{"title":"双层核苷微针联合递送地塞米松囊泡和腺苷克服假膜屏障治疗口腔溃疡。","authors":"Beibei Zhang, Yuyan Qian, Jianhua Li, Yu Fan, Mingyuan Gao, Qianqian Wu, Zhouxiang Li, Yong Hu* and Jianzhong Du*, ","doi":"10.1021/acsnano.5c05542","DOIUrl":null,"url":null,"abstract":"<p >Oral ulcers are common, painful mucosal lesions that significantly impair patients’ quality of life. The dynamic and moist oral environment, pseudomembrane formation, and limitations of corticosteroid therapies present ongoing clinical challenges. To address these important challenges, we developed double-layer microneedles integrating three functional components: a rapidly dissolving poly(vinyl alcohol) (PVA) substrate for immediate mucosal adhesion, nucleoside-based microneedles for pseudomembrane penetration and oxidative stress relief, and dexamethasone-loaded polymer vesicles (Dex-PVs). The vesicle improves the bioavailability of dexamethasone and enables a slow, sustained release, enhancing its therapeutic effects. Nucleoside microneedles, incorporating adenosine, synergistically enhance anti-inflammatory and analgesic effects by reducing the release of inflammatory cytokines and decreasing neuronal excitability and reverse the glucocorticoid-induced inhibition of cell migration by promoting CD31 and Ki67 expression. <i>In vivo</i> experiments confirmed that the microneedle reduced the ulcer area to 6.3% after 9 days of treatment (a 69.3% reduction compared to commercial formulations), with significant analgesic effects. This multiscale engineering approach addresses key challenges in oral drug retention, pseudomembrane penetration, and healing regulation, offering a paradigm for the treatment of mucosal diseases.</p>","PeriodicalId":21,"journal":{"name":"ACS Nano","volume":"19 27","pages":"25204–25227"},"PeriodicalIF":16.0000,"publicationDate":"2025-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Double-Layer Nucleoside-Microneedles Co-Delivering Dexamethasone Vesicles and Adenosine Overcome Pseudomembrane Barriers for the Treatment of Oral Ulcer\",\"authors\":\"Beibei Zhang, Yuyan Qian, Jianhua Li, Yu Fan, Mingyuan Gao, Qianqian Wu, Zhouxiang Li, Yong Hu* and Jianzhong Du*, \",\"doi\":\"10.1021/acsnano.5c05542\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p >Oral ulcers are common, painful mucosal lesions that significantly impair patients’ quality of life. The dynamic and moist oral environment, pseudomembrane formation, and limitations of corticosteroid therapies present ongoing clinical challenges. To address these important challenges, we developed double-layer microneedles integrating three functional components: a rapidly dissolving poly(vinyl alcohol) (PVA) substrate for immediate mucosal adhesion, nucleoside-based microneedles for pseudomembrane penetration and oxidative stress relief, and dexamethasone-loaded polymer vesicles (Dex-PVs). The vesicle improves the bioavailability of dexamethasone and enables a slow, sustained release, enhancing its therapeutic effects. Nucleoside microneedles, incorporating adenosine, synergistically enhance anti-inflammatory and analgesic effects by reducing the release of inflammatory cytokines and decreasing neuronal excitability and reverse the glucocorticoid-induced inhibition of cell migration by promoting CD31 and Ki67 expression. <i>In vivo</i> experiments confirmed that the microneedle reduced the ulcer area to 6.3% after 9 days of treatment (a 69.3% reduction compared to commercial formulations), with significant analgesic effects. This multiscale engineering approach addresses key challenges in oral drug retention, pseudomembrane penetration, and healing regulation, offering a paradigm for the treatment of mucosal diseases.</p>\",\"PeriodicalId\":21,\"journal\":{\"name\":\"ACS Nano\",\"volume\":\"19 27\",\"pages\":\"25204–25227\"},\"PeriodicalIF\":16.0000,\"publicationDate\":\"2025-07-03\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"ACS Nano\",\"FirstCategoryId\":\"88\",\"ListUrlMain\":\"https://pubs.acs.org/doi/10.1021/acsnano.5c05542\",\"RegionNum\":1,\"RegionCategory\":\"材料科学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"ACS Nano","FirstCategoryId":"88","ListUrlMain":"https://pubs.acs.org/doi/10.1021/acsnano.5c05542","RegionNum":1,"RegionCategory":"材料科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Double-Layer Nucleoside-Microneedles Co-Delivering Dexamethasone Vesicles and Adenosine Overcome Pseudomembrane Barriers for the Treatment of Oral Ulcer
Oral ulcers are common, painful mucosal lesions that significantly impair patients’ quality of life. The dynamic and moist oral environment, pseudomembrane formation, and limitations of corticosteroid therapies present ongoing clinical challenges. To address these important challenges, we developed double-layer microneedles integrating three functional components: a rapidly dissolving poly(vinyl alcohol) (PVA) substrate for immediate mucosal adhesion, nucleoside-based microneedles for pseudomembrane penetration and oxidative stress relief, and dexamethasone-loaded polymer vesicles (Dex-PVs). The vesicle improves the bioavailability of dexamethasone and enables a slow, sustained release, enhancing its therapeutic effects. Nucleoside microneedles, incorporating adenosine, synergistically enhance anti-inflammatory and analgesic effects by reducing the release of inflammatory cytokines and decreasing neuronal excitability and reverse the glucocorticoid-induced inhibition of cell migration by promoting CD31 and Ki67 expression. In vivo experiments confirmed that the microneedle reduced the ulcer area to 6.3% after 9 days of treatment (a 69.3% reduction compared to commercial formulations), with significant analgesic effects. This multiscale engineering approach addresses key challenges in oral drug retention, pseudomembrane penetration, and healing regulation, offering a paradigm for the treatment of mucosal diseases.
期刊介绍:
ACS Nano, published monthly, serves as an international forum for comprehensive articles on nanoscience and nanotechnology research at the intersections of chemistry, biology, materials science, physics, and engineering. The journal fosters communication among scientists in these communities, facilitating collaboration, new research opportunities, and advancements through discoveries. ACS Nano covers synthesis, assembly, characterization, theory, and simulation of nanostructures, nanobiotechnology, nanofabrication, methods and tools for nanoscience and nanotechnology, and self- and directed-assembly. Alongside original research articles, it offers thorough reviews, perspectives on cutting-edge research, and discussions envisioning the future of nanoscience and nanotechnology.