Topical delivery of Lidocaine using spicules for local anesthesia

Topical delivery of Lidocaine using spicules for local anesthesia | Research Square window.SnipcartSettings = { analytics: { enabled: false } }; (function() { var accessVector = localStorage.getItem('access_vector') || ''; window.dataLayer = window.dataLayer || []; if (accessVector) { window.dataLayer.push({ user: { profile: { profileInfo: { snid: accessVector } } } }); } })(); (function(w,d,s,l,i){w[l]=w[l]||[];w[l].push({'gtm.start':new Date().getTime(),event:'gtm.js'});var f=d.getElementsByTagName(s)[0],j=d.createElement(s),dl=l!='dataLayer'?'&l='+l:'';j.async=true;j.src='https://www.googletagmanager.com/gtm.js?id='+i+dl;f.parentNode.insertBefore(j,f);})(window,document,'script','dataLayer','GTM-K279D39R'); Browse Preprints In Review Journals COVID-19 Preprints AJE Video Bytes Research Tools Research Promotion AJE Professional Editing AJE Rubriq About Preprint Platform In Review Editorial Policies Our Team Advisory Board Help Center Sign In Submit a Preprint Cite Share Download PDF Research Article Topical delivery of Lidocaine using spicules for local anesthesia Chi Zhang, Ping Yang, Xueke Lin, Huijung Lai, Yi Liu, Shifeng Yu, and 2 more This is a preprint; it has not been peer reviewed by a journal. https://doi.org/ 10.21203/rs.3.rs-7201057/v1 This work is licensed under a CC BY 4.0 License Status: Published Journal Publication published 16 Dec, 2025 Read the published version in Drug Delivery and Translational Research → Version 1 posted 5 You are reading this latest preprint version Abstract Local anesthesia has been extensively utilized in medical and surgical fields. We screened and optimized the application formula of lidocaine hydrochloride (LH). We utilized the combination of Sponge Haliclona sp. Spicules (SHS) with Carbomer gel to overcome the skin barrier and increase the skin absorption of lidocaine hydrochloride in vitro and in vivo . We first investigated the skin permeation and deposition behavior of LH with or without SHS in vitro . SHS can dramatically ( p < 0.001) increase the total skin absorption of LH (78.45 ± 6.96%) compared to the control group (passive penetration, 8.20 ± 1.60%). We also found most of LH (97.51 ± 0.17%) accumulated in deep skin layers (dermis and receptors), while only 35.99 ± 4.80% of LH accumulated there in the control. We next investigated the local anesthetics efficacy of LH with or without SHS using tail-flick latency (TFL) test in rats. SHS resulted in the highest MEP (maximum possible effect) of 5.15 ± 0.82 s at approximately 10 minutes, while the highest MEP of 2.60 ± 0.27 s appeared at around 45 minutes in the control group. Further, we carried out an investigator initiated clinical trial (IIT) to verify the clinical effectiveness of LH with or without SHS. SHS resulted in a significant difference in laser pain scores (4.40 ± 0.55, p <0.05) since 10 minutes post-application of LH cream compared to the control group (5.00 ± 0.00). Therefore, SHS can significantly enhance the skin absorption of lidocaine hydrochloride, effectively shorten the onset time of anesthesia and significantly improve the anesthetic effect of LH in clinical practice. Topical delivery Sponge Spicules Local anesthesia Full Text Cite Share Download PDF Status: Published Journal Publication published 16 Dec, 2025 Read the published version in Drug Delivery and Translational Research → Version 1 posted Editorial decision: Major Revisions Needed 14 Oct, 2025 Reviewers agreed at journal 15 Aug, 2025 Reviewers invited by journal 15 Aug, 2025 Editor assigned by journal 06 Aug, 2025 First submitted to journal 01 Aug, 2025 You are reading this latest preprint version Research Square lets you share your work early, gain feedback from the community, and start making changes to your manuscript prior to peer review in a journal. As a division of Research Square Company, we’re committed to making research communication faster, fairer, and more useful. We do this by developing innovative software and high quality services for the global research community. 