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具有抗菌活性的姜黄素修饰两亲性聚合物胶束的合成与自组装。

Synthesis and self-assembly of curcumin-modified amphiphilic polymeric micelles with antibacterial activity.

机构信息

School of Chemical and Bioprocess Engineering, University College Dublin, Dublin, Ireland.

National Institute for Bioprocessing Research and Training (NIBRT), Dublin, Ireland.

出版信息

J Nanobiotechnology. 2021 Apr 13;19(1):104. doi: 10.1186/s12951-021-00851-2.

Abstract

BACKGROUND

The ubiquitous nature of bacterial biofilms combined with the enhanced resistance towards antimicrobials has led to the development of an increasing number of strategies for biofilm eradication. Such strategies must take into account the existence of extracellular polymeric substances, which obstruct the diffusion of antibiofilm agents and assists in the maintenance of a well-defended microbial community. Within this context, nanoparticles have been studied for their drug delivery efficacy and easily customised surface. Nevertheless, there usually is a requirement for nanocarriers to be used in association with an antimicrobial agent; the intrinsically antimicrobial nanoparticles are most often made of metals or metal oxides, which is not ideal from ecological and biomedical perspectives. Based on this, the use of polymeric micelles as nanocarriers is appealing as they can be easily prepared using biodegradable organic materials.

RESULTS

In the present work, micelles comprised of poly(lactic-co-glycolic acid) and dextran are prepared and then functionalised with curcumin. The effect of the functionalisation in the micelle's physical properties was elucidated, and the antibacterial and antibiofilm activities were assessed for the prepared polymeric nanoparticles against Pseudomonas spp. cells and biofilms. It was found that the nanoparticles have good penetration into the biofilms, which resulted in enhanced antibacterial activity of the conjugated micelles when compared to free curcumin. Furthermore, the curcumin-functionalised micelles were efficient at disrupting mature biofilms and demonstrated antibacterial activity towards biofilm-embedded cells.

CONCLUSION

Curcumin-functionalised poly(lactic-co-glycolic acid)-dextran micelles are novel nanostructures with an intrinsic antibacterial activity tested against two Pseudomonas spp. strains that have the potential to be further exploited to deliver a secondary bioactive molecule within its core.

摘要

背景

细菌生物膜的普遍存在以及对抗菌药物的增强抗性导致了越来越多的生物膜清除策略的发展。这些策略必须考虑到细胞外聚合物的存在,这些物质阻碍了抗生物膜剂的扩散,并有助于维持一个防御良好的微生物群落。在这种情况下,纳米颗粒因其药物输送效果和易于定制的表面而被研究。然而,纳米载体通常需要与抗菌剂一起使用;具有内在抗菌性的纳米颗粒通常由金属或金属氧化物制成,从生态和生物医学的角度来看并不理想。基于此,使用聚合物胶束作为纳米载体很有吸引力,因为它们可以使用可生物降解的有机材料轻松制备。

结果

在本工作中,制备了由聚(乳酸-共-羟基乙酸)和葡聚糖组成的胶束,然后用姜黄素对其进行功能化。阐明了功能化对胶束物理性质的影响,并评估了制备的聚合物纳米颗粒对铜绿假单胞菌细胞和生物膜的抗菌和抗生物膜活性。结果发现,纳米颗粒可以很好地渗透到生物膜中,与游离姜黄素相比,共轭胶束的抗菌活性增强。此外,姜黄素功能化的胶束能够有效地破坏成熟的生物膜,并对生物膜嵌入的细胞表现出抗菌活性。

结论

姜黄素功能化的聚(乳酸-共-羟基乙酸)-葡聚糖胶束是具有内在抗菌活性的新型纳米结构,针对两种铜绿假单胞菌菌株进行了测试,它们有可能进一步被开发用于在其核心内输送第二种生物活性分子。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b5f/8045376/ef6736aa5214/12951_2021_851_Fig1_HTML.jpg

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