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<p>Rheumatoid arthritis (RA) is a chronic autoimmune inflammatory disorder which is characterized by severe synovial inflammation, joint destruction and functional disability. Methotrexate (MTX) is the first line disease modifying antirheumatic drug but its clinical applicability is limited due to poor water solubility, systemic toxicity and reduced patient compliance associated with long term oral or parenteral adminisatrtion. Although topical delivery systems based on nanotechnology have been investigated to overcome these limitations, problems like poor drug solubilization, restricted skin penetration, and suboptimal therapeutic efficacy still exist. Specifically there is a significiant research gap regarding the integration of β-cyclodextrin (β-CD) inclusion complexation with nanoemulsion-based gel systems for improving MTX delivery. Thus the goal of this present study was to develop and evaluate a nanoemulsion based gel loaded with the β-CD-MTX inclusion complex for better topical delivery in the treatment of RA. To confirm complexation and improved physiochemical properties, the MTX-β-CD inclusion complex was prepared and characterized using phase solubility analysis (Higuchi and Connors method), FT-IR, DSC, XRD, TGA, and ¹H NMR. The optimized nanoemulsion was composed of chaulmogra oil, tween 80 and PEG 400, which exhibits a droplet size of of 199.1 ± 14.55&#xa0;nm and a zeta potential of -14.7 ± 1.45 mV. To improve skin retention and applicability, the nanoemulsion was further integrated into a gel matrix. <i>In-vitro </i>drug release studies showed sustained MTX release (77.99 ± 0.79% over 24&#xa0;h), while <i>Ex-vivo&#xa0;</i>studies revealed enhanced permeation (83.79 ± 2.63%) compared to conventional gel (53.99 ± 2.22%). Additionally, the nanogel-treated group demonstrated a considerable improvement in inflammatory symptoms and joint integrity in an <i>in-vivo </i> anti-arthritic evaluation using the Complete Freund’s adjuvant-induced model. Over all, the developed β-CD-MTX nanoemulsion gel provides a hopeful approach to enhance topical MTX delivery, improves therapeutic efficacy, and reduces systemic side effects, thereby addressing important limitations of traditional RA therapy.</p> Graphical Abstract <p></p>

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Development and Characterization of β-Cyclodextrin and Methotrexate Inclusion Complex-Based Nanogel for the Management of Rheumatoid Arthritis

  • 期刊论文

  • 发表日期：

    2026年7月28日

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  • Aman Kumar,
  • Ravi Raj Pal,
  • Manish Kumar,
  • Preeti Patel,
  • Sourabh Kosey,
  • Balak Das Kurmi

摘要

Rheumatoid arthritis (RA) is a chronic autoimmune inflammatory disorder which is characterized by severe synovial inflammation, joint destruction and functional disability. Methotrexate (MTX) is the first line disease modifying antirheumatic drug but its clinical applicability is limited due to poor water solubility, systemic toxicity and reduced patient compliance associated with long term oral or parenteral adminisatrtion. Although topical delivery systems based on nanotechnology have been investigated to overcome these limitations, problems like poor drug solubilization, restricted skin penetration, and suboptimal therapeutic efficacy still exist. Specifically there is a significiant research gap regarding the integration of β-cyclodextrin (β-CD) inclusion complexation with nanoemulsion-based gel systems for improving MTX delivery. Thus the goal of this present study was to develop and evaluate a nanoemulsion based gel loaded with the β-CD-MTX inclusion complex for better topical delivery in the treatment of RA. To confirm complexation and improved physiochemical properties, the MTX-β-CD inclusion complex was prepared and characterized using phase solubility analysis (Higuchi and Connors method), FT-IR, DSC, XRD, TGA, and ¹H NMR. The optimized nanoemulsion was composed of chaulmogra oil, tween 80 and PEG 400, which exhibits a droplet size of of 199.1 ± 14.55 nm and a zeta potential of -14.7 ± 1.45 mV. To improve skin retention and applicability, the nanoemulsion was further integrated into a gel matrix. In-vitro drug release studies showed sustained MTX release (77.99 ± 0.79% over 24 h), while Ex-vivo studies revealed enhanced permeation (83.79 ± 2.63%) compared to conventional gel (53.99 ± 2.22%). Additionally, the nanogel-treated group demonstrated a considerable improvement in inflammatory symptoms and joint integrity in an in-vivo anti-arthritic evaluation using the Complete Freund’s adjuvant-induced model. Over all, the developed β-CD-MTX nanoemulsion gel provides a hopeful approach to enhance topical MTX delivery, improves therapeutic efficacy, and reduces systemic side effects, thereby addressing important limitations of traditional RA therapy.

Graphical Abstract