Multifunctionalised cationic fullerene adducts for gene transfer: Design, synthesis and DNA complexation

Cationic poly-N,N-dimethylfulleropyrrolidinium derivatives have been designed and synthesised to complex plasmid DNA for gene delivery.  The biological applications of fullerenes continue to attract increasing attention. Fullerenes can be considered useful systems for drug delivery because they can be multifunctionalised, they can act as drug adsorbents and form particles in the nanoscale range. Very few examples of delivery of therapeutic agents using fullerenes as the active carrier have been reported in the literature. Fullerene has been conjugated to paclitaxel or complexed to a melanoma targeting antibody for chemo- and immunotherapy, respectively. Pristine fullerene has been used as solid adsorbent for erythropoietin to engineer a new drug vector with improved bioavailability and uptake. Alternatively, fullerene derivatives were used as counter-ions to modulate the cellular uptake and the anion carrier activity of cell-penetrating peptides.