• Coupling quaternary ammonium surfactants to the surface of liposomes improves both antibacterial efficacy and host cell biocompatibility

      Montefusco-Pereira, Carlos V.; Formicola, Beatrice; Goes, Adriely; Re, Francesca; Marrano, Claudia A.; Mantegazza, Francesco; Carvalho-Wodarz, Cristiane; Fuhrmann, Gregor; Caneva, Enrico; Nicotra, Francesco; et al. (Elsevier BV, 2020-04)
      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.
    • The synergistic effect of chlorotoxin-mApoE in boosting drug-loaded liposomes across the BBB.

      Formicola, Beatrice; Dal Magro, Roberta; Montefusco-Pereira, Carlos V; Lehr, Claus-Michael; Koch, Marcus; Russo, Laura; Grasso, Gianvito; Deriu, Marco A; Danani, Andrea; Bourdoulous, Sandrine; et al. (BMC, 2019-11-11)
      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.