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...

Full description

Bibliographic Details
Main Authors: Yixuan Xie, Ruomei Shao, Yali Lin, Chunnan Wang, Ying Tan, Weidong Xie, Shuqing Sun
Format: Article
Language:English
Published: MDPI AG 2021-06-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/13/6/827
_version_ 1827690768343498752
author Yixuan Xie
Ruomei Shao
Yali Lin
Chunnan Wang
Ying Tan
Weidong Xie
Shuqing Sun
author_facet Yixuan Xie
Ruomei Shao
Yali Lin
Chunnan Wang
Ying Tan
Weidong Xie
Shuqing Sun
author_sort Yixuan Xie
collection DOAJ
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.
first_indexed 2024-03-10T10:45:44Z
format Article
id doaj.art-3acfadb659b444009d84ae5275af9ed6
institution Directory Open Access Journal
issn 1999-4923
language English
last_indexed 2024-03-10T10:45:44Z
publishDate 2021-06-01
publisher MDPI AG
record_format Article
series Pharmaceutics
spelling doaj.art-3acfadb659b444009d84ae5275af9ed62023-11-21T22:35:21ZengMDPI AGPharmaceutics1999-49232021-06-0113682710.3390/pharmaceutics13060827Improved Therapeutic Efficiency against Obesity through Transdermal Drug Delivery Using Microneedle ArraysYixuan Xie0Ruomei Shao1Yali Lin2Chunnan Wang3Ying Tan4Weidong Xie5Shuqing Sun6Institute of Biopharmaceutical and Health Engineering, Shenzhen International Graduate School, Tsinghua University, Shenzhen 518055, ChinaInstitute of Biopharmaceutical and Health Engineering, Shenzhen International Graduate School, Tsinghua University, Shenzhen 518055, ChinaInstitute of Biopharmaceutical and Health Engineering, Shenzhen International Graduate School, Tsinghua University, Shenzhen 518055, ChinaInstitute of Biopharmaceutical and Health Engineering, Shenzhen International Graduate School, Tsinghua University, Shenzhen 518055, ChinaInstitute of Biopharmaceutical and Health Engineering, Shenzhen International Graduate School, Tsinghua University, Shenzhen 518055, ChinaInstitute of Biopharmaceutical and Health Engineering, Shenzhen International Graduate School, Tsinghua University, Shenzhen 518055, ChinaInstitute of Biopharmaceutical and Health Engineering, Shenzhen International Graduate School, Tsinghua University, Shenzhen 518055, ChinaIn 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.https://www.mdpi.com/1999-4923/13/6/827CL-316243obesitydegradable microneedledrug delivery
spellingShingle Yixuan Xie
Ruomei Shao
Yali Lin
Chunnan Wang
Ying Tan
Weidong Xie
Shuqing Sun
Improved Therapeutic Efficiency against Obesity through Transdermal Drug Delivery Using Microneedle Arrays
Pharmaceutics
CL-316243
obesity
degradable microneedle
drug delivery
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 CL-316243
obesity
degradable microneedle
drug delivery
url https://www.mdpi.com/1999-4923/13/6/827
work_keys_str_mv AT yixuanxie improvedtherapeuticefficiencyagainstobesitythroughtransdermaldrugdeliveryusingmicroneedlearrays
AT ruomeishao improvedtherapeuticefficiencyagainstobesitythroughtransdermaldrugdeliveryusingmicroneedlearrays
AT yalilin improvedtherapeuticefficiencyagainstobesitythroughtransdermaldrugdeliveryusingmicroneedlearrays
AT chunnanwang improvedtherapeuticefficiencyagainstobesitythroughtransdermaldrugdeliveryusingmicroneedlearrays
AT yingtan improvedtherapeuticefficiencyagainstobesitythroughtransdermaldrugdeliveryusingmicroneedlearrays
AT weidongxie improvedtherapeuticefficiencyagainstobesitythroughtransdermaldrugdeliveryusingmicroneedlearrays
AT shuqingsun improvedtherapeuticefficiencyagainstobesitythroughtransdermaldrugdeliveryusingmicroneedlearrays