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Microneedle-Assisted Transfersomes as a Transdermal Delivery System for Aspirin

Raha Rahbari, Lewis Francis, Owen Guy Orcid Logo, Sanjiv Sharma Orcid Logo, Christopher Von Ruhland, Zhidao Xia Orcid Logo

Pharmaceutics, Volume: 16, Issue: 1, Start page: 57

Swansea University Authors: Raha Rahbari, Owen Guy Orcid Logo, Sanjiv Sharma Orcid Logo, Zhidao Xia Orcid Logo

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DOI (Published version): 10.3390/pharmaceutics16010057

Abstract

Transdermal drug delivery systems offer several advantages over conventional oral or hypodermic administration due to the avoidance of first-pass drug metabolism and gastrointestinal degradation as well as patients’ convenience due to a minimally invasive and painless approach. A novel transdermal d...

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Published in: Pharmaceutics
ISSN: 1999-4923
Published: MDPI AG 2023
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URI: https://cronfa.swan.ac.uk/Record/cronfa65386
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A novel transdermal drug delivery system, comprising a combination of transfersomes with either solid silicon or solid polycarbonate microneedles has been developed for the transdermal delivery of aspirin. Aspirin was encapsulated inside transfersomes using a “thin-film hydration sonication” technique, yielding an encapsulation efficiency of approximately 67.5%. The fabricated transfersomes have been optimised and fully characterised in terms of average size distribution and uniformity, surface charge and stability (shelf-life). Transdermal delivery, enhanced by microneedle penetration, allows the superior permeation of transfersomes into perforated porcine skin and has been extensively characterised using optical coherence tomography (OCT) and transmission electron microscopy (TEM). In vitro permeation studies revealed that transfersomes enhanced the permeability of aspirin by more than four times in comparison to the delivery of unencapsulated “free” aspirin. The microneedle-assisted delivery of transfersomes encapsulating aspirin yielded 13-fold and 10-fold increases in permeation using silicon and polycarbonate microneedles, respectively, in comparison with delivery using only transfersomes. The cytotoxicity of different dose regimens of transfersomes encapsulating aspirin showed that encapsulated aspirin became cytotoxic at concentrations of ≥100 μg/mL. The results presented demonstrate that the transfersomes could resolve the solubility issues of low-water-soluble drugs and enable their slow and controlled release. Microneedles enhance the delivery of transfersomes into deeper skin layers, providing a very effective system for the systemic delivery of drugs. 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spelling v2 65386 2023-12-28 Microneedle-Assisted Transfersomes as a Transdermal Delivery System for Aspirin 82f146efc345b9f4b3fd4e3aaceafdf4 Raha Rahbari Raha Rahbari true false c7fa5949b8528e048c5b978005f66794 0000-0002-6449-4033 Owen Guy Owen Guy true false b6b7506358522f607b171ec9c94757b7 0000-0003-3828-737X Sanjiv Sharma Sanjiv Sharma true false c9307abfed1b43987a19da0c0e30d7a4 0000-0002-2047-7282 Zhidao Xia Zhidao Xia true false 2023-12-28 REIS Transdermal drug delivery systems offer several advantages over conventional oral or hypodermic administration due to the avoidance of first-pass drug metabolism and gastrointestinal degradation as well as patients’ convenience due to a minimally invasive and painless approach. A novel transdermal drug delivery system, comprising a combination of transfersomes with either solid silicon or solid polycarbonate microneedles has been developed for the transdermal delivery of aspirin. Aspirin was encapsulated inside transfersomes using a “thin-film hydration sonication” technique, yielding an encapsulation efficiency of approximately 67.5%. The fabricated transfersomes have been optimised and fully characterised in terms of average size distribution and uniformity, surface charge and stability (shelf-life). Transdermal delivery, enhanced by microneedle penetration, allows the superior permeation of transfersomes into perforated porcine skin and has been extensively characterised using optical coherence tomography (OCT) and transmission electron microscopy (TEM). In vitro permeation studies revealed that transfersomes enhanced the permeability of aspirin by more than four times in comparison to the delivery of unencapsulated “free” aspirin. The microneedle-assisted delivery of transfersomes encapsulating aspirin yielded 13-fold and 10-fold increases in permeation using silicon and polycarbonate microneedles, respectively, in comparison with delivery using only transfersomes. The cytotoxicity of different dose regimens of transfersomes encapsulating aspirin showed that encapsulated aspirin became cytotoxic at concentrations of ≥100 μg/mL. The results presented demonstrate that the transfersomes could resolve the solubility issues of low-water-soluble drugs and enable their slow and controlled release. Microneedles enhance the delivery of transfersomes into deeper skin layers, providing a very effective system for the systemic delivery of drugs. This combined drug delivery system can potentially be utilised for numerous drug treatments. Journal