Abstract
The present piece of research work is framed for improving the solubility of ketoprofen by forming co-crystal using fumaric acid as a coformer. Co-crystal of ketoprofen and fumaric acid was prepared by simple solvent-assisted grinding method, containing drug and coformer as independent variables and solubility and % drug release were assumed to be dependent variables. Differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction, nuclear magnetic resonance and scanning electron microscopy techniques were used to characterize the preparation of optimized batch of co-crystal and further, evaluated for in vitro and in vivo anti-inflammatory and analgesic activities. Based on results of solubility and dissolution rate studies the formulation showed magnified improvement in both the properties on co-crystallization. The values of Gibbs free energy are negative at all levels of carrier demonstrating spontaneity of the drug solubilization process. The IC50 value of optimized batch of co-crystal formulation and the pure drug was observed as 327.33 μg/ml and 556.11 μg/ml, respectively, demonstrating that co-crystal formulation possesses more percentage protection against protein denaturation than the drug ketoprofen. In vivo (anti-inflammatory and analgesic) activities revealed that optimized batch of co-crystal formulation delivered a rapid pharmacological response in Wistar rats and albino mice when compared with standard drug.
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References
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Sunita Devi contributed to conceptualization and writing—original draft preparation; Meenakshi Bhatia contributed to conceptualization and supervision; Ashwini Kumar contributed to review & editing and software; Vikas Verma contributed to writing—review & editing; Snehlata Yadav contributed to review & editing and data curation.
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Theme: Advancements in Modified-release Oral Drug Delivery - Delivery throughout the Gastro-intestinal Tract
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Devi, S., Kumar, A., Kapoor, A. et al. Ketoprofen–FA Co-crystal: In Vitro and In Vivo Investigation for the Solubility Enhancement of Drug by Design of Expert. AAPS PharmSciTech 23, 101 (2022). https://doi.org/10.1208/s12249-022-02253-5
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DOI: https://doi.org/10.1208/s12249-022-02253-5