Department of Dermatology, University Medical Center Jena, Erfurter Str. 35, D-07740 Jena, Germany.
Int J Pharm. 2013 Nov 1;456(1):165-74. doi: 10.1016/j.ijpharm.2013.08.001. Epub 2013 Aug 12.
Cationic polyamines, such as poly(ethyleneimines) (PEIs), may recommend themselves for antimicrobial applications as they can interact with microbial membranes resulting in their disruption. The purpose of the study was the assessment of biocompatibility and antibacterial activity of PEIs with different architectures (branched (b) and linear (l)) and molar masses (0.8-750 kDa). lPEI and bPEI exhibited a strong antibacterial activity against Staphylococcus aureus and Escherichia coli with a more pronounced effect on the Gram-positive bacteria. lPEIs further demonstrated a higher antibacterial efficacy compared to bPEIs but no significant differences between 5 and 25 kDa were observed. In accordance, antibacterial activity of bPEI did not specifically depend on molar mass. Only slightly lower minimal inhibitory concentrations (MIC) were observed at 5 kDa (S. aureus) and 25 kDa (E. coli) in the tests. As PEIs are compelling candidates for use in antimicrobial treatment, two basic aspects have to be investigated: treatment effectiveness and safety. PEIs clearly induced molecular weight dependent cytotoxic effects in vitro. PEIs with low molecular weight (0.8 and 5 kDa) exhibited higher biocompatibility. Nonetheless, the results confirmed a low genotoxic potential of lPEI and bPEIs. In conclusion, 2.5 kDa-lPEI and 0.8 kDa-bPEI can be recommended for use as antimicrobial polymers in dermal applications due to their high biocompatibility with concomitant antibacterial efficacy.
阳离子聚胺,如聚(亚乙基亚胺)(PEI),可以与微生物膜相互作用导致其破坏,因此可能适合用于抗菌应用。本研究的目的是评估具有不同结构(支化(b)和线性(l))和摩尔质量(0.8-750 kDa)的 PEI 的生物相容性和抗菌活性。lPEI 和 bPEI 对金黄色葡萄球菌和大肠杆菌表现出很强的抗菌活性,对革兰氏阳性菌的作用更为明显。lPEIs 表现出比 bPEIs 更高的抗菌功效,但在 5 和 25 kDa 之间没有观察到显著差异。相应地,bPEI 的抗菌活性并不特别取决于摩尔质量。在测试中,仅在 5 kDa(金黄色葡萄球菌)和 25 kDa(大肠杆菌)观察到稍低的最小抑菌浓度(MIC)。由于 PEIs 是用于抗菌治疗的有吸引力的候选物,因此必须研究两个基本方面:治疗效果和安全性。PEIs 在体外明显诱导了分子量依赖性细胞毒性作用。低分子量(0.8 和 5 kDa)的 PEIs 表现出更高的生物相容性。尽管如此,结果证实了 lPEI 和 bPEIs 的遗传毒性潜力较低。总之,由于具有高生物相容性和同时具有抗菌功效,2.5 kDa-lPEI 和 0.8 kDa-bPEI 可以推荐用于皮肤应用中的抗菌聚合物。