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Improved Therapeutic Efficiency against Obesity through Transdermal Drug Delivery Using Microneedle Arrays

In this paper, we prepared patches that were composed of a degradable microneedle (MN) array with a soft backing provided for the skin tissue. We then performed a transdermal delivery of anti-obesity drugs to evaluate the effectiveness of β3 adrenergic receptor CL316243 in obesity treatment in overw...

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Autores principales: Xie, Yixuan, Shao, Ruomei, Lin, Yali, Wang, Chunnan, Tan, Ying, Xie, Weidong, Sun, Shuqing
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8226838/
https://www.ncbi.nlm.nih.gov/pubmed/34199630
http://dx.doi.org/10.3390/pharmaceutics13060827
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author Xie, Yixuan
Shao, Ruomei
Lin, Yali
Wang, Chunnan
Tan, Ying
Xie, Weidong
Sun, Shuqing
author_facet Xie, Yixuan
Shao, Ruomei
Lin, Yali
Wang, Chunnan
Tan, Ying
Xie, Weidong
Sun, Shuqing
author_sort Xie, Yixuan
collection PubMed
description In this paper, we prepared patches that were composed of a degradable microneedle (MN) array with a soft backing provided for the skin tissue. We then performed a transdermal delivery of anti-obesity drugs to evaluate the effectiveness of β3 adrenergic receptor CL316243 in obesity treatment in overweight mice induced by a high-fat diet. Eighty male National Institutes of Health (NIH) mice were randomly divided into four obese groups or the control group. The obesity groups were given a high-fat diet for 15–18 weeks to establish an obese model. Afterward, the obese groups were divided into the following four groups: the control group, the unloaded MN group, the CL-316243 MN group, and the injection group. For the injection group, the group of mice was injected subcutaneously with CL316243 (1 mg/(kg·day)) for 15 days. Furthermore, the CL-316243 MN group was given a lower dose (0.1 mg/(kg·day)) for 15 days. After weighing the mice, we used Western blotting to detect the expression of uncoupling protein 1 (UCP1) in the adipose tissue around the mouse viscera. The results stated that the weight of the CL-316243 MN group and the injection group dropped, and the UCP1 protein expression of brown adipose tissue (BAT) significantly increased. The results demonstrated the β3 adrenergic receptor agonist CL316243 could be carried into the body through MN, and the dose applied was considerably smaller than the injection dose. The reason for this may arise from the CL-316243 being delivered by MN arrays to subcutaneous adipose tissue more efficiently, with an even distribution, compared to that of the injection dose. This technique provides a new and feasible way to treat obesity more effectively.
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spelling pubmed-82268382021-06-26 Improved Therapeutic Efficiency against Obesity through Transdermal Drug Delivery Using Microneedle Arrays Xie, Yixuan Shao, Ruomei Lin, Yali Wang, Chunnan Tan, Ying Xie, Weidong Sun, Shuqing Pharmaceutics Article In this paper, we prepared patches that were composed of a degradable microneedle (MN) array with a soft backing provided for the skin tissue. We then performed a transdermal delivery of anti-obesity drugs to evaluate the effectiveness of β3 adrenergic receptor CL316243 in obesity treatment in overweight mice induced by a high-fat diet. Eighty male National Institutes of Health (NIH) mice were randomly divided into four obese groups or the control group. The obesity groups were given a high-fat diet for 15–18 weeks to establish an obese model. Afterward, the obese groups were divided into the following four groups: the control group, the unloaded MN group, the CL-316243 MN group, and the injection group. For the injection group, the group of mice was injected subcutaneously with CL316243 (1 mg/(kg·day)) for 15 days. Furthermore, the CL-316243 MN group was given a lower dose (0.1 mg/(kg·day)) for 15 days. After weighing the mice, we used Western blotting to detect the expression of uncoupling protein 1 (UCP1) in the adipose tissue around the mouse viscera. The results stated that the weight of the CL-316243 MN group and the injection group dropped, and the UCP1 protein expression of brown adipose tissue (BAT) significantly increased. The results demonstrated the β3 adrenergic receptor agonist CL316243 could be carried into the body through MN, and the dose applied was considerably smaller than the injection dose. The reason for this may arise from the CL-316243 being delivered by MN arrays to subcutaneous adipose tissue more efficiently, with an even distribution, compared to that of the injection dose. This technique provides a new and feasible way to treat obesity more effectively. MDPI 2021-06-02 /pmc/articles/PMC8226838/ /pubmed/34199630 http://dx.doi.org/10.3390/pharmaceutics13060827 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
Xie, Yixuan
Shao, Ruomei
Lin, Yali
Wang, Chunnan
Tan, Ying
Xie, Weidong
Sun, Shuqing
Improved Therapeutic Efficiency against Obesity through Transdermal Drug Delivery Using Microneedle Arrays
title Improved Therapeutic Efficiency against Obesity through Transdermal Drug Delivery Using Microneedle Arrays
title_full Improved Therapeutic Efficiency against Obesity through Transdermal Drug Delivery Using Microneedle Arrays
title_fullStr Improved Therapeutic Efficiency against Obesity through Transdermal Drug Delivery Using Microneedle Arrays
title_full_unstemmed Improved Therapeutic Efficiency against Obesity through Transdermal Drug Delivery Using Microneedle Arrays
title_short Improved Therapeutic Efficiency against Obesity through Transdermal Drug Delivery Using Microneedle Arrays
title_sort improved therapeutic efficiency against obesity through transdermal drug delivery using microneedle arrays
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8226838/
https://www.ncbi.nlm.nih.gov/pubmed/34199630
http://dx.doi.org/10.3390/pharmaceutics13060827
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