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Purpose <p>Topical local anesthetics have become increasingly important with the recent development of laser therapy. Lidocaine, the most commonly used anesthetic in clinical practice, not only has analgesic effects but also possesses properties such as suppression of neonatal seizures and antiarrhythmic, anti-inflammatory, antibacterial, and antifungal effects. This study aimed to improve the solubility and permeability of lidocaine (Lid) by preparing solid dispersions of Lid and ascorbic acid 2-glucoside (AG) and evaluating their physicochemical properties, solubility, and permeability.</p> Methods <p>Here, we evaluated the physicochemical properties and solubility of solid dispersions of Lid and AG prepared by freeze-drying (freeze-dried [FD] Lid/SSA = 1/1).</p> Results <p>For Differential scanning calorimetry measurements revealed the disappearance of the endothermic peaks associated with the melting of Lid and AG in the freeze-dried formulation (FD) (Lid/AG = 1/1), with the emergence of a new glass transition point. Powder X-ray diffraction measurements confirmed the absence of the characteristic peaks of both Lid and AG in the FD (Lid/AG = 1/1), showing a halo pattern. Near-infrared measurements indicated peak shifts and broadening of the -CH and -NH groups of Lid and the -OH and -CH groups of AG in the FD (Lid/AG = 1/1), suggesting the involvement of complex formation. Solubility tests revealed that the solubility of FD (Lid/AG = 1/1) was approximately 220&#xa0;mg/mL, which is approximately 50 times higher than that of Lid (approximately 4.0&#xa0;mg/mL). Nuclear Overhauser effect spectroscopy nuclear magnetic resonance (NMR) measurements revealed cross-peaks between the -CH groups of Lid and the -OH groups of AG, suggesting intermolecular interactions via hydrogen bonding. Diffusion-ordered spectroscopy NMR measurements showed that the diffusion coefficients of Lid and AG in the FD (Lid/AG = 1/1) converged, indicating that the formation of a complex with AG altered the dispersion behavior of Lid in the solvent. In the silicon membrane permeability test, the cumulative amount permeated after 24&#xa0;h was approximately 700&#xa0;µg/cm<sup>2</sup> for Lid, compared to approximately 4.0&#xa0;µg/cm<sup>2</sup> for FD (Lid/AG = 1/1), suggesting that membrane permeability was inhibited.</p> Conclusion <p>These findings suggest that complex formation occurred in FD Lid/ AG; this enhanced the solubility, membrane permeability was inhibited of this dispersion.</p> Graphical Abstract <p></p>

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Characterization, solubility, and skin penetration of lidocaine through complexation with ascorbic acid 2-glucoside

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年8月25日

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  • Manami Nomura,
  • Junki Tomita,
  • Masahiro Sugino,
  • Syuuhei Komatsu,
  • Hiroaki Todo,
  • Nao Kodama,
  • Yutaka Inoue

摘要

Purpose

Topical local anesthetics have become increasingly important with the recent development of laser therapy. Lidocaine, the most commonly used anesthetic in clinical practice, not only has analgesic effects but also possesses properties such as suppression of neonatal seizures and antiarrhythmic, anti-inflammatory, antibacterial, and antifungal effects. This study aimed to improve the solubility and permeability of lidocaine (Lid) by preparing solid dispersions of Lid and ascorbic acid 2-glucoside (AG) and evaluating their physicochemical properties, solubility, and permeability.

Methods

Here, we evaluated the physicochemical properties and solubility of solid dispersions of Lid and AG prepared by freeze-drying (freeze-dried [FD] Lid/SSA = 1/1).

Results

For Differential scanning calorimetry measurements revealed the disappearance of the endothermic peaks associated with the melting of Lid and AG in the freeze-dried formulation (FD) (Lid/AG = 1/1), with the emergence of a new glass transition point. Powder X-ray diffraction measurements confirmed the absence of the characteristic peaks of both Lid and AG in the FD (Lid/AG = 1/1), showing a halo pattern. Near-infrared measurements indicated peak shifts and broadening of the -CH and -NH groups of Lid and the -OH and -CH groups of AG in the FD (Lid/AG = 1/1), suggesting the involvement of complex formation. Solubility tests revealed that the solubility of FD (Lid/AG = 1/1) was approximately 220 mg/mL, which is approximately 50 times higher than that of Lid (approximately 4.0 mg/mL). Nuclear Overhauser effect spectroscopy nuclear magnetic resonance (NMR) measurements revealed cross-peaks between the -CH groups of Lid and the -OH groups of AG, suggesting intermolecular interactions via hydrogen bonding. Diffusion-ordered spectroscopy NMR measurements showed that the diffusion coefficients of Lid and AG in the FD (Lid/AG = 1/1) converged, indicating that the formation of a complex with AG altered the dispersion behavior of Lid in the solvent. In the silicon membrane permeability test, the cumulative amount permeated after 24 h was approximately 700 µg/cm2 for Lid, compared to approximately 4.0 µg/cm2 for FD (Lid/AG = 1/1), suggesting that membrane permeability was inhibited.

Conclusion

These findings suggest that complex formation occurred in FD Lid/ AG; this enhanced the solubility, membrane permeability was inhibited of this dispersion.

Graphical Abstract