Characteristics of Hydrogels as a Coating for Microneedle Transdermal Delivery Systems with Agomelatine

Agomelatine (AGM) is an effective antidepressant with low oral bioavailability due to intensive hepatic metabolism. Transdermal administration of agomelatine may increase its bioavailability and reduce the doses necessary for therapeutic effects. However, transdermal delivery requires crossing the &...

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Main Authors: Monika Wojtyłko, Ariadna B. Nowicka, Anna Froelich, Mirosław Szybowicz, Tobiasz Banaszek, Dorota Tomczak, Wiesław Kuczko, Radosław Wichniarek, Irena Budnik, Barbara Jadach, Oliwia Kordyl, Antoni Białek, Julia Krysztofiak, Tomasz Osmałek, Dimitrios A. Lamprou
Format: Article
Language:English
Published: MDPI AG 2025-01-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/30/2/322
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author Monika Wojtyłko
Ariadna B. Nowicka
Anna Froelich
Mirosław Szybowicz
Tobiasz Banaszek
Dorota Tomczak
Wiesław Kuczko
Radosław Wichniarek
Irena Budnik
Barbara Jadach
Oliwia Kordyl
Antoni Białek
Julia Krysztofiak
Tomasz Osmałek
Dimitrios A. Lamprou
author_facet Monika Wojtyłko
Ariadna B. Nowicka
Anna Froelich
Mirosław Szybowicz
Tobiasz Banaszek
Dorota Tomczak
Wiesław Kuczko
Radosław Wichniarek
Irena Budnik
Barbara Jadach
Oliwia Kordyl
Antoni Białek
Julia Krysztofiak
Tomasz Osmałek
Dimitrios A. Lamprou
author_sort Monika Wojtyłko
collection DOAJ
description Agomelatine (AGM) is an effective antidepressant with low oral bioavailability due to intensive hepatic metabolism. Transdermal administration of agomelatine may increase its bioavailability and reduce the doses necessary for therapeutic effects. However, transdermal delivery requires crossing the <i>stratum corneum</i> barrier. For this purpose, the use of microneedles may increase the efficiency of administration. The aim of this study was to prepare an agomelatine-loaded hydrogel suitable for coating microneedles for the transdermal drug delivery of AGM. The optimized formulations were subjected to spectroscopic and rheological characterization and mechanical tests, as well as tested for release through an artificial membrane and permeation through human skin ex vivo. Both hydrogels were found to have suitable parameters for coating microneedles using the dip-coating method, including the stability of the substance at the process temperature, shear-thinning behavior, and appropriate textural parameters such as adhesion or hardness. Additionally, two formulations were tested for potential application to the skin alone because the gels showed suitable mechanical properties for the skin application. In this case, the ethanol gel was characterized by higher skin permeability and better spreadability. The information obtained in this study will allow the preparation of coated microneedles for the transdermal administration of agomelatine.
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spelling doaj-art-cbd8a6a43c214e39aa4e4833272a1a1e2025-01-24T13:43:36ZengMDPI AGMolecules1420-30492025-01-0130232210.3390/molecules30020322Characteristics of Hydrogels as a Coating for Microneedle Transdermal Delivery Systems with AgomelatineMonika Wojtyłko0Ariadna B. Nowicka1Anna Froelich2Mirosław Szybowicz3Tobiasz Banaszek4Dorota Tomczak5Wiesław Kuczko6Radosław Wichniarek7Irena Budnik8Barbara Jadach9Oliwia Kordyl10Antoni Białek11Julia Krysztofiak12Tomasz Osmałek13Dimitrios A. Lamprou143D Printing Division, Chair and Department of Pharmaceutical Technology, Poznan University of Medical Sciences, 3 Rokietnicka Street, 60-806 Poznań, PolandInstitute of Materials Research and Quantum Engineering, The Faculty of Materials Engineering and Technical Physics, Poznan University of Technology, 3 Piotrowo Street, 60-965 Poznań, Poland3D Printing Division, Chair and Department of Pharmaceutical Technology, Poznan University of Medical Sciences, 3 Rokietnicka Street, 60-806 Poznań, PolandInstitute of Materials Research and Quantum Engineering, The Faculty of Materials Engineering and Technical Physics, Poznan University of Technology, 3 Piotrowo Street, 60-965 Poznań, PolandInstitute of Materials Research and Quantum Engineering, The Faculty of Materials Engineering and