Polyamide Microsized Particulate Polyplex Carriers for the 2'-MethylRNA Antisense Oligonucleotide.

Anti- 2'-MethylRNA is an antisense oligonucleotide (ASO) that has the ability to recognize and block the gene and to control filamentation. However, it is important to protect the anti- 2'-MethylRNA ASO from the environmental human body conditions and to ensure that they will be delivered to their site of action, and polyplex microparticles (MPs) represent a class of vehicles to ASO cargo with these functionalities. Thus, the goal of this work was to develop polyplexes based on porous poly(γ-butyrolactam) (PA4) or poly(ε-caprolactam) (PA6) MPs for the anti- 2'-MethylRNA ASO cargo and delivery. Two types of polyplexes were prepared with payloads of anti- 2'-MethylRNA molecules, either entrapped or immobilized on prefabricated polyamide MPs. Our data confirm that PA4 and PA6 polyplex MPs can be feasible carriers for anti- 2'-MethylRNA ASO molecules, using either the entrapment or immobilization strategies, whereby the released ASO maintains its activity against cells.