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Open AccessArticle

Microneedle-Assisted Transdermal Delivery of Etanercept for Rheumatoid Arthritis Treatment

by Jian Cao 1,2,†, Nan Zhang 1,2,3,†, Ziyi Wang 1,2, Jingjing Su 1,2, Jing Yang 1,2, Jiabing Han 1 and Yongxing Zhao 1,2,3,*
Department of Pharmaceutics, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China
Key Laboratory of Targeting Therapy and Diagnosis for Critical Diseases, Zhengzhou 450001, China
Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Zhengzhou 450001, China
Author to whom correspondence should be addressed.
These authors contributed equally to the work.
Pharmaceutics 2019, 11(5), 235;
Received: 9 April 2019 / Revised: 9 May 2019 / Accepted: 13 May 2019 / Published: 15 May 2019
Rheumatoid arthritis (RA) is a complicated autoimmune disease. The clinical applications of etanercept (EN), a TNF-α inhibitor, can efficiently halt the development of RA. EN is mainly administrated by subcutaneous injection, which may cause low compliance, side effects, and infection risk. In this study, a hyaluronic acid crosslinked microneedle system (MN) was constructed as the transdermal alternative to deliver EN. We describe the formulation, fabrication, characterization, and transdermal insertion study of MN. In vitro bioactivity of EN was conducted and analyzed by dynamic light scattering and circular dichroism spectrum. In vivo evaluation of MN was studied on adjuvant-induced arthritis mice. The MN possessed sufficient mechanical strength, good biocompatibility, little influence on the bioactivity of EN, and high anti-inflammatory efficacy. This work represents a successful example of delivering macromolecule therapeutic treatment by MN for RA treatment. The transdermal delivery of EN by MN offers a new treatment option for RA patients. View Full-Text
Keywords: microneedle; etanercept; rheumatoid arthritis; drug delivery; hyaluronic acid microneedle; etanercept; rheumatoid arthritis; drug delivery; hyaluronic acid
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Cao, J.; Zhang, N.; Wang, Z.; Su, J.; Yang, J.; Han, J.; Zhao, Y. Microneedle-Assisted Transdermal Delivery of Etanercept for Rheumatoid Arthritis Treatment. Pharmaceutics 2019, 11, 235.

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