Enhanced bioactivity of internally functionalized cationic dendrimers with PEG cores

Lorenzo Albertazzi, Frauke M. Mickler, Giovanni M. Pavan, Fabrizio Salomone, Giuseppe Bardi, Mariangela Panniello, Elizabeth Amir, Taegon Kang, Kato L. Killops, Christoph Bräuchle, Roey J. Amir*, Craig J. Hawker

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review


Hybrid dendritic-linear block copolymers based on a 4-arm poly(ethylene glycol) (PEG) core were synthesized using an accelerated AB2/CD 2 dendritic growth approach through orthogonal amine/epoxy and thiol-yne chemistries. The biological activity of these 4-arm and the corresponding 2-arm hybrid dendrimers revealed an enhanced, dendritic effect with an exponential increase in cell internalization concomitant with increasing amine end groups and low cytotoxicity. Furthermore, the ability of these hybrid dendrimers to induce endosomal escape combined with their facile and efficient synthesis makes them attractive platforms for gene transfection. The 4-arm-based dendrimer showed significantly improved DNA binding and gene transfection capabilities in comparison with the 2-arm derivative. These results combined with the MD simulation indicate a significant effect of both the topology of the PEG core and the multivalency of these hybrid macromolecules on their DNA binding and delivery capablities.

Original languageEnglish
Pages (from-to)4089-4097
Number of pages9
Issue number12
StatePublished - 10 Dec 2012


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