Abstract:
:Hybrid dendritic-linear block copolymers based on a 4-arm poly(ethylene glycol) (PEG) core were synthesized using an accelerated AB2/CD2 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.
journal_name
Biomacromoleculesjournal_title
Biomacromoleculesauthors
Albertazzi L,Mickler FM,Pavan GM,Salomone F,Bardi G,Panniello M,Amir E,Kang T,Killops KL,Bräuchle C,Amir RJ,Hawker CJdoi
10.1021/bm301384ysubject
Has Abstractpub_date
2012-12-10 00:00:00pages
4089-97issue
12eissn
1525-7797issn
1526-4602journal_volume
13pub_type
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