Technical Physics, Poznan University of Technology, 3 Piotrowo Street, 60-965 Poznań, PolandInstitute of Chemical Technology and Engineering, Poznan University of Technology, 4 Berdychowo Street, 60-965 Poznań, PolandInstitute of Materials Technology, Faculty of Mechanical Engineering, Poznan University of Technology, 3 Piotrowo Street, 60-965 Poznań, PolandInstitute of Materials Technology, Faculty of Mechanical Engineering, Poznan University of Technology, 3 Piotrowo Street, 60-965 Poznań, PolandChair and Department of Pharmaceutical Technology, Poznan University of Medical Sciences, 3 Rokietnicka Street, 60-806 Poznań, PolandDivision of Industrial Pharmacy, Chair and Department of Pharmaceutical Technology, Poznan University of Medical Sciences, 3 Rokietnicka Street, 60-806 Poznań, Poland3D Printing Division, Chair and Department of Pharmaceutical Technology, Poznan University of Medical Sciences, 3 Rokietnicka Street, 60-806 Poznań, PolandChair and Department of Pharmaceutical Technology, Poznan University of Medical Sciences, 3 Rokietnicka Street, 60-806 Poznań, PolandChair and Department of Pharmaceutical Technology, Poznan University of Medical Sciences, 3 Rokietnicka Street, 60-806 Poznań, PolandChair and Department of Pharmaceutical Technology, Poznan University of Medical Sciences, 3 Rokietnicka Street, 60-806 Poznań, PolandSchool of Pharmacy, Queen’s University Belfast, Belfast BT9 7BL, UKAgomelatine (AGM) is an effective antidepressant with low oral bioavailability due to intensive hepatic metabolism. Transdermal administration of agomelatine may increase its bioavailability and reduce the doses necessary for therapeutic effects. However, transdermal delivery requires crossing the <i>stratum corneum</i> barrier. For this purpose, the use of microneedles may increase the efficiency of administration. The aim of this study was to prepare an agomelatine-loaded hydrogel suitable for coating microneedles for the transdermal drug delivery of AGM. The optimized formulations were subjected to spectroscopic and rheological characterization and mechanical tests, as well as tested for release through an artificial membrane and permeation through human skin ex vivo. Both hydrogels were found to have suitable parameters for coating microneedles using the dip-coating method, including the stability of the substance at the process temperature, shear-thinning behavior, and appropriate textural parameters such as adhesion or hardness. Additionally, two formulations were tested for potential application to the skin alone because the gels showed suitable mechanical properties for the skin application. In this case, the ethanol gel was characterized by higher skin permeability and better spreadability. The information obtained in this study will allow the preparation of coated microneedles for the transdermal administration of agomelatine.https://www.mdpi.com/1420-3049/30/2/322agomelatinetransdermal deliveryhydrogelcoated microneedles
spellingShingle Monika Wojtyłko
Ariadna B. Nowicka
Anna Froelich
Mirosław Szybowicz
Tobiasz Banaszek
Dorota Tomczak
Wiesław Kuczko
Radosław Wichniarek
Irena Budnik
Barbara Jadach
Oliwia Kordyl
Antoni Białek
Julia Krysztofiak
Tomasz Osmałek
Dimitrios A. Lamprou
Characteristics of Hydrogels as a Coating for Microneedle Transdermal Delivery Systems with Agomelatine
Molecules
agomelatine
transdermal delivery
hydrogel
coated microneedles
title Characteristics of Hydrogels as a Coating for Microneedle Transdermal Delivery Systems with Agomelatine
title_full Characteristics of Hydrogels as a Coating for Microneedle Transdermal Delivery Systems with Agomelatine
title_fullStr Characteristics of Hydrogels as a Coating for Microneedle Transdermal Delivery Systems with Agomelatine
title_full_unstemmed Characteristics of Hydrogels as a Coating for Microneedle Transdermal Delivery Systems with Agomelatine
title_short Characteristics of Hydrogels as a Coating for Microneedle Transdermal Delivery Systems with Agomelatine
title_sort characteristics of hydrogels as a coating for microneedle transdermal delivery systems with agomelatine
topic agomelatine
transdermal delivery
hydrogel
coated microneedles
url https://www.mdpi.com/1420-3049/30/2/322
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