Article Pharmaceutics 16 1 57 MDPI AG 1999-4923 microneedle; transfersome; transdermal delivery; aspirin 29 12 2023 2023-12-29 10.3390/pharmaceutics16010057 http://dx.doi.org/10.3390/pharmaceutics16010057 The data presented in this study are available in this article. COLLEGE NANME Research Engagement & Innovation Services COLLEGE CODE REIS Swansea University SU College/Department paid the OA fee This research received funding from the European Social Fund (ESF) Knowledge Economy Skills Scholarships II (KESSII) convergence programme, with co-sponsorship from P&S Nano Ltd., Boca Raton, FL, USA. 2024-03-21T15:43:14.8200363 2023-12-28T15:50:06.4987324 Faculty of Science and Engineering School of Engineering and Applied Sciences - Chemical Engineering Raha Rahbari 1 Lewis Francis 2 Owen Guy 0000-0002-6449-4033 3 Sanjiv Sharma 0000-0003-3828-737X 4 Christopher Von Ruhland 5 Zhidao Xia 0000-0002-2047-7282 6 65386__29791__0ec0f57c01904c9fa94cc720164075e6.pdf 65386.VOR.pdf 2024-03-21T15:40:40.3041398 Output 11591364 application/pdf Version of Record true Copyright: © 2023 by the authors. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license. true eng https://creativecommons.org/licenses/by/4.0/
title Microneedle-Assisted Transfersomes as a Transdermal Delivery System for Aspirin
spellingShingle Microneedle-Assisted Transfersomes as a Transdermal Delivery System for Aspirin
Raha Rahbari
Owen Guy
Sanjiv Sharma
Zhidao Xia
title_short Microneedle-Assisted Transfersomes as a Transdermal Delivery System for Aspirin
title_full Microneedle-Assisted Transfersomes as a Transdermal Delivery System for Aspirin
title_fullStr Microneedle-Assisted Transfersomes as a Transdermal Delivery System for Aspirin
title_full_unstemmed Microneedle-Assisted Transfersomes as a Transdermal Delivery System for Aspirin
title_sort Microneedle-Assisted Transfersomes as a Transdermal Delivery System for Aspirin
author_id_str_mv 82f146efc345b9f4b3fd4e3aaceafdf4
c7fa5949b8528e048c5b978005f66794
b6b7506358522f607b171ec9c94757b7
c9307abfed1b43987a19da0c0e30d7a4
author_id_fullname_str_mv 82f146efc345b9f4b3fd4e3aaceafdf4_***_Raha Rahbari
c7fa5949b8528e048c5b978005f66794_***_Owen Guy
b6b7506358522f607b171ec9c94757b7_***_Sanjiv Sharma
c9307abfed1b43987a19da0c0e30d7a4_***_Zhidao Xia
author Raha Rahbari
Owen Guy
Sanjiv Sharma
Zhidao Xia
author2 Raha Rahbari
Lewis Francis
Owen Guy
Sanjiv Sharma
Christopher Von Ruhland
Zhidao Xia
format Journal article
container_title Pharmaceutics
container_volume 16
container_issue 1
container_start_page 57
publishDate 2023
institution Swansea University
issn 1999-4923
doi_str_mv 10.3390/pharmaceutics16010057
publisher MDPI AG
college_str Faculty of Science and Engineering
hierarchytype
hierarchy_top_id facultyofscienceandengineering
hierarchy_top_title Faculty of Science and Engineering
hierarchy_parent_id facultyofscienceandengineering
hierarchy_parent_title Faculty of Science and Engineering
department_str School of Engineering and Applied Sciences - Chemical Engineering{{{_:::_}}}Faculty of Science and Engineering{{{_:::_}}}School of Engineering and Applied Sciences - Chemical Engineering
url http://dx.doi.org/10.3390/pharmaceutics16010057
document_store_str 1
active_str 0
description Transdermal drug delivery systems offer several advantages over conventional oral or hypodermic administration due to the avoidance of first-pass drug metabolism and gastrointestinal degradation as well as patients’ convenience due to a minimally invasive and painless approach. A novel transdermal drug delivery system, comprising a combination of transfersomes with either solid silicon or solid polycarbonate microneedles has been developed for the transdermal delivery of aspirin. Aspirin was encapsulated inside transfersomes using a “thin-film hydration sonication” technique, yielding an encapsulation efficiency of approximately 67.5%. The fabricated transfersomes have been optimised and fully characterised in terms of average size distribution and uniformity, surface charge and stability (shelf-life). Transdermal delivery, enhanced by microneedle penetration, allows the superior permeation of transfersomes into perforated porcine skin and has been extensively characterised using optical coherence tomography (OCT) and transmission electron microscopy (TEM). In vitro permeation studies revealed that transfersomes enhanced the permeability of aspirin by more than four times in comparison to the delivery of unencapsulated “free” aspirin. The microneedle-assisted delivery of transfersomes encapsulating aspirin yielded 13-fold and 10-fold increases in permeation using silicon and polycarbonate microneedles, respectively, in comparison with delivery using only transfersomes. The cytotoxicity of different dose regimens of transfersomes encapsulating aspirin showed that encapsulated aspirin became cytotoxic at concentrations of ≥100 μg/mL. The results presented demonstrate that the transfersomes could resolve the solubility issues of low-water-soluble drugs and enable their slow and controlled release. Microneedles enhance the delivery of transfersomes into deeper skin layers, providing a very effective system for the systemic delivery of drugs. This combined drug delivery system can potentially be utilised for numerous drug treatments.
published_date 2023-12-29T15:43:15Z
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