Solvent-Free Synthesis of Multifunctional Block Copolymer and Formation of DNA and Drug Nanocarriers

The synthesis of well-defined multifunctional polymers is of great importance for the development of complex materials for biomedical applications. In the current work, novel and multi-amino-functional diblock copolymer for potential gene and drug delivery applications was successfully synthesized. A highly efficient one-step and quantitative modification of an alkyne-functional polycarbonate-based precursor was performed, yielding double hydrophilic block copolymer with densely grafted primary amine side groups. The obtained positively charged block copolymer co-associated with DNA, forming stable and biocompatible nanosized polyplexes. Furthermore, polyion complex (PIC) micelles with tunable surface charge and decorated with cell targeting moieties were obtained as a result of direct mixing in aqueous media of the multi-amino-functional block copolymer and a previously synthesized oppositely charged block copolymer bearing disaccharide end-group. The obtained well-defined nanosized PIC-micelles were loaded with the hydrophobic drug curcumin. Both types of nanoaggregates (polyplexes and PIC-micelles) were physico-chemically characterized. Moreover, initial in vitro evaluations were performed to assess the nanocarriers' potential for biomedical applications.

Automated summary

The synthesis of well-defined multifunctional polymers is critical for the development of complex materials in biomedical applications. In this study, a novel multi-amino-functional diblock copolymer was successfully synthesized for potential gene and drug delivery applications. The copolymer was obtained through one-step modification of an alkyne-functional polycarbonate-based precursor, resulting in a hydrophilic block copolymer with densely grafted primary amine side groups. Additionally, polyion complex micelles with tunable surface charge, decorated with cell targeting moieties, were obtained through direct mixing of the multi-amino-functional block copolymer and an oppositely charged block copolymer.