Mucoadhesive assessment of different antifungal nanoformulations

Area of Science:

• Pharmaceutical Sciences
• Biomaterials Engineering
• Mycology

Background:

• Oral candidiasis is a common opportunistic fungal infection often treated with polyenes and azoles.
• Current treatments suffer from poor oral absorption, necessitating frequent administration.
• Enhancing antifungal agent retention in the buccal mucosa is crucial for effective treatment.

Purpose of the Study:

• To develop and evaluate mucoadhesive polymeric nanoparticles for improved delivery of antifungal agents.
• To encapsulate nystatin into polylactic acid (PLA), polylactic-co-glycolic acid (PLGA), and alginate nanoparticles.
• To incorporate these nanoparticles into various oral formulations (toothpaste, oral gel, oral films) and assess their mucoadhesion and drug retention.

Main Methods:

• Preparation of PLA, PLGA, and alginate nanoparticles loaded with nystatin.
• Characterization of nanoparticles for size, surface charge, and encapsulation efficiency.
• In vitro assessment of mucoadhesion for different nanoparticle formulations.
• Evaluation of drug retention using an in vitro mucus model (HT29-MTX cells) and simulated saliva flow.

Main Results:

• Nystatin-loaded nanoparticles were successfully produced with sizes between 300-900 nm and negative surface charge.
• Encapsulation efficiency for all nanoparticles exceeded 70%.
• Oral films with PLGA nanoparticles demonstrated superior in vitro mucoadhesion and nystatin retention (10-27%) compared to PLA/gel and alginate/toothpaste formulations, and significantly better than free nystatin (4%).

Conclusions:

• Mucoadhesive nanoparticles, particularly PLGA nanoparticles in oral films, offer a promising strategy to enhance antifungal drug retention in the buccal mucosa.
• This approach could lead to more effective treatments for oral candidiasis with potentially reduced administration frequency.
• Further in vivo studies are warranted to validate these findings in animal models.