Key Laboratory of Textile Science and Technology, Ministry of Education, College of Textiles, Donghua University, Songjiang District, Shanghai 201620, China.
Key Laboratory of Textile Science and Technology, Ministry of Education, College of Textiles, Donghua University, Songjiang District, Shanghai 201620, China.
J Colloid Interface Sci. 2019 Mar 22;540:634-646. doi: 10.1016/j.jcis.2018.12.091. Epub 2018 Dec 27.
Bacterial infection is one of the most significant complications worldwide and has been one of the main factors of morbidity and mortality for the chronic wounds. Considering the negative charged feature of bacterial pathogens, a positive charged poly(ester amide) (PEA) micellar system based on lysine, arginine and phenylalanine is developed. In this study, a serials of PEA random copolymers can be obtained by altering the sorts of amino acids and feed ratio, and the self-assembled PEA micelles with an average diameter ranging from 150 to 200 nm exhibit the integrated properties of excellent biocompatibility and enzymatic biodegradation. More interesting, the degraded random block micelles can reassemble into smaller sized micelles with the diameter less than 20 nm which have promising applications in drug delivery. The PEA micellar nanocarriers display an intrinsic antibacterial property due to the pendant groups of lysine and arginine based moieties and this killing capacity can be enhanced by grafting levofloxacin without losing the original performance. The in vitro antibacterial evaluation proves all of the micelles display a concentration dependent efficiency of killing bacteria (up to 99.99%). The in vivo Staphylococcus aureus induced infection model demonstrates that the micelles are effective in killing the bacteria and infection treatment. The successful synthesis of the biocompatible and biodegradable amino acid based micellar nanocarriers may provide new insights into the development of biomedical materials for antibacterial applications and drug delivery.
细菌感染是全球范围内最严重的并发症之一，也是慢性伤口发病率和死亡率的主要因素之一。考虑到细菌病原体带负电荷的特点，开发了一种基于赖氨酸、精氨酸和苯丙氨酸的带正电荷的聚（酯酰胺）（PEA）胶束系统。在本研究中，可以通过改变氨基酸的种类和进料比来获得一系列 PEA 无规共聚物，并且自组装的 PEA 胶束具有平均直径在 150 至 200nm 之间的整合特性，具有优异的生物相容性和酶降解性。更有趣的是，降解的无规嵌段胶束可以重新组装成直径小于 20nm 的更小尺寸的胶束，这在药物传递方面具有广阔的应用前景。PEA 胶束纳米载体由于赖氨酸和精氨酸基部分的侧基而具有内在的抗菌特性，并且通过嫁接左氧氟沙星可以增强这种杀菌能力而不会失去原始性能。体外抗菌评价证明所有胶束都表现出浓度依赖性的杀菌效率（高达 99.99%）。金黄色葡萄球菌诱导的体内感染模型表明，胶束在杀灭细菌和感染治疗方面是有效的。这种生物相容性和可生物降解的基于氨基酸的胶束纳米载体的成功合成可能为抗菌应用和药物传递的生物医学材料的开发提供新的思路。
