using conventional antimicrobial agents are the development of multiple drug resistance due to the use of high concentrations of antibiotics for extended periods. This vicious cycle often generates complications of persistent infections, and intolerable antibiotic toxicity. The problem is that while all new discovered antimicrobials are effective and promising, they remain as only short-term solutions to the overall challenge of drug-resistant bacteria.
Recently, nanoantibiotics (nAbts) have been of tremendous interest in overcoming the drug resistance developed by several pathogenic microorganisms against most of the commonly used antibiotics. Compared with free antibiotic at the same concentration, drug delivered via a nanoparticle carrier has a much more prominent inhibitory effect on bacterial growth, and drug toxicity, along with prolonged drug release. Additionally, multiple drugs or antimicrobials can be packaged within the same smart polymer which can be designed with stimuli-responsive linkers. These stimuli-responsive nAbts open up the possibility of creating multipurpose and targeted antimicrobials. Biofilm formation still remains the leading cause of conventional antibiotic treatment failure. In contrast to conventional antibiotics nAbts easily penetrate into the biofilm, and selectively target biofilm matrix constituents through the introduction of bacteria specific ligands. In this context, various nanoparticles can be stabilized and functionalized with conventional antibiotics. These composites have a largely enhanced bactericidal efficiency compared to the free antibiotic.
Nanoparticle-based carriers deliver antibiotics with better biofilm penetration and lower toxicity, thus combating bacterial resistance. However, the successful adaptation of nanoformulations to clinical practice involves a detailed assessment of their safety profiles and potential immunotoxicity.
由于抗生素的高浓度和长时间使用，导致了多重耐药性的发展，这使得传统抗菌药物的使用受到了限制。这种恶性循环常常导致持续感染和不可耐受的抗生素毒性等并发症。问题是，虽然所有新发现的抗菌药物都有效且有前途，但它们仍然只是解决耐药细菌这一整体挑战的短期解决方案。
最近，纳米抗生素（nAbts）在克服几种致病微生物对大多数常用抗生素产生的耐药性方面引起了极大的兴趣。与相同浓度的游离抗生素相比，通过纳米颗粒载体递送的药物对细菌生长具有更显著的抑制作用，并且降低了药物毒性，同时延长了药物释放时间。此外，多种药物或抗菌药物可以包装在同一智能聚合物中，该聚合物可以用具有刺激响应性连接子设计。这些刺激响应性 nAbts 为开发多用途和靶向抗菌药物提供了可能性。生物膜形成仍然是传统抗生素治疗失败的主要原因。与传统抗生素不同，nAbts 很容易穿透生物膜，并通过引入细菌特异性配体来选择性地靶向生物膜基质成分。在这种情况下，各种纳米颗粒可以用常规抗生素进行稳定和功能化。与游离抗生素相比，这些复合材料具有大大增强的杀菌效率。
基于纳米颗粒的载体可输送抗生素，具有更好的生物膜穿透性和更低的毒性，从而对抗细菌耐药性。然而，成功地将纳米制剂应用于临床实践需要详细评估其安全性概况和潜在的免疫毒性。
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