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Also discoverable on Platform About Our Team In Review Editorial Policies Advisory Board Help Center Resources Author Services Accessibility API Access RSS feed Manage Cookie Preferences © Research Square 2026 | ISSN 2693-5015 (online) Privacy Policy Terms of Service Do Not Sell My Personal Information {"props":{"pageProps":{"initialData":{"identity":"rs-7201057","acceptedTermsAndConditions":true,"allowDirectSubmit":false,"archivedVersions":[],"articleType":"Research Article","associatedPublications":[],"authors":[{"id":500973322,"identity":"c63a8501-bc81-401d-99be-a49b722cf642","order_by":0,"name":"Chi Zhang","email":"","orcid":"","institution":"Department of Marine Biological Science \u0026 Technology, College of Ocean \u0026 Earth Sciences, Xiamen University, Xiamen 361102, China","correspondingAuthor":false,"prefix":"","firstName":"Chi","middleName":"","lastName":"Zhang","suffix":""},{"id":500973323,"identity":"24432668-6aef-44af-bc6d-f027166f5fdd","order_by":1,"name":"Ping Yang","email":"","orcid":"","institution":"Department of Marine Biological Science \u0026 Technology, College of Ocean \u0026 Earth Sciences, Xiamen University, Xiamen 361102, China","correspondingAuthor":false,"prefix":"","firstName":"Ping","middleName":"","lastName":"Yang","suffix":""},{"id":500973324,"identity":"7c498837-603e-4f2f-a208-415ada447a7d","order_by":2,"name":"Xueke Lin","email":"","orcid":"","institution":"Department of Marine Biological Science \u0026 Technology, College of Ocean \u0026 Earth Sciences, Xiamen University, Xiamen 361102, China","correspondingAuthor":false,"prefix":"","firstName":"Xueke","middleName":"","lastName":"Lin","suffix":""},{"id":500973325,"identity":"9e493330-1194-4a2e-901c-fc26c118cc6e","order_by":3,"name":"Huijung Lai","email":"","orcid":"","institution":"Department of Dermatology Xiang’an Hospital of Xiamen University，School of Medicine, Xiamen University, Xiamen 361102, 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Research","twitterHandle":"","acdcEnabled":true,"dfaEnabled":true,"editorialSystem":"em","reportingPortfolio":"Springer Hybrid","inReviewEnabled":true,"inReviewRevisionsEnabled":false},"keywords":"Topical delivery, Sponge Spicules, Local anesthesia","lastPublishedDoi":"10.21203/rs.3.rs-7201057/v1","lastPublishedDoiUrl":"https://doi.org/10.21203/rs.3.rs-7201057/v1","license":{"name":"CC BY 4.0","url":"https://creativecommons.org/licenses/by/4.0/"},"manuscriptAbstract":"\u003cp\u003eLocal anesthesia has been extensively utilized in medical and surgical fields. We screened and optimized the application formula of lidocaine hydrochloride (LH). We utilized the combination of Sponge\u003cem\u003e Haliclona \u003c/em\u003esp. Spicules (SHS) with Carbomer gel to overcome the skin barrier and increase the skin absorption of lidocaine hydrochloride \u003cem\u003ein vitro\u003c/em\u003e and \u003cem\u003ein vivo\u003c/em\u003e. We first investigated the skin permeation and deposition behavior of LH with or without SHS\u003cem\u003e in vitro\u003c/em\u003e. SHS can dramatically (\u003cem\u003ep \u003c/em\u003e\u0026lt; 0.001) increase the total skin absorption of LH (78.45 ± 6.96%) compared to the control group (passive