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

Chao ZhongInternational Scientific and Technological Cooperation Base of Intelligent Biomaterials and Functional Fibers, Hangzhou, ChinaXiufeng ZhangDepartment of Anorectal Surgery, Hangzhou Third People’s Hospital, Hangzhou, ChinaYanfang SunCollege of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou, ChinaZhong ShenDepartment of Anorectal Surgery, Hangzhou Third People’s Hospital, Hangzhou, ChinaYanan MaoInternational Scientific and Technological Cooperation Base of Intelligent Biomaterials and Functional Fibers, Hangzhou, ChinaTianqi LiuInternational Scientific and Technological Cooperation Base of Intelligent Biomaterials and Functional Fibers, Hangzhou, ChinaRui WangInternational Scientific and Technological Cooperation Base of Intelligent Biomaterials and Functional Fibers, Hangzhou, ChinaLei NieCollege of Life Sciences, Xinyang Normal University, Xinyang, ChinaAmin ShavandiÉcole polytechnique de Bruxelles, 3BIO-BioMatter, Université Libre de Bruxelles (ULB), Brussels, BelgiumKhaydar E. YunusovInstitute of Polymer Chemistry and Physics, Uzbekistan Academy of Sciences, Tashkent, UzbekistanGuohua JiangInternational Scientific and Technological Cooperation Base of Intelligent Biomaterials and Functional Fibers, Hangzhou, China
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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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