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

1
Institute of Biopharmaceutical and Health Engineering, Shenzhen International Graduate School, Tsinghua University, Shenzhen 518055, China
2
Department of Biomedical Engineering, Tsinghua University, Beijing 100084, China
3
Department of Physics, Tsinghua University, Beijing 100084, China
*
Author to whom correspondence should be addressed.
Academic Editor: Diganta B. Das
Pharmaceutics 2021, 13(6), 827; https://doi.org/10.3390/pharmaceutics13060827
Received: 1 March 2021 / Revised: 16 May 2021 / Accepted: 20 May 2021 / Published: 2 June 2021
(This article belongs to the Section Drug Delivery and Controlled Release)
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. View Full-Text
Keywords: CL-316243; obesity; degradable microneedle; drug delivery CL-316243; obesity; degradable microneedle; drug delivery
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MDPI and ACS Style

Xie, Y.; Shao, R.; Lin, Y.; Wang, C.; Tan, Y.; Xie, W.; Sun, S. Improved Therapeutic Efficiency against Obesity through Transdermal Drug Delivery Using Microneedle Arrays. Pharmaceutics 2021, 13, 827. https://doi.org/10.3390/pharmaceutics13060827

AMA Style

Xie Y, Shao R, Lin Y, Wang C, Tan Y, Xie W, Sun S. Improved Therapeutic Efficiency against Obesity through Transdermal Drug Delivery Using Microneedle Arrays. Pharmaceutics. 2021; 13(6):827. https://doi.org/10.3390/pharmaceutics13060827

Chicago/Turabian Style

Xie, Yixuan, Ruomei Shao, Yali Lin, Chunnan Wang, Ying Tan, Weidong Xie, and Shuqing Sun. 2021. "Improved Therapeutic Efficiency against Obesity through Transdermal Drug Delivery Using Microneedle Arrays" Pharmaceutics 13, no. 6: 827. https://doi.org/10.3390/pharmaceutics13060827

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