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Pharmacokinetic Evaluation of a Novel Donepezil-Loaded Dissolving Microneedle Patch in Rats

Research on the development of dissolving microneedles (DMNs) has focused on bolus drug delivery, with little attention on sustained release. Here, we evaluated the sustained release, absorption pattern, and effective drug permeation of a novel donepezil-loaded DMN patch through an in vivo investiga...

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Autores principales: Rehman, Naveed Ur, Song, Chanwoo, Kim, Junhyeong, Noh, Inhwan, Rhee, Yun-Seok, Chung, Hye Jin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8778454/
https://www.ncbi.nlm.nih.gov/pubmed/35056902
http://dx.doi.org/10.3390/pharmaceutics14010005
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author Rehman, Naveed Ur
Song, Chanwoo
Kim, Junhyeong
Noh, Inhwan
Rhee, Yun-Seok
Chung, Hye Jin
author_facet Rehman, Naveed Ur
Song, Chanwoo
Kim, Junhyeong
Noh, Inhwan
Rhee, Yun-Seok
Chung, Hye Jin
author_sort Rehman, Naveed Ur
collection PubMed
description Research on the development of dissolving microneedles (DMNs) has focused on bolus drug delivery, with little attention on sustained release. Here, we evaluated the sustained release, absorption pattern, and effective drug permeation of a novel donepezil-loaded DMN patch through an in vivo investigation on rats. The applications of DMN patches to the shaved skin of rats for 1 week and 1 h were compared with oral donepezil administration to assess their sustained release capabilities. We used a validated liquid chromatography–tandem mass spectrometry method to quantify donepezil in the plasma. We found that the microneedle arrays effectively delivered donepezil across the skin, with dissolution observed within 1 h of application. Furthermore, skin irritation test showed that the patches produced no irritation response. The DMN arrays also effectively increased drug permeation and demonstrated sustained release and absorption of donepezil from DMN patches. These patches allow extended dosing intervals, reduced gastrointestinal adverse effects, and convenient self-administration to mitigate poor drug compliance, making them beneficial for the treatment of elderly patients with Alzheimer’s disease.
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spelling pubmed-87784542022-01-22 Pharmacokinetic Evaluation of a Novel Donepezil-Loaded Dissolving Microneedle Patch in Rats Rehman, Naveed Ur Song, Chanwoo Kim, Junhyeong Noh, Inhwan Rhee, Yun-Seok Chung, Hye Jin Pharmaceutics Article Research on the development of dissolving microneedles (DMNs) has focused on bolus drug delivery, with little attention on sustained release. Here, we evaluated the sustained release, absorption pattern, and effective drug permeation of a novel donepezil-loaded DMN patch through an in vivo investigation on rats. The applications of DMN patches to the shaved skin of rats for 1 week and 1 h were compared with oral donepezil administration to assess their sustained release capabilities. We used a validated liquid chromatography–tandem mass spectrometry method to quantify donepezil in the plasma. We found that the microneedle arrays effectively delivered donepezil across the skin, with dissolution observed within 1 h of application. Furthermore, skin irritation test showed that the patches produced no irritation response. The DMN arrays also effectively increased drug permeation and demonstrated sustained release and absorption of donepezil from DMN patches. These patches allow extended dosing intervals, reduced gastrointestinal adverse effects, and convenient self-administration to mitigate poor drug compliance, making them beneficial for the treatment of elderly patients with Alzheimer’s disease. MDPI 2021-12-21 /pmc/articles/PMC8778454/ /pubmed/35056902 http://dx.doi.org/10.3390/pharmaceutics14010005 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/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/).
spellingShingle Article
Rehman, Naveed Ur
Song, Chanwoo
Kim, Junhyeong
Noh, Inhwan
Rhee, Yun-Seok
Chung, Hye Jin
Pharmacokinetic Evaluation of a Novel Donepezil-Loaded Dissolving Microneedle Patch in Rats
title Pharmacokinetic Evaluation of a Novel Donepezil-Loaded Dissolving Microneedle Patch in Rats
title_full Pharmacokinetic Evaluation of a Novel Donepezil-Loaded Dissolving Microneedle Patch in Rats
title_fullStr Pharmacokinetic Evaluation of a Novel Donepezil-Loaded Dissolving Microneedle Patch in Rats
title_full_unstemmed Pharmacokinetic Evaluation of a Novel Donepezil-Loaded Dissolving Microneedle Patch in Rats
title_short Pharmacokinetic Evaluation of a Novel Donepezil-Loaded Dissolving Microneedle Patch in Rats
title_sort pharmacokinetic evaluation of a novel donepezil-loaded dissolving microneedle patch in rats
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8778454/
https://www.ncbi.nlm.nih.gov/pubmed/35056902
http://dx.doi.org/10.3390/pharmaceutics14010005
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