Rizatriptan benzoate-loaded dissolving microneedle patch for management of acute migraine therapy.

IF 2.3 4区医学 Q3 ENGINEERING, BIOMEDICAL Journal of Biomaterials Applications Pub Date : 2024-04-01 Epub Date: 2024-03-01 DOI:10.1177/08853282241237323

Chao Zhong, Xiufeng Zhang, Yanfang Sun, Zhong Shen, Yanan Mao, Tianqi Liu, Rui Wang, Lei Nie, Amin Shavandi, Khaydar E Yunusov, Guohua Jiang

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Abstract

In this study, dissolving microneedles (MNs) using polyvinyl alcohol (PVA) and poly (1-vinylpyrrolidone-co-vinyl acetate) (P(VP-co-VA)) as matrix materials were developed for transdermal delivery of rizatriptan benzoate (RB) for acute migraine treatment. In-vitro permeation studies were conducted to assess the feasibility of the as-fabricated dissolving MNs to release RB. Drug skin penetration were tested by Franz diffusion cells, showing an increase of the transdermal flux compared to passive diffusion due to the as-fabricated dissolving MNs having a sufficient mechanical strength to penetrate the skin and form microchannels. The pharmacological study in vivo showed that RB-loaded dissolving MNs significantly alleviated migraine-related response by up-regulating the level of 5-hydroxytryptamine (5-HT) and down-regulating the levels of calcitonin gene-related peptide (CGRP) and substance P (SP). In conclusion, the RB-loaded dissolving MNs have advantages of safety, convenience, and high efficacy over conventional administrations, laying a foundation for the transdermal drug delivery system treatment for acute migraine.

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用于急性偏头痛治疗的苯甲酸利扎曲普坦溶解微针贴片。

本研究开发了以聚乙烯醇（PVA）和聚（1-乙烯基吡咯烷酮-醋酸乙烯酯）（P(VP-co-VA)）为基质材料的溶解微针（MNs），用于透皮给药苯甲酸利扎曲普坦（RB）以治疗急性偏头痛。进行了体外渗透研究，以评估制成的可溶解 MN 释放 RB 的可行性。通过弗朗兹扩散细胞测试了药物的皮肤渗透性，结果表明，与被动扩散相比，透皮通量有所增加，这归功于预制的可溶解 MNs 具有足够的机械强度，能够穿透皮肤并形成微通道。体内药理学研究表明，RB 负载的可溶解 MNs 能上调 5- 羟色胺（5-HT）的水平，下调降钙素基因相关肽（CGRP）和 P 物质（SP）的水平，从而显著缓解偏头痛相关反应。总之，与传统给药方法相比，RB负载的可溶解MNs具有安全、方便、疗效高等优点，为透皮给药系统治疗急性偏头痛奠定了基础。

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来源期刊

Journal of Biomaterials Applications 工程技术-材料科学：生物材料

CiteScore

5.10

自引率

3.40%

发文量

144

审稿时长

1.5 months

期刊介绍： The Journal of Biomaterials Applications is a fully peer reviewed international journal that publishes original research and review articles that emphasize the development, manufacture and clinical applications of biomaterials. Peer-reviewed articles by biomedical specialists from around the world cover: New developments in biomaterials, R&D, properties and performance, evaluation and applications Applications in biomedical materials and devices - from sutures and wound dressings to biosensors and cardiovascular devices Current findings in biological compatibility/incompatibility of biomaterials The Journal of Biomaterials Applications publishes original articles that emphasize the development, manufacture and clinical applications of biomaterials. Biomaterials continue to be one of the most rapidly growing areas of research in plastics today and certainly one of the biggest technical challenges, since biomaterial performance is dependent on polymer compatibility with the aggressive biological environment. The Journal cuts across disciplines and focuses on medical research and topics that present the broadest view of practical applications of biomaterials in actual clinical use. The Journal of Biomaterial Applications is devoted to new and emerging biomaterials technologies, particularly focusing on the many applications which are under development at industrial biomedical and polymer research facilities, as well as the ongoing activities in academic, medical and applied clinical uses of devices.