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Purpose <p>The study aimed to enhance the physicochemical and pharmacological properties of albendazole by developing cocrystals with para-hydroxybenzoic acid (PHBA) as a coformer, thereby improving its solubility, dissolution rate, and therapeutic efficacy while minimizing hepatotoxicity.</p> Methods <p>Albendazole–PHBA cocrystals were synthesized using the lyophilization technique. Solid-state characterization was performed through differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM) to confirm cocrystal formation. Molecular interactions were elucidated using Fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (¹H NMR) spectroscopy. Saturation solubility and in-vitro dissolution studies were conducted in different media (0.1N HCl, phosphate buffer pH 6.8, and distilled water pH 7.0). Molecular docking studies were performed to predict the binding affinity of albendazole and its cocrystals with α- and β-tubulin targets.</p> Results <p>DSC, PXRD, and SEM analyses confirmed successful formation of albendazole–PHBA cocrystals. Spectroscopic studies indicated hydrogen bonding between the C=O group of PHBA and the N–H group of albendazole. Solubility increased by 1.24-fold in 0.1N HCl, 91.94-fold in phosphate buffer (pH 6.8), and 119.49-fold in distilled water compared to the pure drug. The cocrystals exhibited significantly improved dissolution rates in both acidic and neutral media. Reduced hepatotoxicity were observed relative to pure albendazole. Molecular docking revealed stronger binding affinity and lower binding energy for cocrystals with tubulin targets.</p> Conclusion <p>Albendazole–PHBA cocrystals demonstrated marked improvements in solubility, dissolution behavior, and therapeutic performance, along with reduced hepatotoxicity. This study underscores the potential of cocrystallization with phenolic acid coformers as an effective approach for optimizing the bioavailability and safety of poorly soluble antiparasitic drugs.</p>

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Albendazole-Para-Hydroxybenzoic Acid Cocrystals: A Lyophilization-Based Strategy for Enhanced Solubility and Therapeutic Performance

  • 期刊论文

  • 发表日期：

    2025年11月17日

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  • Jaydeep Mehta,
  • Chetan Borkhataria,
  • Payal Vaja,
  • Saina Jyotishi

摘要

Purpose

The study aimed to enhance the physicochemical and pharmacological properties of albendazole by developing cocrystals with para-hydroxybenzoic acid (PHBA) as a coformer, thereby improving its solubility, dissolution rate, and therapeutic efficacy while minimizing hepatotoxicity.

Methods

Albendazole–PHBA cocrystals were synthesized using the lyophilization technique. Solid-state characterization was performed through differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM) to confirm cocrystal formation. Molecular interactions were elucidated using Fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (¹H NMR) spectroscopy. Saturation solubility and in-vitro dissolution studies were conducted in different media (0.1N HCl, phosphate buffer pH 6.8, and distilled water pH 7.0). Molecular docking studies were performed to predict the binding affinity of albendazole and its cocrystals with α- and β-tubulin targets.

Results

DSC, PXRD, and SEM analyses confirmed successful formation of albendazole–PHBA cocrystals. Spectroscopic studies indicated hydrogen bonding between the C=O group of PHBA and the N–H group of albendazole. Solubility increased by 1.24-fold in 0.1N HCl, 91.94-fold in phosphate buffer (pH 6.8), and 119.49-fold in distilled water compared to the pure drug. The cocrystals exhibited significantly improved dissolution rates in both acidic and neutral media. Reduced hepatotoxicity were observed relative to pure albendazole. Molecular docking revealed stronger binding affinity and lower binding energy for cocrystals with tubulin targets.

Conclusion

Albendazole–PHBA cocrystals demonstrated marked improvements in solubility, dissolution behavior, and therapeutic performance, along with reduced hepatotoxicity. This study underscores the potential of cocrystallization with phenolic acid coformers as an effective approach for optimizing the bioavailability and safety of poorly soluble antiparasitic drugs.