Elucidating of Fluconazole Cocrystallization With a Cutting-Edge Nutraceutical Coformer for Enhanced Formulation Strategies

IF 2.7 4区医学 Q2 PHARMACOLOGY & PHARMACY Journal of Pharmaceutical Innovation Pub Date : 2024-06-25 DOI:10.1007/s12247-024-09848-4

Payal Vithlapara, Malaykumar Chotaliya, Dhaval Mori, Kiran Dudhat

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Abstract

Introduction

This current research reports the synthesis and characterization of a cocrystal of Fluconazole (FLU), a widely used antifungal drug, with a nutraceutical coformer (NCF) that has potential health benefits as well as improving its solubility and antifungal activity.

Method

The co-crystal was obtained by solvent evaporation in a stoichiometric ratio using three natural coformers: Ferulic acid, caffeic acid, and glycerine, and characterized by various analytical techniques, including Powder x-ray diffraction (PXRD), Differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) spectroscopy.

Results

The cocrystals showed lower heats of fusion (ΔH) compared to pure Fluconazole, indicating the possibility of increased entropy and solubility for all cocrystals. Using the solvent evaporation method with ferulic acid, caffeic acid, and glycine showed significant enhancement of solubility, ranging from 1.06-fold to 4.80-fold, depending on the co-former and different media used.

Discussion and Conclusion

The zone of inhibition assay showed that cocrystals of Fluconazole with nutraceuticals (FLU+CAF, FLU+GLY, and FLU+FER) exhibited higher zones of inhibition compared to pure Fluconazole and DMSO control. Solubility and dissolution studies revealed that cocrystals of Fluconazole with nutraceutical coformers could be an effective approach to enhancing the solubility and antifungal activity of Fluconazole.

Graphical Abstract

Abstract Image

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利用先进的营养保健品共聚物阐明氟康唑的结晶过程，从而改进配方策略

引言本研究报告了氟康唑（FLU）共晶体的合成和表征，氟康唑是一种广泛使用的抗真菌药物，与营养保健品共聚物（NCF）的共晶体具有潜在的健康益处，并能改善其溶解性和抗真菌活性：结果与纯氟康唑相比，共晶体的熔点（ΔH）较低，这表明所有共晶体的熵和溶解度都有可能增加。使用阿魏酸、咖啡酸和甘氨酸的溶剂蒸发法显示，溶解度显著提高，从 1.06 倍到 4.80 倍不等，取决于共形物和使用的不同介质。讨论与结论抑菌区测定显示，与纯氟康唑和 DMSO 对照组相比，氟康唑与营养保健品（FLU+CAF、FLU+GLY 和 FLU+FER）的共晶体显示出更高的抑菌区。溶解度和溶解度研究表明，氟康唑与营养保健品共聚物的共晶体可以有效提高氟康唑的溶解度和抗真菌活性。

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来源期刊

Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-

CiteScore

3.70

自引率

3.80%

发文量

审稿时长

>12 weeks

期刊介绍： The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.