Linear release nanoparticle devices for advanced targeted cancer therapies with increased efficacy

The cross-linked supramolecular structure of prepared polyester based nanoparticles enable increased and efficient small molecule drug loading after nanoparticle formation and post-modification with targeting peptides via thiol-ene ‘click’ chemistry. It could be demonstrated that the drug loading does not influence the structural integrity of the particle and its diameter was not significantly changed. A prolonged linear release profile of the drug without the typical ‘burst effect’ was observed in emulsified particles and mirrored the linear degradation profile of the investigated particles, which are critical properties for controlled and predictable pharmacokinetics in cancer therapies. Furthermore, the final peptide-targeted and drug-loaded particles were found to be readily dispersed in buffer or water, and with the confirmed biocompatibility, these novel and adjustable drug delivery systems are promising vectors for the treatment of various cancers.