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Objective <p>This study was aimed at developing Warfarin composites and preliminarily evaluating them as controlled drug delivery (CDD) systems.</p> Methods <p>The Warfarin-β-CD-loaded chitosan nanoparticles (WCS) and Warfarin-β-CD-silica composite (WSi) were synthesized through polymeric nanoparticles and sol-gel processes, respectively. Warfarin-β-CD-loaded chitosan nanoparticles were produced through ionic gelation of chitosan (CS) with tripolyphosphate (TPP) in a specific ratio, followed by loading with the Warfarin-β-CD complex. Warfarin-β-CD-silica composite was synthesized through the sol-gel approach by incorporating the inclusion of Warfarin-β-CD into the silica precursor.</p> Results <p>X-ray diffraction analysis revealed a crystalline peak of pure Warfarin at 21.9º of 2θ angle. This peak was shifted to 22.5º in Warfarin-β-CD-CS nanoparticles, indicating the presence of the crystalline nature of Warfarin in this composite. In contrast, no sharp peak was observed in the Warfarin-β-CD-silica composite, suggesting the amorphous nature of the silica-based composite. During FTIR analysis, the characteristic carbon-carbon double bonds (C = C) stretching vibrations corresponding to the phenyl groups 1 and 2 of Warfarin were observed at 1617&#xa0;cm<sup>− 1</sup> and 1570&#xa0;cm<sup>− 1</sup> wavenumbers, respectively. The asymmetric stretch of CH<sub>2</sub> group was observed at 2940&#xa0;cm⁻¹ and an asymmetric bend of CH<sub>3</sub> group revealed at 1451&#xa0;cm⁻¹. At 1681&#xa0;cm⁻¹ the stretching of the lactone group (C = O) was indicated. The in vitro drug release revealed that pure Warfarin had a rapid release rate (at pH 1.6, it reached 84.6% in just 28&#xa0;h, while at pH 7.4, it released around 59.95%) when compared to both composites. In vivo investigations revealed that Warfarin-β-CD-silica composite group showed higher PT (61.2&#xa0;s at day 3 and 33.9&#xa0;s at day 9) and INR (4.7 at day 3 and 2.2 at day 9) values compared to the positive control and Warfarin-β-CD-CS groups, suggesting improved Warfarin release control under tested conditions.</p> Conclusions <p>Warfarin-β-CD-silica composite exhibited a slow and sustained release of Warfarin, making it a promising candidate for the CDD system for Warfarin.</p> Graphical Abstract <p></p>

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Design and Evaluation of β-Cyclodextrin-Modified Warfarin-Chitosan and Warfarin-Silica Composites for Controlled Drug Release: In Vitro and in Vivo Approach

  • 期刊论文

  • 发表日期：

    2026年1月9日

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  • Amna Hussain,
  • Wen-Nee Tan,
  • Abdullah Ijaz Hussain,
  • Tabinda Fatima,
  • Esraa M Haji,
  • Ali F Almutairy,
  • Sulaiman Mohammed Abdullah Alnasser,
  • Hajar Alghamdi,
  • Abdulkareem A. Alanezi,
  • Ashfaq Ahmad

摘要

Objective

This study was aimed at developing Warfarin composites and preliminarily evaluating them as controlled drug delivery (CDD) systems.

Methods

The Warfarin-β-CD-loaded chitosan nanoparticles (WCS) and Warfarin-β-CD-silica composite (WSi) were synthesized through polymeric nanoparticles and sol-gel processes, respectively. Warfarin-β-CD-loaded chitosan nanoparticles were produced through ionic gelation of chitosan (CS) with tripolyphosphate (TPP) in a specific ratio, followed by loading with the Warfarin-β-CD complex. Warfarin-β-CD-silica composite was synthesized through the sol-gel approach by incorporating the inclusion of Warfarin-β-CD into the silica precursor.

Results

X-ray diffraction analysis revealed a crystalline peak of pure Warfarin at 21.9º of 2θ angle. This peak was shifted to 22.5º in Warfarin-β-CD-CS nanoparticles, indicating the presence of the crystalline nature of Warfarin in this composite. In contrast, no sharp peak was observed in the Warfarin-β-CD-silica composite, suggesting the amorphous nature of the silica-based composite. During FTIR analysis, the characteristic carbon-carbon double bonds (C = C) stretching vibrations corresponding to the phenyl groups 1 and 2 of Warfarin were observed at 1617 cm− 1 and 1570 cm− 1 wavenumbers, respectively. The asymmetric stretch of CH2 group was observed at 2940 cm⁻¹ and an asymmetric bend of CH3 group revealed at 1451 cm⁻¹. At 1681 cm⁻¹ the stretching of the lactone group (C = O) was indicated. The in vitro drug release revealed that pure Warfarin had a rapid release rate (at pH 1.6, it reached 84.6% in just 28 h, while at pH 7.4, it released around 59.95%) when compared to both composites. In vivo investigations revealed that Warfarin-β-CD-silica composite group showed higher PT (61.2 s at day 3 and 33.9 s at day 9) and INR (4.7 at day 3 and 2.2 at day 9) values compared to the positive control and Warfarin-β-CD-CS groups, suggesting improved Warfarin release control under tested conditions.

Conclusions

Warfarin-β-CD-silica composite exhibited a slow and sustained release of Warfarin, making it a promising candidate for the CDD system for Warfarin.

Graphical Abstract