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Polymeric Microneedles for Transdermal Delivery of Rivastigmine: Design and Application in Skin Mimetic Model

In the last years, microneedles (MNs) have been considered a valuable, painless, and minimally invasive approach for controlled transdermal drug delivery (TDD). Rivastigmine (RV), a drug administered to patients suffering from dementia, is currently delivered by oral or transdermal routes; however,...

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Autores principales: Guimarães, Tânia M. T., Moniz, Tânia, Nunes, Cláudia, Zaharieva, Maya Margaritova, Kaleva, Mila, Yoncheva, Krassimira, Najdenski, Hristo, Costa Lima, Sofia A., Reis, Salette
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9028500/
https://www.ncbi.nlm.nih.gov/pubmed/35456586
http://dx.doi.org/10.3390/pharmaceutics14040752
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author Guimarães, Tânia M. T.
Moniz, Tânia
Nunes, Cláudia
Zaharieva, Maya Margaritova
Kaleva, Mila
Yoncheva, Krassimira
Najdenski, Hristo
Costa Lima, Sofia A.
Reis, Salette
author_facet Guimarães, Tânia M. T.
Moniz, Tânia
Nunes, Cláudia
Zaharieva, Maya Margaritova
Kaleva, Mila
Yoncheva, Krassimira
Najdenski, Hristo
Costa Lima, Sofia A.
Reis, Salette
author_sort Guimarães, Tânia M. T.
collection PubMed
description In the last years, microneedles (MNs) have been considered a valuable, painless, and minimally invasive approach for controlled transdermal drug delivery (TDD). Rivastigmine (RV), a drug administered to patients suffering from dementia, is currently delivered by oral or transdermal routes; however, both present limitations, mainly gastrointestinal adverse symptoms or local skin irritation and drug losses, respectively, for each route. Given this, the objective of the present work was to develop and evaluate the potential of polymeric MNs for RV transdermal delivery in a controlled manner. Polymeric MNs with two needle heights and different compositions were developed with calcein as a fluorescent model molecule. Morphology and mechanical characterisation were accessed. Skin permeation experiments showed the ability of the devices to deliver calcein and confirmed that the arrays were able to efficiently pierce the skin. To obtain a new TDD anti-dementia therapeutic solution, RV was loaded in 800 µm polymeric MNs of alginate and alginate/k-carrageenan MNs. In the presence of RV, the MN’s morphology was maintained; however, the presence of RV influenced the compression force. Skin permeation studies revealed that RV-loaded MNs allowed a more efficient controlled release of the drug than the commercial patch. In vivo, skin irritation tests in rabbits revealed that the developed MNs were innocuous upon removal, in contrast with the evidence found for Exelon(®), the commercial patch, which caused slight mechanical damage to the skin. The herein-produced MNs demonstrated a more controlled release of the drug, being the more suitable option for the transdermal delivery of RV.
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spelling pubmed-90285002022-04-23 Polymeric Microneedles for Transdermal Delivery of Rivastigmine: Design and Application in Skin Mimetic Model Guimarães, Tânia M. T. Moniz, Tânia Nunes, Cláudia Zaharieva, Maya Margaritova Kaleva, Mila Yoncheva, Krassimira Najdenski, Hristo Costa Lima, Sofia A. Reis, Salette Pharmaceutics Article In the last years, microneedles (MNs) have been considered a valuable, painless, and minimally invasive approach for controlled transdermal drug delivery (TDD). Rivastigmine (RV), a drug administered to patients suffering from dementia, is currently delivered by oral or transdermal routes; however, both present limitations, mainly gastrointestinal adverse symptoms or local skin irritation and drug losses, respectively, for each route. Given this, the objective of the present work was to develop and evaluate the potential of polymeric MNs for RV transdermal delivery in a controlled manner. Polymeric MNs with two needle heights and different compositions were developed with calcein as a fluorescent model molecule. Morphology and mechanical characterisation were accessed. Skin permeation experiments showed the ability of the devices to deliver calcein and confirmed that the arrays were able to efficiently pierce the skin. To obtain a new TDD anti-dementia therapeutic solution, RV was loaded in 800 µm polymeric MNs of alginate and alginate/k-carrageenan MNs. In the presence of RV, the MN’s morphology was maintained; however, the presence of RV influenced the compression force. Skin permeation studies revealed that RV-loaded MNs allowed a more efficient controlled release of the drug than the commercial patch. In vivo, skin irritation tests in rabbits revealed that the developed MNs were innocuous upon removal, in contrast with the evidence found for Exelon(®), the commercial patch, which caused slight mechanical damage to the skin. The herein-produced MNs demonstrated a more controlled release of the drug, being the more suitable option for the transdermal delivery of RV. MDPI 2022-03-30 /pmc/articles/PMC9028500/ /pubmed/35456586 http://dx.doi.org/10.3390/pharmaceutics14040752 Text en © 2022 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
Guimarães, Tânia M. T.
Moniz, Tânia
Nunes, Cláudia
Zaharieva, Maya Margaritova
Kaleva, Mila
Yoncheva, Krassimira
Najdenski, Hristo
Costa Lima, Sofia A.
Reis, Salette
Polymeric Microneedles for Transdermal Delivery of Rivastigmine: Design and Application in Skin Mimetic Model
title Polymeric Microneedles for Transdermal Delivery of Rivastigmine: Design and Application in Skin Mimetic Model
title_full Polymeric Microneedles for Transdermal Delivery of Rivastigmine: Design and Application in Skin Mimetic Model
title_fullStr Polymeric Microneedles for Transdermal Delivery of Rivastigmine: Design and Application in Skin Mimetic Model
title_full_unstemmed Polymeric Microneedles for Transdermal Delivery of Rivastigmine: Design and Application in Skin Mimetic Model
title_short Polymeric Microneedles for Transdermal Delivery of Rivastigmine: Design and Application in Skin Mimetic Model
title_sort polymeric microneedles for transdermal delivery of rivastigmine: design and application in skin mimetic model
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9028500/
https://www.ncbi.nlm.nih.gov/pubmed/35456586
http://dx.doi.org/10.3390/pharmaceutics14040752
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