{"title":"可注射的电纺纤维-水凝胶复合给药系统,用于延长镇痛时间并具有痛觉选择性","authors":"Sufang Chen, Weifeng Yao, Zhendong Ding, Jingyi Du, Tienan Wang, Xue Xiao, Linan Zhang, Jing Yang, Yu Guan, Chaojin Chen, Yu Tao, Mingqiang Li, Haixia Wang, Ziqing Hei","doi":"10.1007/s42765-024-00422-8","DOIUrl":null,"url":null,"abstract":"<div><p>Nociceptive-selective analgesia is often preferred over traditional methods, providing effective pain relief with minimum systemic side effects.The quaternary lidocaine derivative QX-314, is a promising local anesthetic for achieving selective analgesia. However, due to its inability to penetrate the cell membrane, its efficacy is limited to intracellular administration. In this study, we aimed to develop an injectable electrospun fiber-hydrogel composite comprising QX-314-loaded poly(ε-caprolactone) electrospun fiber and capsaicin (Cap)-loaded F127 hydrogel (Fiber-QX314/Gel-Cap composite) for long-term and nociceptive-selective analgesia. The sequential and sustained release mechanism of Cap and QX-314 helped remarkably extend the sensory blockade duration up to 44.0 h, and prevent motor blockade. Specifically, our findings indicated that QX-314 can traverse the cell membrane through the transient receptor potential vanilloid 1 channel activated by Cap, thus targeting the intracellular Na<sup>+</sup> channel receptor to achieve selective analgesia. Moreover, the composite effectively alleviated incision pain by suppressing c-Fos expression in the dorsal root ganglion and reducing the activation of glial cells in the dorsal horn of the spinal cord. Consequently, the Fiber-QX314/Gel-Cap composite, designed for exceptional biosafety and sustained selective analgesia, holds great promise as a non-opioid analgesic.</p><h3>Graphical abstract</h3>\n<div><figure><div><div><picture><source><img></source></picture></div><div><p>Injectable composite comprising QX-314-loaded electrospun fiber and capsaicin-loaded thermosensitive hydrogel sequentially releasing drugs for prolonged and nociceptive-selective local analgesia.</p></div></div></figure></div></div>","PeriodicalId":459,"journal":{"name":"Advanced Fiber Materials","volume":"6 5","pages":"1428 - 1445"},"PeriodicalIF":17.2000,"publicationDate":"2024-05-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Injectable Electrospun Fiber-Hydrogel Composite Delivery System for Prolonged and Nociceptive-Selective Analgesia\",\"authors\":\"Sufang Chen, Weifeng Yao, Zhendong Ding, Jingyi Du, Tienan Wang, Xue Xiao, Linan Zhang, Jing Yang, Yu Guan, Chaojin Chen, Yu Tao, Mingqiang Li, Haixia Wang, Ziqing Hei\",\"doi\":\"10.1007/s42765-024-00422-8\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Nociceptive-selective analgesia is often preferred over traditional methods, providing effective pain relief with minimum systemic side effects.The quaternary lidocaine derivative QX-314, is a promising local anesthetic for achieving selective analgesia. However, due to its inability to penetrate the cell membrane, its efficacy is limited to intracellular administration. In this study, we aimed to develop an injectable electrospun fiber-hydrogel composite comprising QX-314-loaded poly(ε-caprolactone) electrospun fiber and capsaicin (Cap)-loaded F127 hydrogel (Fiber-QX314/Gel-Cap composite) for long-term and nociceptive-selective analgesia. The sequential and sustained release mechanism of Cap and QX-314 helped remarkably extend the sensory blockade duration up to 44.0 h, and prevent motor blockade. Specifically, our findings indicated that QX-314 can traverse the cell membrane through the transient receptor potential vanilloid 1 channel activated by Cap, thus targeting the intracellular Na<sup>+</sup> channel receptor to achieve selective analgesia. Moreover, the composite effectively alleviated incision pain by suppressing c-Fos expression in the dorsal root ganglion and reducing the activation of glial cells in the dorsal horn of the spinal cord. Consequently, the Fiber-QX314/Gel-Cap composite, designed for exceptional biosafety and sustained selective analgesia, holds great promise as a non-opioid analgesic.</p><h3>Graphical abstract</h3>\\n<div><figure><div><div><picture><source><img></source></picture></div><div><p>Injectable composite comprising QX-314-loaded electrospun fiber and capsaicin-loaded thermosensitive hydrogel sequentially releasing drugs for prolonged and nociceptive-selective local analgesia.</p></div></div></figure></div></div>\",\"PeriodicalId\":459,\"journal\":{\"name\":\"Advanced Fiber Materials\",\"volume\":\"6 5\",\"pages\":\"1428 - 1445\"},\"PeriodicalIF\":17.2000,\"publicationDate\":\"2024-05-14\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Advanced Fiber Materials\",\"FirstCategoryId\":\"88\",\"ListUrlMain\":\"https://link.springer.com/article/10.1007/s42765-024-00422-8\",\"RegionNum\":1,\"RegionCategory\":\"工程技术\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"MATERIALS SCIENCE, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Advanced Fiber Materials","FirstCategoryId":"88","ListUrlMain":"https://link.springer.com/article/10.1007/s42765-024-00422-8","RegionNum":1,"RegionCategory":"工程技术","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"MATERIALS SCIENCE, MULTIDISCIPLINARY","Score":null,"Total":0}
Injectable Electrospun Fiber-Hydrogel Composite Delivery System for Prolonged and Nociceptive-Selective Analgesia
Nociceptive-selective analgesia is often preferred over traditional methods, providing effective pain relief with minimum systemic side effects.The quaternary lidocaine derivative QX-314, is a promising local anesthetic for achieving selective analgesia. However, due to its inability to penetrate the cell membrane, its efficacy is limited to intracellular administration. In this study, we aimed to develop an injectable electrospun fiber-hydrogel composite comprising QX-314-loaded poly(ε-caprolactone) electrospun fiber and capsaicin (Cap)-loaded F127 hydrogel (Fiber-QX314/Gel-Cap composite) for long-term and nociceptive-selective analgesia. The sequential and sustained release mechanism of Cap and QX-314 helped remarkably extend the sensory blockade duration up to 44.0 h, and prevent motor blockade. Specifically, our findings indicated that QX-314 can traverse the cell membrane through the transient receptor potential vanilloid 1 channel activated by Cap, thus targeting the intracellular Na+ channel receptor to achieve selective analgesia. Moreover, the composite effectively alleviated incision pain by suppressing c-Fos expression in the dorsal root ganglion and reducing the activation of glial cells in the dorsal horn of the spinal cord. Consequently, the Fiber-QX314/Gel-Cap composite, designed for exceptional biosafety and sustained selective analgesia, holds great promise as a non-opioid analgesic.
期刊介绍:
Advanced Fiber Materials is a hybrid, peer-reviewed, international and interdisciplinary research journal which aims to publish the most important papers in fibers and fiber-related devices as well as their applications.Indexed by SCIE, EI, Scopus et al.
Publishing on fiber or fiber-related materials, technology, engineering and application.