Formulation and development of frovatriptan succinate in situ gel for nasal drug delivery: In vitro and ex vivo evaluation.

IF 0.7 4区 医学 Q4 PHARMACOLOGY & PHARMACY
Mohammed Layth Hamzah, Hanan Jalal Kassab
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引用次数: 0

Abstract

Magrain is a depleting disease that sometimes requires extensive treatment, ideally with medication that targets the brain, with minimized systemic adverse effects, preferably with a single daily medication; these properties are offered partially by the current dosage form of Frovatriptan. formulation of Frovatriptan binary ethosome into mucoadhesive nasal in situ gel to extend the drug's residence time. The particle size was ‎154.1±4.38‎ nm of the Frovatriptan binary ethosome. In situ, gel formulas were prepared to utilize the cold technique, using 18%w/v poloxamer 407 with different concentrations of Carbopol 934 and the clarity, pH, Frovatriptan content spreadability, mucoadhesive force, in vitro diffusion via nasal mucosa and the optimal formula underwent further investigations. In-situ gel F2 (0.2% Carbopol) demonstrated the best spreadability of 12.88±0.186 cm2/min, 99% drug content mucoadhesive strength of 645.32±0.054 dynes/cm2, percent release of 98.56±0.041 after 24 hours and permeability increased by around 3.68-fold compared to the pure drug and histopathologically showed favorable outcomes. Mucoadhesive Frovatriptan-binary ethosome-loaded nasal in situ gel is an effective method of treating migraines.

用于鼻腔给药的琥珀酸伐他普坦原位凝胶的配制与开发:体外和体内评估。
马格列是一种消耗性疾病,有时需要广泛的治疗,理想的治疗方法是使用针对大脑的药物,将全身不良反应降至最低,最好每天只需服用一种药物;弗罗阿曲普坦的现有剂型部分具备这些特性。弗罗阿曲普坦二元乙素体的粒径为 154.1±4.38 nm。利用冷冻技术,使用18%w/v的poloxamer 407和不同浓度的Carbopol 934制备了原位凝胶配方,并对其透明度、pH值、弗罗阿曲普坦含量的铺展性、粘附力、体外经鼻粘膜扩散性和最佳配方进行了进一步研究。与纯药物相比,原位凝胶 F2(0.2% Carbopol)具有最佳的铺展性(12.88±0.186 cm2/min)、99%药物含量的粘附力(645.32±0.054 dynes/cm2)、24 小时后的释放率(98.56±0.041)和渗透性增加了约 3.68 倍,组织病理学也显示了良好的结果。粘液黏附型弗罗阿曲普坦-二元乙素鼻腔原位凝胶是治疗偏头痛的一种有效方法。
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来源期刊
CiteScore
1.40
自引率
12.50%
发文量
211
审稿时长
4.5 months
期刊介绍: Pakistan Journal of Pharmaceutical Sciences (PJPS) is a peer reviewed multi-disciplinary pharmaceutical sciences journal. The PJPS had its origin in 1988 from the Faculty of Pharmacy, University of Karachi as a biannual journal, frequency converted as quarterly in 2005, and now PJPS is being published as bi-monthly from January 2013. PJPS covers Biological, Pharmaceutical and Medicinal Research (Drug Delivery, Pharmacy Management, Molecular Biology, Biochemical, Pharmacology, Pharmacokinetics, Phytochemical, Bio-analytical, Therapeutics, Biotechnology and research on nano particles.
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