What is it about?

In this study, Hydroxypropyl β-cyclodextrin (HPβCD) based polymeric nanobeads containing voriconazole (VRC) were synthesized using free radical polymerization with N, N′-methylene bisacrylamide (MBA) as a cross-linker, 2-acrylamide-2-methylpropane sulfonic acid (AMPS) as a monomer and ammonium persulfate (APS) as a reaction promoter. The optimized formulation (CDN5) had a particle size of 320 nm, zeta potential of −35.5 mV and 87% encapsulation efficiency. The nanobeads were porous and non-spherical in shape, and showed no evidence of chemical interaction through FT-IR studies, while high-intensity VRC peaks were observed in XRD. DSC studies indicated stable polymeric network formation, resulting in a lower breakdown of VRC-loaded HPβCD in comparison to blank HPβCD. In vitro release studies showed 91% and 92% drug release for optimized formulation at pH 1.2 and 6.8, respectively, with first-order kinetics as the best-fit model and non-Fickian diffusion as the release mechanism. No toxicity was observed upon oral administration of HPβCD loaded VRC polymeric nanobeads, as observed through histopathology. Molecular docking indicated hydrophobic patching mediated by nanogel formulation. These findings suggest that the development of polymeric nanobeads can be a promising tool to enhance the solubility and efficacy of hydrophobic drugs such as VRC, while decreasing toxicity for the effective management of fungal infections.

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Why is it important?

This study is important because it addresses a major challenge in drug delivery - the solubility of hydrophobic drugs such as voriconazole (VRC). Hydrophobic drugs are poorly soluble in water and, as a result, have limited bioavailability and efficacy. The development of polymeric nanobeads, as demonstrated in this study, can effectively encapsulate hydrophobic drugs and improve their solubility, resulting in improved therapeutic outcomes. The findings of this study suggest that this approach could be a promising tool for the effective management of fungal infections. Additionally, the study provides insights into the formulation and optimization of polymeric nanobeads, which could have implications for the delivery of other poorly soluble drugs in various therapeutic applications. Overall, this study is significant as it presents a potential solution to a critical problem in drug delivery, which could have a positive impact on patient outcomes.

Perspectives

As an author of the mentioned study, I feel honored to have been part of this research project. It was an exciting opportunity to collaborate with my co-authors and bring together our expertise to address a critical challenge in drug delivery. Our findings have the potential to make a significant impact on the management of fungal infections, as well as on the development of drug delivery systems for other poorly soluble drugs. Moreover, it is immensely gratifying to know that this study has caught the attention of rare disease groups. This has led to an increased involvement in rare disease research, which is a field that I am passionate about. It is encouraging to know that our work has sparked interest and could contribute to the development of treatments for rare diseases. Overall, this study has been a positive and rewarding experience for me, both in terms of the scientific findings and the opportunities for future research collaborations.

Mudassir Farooq
Bahauddin Zakariya University

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This page is a summary of: Voriconazole Cyclodextrin Based Polymeric Nanobeads for Enhanced Solubility and Activity: In Vitro/In Vivo and Molecular Simulation Approach, Pharmaceutics, January 2023, MDPI AG,
DOI: 10.3390/pharmaceutics15020389.
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