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Development, Safety, and Therapeutic Evaluation of Voriconazole-Loaded Zein-Pectin-Hyaluronic Acid Nanoparticles
Margani Taise Fin1, Kelvin Sousa Dos Santos2, Marcos William de Lima Gualque2
1Laboratory of Nanostructured Formulations, Universidade Estadual do Centro-Oeste (UNICENTRO), Alameda Élio Antônio Dalla Vecchia, 838, Guarapuava 85040-167, PR, Brazil.
Abstract:
Background/Objectives: Fungal infections caused by Candida species remain a significant clinical challenge, exacerbated by limitations in current antifungal therapies, including toxicity and poor bioavailability. This study aimed to develop and evaluate voriconazole-loaded zein-pectin-hyaluronic acid nanoparticles (ZPHA-VRC NPs) as a novel drug delivery system to enhance efficacy and reduce toxicity. Alternative in vitro and in vivo models were utilized to assess the safety and therapeutic potential of the nanoparticles. Methods: ZPHA-VRC NPs were prepared using a nanoprecipitation method and characterized for particle size, polydispersity index, zeta potential, and encapsulation efficiency. Antifungal activity was assessed via MIC assays against Candida albicans, C. krusei, and C. parapsilosis. Cytotoxicity was evaluated on Vero cells, while in vivo toxicity and efficacy were assessed using Galleria mellonella and Caenorhabditis elegans models. The therapeutic efficacy was further evaluated in an infected Caenorhabditis elegans model using survival and health scores. Results: ZPHA-VRC nanoparticles exhibited favorable physicochemical properties, including a particle size of approximately 192 nm, a polydispersity index of 0.079, a zeta potential of -24 mV, and an encapsulation efficiency of 34%. The nanoparticles retained antifungal activity comparable to free voriconazole while significantly reducing cytotoxicity. In vivo studies using G. mellonella and C. elegans demonstrated that ZPHA-VRC NPs markedly improved survival rates, reduced fungal burden, and enhanced health scores in infected models, outperforming the free drug. Additionally, the nanoparticles exhibited a superior safety profile, minimizing systemic toxicity while maintaining therapeutic efficacy. Conclusions: ZPHA-VRC NPs offer a safer and more effective delivery system for VRC, addressing the limitations of conventional formulations. The integration of alternative efficacy and safety models highlights their value in preclinical research.
Insights
Novel voriconazole-loaded nanoparticles (ZPHA-VRC NPs) demonstrate enhanced antifungal efficacy and reduced toxicity. These advanced nanoparticles offer a safer and more effective treatment for fungal infections compared to traditional voriconazole formulations.
Area of Science:
- Nanotechnology
- Pharmaceutical Sciences
- Mycology
Background:
- Fungal infections caused by Candida species present significant clinical challenges.
- Current antifungal therapies, like voriconazole, suffer from toxicity and poor bioavailability.
- Novel drug delivery systems are needed to improve voriconazole's therapeutic profile.
Purpose of the Study:
- To develop and characterize voriconazole-loaded zein-pectin-hyaluronic acid nanoparticles (ZPHA-VRC NPs).
- To evaluate the enhanced efficacy and reduced toxicity of ZPHA-VRC NPs.
- To assess the safety and therapeutic potential using alternative in vitro and in vivo models.
Main Methods:
- Nanoparticle formulation via nanoprecipitation.
- Physicochemical characterization (particle size, PDI, zeta potential, EE).
- Antifungal activity (MIC), cytotoxicity (Vero cells), and in vivo studies (Galleria mellonella, Caenorhabditis elegans).
Main Results:
- ZPHA-VRC NPs showed optimal physicochemical properties (192 nm size, -24 mV zeta potential, 34% EE).
- Nanoparticles maintained antifungal activity while significantly reducing cytotoxicity.
- In vivo models demonstrated improved survival, reduced fungal burden, and enhanced health scores with ZPHA-VRC NPs compared to free voriconazole.
Conclusions:
- ZPHA-VRC NPs represent a promising, safer, and more effective delivery system for voriconazole.
- The study highlights the utility of alternative models in evaluating nanoparticle safety and efficacy.
- This novel formulation addresses limitations of conventional voriconazole treatments.
