Novel nasal niosomes loaded with lacosamide and coated with chitosan: A possible pathway to target the brain to control partial-onset seizures

IF 5.2 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Alaa S. Tulbah , Mohammed H. Elkomy , Randa Mohammed Zaki , Hussein M. Eid , Essam M. Eissa , Adel A. Ali , Heba A. Yassin , Basmah Nasser Aldosari , Ibrahim A. Naguib , Amira H. Hassan
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Abstract

This work aimed to develop and produce lacosamide-loaded niosomes coated with chitosan (LCA-CTS-NSM) using a thin-film hydration method and the Box-Behnken design. The effect of three independent factors (Span 60 amount, chitosan concentration, and cholesterol amount) on vesicle size, entrapment efficiency, zeta potential, and cumulative release (8 h) was studied. The optimal formulation of LCA-CTS-NSM was chosen from the design space and assessed for morphology, in vitro release, nasal diffusion, stability, tolerability, and in vivo biodistribution for brain targeting after intranasal delivery. The vesicle size, entrapment, surface charge, and in vitro release of the optimal formula were found to be 194.3 nm, 58.3%, +35.6 mV, and 81.3%, respectively. Besides, it exhibits sustained release behavior, enhanced nasal diffusion, and improved physical stability. Histopathological testing revealed no evidence of toxicity or structural damage to the nasal mucosa. It demonstrated significantly more brain distribution than the drug solution. Overall, the data is encouraging since it points to the potential for non-invasive intranasal administration of LCA as an alternative to oral or parenteral routes.

Abstract Image

负载拉可沙胺并包覆壳聚糖的新型鼻小体:一种靶向大脑控制部分发作性癫痫的可能途径
本研究旨在利用薄膜水化法和Box-Behnken设计,制备壳聚糖包被的lacosamide负载niosomes (LCA-CTS-NSM)。考察了3个独立因素(Span 60用量、壳聚糖浓度和胆固醇用量)对囊泡大小、包封效率、zeta电位和累积释放(8 h)的影响。从设计空间中选择LCA-CTS-NSM的最佳配方,并评估其形态、体外释放、鼻腔扩散、稳定性、耐受性和经鼻给药后脑靶向的体内生物分布。最佳配方的囊泡大小为194.3 nm,包载量为58.3%,表面电荷为+35.6 mV,体外释放量为81.3%。此外,它具有缓释行为,增强鼻腔扩散,改善物理稳定性。组织病理学检查未发现对鼻黏膜的毒性或结构性损伤。与药物溶液相比,它在大脑中的分布明显更广。总的来说,这些数据是令人鼓舞的,因为它指出了无创鼻内给药LCA作为口服或肠外途径的替代方案的潜力。
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来源期刊
International Journal of Pharmaceutics: X
International Journal of Pharmaceutics: X Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.60
自引率
0.00%
发文量
32
审稿时长
24 days
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