Polyamide Microsized Particulate Polyplex Carriers for the 2'-OMethylRNA EFG1 Antisense Oligonucleotide.

ABSTRACT

Anti-EFG1 2'-OMethylRNA is an antisense oligonucleotide (ASO) that has the ability to recognize and block the EFG1 gene and to control Candida albicans filamentation. However, it is important to protect the anti-EFG1 2'-OMethylRNA 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-EFG1 2'-OMethylRNA ASO cargo and delivery. Two types of polyplexes were prepared with payloads of anti-EFG1 2'-OMethylRNA molecules, either entrapped or immobilized on prefabricated polyamide MPs. Our data confirm that PA4 and PA6 polyplex MPs can be feasible carriers for anti-EFG1 2'-OMethylRNA ASO molecules, using either the entrapment or immobilization strategies, whereby the released ASO maintains its activity against C. albicans cells.