Design and synthesis of nanocarriers containing posaconazole against etiological agents of mucormycosis

Posaconazole is an effective antifungal agent used for many fungal diseases, and its application has grown recently. Posaconazole was studied as a treatment option after the increase in mucormycosis cases linked to COVID-19, and promising results were obtained. However, despite its effectiveness, researchers are looking into new approaches to drug delivery due to problems including restricted bioavailability and short half-life. To address these issues, this project intends to create and synthesize posaconazole-containing liposomes.

Methods

In this study, according to the synthesis of Posaconazole-loaded liposomes, their physical and chemical properties were assessed using SEM, DLS, and FTIR techniques. The drug loading capacity in the nanoparticles, its release in vitro, and the antifungal activity against mucormycosis-causing fungi were evaluated. Finally, the cytotoxicity of these nanoparticles was assessed using the MTT Assay.

Results

The synthesized nanoparticles were spherical with an average size of approximately 60 nm. The drug loading efficiency was found to be 78.41%. The results indicated that the posaconazole nanoparticles demonstrated a slow and continuous drug release over five days. These nanoparticles demonstrated higher efficacy than posaconazole individually in antifungal tests. Additionally, cytotoxicity tests revealed that, up to a 400 µg/ml concentration, posaconazole-loaded nanoparticles were less toxic than free posaconazole.

Conclusions

These nanoparticles may provide a useful therapeutic option for the treatment of mucormycosis while circumventing the disadvantages of posaconazole due to their improved antifungal activities and decreased toxicity compared to free posaconazole.