penetration, 8.20 ± 1.60%). We also found most of LH (97.51 ± 0.17%) accumulated in deep skin layers (dermis and receptors), while only 35.99 ± 4.80% of LH accumulated there in the control. We next investigated the local anesthetics efficacy of LH with or without SHS using tail-flick latency (TFL) test in rats. SHS resulted in the highest MEP (maximum possible effect) of 5.15 ± 0.82 s at approximately 10 minutes, while the highest MEP of 2.60 ± 0.27 s appeared at around 45 minutes in the control group. Further, we carried out an investigator initiated clinical trial (IIT) to verify the clinical effectiveness of LH with or without SHS. SHS resulted in a significant difference in laser pain scores (4.40 ± 0.55, \u003cem\u003ep\u003c/em\u003e\u0026lt;0.05) since 10 minutes post-application of LH cream compared to the control group (5.00 ± 0.00). Therefore, SHS can significantly enhance the skin absorption of lidocaine hydrochloride, effectively shorten the onset time of anesthesia and significantly improve the anesthetic effect of LH in clinical practice.\u003c/p\u003e","manuscriptTitle":"Topical delivery of Lidocaine using spicules for local anesthesia","msid":"","msnumber":"","nonDraftVersions":[{"code":1,"date":"2025-08-22 07:55:34","doi":"10.21203/rs.3.rs-7201057/v1","editorialEvents":[{"type":"communityComments","content":0},{"type":"decision","content":"Major Revisions Needed","date":"2025-10-14T10:26:55+00:00","index":"","fulltext":""},{"type":"reviewerAgreed","content":"","date":"2025-08-15T17:31:49+00:00","index":0,"fulltext":""},{"type":"reviewersInvited","content":"","date":"2025-08-15T11:56:42+00:00","index":"","fulltext":""},{"type":"editorAssigned","content":"","date":"2025-08-06T07:16:05+00:00","index":"","fulltext":""},{"type":"submitted","content":"Drug Delivery and Translational Research","date":"2025-08-01T10:42:18+00:00","index":"","fulltext":""}],"status":"published","journal":{"display":true,"email":"[email protected]","identity":"drug-delivery-and-translational-research","isNatureJournal":false,"hasQc":true,"allowDirectSubmit":false,"externalIdentity":"ddtr","sideBox":"Learn more about [Drug Delivery and Translational Research](https://www.springer.com/journal/13346)","snPcode":"","submissionUrl":"https://www.editorialmanager.com/ddtr/default.aspx","title":"Drug Delivery and Translational Research","twitterHandle":"","acdcEnabled":true,"dfaEnabled":true,"editorialSystem":"em","reportingPortfolio":"Springer Hybrid","inReviewEnabled":true,"inReviewRevisionsEnabled":false}}],"origin":"","ownerIdentity":"ae52b6ea-3875-4c2f-94b1-c0173eed40e2","owner":[],"postedDate":"August 22nd, 2025","published":true,"recentEditorialEvents":[],"rejectedJournal":[],"revision":"","amendment":"","status":"published-in-journal","subjectAreas":[],"tags":[],"updatedAt":"2025-12-22T16:02:03+00:00","versionOfRecord":{"articleIdentity":"rs-7201057","link":"https://doi.org/10.1007/s13346-025-02030-4","journal":{"identity":"drug-delivery-and-translational-research","isVorOnly":false,"title":"Drug Delivery and Translational Research"},"publishedOn":"2025-12-16 15:57:17","publishedOnDateReadable":"December 16th, 2025"},"versionCreatedAt":"2025-08-22 07:55:34","video":"","vorDoi":"10.1007/s13346-025-02030-4","vorDoiUrl":"https://doi.org/10.1007/s13346-025-02030-4","workflowStages":[]},"version":"v1","identity":"rs-7201057","journalConfig":"researchsquare"},"__N_SSP":true},"page":"/article/[identity]/[[...version]]","query":{"redirect":"/article/rs-7201057","identity":"rs-7201057","version":["v1"]},"buildId":"8U1c8b4HqxoKbykW_rLl7","isFallback":false,"isExperimentalCompile":false,"dynamicIds":[84888],"gssp":true,"scriptLoader":[]}