Formulation and Characterization of Intranasal Drug Delivery of Frovatriptan-Loaded Binary Ethosomes Gel for Brain Targeting.

IF 4.9 Q2 NANOSCIENCE & NANOTECHNOLOGY Nanotechnology, Science and Applications Pub Date : 2024-01-16 eCollection Date: 2024-01-01 DOI:10.2147/NSA.S442951

Mohammed Layth Hamzah, Hanan Jalal Kassab

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Abstract

Background: Frovatriptan succinate (FVT) is an effective medication used to treat migraines; however, available oral formulations suffer from low permeability; accordingly, several formulations of FVT were prepared.

Objective: Prepare, optimize, and evaluate FVT-BE formulation to develop enhanced intranasal binary nano-ethosome gel.‎.

Methods: Binary ethosomes were prepared using different concentrations of phospholipid PLH90, ethanol, propylene glycol, and cholesterol by thin film hydration and characterized by particle size, zeta potential, and entrapment efficiency. Furthermore, in-vitro, in-vivo, ex-vivo, pharmacokinetics, and histopathological studies were done.

Results: Regarding FVT-loaded BE, formula (F9) demonstrated the best parameters from the other formulas; with the lowest particle size (154.1±4.38‎ nm), lowest PDI (‎0.213±0.05), highest zeta potential (‎-46.94±1.05), and highest entrapment efficiency (89.34±2.37%). Regarding gel formulation, G2 showed the best gel formula with drug content (‎99.82±0.02‎%) and spreadability (12.88 g/cm²). In-vitro study results showed that, in the first 30 minutes, around 22.3% of the medication is released, whereas, after 24 hours, about 98.56% is released in G2.

Conclusion: Based on enhancing the bioavailability and sustaining the drug release, it can be concluded that the Frovatriptan-Loaded Binary ethosome Gel as nano-delivery was developed as a promising non-invasive drug delivery system for treating migraine.

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用于脑靶向的弗罗阿曲普坦二元乙素体凝胶的鼻内给药配方与表征

背景：琥珀酸氟伐曲普坦（FVT）是一种治疗偏头痛的有效药物；然而，现有的口服制剂存在渗透性低的问题；因此，制备了几种FVT制剂：制备、优化和评估 FVT-BE 配方，以开发增强型鼻内二元纳米乙素体凝胶：方法：使用不同浓度的磷脂 PLH90、乙醇、丙二醇和胆固醇，通过薄膜水合法制备二元乙硫体，并通过粒度、ZETA电位和夹持效率对其进行表征。此外，还进行了体外、体内、体外、药代动力学和组织病理学研究：在负载 FVT 的 BE 方面，配方（F9）的参数是其他配方中最好的；粒度最小（154.1±4.38 nm），PDI 最低（0.213±0.05），zeta 电位最高（-46.94±1.05），包埋效率最高（89.34±2.37%）。在凝胶配方方面，G2 的药物含量（99.82±0.02%）和铺展性（12.88 g/cm2）均为最佳。体外研究结果表明，在最初的 30 分钟内，约有 22.3% 的药物被释放出来，而在 24 小时后，G2 中约有 98.56% 的药物被释放出来：基于提高生物利用度和维持药物释放的原理，可以得出结论：弗罗阿曲普坦负载二元乙素体凝胶作为纳米给药，是一种治疗偏头痛的前景广阔的非侵入性给药系统。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Nanotechnology, Science and Applications NANOSCIENCE & NANOTECHNOLOGY-

CiteScore

11.70

自引率

0.00%

发文量

审稿时长

16 weeks

期刊介绍： Nanotechnology, Science and Applications is an international, peer-reviewed, Open Access journal that focuses on the science of nanotechnology in a wide range of industrial and academic applications. The journal is characterized by the rapid reporting of reviews, original research, and application studies across all sectors, including engineering, optics, bio-medicine, cosmetics, textiles, resource sustainability and science. Applied research into nano-materials, particles, nano-structures and fabrication, diagnostics and analytics, drug delivery and toxicology constitute the primary direction of the journal.