Polymeric microneedle-mediated transdermal delivery of melittin for rheumatoid arthritis treatment

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Polymeric microneedle-mediated transdermal delivery of melittin for rheumatoid arthritis treatment. / Du, Guangsheng ; He, Penghui; Zhao, Jiaxuan; He, Chunting; Zhang, Zhihua; Zhang, Zhibing; Sun, Xun.

In: Journal of Controlled Release, Vol. 336, 10.08.2021, p. 537-548.

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Du, Guangsheng ; He, Penghui ; Zhao, Jiaxuan ; He, Chunting ; Zhang, Zhihua ; Zhang, Zhibing ; Sun, Xun. / Polymeric microneedle-mediated transdermal delivery of melittin for rheumatoid arthritis treatment. In: Journal of Controlled Release. 2021 ; Vol. 336. pp. 537-548.

Bibtex

@article{e1a474c8bf834087b7a8e29bac0a33d9,
title = "Polymeric microneedle-mediated transdermal delivery of melittin for rheumatoid arthritis treatment",
abstract = "Transdermal drug delivery systems for rheumatoid arthritis (RA) have been receiving increasing attention as they can potentially overcome drawbacks which exist in traditional oral or injection strategies, including low patient compliance and serious gastrointestinal side effects. However, transdermal delivery of RA drugs especially biological drugs suffers from low drug delivery efficiency due to the robust skin barrier. Herein, we fabricated melittin-loaded hyaluronic acid (HA) microneedles and investigated their capacity for inhibiting RA. We showed that melittin-loaded HA microneedles possessed high mechanical strength for successful delivery of melittin into the skin and effectively inhibited RA progression in adjuvant induced both rodent and murine models, as shown by results in histological, paw swelling and arthritis score. Furthermore, after modifying HA with cross-linkable groups, the fabricated microneedles with sustained release properties could further improve the therapeutic potency. Cytokine and T cell analysis in the paws and lymphatic organs indicated that the application of microneedles suppressed the levels of pro-inflammation cytokines including IL-17 and TNF-α, and increased the percentage of regulatory CD4 T cells. Our study revealed that polymeric microneedle-mediated transdermal delivery of melittin could serve as a new therapy with high compliance and good therapeutic efficacy for RA and other autoimmune diseases.",
keywords = "Polymeric microneedles, Melittin, Rheumatoid arthritis, Sustained release, Hyaluronic acid",
author = "Guangsheng Du and Penghui He and Jiaxuan Zhao and Chunting He and Zhihua Zhang and Zhibing Zhang and Xun Sun",
year = "2021",
month = aug,
day = "10",
doi = "10.1016/j.jconrel.2021.07.005",
language = "English",
volume = "336",
pages = "537--548",
journal = "Journal of Controlled Release",
issn = "0168-3659",
publisher = "Elsevier",

}

RIS

TY - JOUR

T1 - Polymeric microneedle-mediated transdermal delivery of melittin for rheumatoid arthritis treatment

AU - Du, Guangsheng

AU - He, Penghui

AU - Zhao, Jiaxuan

AU - He, Chunting

AU - Zhang, Zhihua

AU - Zhang, Zhibing

AU - Sun, Xun

PY - 2021/8/10

Y1 - 2021/8/10

N2 - Transdermal drug delivery systems for rheumatoid arthritis (RA) have been receiving increasing attention as they can potentially overcome drawbacks which exist in traditional oral or injection strategies, including low patient compliance and serious gastrointestinal side effects. However, transdermal delivery of RA drugs especially biological drugs suffers from low drug delivery efficiency due to the robust skin barrier. Herein, we fabricated melittin-loaded hyaluronic acid (HA) microneedles and investigated their capacity for inhibiting RA. We showed that melittin-loaded HA microneedles possessed high mechanical strength for successful delivery of melittin into the skin and effectively inhibited RA progression in adjuvant induced both rodent and murine models, as shown by results in histological, paw swelling and arthritis score. Furthermore, after modifying HA with cross-linkable groups, the fabricated microneedles with sustained release properties could further improve the therapeutic potency. Cytokine and T cell analysis in the paws and lymphatic organs indicated that the application of microneedles suppressed the levels of pro-inflammation cytokines including IL-17 and TNF-α, and increased the percentage of regulatory CD4 T cells. Our study revealed that polymeric microneedle-mediated transdermal delivery of melittin could serve as a new therapy with high compliance and good therapeutic efficacy for RA and other autoimmune diseases.

AB - Transdermal drug delivery systems for rheumatoid arthritis (RA) have been receiving increasing attention as they can potentially overcome drawbacks which exist in traditional oral or injection strategies, including low patient compliance and serious gastrointestinal side effects. However, transdermal delivery of RA drugs especially biological drugs suffers from low drug delivery efficiency due to the robust skin barrier. Herein, we fabricated melittin-loaded hyaluronic acid (HA) microneedles and investigated their capacity for inhibiting RA. We showed that melittin-loaded HA microneedles possessed high mechanical strength for successful delivery of melittin into the skin and effectively inhibited RA progression in adjuvant induced both rodent and murine models, as shown by results in histological, paw swelling and arthritis score. Furthermore, after modifying HA with cross-linkable groups, the fabricated microneedles with sustained release properties could further improve the therapeutic potency. Cytokine and T cell analysis in the paws and lymphatic organs indicated that the application of microneedles suppressed the levels of pro-inflammation cytokines including IL-17 and TNF-α, and increased the percentage of regulatory CD4 T cells. Our study revealed that polymeric microneedle-mediated transdermal delivery of melittin could serve as a new therapy with high compliance and good therapeutic efficacy for RA and other autoimmune diseases.

KW - Polymeric microneedles

KW - Melittin

KW - Rheumatoid arthritis

KW - Sustained release

KW - Hyaluronic acid

U2 - 10.1016/j.jconrel.2021.07.005

DO - 10.1016/j.jconrel.2021.07.005

M3 - Article

VL - 336

SP - 537

EP - 548

JO - Journal of Controlled Release

JF - Journal of Controlled Release

SN - 0168-3659

ER -