Microneedle-Assisted Transdermal Delivery of Etanercept for Rheumatoid Arthritis Treatment

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....

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Main Authors: Jian Cao, Nan Zhang, Ziyi Wang, Jingjing Su, Jing Yang, Jiabing Han, Yongxing Zhao
Format: Article
Language:English
Published: MDPI AG 2019-05-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/11/5/235
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author Jian Cao
Nan Zhang
Ziyi Wang
Jingjing Su
Jing Yang
Jiabing Han
Yongxing Zhao
author_facet Jian Cao
Nan Zhang
Ziyi Wang
Jingjing Su
Jing Yang
Jiabing Han
Yongxing Zhao
author_sort Jian Cao
collection DOAJ
description 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.
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spelling doaj.art-c2f79530f320426196f164888df991a82022-12-22T04:25:15ZengMDPI AGPharmaceutics1999-49232019-05-0111523510.3390/pharmaceutics11050235pharmaceutics11050235Microneedle-Assisted Transdermal Delivery of Etanercept for Rheumatoid Arthritis TreatmentJian Cao0Nan Zhang1Ziyi Wang2Jingjing Su3Jing Yang4Jiabing Han5Yongxing Zhao6Department of Pharmaceutics, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, ChinaDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, ChinaDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, ChinaDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, ChinaDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, ChinaDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, ChinaDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, ChinaRheumatoid 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.https://www.mdpi.com/1999-4923/11/5/235microneedleetanerceptrheumatoid arthritisdrug deliveryhyaluronic acid
spellingShingle Jian Cao
Nan Zhang
Ziyi Wang
Jingjing Su
Jing Yang
Jiabing Han
Yongxing Zhao
Microneedle-Assisted Transdermal Delivery of Etanercept for Rheumatoid Arthritis Treatment
Pharmaceutics
microneedle
etanercept
rheumatoid arthritis
drug delivery
hyaluronic acid
title Microneedle-Assisted Transdermal Delivery of Etanercept for Rheumatoid Arthritis Treatment
title_full Microneedle-Assisted Transdermal Delivery of Etanercept for Rheumatoid Arthritis Treatment
title_fullStr Microneedle-Assisted Transdermal Delivery of Etanercept for Rheumatoid Arthritis Treatment
title_full_unstemmed Microneedle-Assisted Transdermal Delivery of Etanercept for Rheumatoid Arthritis Treatment
title_short Microneedle-Assisted Transdermal Delivery of Etanercept for Rheumatoid Arthritis Treatment
title_sort microneedle assisted transdermal delivery of etanercept for rheumatoid arthritis treatment
topic microneedle
etanercept
rheumatoid arthritis
drug delivery
hyaluronic acid
url https://www.mdpi.com/1999-4923/11/5/235
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AT ziyiwang microneedleassistedtransdermaldeliveryofetanerceptforrheumatoidarthritistreatment
AT jingjingsu microneedleassistedtransdermaldeliveryofetanerceptforrheumatoidarthritistreatment
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