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

Area of Science:

• Biotechnology
• Antimicrobial drug development
• Oligonucleotide therapeutics

Background:

• Antisense oligonucleotides (ASOs) offer targeted gene control but require protective delivery systems.
• Controlling Candida albicans filamentation is crucial for effective antifungal strategies.
• Polyamide microparticles (MPs) are potential carriers for therapeutic oligonucleotides.

Purpose of the Study:

• To develop and evaluate polyamide microparticles (PA4 and PA6) as carriers for anti-EFG1 2'-O-MethylRNA ASOs.
• To assess the efficacy of entrapped and immobilized ASO delivery systems.
• To confirm the functional activity of delivered ASOs against Candida albicans.

Main Methods:

• Preparation of porous poly(γ-butyrolactam) (PA4) and poly(ε-caprolactam) (PA6) microparticles.
• Loading anti-EFG1 2'-O-MethylRNA ASOs into microparticles via entrapment and immobilization.
• Assessing the stability and release of ASOs from microparticle carriers.
• Evaluating the biological activity of released ASOs against Candida albicans.

Main Results:

• Both PA4 and PA6 microparticles successfully carried anti-EFG1 2'-O-MethylRNA ASOs.
• Entrapment and immobilization strategies proved effective for ASO loading.
• The delivered anti-EFG1 2'-O-MethylRNA ASOs retained their biological activity against C. albicans.
• Polyamide microparticles demonstrate feasibility as ASO delivery vehicles.

Conclusions:

• PA4 and PA6 polyplex microparticles are effective carriers for anti-EFG1 2'-O-MethylRNA ASOs.
• Both entrapment and immobilization methods are suitable for ASO delivery using these microparticles.
• The developed systems maintain ASO functionality, offering a promising approach for Candida albicans infections.