{"title":"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","authors":"Mohammed Layth Hamzah, Hanan Jalal Kassab","doi":"10.2147/NSA.S442951","DOIUrl":null,"url":null,"abstract":"<p><strong>Background: </strong>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.</p><p><strong>Objective: </strong>Prepare, optimize, and evaluate FVT-BE formulation to develop enhanced intranasal binary nano-ethosome gel..</p><p><strong>Methods: </strong>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.</p><p><strong>Results: </strong>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/cm<sup>2</sup>). 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.</p><p><strong>Conclusion: </strong>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.</p>","PeriodicalId":18881,"journal":{"name":"Nanotechnology, Science and Applications","volume":"17 ","pages":"1-19"},"PeriodicalIF":4.9000,"publicationDate":"2024-01-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10799622/pdf/","citationCount":"0","resultStr":"{\"title\":\"Formulation and Characterization of Intranasal Drug Delivery of Frovatriptan-Loaded Binary Ethosomes Gel for Brain Targeting.\",\"authors\":\"Mohammed Layth Hamzah, Hanan Jalal Kassab\",\"doi\":\"10.2147/NSA.S442951\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Background: </strong>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.</p><p><strong>Objective: </strong>Prepare, optimize, and evaluate FVT-BE formulation to develop enhanced intranasal binary nano-ethosome gel..</p><p><strong>Methods: </strong>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.</p><p><strong>Results: </strong>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/cm<sup>2</sup>). 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.</p><p><strong>Conclusion: </strong>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.</p>\",\"PeriodicalId\":18881,\"journal\":{\"name\":\"Nanotechnology, Science and Applications\",\"volume\":\"17 \",\"pages\":\"1-19\"},\"PeriodicalIF\":4.9000,\"publicationDate\":\"2024-01-16\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10799622/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Nanotechnology, Science and Applications\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2147/NSA.S442951\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/1/1 0:00:00\",\"PubModel\":\"eCollection\",\"JCR\":\"Q2\",\"JCRName\":\"NANOSCIENCE & NANOTECHNOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Nanotechnology, Science and Applications","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2147/NSA.S442951","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/1/1 0:00:00","PubModel":"eCollection","JCR":"Q2","JCRName":"NANOSCIENCE & NANOTECHNOLOGY","Score":null,"Total":0}
Formulation and Characterization of Intranasal Drug Delivery of Frovatriptan-Loaded Binary Ethosomes Gel for Brain Targeting.
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.
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.
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