当前位置: X-MOL 学术Eur. J. Pharm. Biopharm. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Coupling quaternary ammonium surfactants to the surface of liposomes improves both antibacterial efficacy and host cell biocompatibility.
European Journal of Pharmaceutics and Biopharmaceutics ( IF 4.9 ) Pub Date : 2020-01-30 , DOI: 10.1016/j.ejpb.2020.01.013
Carlos V Montefusco-Pereira 1 , Beatrice Formicola 2 , Adriely Goes 3 , Francesca Re 2 , Claudia A Marrano 2 , Francesco Mantegazza 2 , Cristiane Carvalho-Wodarz 4 , Gregor Fuhrmann 3 , Enrico Caneva 5 , Francesco Nicotra 6 , Claus-Michael Lehr 1 , Laura Russo 6
Affiliation  

By functionalizing the surface of PEG-liposomes with linkers bearing quaternary ammonium compounds (QACs), we generated novel bacteria disruptors with anti-adhesive properties and reduced cytotoxicity compared to free QACs. Furthermore, QAC-functionalized liposomes are a promising platform for future drug encapsulation. The QAC (11-mercaptoundecyl)-N,N,N-trimethylammonium bromide (MTAB) was attached to maleimide-functionalized liposomes (DSPE-PEG) via thiol linker. The MTAB-functionalized liposomes were physicochemically characterized and their biological activity, in terms of anti-adherence activity and biofilm prevention in Escherichia coli were assessed. The results showed that MTAB-functionalized liposomes inhibit bacterial adherence and biofilm formation while reducing MTAB toxicity.

中文翻译:

将季铵表面活性剂偶联至脂质体表面可提高抗菌功效和宿主细胞生物相容性。

通过使用带有季铵化合物(QAC)的接头对PEG-脂质体的表面进行功能化,与游离QAC相比,我们产生了具有抗黏附特性并降低了细胞毒性的新型细菌破坏剂。此外,QAC功能化脂质体是未来药物封装的有前途的平台。QAC(11-巯基癸基)-N,N,N-三甲基溴化铵(MTAB)通过硫醇连接基连接到马来酰亚胺官能化脂质体(DSPE-PEG)上。对MTAB-官能化脂质体进行了物理化学表征,并评估了它们在大肠杆菌中的抗粘附活性和生物膜预防方面的生物学活性。结果表明,MTAB功能化的脂质体抑制细菌粘附和生物膜形成,同时降低MTAB毒性。
更新日期:2020-01-31
down
wechat
bug