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Background <p>The solubility of poorly water-soluble drugs like Ticagrelor poses a significant challenge in developing effective dosage forms.</p> Objectives <p>The current study aimed to formulate β-cyclodextrin (β-CD) and Itaconic acid-based microgels to mitigate the solubility limitations of Ticagrelor, a BCS class IV drug.</p> Methods <p>The microgels were synthesized via a free radical polymerization technique, using methylene bisacrylamide as a cross-linker and methacrylic acid as a monomer, initiated by ammonium persulfate. A range of characterization techniques, including FTIR, TGA, DSC, SEM, PXRD, Zeta size, and Zeta potential, were employed to characterize the structural, thermal, morphological and physicochemical properties of the developed microgels.</p> Results <p>The FTIR spectra of the IA/β-CD based microgel optimized formulation F-7 and Ticagrelor loaded TF-7 showed major absorption peaks at 3380.6 cm<sup>− 1</sup> and 3295.75 cm<sup>− 1</sup>. The SEM image of Ticagrelor loaded optimized formulation TF-7 confirmed the dense compact morphology with smooth and well-defined porous surfaces. This microgel’s network also confirmed reduction in peak intensities indicating partial or substantial amorphization and successful encapsulation of Ticagrelor via PXRD analysis. The DSC thermogram of the Ticagrelor loaded IA/β-CD based optimized formulation TF-7 predicted an endothermic peak at around 230˚C, associated with the melting point. An exothermic event occurred around 350˚C, aligning with the major weight loss observed in the TGA depicting decomposition. In-vitro drug release and swelling studies were carried out at pH 1.2 and 6.8. The developed IA/β-CD integrated microgels effectively improved Ticagrelor’s solubility, demonstrated pH responsive swelling with enhanced drug release behavior at pH 6.8. TF7 -TF9 formulations followed Korsmeyer Peppas model having n &lt; 0.43 and demonstrated a Fickian diffusion, mostly via passive diffusion through the microgel matrix. The toxicity study confirmed a favorable safety profile.</p> Conclusion <p>The observed outcomes proved that the developed microgels are a valuable tool for overcoming Ticagrelor’s inherent solubility limitations.</p> Graphical Abstract <p></p>

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Smart pH-Responsive Itaconic Acid/β-Cyclodextrin Microgels: Revolutionizing Ticagrelor Solubility and Delivery

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年7月3日

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  • Rabia Imtiaz,
  • Kashif Barkat,
  • Nariman Shahid,
  • Ayesha Umer,
  • Nasir Ali,
  • Syed Faisal Badshah,
  • Esmael M. Alyami,
  • Hafiz Arfat Idrees,
  • Ahsanullah Unar

摘要

Background

The solubility of poorly water-soluble drugs like Ticagrelor poses a significant challenge in developing effective dosage forms.

Objectives

The current study aimed to formulate β-cyclodextrin (β-CD) and Itaconic acid-based microgels to mitigate the solubility limitations of Ticagrelor, a BCS class IV drug.

Methods

The microgels were synthesized via a free radical polymerization technique, using methylene bisacrylamide as a cross-linker and methacrylic acid as a monomer, initiated by ammonium persulfate. A range of characterization techniques, including FTIR, TGA, DSC, SEM, PXRD, Zeta size, and Zeta potential, were employed to characterize the structural, thermal, morphological and physicochemical properties of the developed microgels.

Results

The FTIR spectra of the IA/β-CD based microgel optimized formulation F-7 and Ticagrelor loaded TF-7 showed major absorption peaks at 3380.6 cm− 1 and 3295.75 cm− 1. The SEM image of Ticagrelor loaded optimized formulation TF-7 confirmed the dense compact morphology with smooth and well-defined porous surfaces. This microgel’s network also confirmed reduction in peak intensities indicating partial or substantial amorphization and successful encapsulation of Ticagrelor via PXRD analysis. The DSC thermogram of the Ticagrelor loaded IA/β-CD based optimized formulation TF-7 predicted an endothermic peak at around 230˚C, associated with the melting point. An exothermic event occurred around 350˚C, aligning with the major weight loss observed in the TGA depicting decomposition. In-vitro drug release and swelling studies were carried out at pH 1.2 and 6.8. The developed IA/β-CD integrated microgels effectively improved Ticagrelor’s solubility, demonstrated pH responsive swelling with enhanced drug release behavior at pH 6.8. TF7 -TF9 formulations followed Korsmeyer Peppas model having n < 0.43 and demonstrated a Fickian diffusion, mostly via passive diffusion through the microgel matrix. The toxicity study confirmed a favorable safety profile.

Conclusion

The observed outcomes proved that the developed microgels are a valuable tool for overcoming Ticagrelor’s inherent solubility limitations.

Graphical Abstract