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Background <p>The effectiveness of conventional oral antiepileptic drug administration is hampered by issues such as inadequate bioavailability, dose-related adverse effects and non-compliance in alleviating epilepsy. Oral antiepileptic drugs have not been successful in treating epilepsy due to high first-pass metabolism, and restriction due to blood–brain barrier and oxidative damage is a significant problem experienced by epileptic patients taking antiepileptic drugs.</p> <p>The major goal of the current study was to explore the ability of the developed chitosan-coated nanostructured lipid carriers of Oxcarbazepine (CS OXC-NLC) integrated with Vitamin E to lessen oxidative stress and offers neuroprotection and aids in boosting the antiepileptic efficacy through intranasal drug delivery.</p> Results <p>In the present work, CS OXC-NLC was fabricated using melt emulsification process. Central Composite Rotatable Design has been utilized to optimize formulation. The study findings showed that optimized CS OXC-NLC exhibited 1.8 times increment in in vitro release and a twofold enhancement in permeability in comparison with the Oxcarbazepine suspension. Confocal microscopy verified the improvement in penetration by showing greater fluorescence in CS OXC-NLC (40&#xa0;µm) than Oxcarbazepine suspension (22.8&#xa0;µm) through the nasal mucosa. The pharmacokinetic parameters and biodistribution of OXC levels in the brain and plasma were duly examined. The rise in the amount of drug inside the brain demonstrates the effectiveness of targeting via intranasal administration.</p> Conclusion <p>The study outcome demonstrated that the developed CS OXC-NLC is a viable synergistic method producing alluring results for alleviating epilepsy. It depicts the potential of chitosan coating in enhancing the in vivo prospect of the developed formulation through intranasal delivery. Chitosan plays a significant role in enhancing the performance of NLC for intranasal delivery owing to its mucoadhesion properties, controlled release, permeation enhancement and biocompatibility.</p> Graphical abstract <p></p>

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Surface-engineered chitosan-coated nanostructured lipid carriers for intranasal delivery of Oxcarbazepine and Vitamin E oil in epilepsy management

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年7月30日

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  • Farhan Haider,
  • Eman Aldosari,
  • Rabea Parveen,
  • Sanjula Baboota,
  • Azka Gull,
  • Saba Khan,
  • Javed Ali

摘要

Background

The effectiveness of conventional oral antiepileptic drug administration is hampered by issues such as inadequate bioavailability, dose-related adverse effects and non-compliance in alleviating epilepsy. Oral antiepileptic drugs have not been successful in treating epilepsy due to high first-pass metabolism, and restriction due to blood–brain barrier and oxidative damage is a significant problem experienced by epileptic patients taking antiepileptic drugs.

The major goal of the current study was to explore the ability of the developed chitosan-coated nanostructured lipid carriers of Oxcarbazepine (CS OXC-NLC) integrated with Vitamin E to lessen oxidative stress and offers neuroprotection and aids in boosting the antiepileptic efficacy through intranasal drug delivery.

Results

In the present work, CS OXC-NLC was fabricated using melt emulsification process. Central Composite Rotatable Design has been utilized to optimize formulation. The study findings showed that optimized CS OXC-NLC exhibited 1.8 times increment in in vitro release and a twofold enhancement in permeability in comparison with the Oxcarbazepine suspension. Confocal microscopy verified the improvement in penetration by showing greater fluorescence in CS OXC-NLC (40 µm) than Oxcarbazepine suspension (22.8 µm) through the nasal mucosa. The pharmacokinetic parameters and biodistribution of OXC levels in the brain and plasma were duly examined. The rise in the amount of drug inside the brain demonstrates the effectiveness of targeting via intranasal administration.

Conclusion

The study outcome demonstrated that the developed CS OXC-NLC is a viable synergistic method producing alluring results for alleviating epilepsy. It depicts the potential of chitosan coating in enhancing the in vivo prospect of the developed formulation through intranasal delivery. Chitosan plays a significant role in enhancing the performance of NLC for intranasal delivery owing to its mucoadhesion properties, controlled release, permeation enhancement and biocompatibility.

Graphical abstract