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Design and In Vitro Evaluation of Intranasal Diazepam for Treating Acute Repetitive Seizures: a Technical Note
Journal of Pharmaceutical Innovation ( IF 2.6 ) Pub Date : 2020-11-19 , DOI: 10.1007/s12247-020-09519-0
Sai HS. Boddu , Sneha Kumari

This study aimed to develop and characterize a novel microemulsion-based intranasal diazepam for treating acute repetitive seizures (ARS). The solubility of diazepam was obtained in different solvents. An oil in water microemulsion was prepared with castor oil as oil phase, polyethylene glycol monostearate as surfactant, ethanol as cosurfactant, and water. The formulation was further evaluated for droplet size, zeta potential, pH, in vitro drug release, morphology using transmission electron microscopy (TEM), thermal property using differential scanning calorimetry (DSC), and stability and toxicity in the bovine nasal mucosa. The developed o/w microemulsion system exhibited a droplet size of 51.23 nm with a neutral zeta potential. The pH of microemulsion was close to the pH of nasal secretions. The TEM image revealed the spherical droplet shape, and the DSC thermogram showed conversion of diazepam from a crystalline form to an amorphous/molecular dispersion form. Histological evaluation of the microemulsion showed an intact bovine nasal mucosa without any signs of toxicity and was found to be stable at 25 °C for up to 3 months. To conclude, the reported microemulsion could be further explored as an alternative for treating ARS.



中文翻译:

鼻内地西am治疗急性重复性癫痫的设计和体外评估:技术说明

这项研究旨在开发和表征一种新型的基于微乳的鼻内地西m治疗急性重复性癫痫发作(ARS)。获得了地西epa在不同溶剂中的溶解度。用蓖麻油作为油相,聚乙二醇单硬脂酸酯作为表面活性剂,乙醇作为助表面活性剂和水制备水包油型微乳液。进一步评估制剂的液滴大小,ζ电位,pH,体外药物释放,使用透射电子显微镜(TEM)的形态,使用差示扫描量热法(DSC)的热性质以及在牛鼻粘膜中的稳定性和毒性。发达的o / w微乳体系显示出液滴大小为51.23 nm,具有中性的ζ电位。微乳液的pH值接近鼻分泌物的pH值。TEM图像显示球形液滴形状,DSC热分析图显示地西epa从结晶形式转化为无定形/分子分散形式。该微乳的组织学评估显示完整的牛鼻粘膜无任何毒性迹象,并且发现在25°C稳定长达3个月。总而言之,可以进一步探索报道的微乳液作为治疗ARS的替代方法。

更新日期:2020-11-19
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