Enhanced Skin Permeation of 5-Fluorouracil through Drug-in-Adhesive Topical Patches

dc.contributor.authorKim, S.
dc.contributor.authorYoussef, S.H.
dc.contributor.authorLee, K.M.K.
dc.contributor.authorSong, Y.
dc.contributor.authorVaidya, S.
dc.contributor.authorGarg, S.
dc.date.issued2024
dc.descriptionData source: Available data set, https://doi.org/10.3390/pharmaceutics16030379
dc.description.abstract5-fluorouracil (5-FU), commercially available as a topical product, is approved for non-melanoma skin cancer (NMSC) treatment with several clinical limitations. This work aimed to develop 5-FU-loaded topical patches as a potential alternative to overcome such drawbacks. The patches offer accurate dosing, controlled drug release and improved patient compliance. Our study highlights the development of Eudragit<sup>®</sup> E (EuE)-based drug-in-adhesive (DIA) patches containing a clinically significant high level of 5-FU (approximately 450 µg/cm<sup>2</sup>) formulated with various chemical permeation enhancers. The patches containing Transcutol<sup>®</sup> (Patch-TRAN) or oleic acid (Patch-OA) demonstrated significantly higher skin penetration ex vivo than their control counterpart, reaching 5-FU concentrations of 76.39 ± 27.7 µg/cm<sup>2</sup> and 82.56 ± 8.2 µg/cm<sup>2</sup>, respectively. Furthermore, the findings from in vitro permeation studies also validated the superior skin permeation of 5-FU achieved by Patch-OA and Patch-TRAN over 72 h. Moreover, the EuE-based DIA patch platform demonstrated suitable adhesive and mechanical properties with an excellent safety profile evaluated through an inaugural in vivo human study involving 11 healthy volunteers. In conclusion, the DIA patches could be a novel alternative option for NMSC as the patches effectively deliver 5-FU into the dermis layer and receptor compartment ex vivo for an extended period with excellent mechanical and safety profiles.
dc.identifier.citationPharmaceutics, 2024; 16(3)
dc.identifier.doi10.3390/pharmaceutics16030379
dc.identifier.issn1999-4923
dc.identifier.issn1999-4923
dc.identifier.orcidGarg, S. [0000-0001-7253-2629]
dc.identifier.urihttps://hdl.handle.net/11541.2/38380
dc.language.isoen
dc.publisherMDPI
dc.rightsCopyright 2024 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/)
dc.source.urihttps://doi.org/10.3390/pharmaceutics16030379
dc.subject5-fluorouracil
dc.subjectEudragit® E
dc.subjectStrat-M® membrane
dc.subjectchemical permeation enhancers
dc.subjectdrug-in-adhesive patches
dc.subjectnon-melanoma skin cancer
dc.titleEnhanced Skin Permeation of 5-Fluorouracil through Drug-in-Adhesive Topical Patches
dc.typeJournal article
pubs.publication-statusPublished
ror.fileinfo12284558800001831 13284558790001831 Open Access Published Version
ror.mmsid9916840421301831

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