ABSTRACT
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.
Subject(s)
Anti-Bacterial Agents/pharmacology , Biofilms/drug effects , Escherichia coli/drug effects , Quaternary Ammonium Compounds/pharmacology , Sulfhydryl Compounds/pharmacology , Anti-Bacterial Agents/chemistry , Liposomes , Maleimides/chemistry , Nanoparticles , Phosphatidylethanolamines/chemistry , Polyethylene Glycols/chemistry , Quaternary Ammonium Compounds/chemistry , Sulfhydryl Compounds/chemistry , Surface-Active Agents/chemistry , Surface-Active Agents/pharmacologyABSTRACT
We designed liposomes dually functionalized with ApoE-derived peptide (mApoE) and chlorotoxin (ClTx) to improve their blood-brain barrier (BBB) crossing. Our results demonstrated the synergistic activity of ClTx-mApoE in boosting doxorubicin-loaded liposomes across the BBB, keeping the anti-tumour activity of the drug loaded: mApoE acts promoting cellular uptake, while ClTx promotes exocytosis of liposomes.
