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Purpose <p>Rheumatoid Arthritis (RA) affects approximately 1.5&#xa0;million people worldwide. Thiocolchicoside (THC) is commonly used in topical gels to alleviate RA-associated symptoms; however, its therapeutic efficacy is limited due to poor skin permeation. This study aimed to develop a THC-loaded niosomal gel to enhance skin permeation and retention.</p> Methods <p>THC-loaded niosomes were formulated using the ethanol injection technique and optimized via a central composite design. The optimized niosomes were characterized for vesicle size, zeta potential, entrapment efficiency, surface morphology, and solid-state properties. The niosomal dispersion was incorporated into a Carbopol-based gel. The formulated gel was evaluated for viscosity, spreadability, <i>in vitro</i> release, <i>ex vivo</i> permeation, skin deposition, skin irritation, anti-inflammatory activity, and stability.</p> Results <p>The optimized niosomes exhibited a vesicle size of 128.1 ± 5.2&#xa0;nm, zeta potential of -32.1 ± 1.3 mV, and entrapment efficiency of 88.51 ± 2.9%, with spherical morphology. The THC-loaded niosomal gel demonstrated significantly higher (<i>p</i> &lt; 0.05) <i>in vitro</i> drug release (83.3 ± 3.2%) over 12&#xa0;h compared to plain gel (42.2 ± 2.9%). <i>Ex vivo</i> permeation showed a 71.4 ± 1.9% (1285.2 ± 34.2&#xa0;µg/cm²) drug permeation from the THC-loaded niosomal gel compared to 31.3 ± 2.3% (563.4 ± 41.4&#xa0;µg/cm²) from the THC-loaded plain gel. Skin deposition studies confirmed significantly greater drug retention from the THC-loaded niosomal gel (<i>p</i> &lt; 0.05). The THC-loaded niosomal gel exhibited superior anti-inflammatory activity (59.62 ± 3% edema inhibition) compared to the THC-loaded plain gel (11.18 ± 0.20%) at 24&#xa0;h. Stability studies confirmed the formulation’s robustness under accelerated conditions for three months.</p> Conclusion <p>The developed THC-loaded niosomal gel demonstrated enhanced skin permeation, improved drug retention, and sustained anti-inflammatory activity, offering a promising therapeutic approach for RA management.</p>

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Thiocolchicoside Niosomal Gel: Design-Driven Optimization for Superior Skin Permeation

  • 期刊论文

  • 发表日期：

    2025年7月14日

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  • Ganesh Shevalkar,
  • Sakshi Pote,
  • Satish Rathod,
  • Meghraj Suryawanshi

摘要

Purpose

Rheumatoid Arthritis (RA) affects approximately 1.5 million people worldwide. Thiocolchicoside (THC) is commonly used in topical gels to alleviate RA-associated symptoms; however, its therapeutic efficacy is limited due to poor skin permeation. This study aimed to develop a THC-loaded niosomal gel to enhance skin permeation and retention.

Methods

THC-loaded niosomes were formulated using the ethanol injection technique and optimized via a central composite design. The optimized niosomes were characterized for vesicle size, zeta potential, entrapment efficiency, surface morphology, and solid-state properties. The niosomal dispersion was incorporated into a Carbopol-based gel. The formulated gel was evaluated for viscosity, spreadability, in vitro release, ex vivo permeation, skin deposition, skin irritation, anti-inflammatory activity, and stability.

Results

The optimized niosomes exhibited a vesicle size of 128.1 ± 5.2 nm, zeta potential of -32.1 ± 1.3 mV, and entrapment efficiency of 88.51 ± 2.9%, with spherical morphology. The THC-loaded niosomal gel demonstrated significantly higher (p < 0.05) in vitro drug release (83.3 ± 3.2%) over 12 h compared to plain gel (42.2 ± 2.9%). Ex vivo permeation showed a 71.4 ± 1.9% (1285.2 ± 34.2 µg/cm²) drug permeation from the THC-loaded niosomal gel compared to 31.3 ± 2.3% (563.4 ± 41.4 µg/cm²) from the THC-loaded plain gel. Skin deposition studies confirmed significantly greater drug retention from the THC-loaded niosomal gel (p < 0.05). The THC-loaded niosomal gel exhibited superior anti-inflammatory activity (59.62 ± 3% edema inhibition) compared to the THC-loaded plain gel (11.18 ± 0.20%) at 24 h. Stability studies confirmed the formulation’s robustness under accelerated conditions for three months.

Conclusion

The developed THC-loaded niosomal gel demonstrated enhanced skin permeation, improved drug retention, and sustained anti-inflammatory activity, offering a promising therapeutic approach for RA management.