利用PLA-PEG纳米颗粒的强大功效,用于对抗抗甲基西林耐药黄金葡萄球菌的Linezolid输送
Roberto Oliva1, Giovanna Ginestra1, Anna Piperno1
1Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, V.le, F. Stagno d'Alcontres, 31, 98166 Messina, Italy.
International journal of pharmaceutics
|May 31, 2023
概括
新型的多聚乳酸-多聚乙烯甘醇纳米颗粒 (PLA-PEGNP) 有效地提供线化物 (LNZ) 延长抗菌作用. 这些纳米颗粒对耐药细菌 (包括MRSA) 具有显著的抗微生物活性,并增强了抗生素的疗效.
科学领域:
- 材料科学 材料科学 材料科学
- 纳米技术纳米技术
- 制药科学 制药科学
背景情况:
- 甲素耐药黄金葡萄球菌 (MRSA) 由于抗生素耐药性而构成重大威胁.
- 有效的药物输送系统对于对抗具有挑战性的细菌感染至关重要.
研究的目的:
- 开发和表征新型的多聚乳酸-多聚乙烯糖醇纳米颗粒 (PLA-PEGNP) 用于增强线化物 (LNZ) 输送.
- 评估LNZ载荷的PLA-PEGNP对抗格兰阳性细菌的抗菌疗效,包括MRSA.
主要方法:
- 使用碳胺合剂和铜催化化酸循环添加,将PLA与PEG结合.
- 通过纳米沉和透析将LNZ封装成PLA-PEGNP.
- 纳米粒子稳定性的表征,药物加载,封装效率和释放动力学.
- 对各种格拉姆阳性细菌和MRSA生物膜的抗微生物活性评估.
主要成果:
- 最佳的PLA-PEG@LNZ NP实现了3.5%的LNZ有效载荷和15%的封装效率.
- 观察到持续的药物释放,在80小时内释放了65%的LNZ.
- 稳定纳米粒子具有负泽塔电位 (-31到-39mV) 经过冷干燥后表现出对聚合的抗性.
- 具有有效的抗菌活性,可以对抗金黄色葡萄球菌 (MRSA),表皮葡萄球菌 (Staphylococcus epidermidis),卢格敦尼斯葡萄球菌 (Staphylococcus lugdunensis) 和抗万科胺素的菌菌 (Enterococcus faecium,VREfm).
- 观察到对浮游生物MRSA生长和预制生物膜的抑制作用.
结论:
- PLA-PEG NPs提供了一个高效和稳定的Linezolid纳米输送系统.
- 开发的纳米配方保留并增强了LNZ的抗菌活性.
- 这种纳米系统有可能改善MRSA相关感染的管理.
相关概念视频
Antibiotic Selection
Overview
Site-Targeted Drug Delivery Systems: Polymeric Carriers
Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
Mechanism of Antibiotic Resistance in MRSA
Antibiotic resistance in bacteria arises when microorganisms evolve the ability to withstand drugs designed to kill them or inhibit their growth, rendering once-effective treatments useless. This phenomenon, driven by genetic change and selection under antibiotic exposure, poses a profound threat to modern medicine. Mechanisms include drug-inactivating enzymes (e.g., β-lactamases), efflux pumps that eject antibiotics, mutations altering antibiotic targets, decreased drug uptake, and acquisition...
Clinical Significance of Antibiotic Resistance
Methicillin-resistant Staphylococcus aureus (MRSA) presents a critical public health threat, arising from its capacity to resist β-lactam antibiotics due to acquisition of the mecA gene within the staphylococcal cassette chromosome mec (SCCmec). This gene encodes penicillin-binding protein 2a (PBP2a), which impairs binding efficacy of methicillin and other β-lactams. MRSA has evolved into distinct clonal lineages impacting humans and animals alike, reinforcing its significance within the One...


