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

IF 3 Q2 PHARMACOLOGY & PHARMACY

Future Journal of Pharmaceutical Sciences Pub Date : 2025-07-30 DOI:10.1186/s43094-025-00855-x

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

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引用次数: 0

Abstract

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

查看原文本刊更多论文

表面工程壳聚糖包被的纳米结构脂质载体用于奥卡西平和维生素E油的鼻内递送治疗癫痫

传统口服抗癫痫药物的有效性受到诸如生物利用度不足、剂量相关的不良反应以及在缓解癫痫方面的不依从性等问题的阻碍。口服抗癫痫药物由于首过代谢高，治疗癫痫效果不佳，而血脑屏障及氧化损伤所致的限制是癫痫患者服用抗癫痫药物时遇到的一个重要问题。本研究的主要目的是探索开发的壳聚糖包被的奥卡西平纳米结构脂质载体（CS OXC-NLC）与维生素E结合减少氧化应激的能力，并通过鼻内给药提供神经保护和帮助提高抗癫痫疗效。结果采用熔融乳化法制备了CS - OXC-NLC。采用中心复合可旋转设计对配方进行优化。研究结果表明，优化后的CS OXC-NLC与奥卡西平混悬液相比，体外释放量增加1.8倍，透性提高2倍。共聚焦显微镜显示，CS - OXC-NLC（40µm）比奥卡西平混悬液（22.8µm）通过鼻黏膜的荧光更强，证实了穿透性的提高。测定了脑和血浆中氧合碳的药动学参数和生物分布。脑内药物量的增加证明了通过鼻内给药靶向治疗的有效性。结论本研究结果表明，开发的CS - OXC-NLC是一种可行的协同治疗癫痫的方法，效果良好。它描述了壳聚糖涂层在通过鼻内给药提高所开发的制剂的体内前景方面的潜力。壳聚糖具有黏附性、缓释性、渗透增强性和生物相容性等特点，在提高NLC的鼻内给药性能方面发挥着重要作用。图形抽象

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来源期刊

Future Journal of Pharmaceutical Sciences PHARMACOLOGY & PHARMACY-

自引率

0.00%

发文量

审稿时长

23 weeks

期刊介绍： Future Journal of Pharmaceutical Sciences (FJPS) is the official journal of the Future University in Egypt. It is a peer-reviewed, open access journal which publishes original research articles, review articles and case studies on all aspects of pharmaceutical sciences and technologies, pharmacy practice and related clinical aspects, and pharmacy education. The journal publishes articles covering developments in drug absorption and metabolism, pharmacokinetics and dynamics, drug delivery systems, drug targeting and nano-technology. It also covers development of new systems, methods and techniques in pharmacy education and practice. The scope of the journal also extends to cover advancements in toxicology, cell and molecular biology, biomedical research, clinical and pharmaceutical microbiology, pharmaceutical biotechnology, medicinal chemistry, phytochemistry and nutraceuticals.